Pectolinaligenin preparations

Abstract

The present invention provides compositions comprising pectolinaligenin. The compositions of the present invention can be administered topically to the skin of a subject. The present invention further provides a method of administering a composition comprising pectolinaligenin for the improvement or treatment of a skin condition. The compositions of the present invention can also be applied to improve the overall appearance of the skin. The present invention relates to compositions comprising pectolinaligenin, and to methods of using compositions for treating, protecting, and / or altering (e.g., improving) skin conditions and / or aesthetic appearance, including, for example, treating, preventing, ameliorating, reducing and / or eliminating fine lines and / or wrinkles of the skin, and / or improving the aesthetic appearance of fine lines and / or wrinkles of the skin.

Description

[Technical Field]

[0001] I. Field of Invention The present invention relates to a pectolinaligenin formulation and a method for using the formulation on a local condition in a subject. [Background technology]

[0002] II. Background of the Invention The epidermis and its appendages (e.g., hair, nails, sebaceous glands, and sweat glands) of mammals provide a barrier to prevent harmful elements from entering the body and essential bodily fluids. As the first line of defense against various physical traumas from the environment, the epidermis must protect itself and the underlying tissues. The epidermis is also exposed to mutagenic ultraviolet radiation. In hairless or sparsely haired areas, such as most of human skin, the epidermis is thicker than hairy skin, and the skin in these areas plays a primarily protective role. Constant attacks on the epidermis necessitate autoregeneration, making it a prime example of adult tissue undergoing continuous and rapid flux.

[0003] Aged skin differs from youthful skin in both appearance and function. The aged epidermis shows decreased keratinocyte proliferation and becomes physically thinner, primarily due to the decline of interpapillary ridges. In addition to thinning, aging slows wound healing, prolongs epidermal turnover, and impairs barrier formation. The skin appears thin, wrinkled, bruised, and rough. Wrinkles and bruising can also result from aging-related changes in the dermis. The dermis, too, is characteristically thinner in older adults. Aged fibroblasts are less likely to synthesize normal amounts of collagen, elastin, laminin, glycosaminoglycans, and fibronectin. In such cases, the dermis may lack elasticity, strength, vascular support, reconstructive capacity, and basal cell structure. For example, interpapillary ridges may disappear, and basal cells may no longer be able to produce villous projections into the dermis. Epidermal cell turnover decreases by up to 50% in older adults compared to younger adults.

[0004] For example, the number of melanocytes can decrease by 8-20% every decade. In older adults, Langerhans cells are fewer, and those present are often functionally impaired. For instance, in women, collagen synthesis decreases by up to 30% within four years of menopause. The number of collagen and elastic fibers also decreases. The dermis also becomes less echogenic to ultrasound, which coincides with changes in collagen and elastic tissue. [Overview of the project] [Means for solving the problem]

[0005] III. Outline of the Invention The present invention relates to compositions of pectolinaligenin, and to methods of using compositions for treating, protecting, and / or altering (e.g., improving) the condition and / or aesthetic appearance of the skin, including, for example, treating, preventing, ameliorating, reducing, and / or eliminating fine lines and / or wrinkles of the skin, and / or improving the aesthetic appearance of fine lines and / or wrinkles of the skin. In certain embodiments, the compositions of the present invention lead to increased resilience of the skin and / or hair. In certain embodiments, the compositions of the present invention lead to increased elasticity of the skin. In certain embodiments, the compositions of the present invention prevent skin damage.

[0006] Topical administration of pectolinaligenin was not known in the art. Beneficially, the present invention is the first to recognize that topical compositions containing pectolinaligenin can be used to improve the condition of a skin subject or to treat any disease related to the skin subject. In one embodiment, the present invention includes a composition for topical administration containing an effective amount of pectolinaligenin. An effective amount of pectolinaligenin is an amount of pectolinaligenin that can be effective in treating, improving or otherwise affecting the underlying condition of the skin. The present invention recognizes that pectolinaligenin is poorly soluble or insoluble in water. The present invention also recognizes that pectolinaligenin is poorly soluble or insoluble in oils; for example, pectolinaligenin is insoluble in Helianthus annuus (sunflower) seed oil. In certain embodiments of the present invention, pectolina ligenin is dissolved in a solvent selected from the group consisting of dimethyl isosorbide, ethoxydiglycol, isopropyl lauryl sarcosinate, pentylene glycol, propanediol, 1,2-hexanediol, and / or butylene glycol. In certain preferred embodiments, pectolina ligenin is dissolved in dimethyl isosorbide.

[0007] In certain embodiments, pectolinaligenin is 1,2-heptanediol, 1,2-hexanediol, 1,2-propanediol, butylene glycol, C 15~19Alkanes, Capric Acid / Caprylic Triglyceride, Dibutyl Adipate, Diisopropyl Adipate, Dimethyl Isosorbide, Dipropylene Glycol, Ethanol, Ethoxydiglycol, Isoamyl Laurate, Isohexadecane, Isopentyl Diol, Isopropyl Myristate, Isopropyl Lauroyl Sarcosinate, Jojoba Oil, Meadowfoam Seed Oil, Mineral Oil, Neopentyl Glycol Diethylhexanoate, Octyldodecanol, Oleyl Alcohol, Pentylene Glycol, Phenylpropanol, Polysorbate 20, Propanediol, Safflower Seed Oil, Squalene, Sunflower Oil, t-Butyl Alcohol, Tributyl Citrate, O-Acetyl Citrate Tributyl Citrate, Tri-C 15~19 It is soluble in a solvent selected from the group consisting of alkyl, triethyl citrate, triethyl O-acetylcitrate, and triisostearin.

[0008] Therefore, in certain embodiments, the composition comprises an emulsion. Preferably, the emulsion is an oil / water emulsion. In certain embodiments, the composition further comprises dimethyl isosorbide. In certain embodiments, pectolina ligenin is dissolved in dimethyl isosorbide. The compositions of the present invention are stable under storage for at least three months. This is beneficial because the compositions of the present invention can be stored before being administered to a subject. In certain embodiments, the compositions of the present invention have less than about 20% degradation when stored at 4°C or 25°C for three months. In certain embodiments, the compositions of the present invention have less than about 30% degradation when stored at 40°C or 50°C for three months.

[0009] In certain embodiments, the composition contains pectolinigenin at a concentration of about 5 nM to about 2500 nM. In certain embodiments, pectolinigenin is present in the composition of the present invention at a concentration of about 0.0001% w / w to about 5.0% w / w. In certain other embodiments, pectolinigenin is present at a concentration of 0.0005% w / w to about 2.0% w / w. In certain other embodiments, pectolinigenin is present at a concentration of 0.0007% w / w to about 1.0% w / w. In certain other embodiments, pectolinigenin is present at a concentration of 0.001% w / w to about 0.75% w / w. In certain other embodiments, pectolinigenin is present at a concentration of 0.001% w / w to about 0.75% w / w. In certain other embodiments, pectolinaligenin is present at a concentration of approximately 0.5% w / w.

[0010] In certain embodiments, the compositions of the present invention can be administered to the target skin as topical compositions. The compositions of the present invention may be included in any formulation suitable for topical administration. In certain embodiments, the compositions of the present invention are fluids, emulsions, encapsulations, suspensions, solids, semi-solids, jellies, pastes, gels, hydrogels, ointments, lotions, emulsions, creams, foams, mousses, liquids, sprays, suspensions, dispersions, powders, aerosols, color cosmetics, and / or hair treatments. In certain embodiments, the compositions of the present invention also include additives. These additives may be selected from the group consisting of solvents, emulsifiers, preservatives, antioxidants, emollients, thickeners, penetration enhancers, surfactants, diluents, fillers, carriers, and / or pH control agents. In certain embodiments, the preservative in the composition is an antimicrobial preservative or a chelating agent. In certain embodiments, the solvent of the present invention is dimethyl isosorbide.

[0011] The compositions of the present invention can be prepared by a variety of methods. For example, the compositions can be prepared by dissolving or dispersing pectolina ligenin and optional additives provided herein in a carrier (e.g., water, saline solution, aqueous dextrose, glycerol, glycol, ethanol, or analogues) or solvent to form solutions, colloids, liposomes, emulsions, complexes (including inclusion complexes), coacervates, or suspensions. In certain embodiments, the compositions of the present invention may also contain additional additives such as wetting agents, emulsifiers, cosolvents, solubilizers, pH buffering agents, and analogues (e.g., sodium acetate, sodium citrate, cyclodextrins and derivatives, sorbitan monolaurate, triethanolamine acetate, triethanolamine oleate, hydroxyethylpiperazine, and analogues). In certain embodiments, the compositions of the present invention may further include one or more additional additives selected from the group consisting of carriers, additives, or diluents, including, but not limited to, absorbents, anti-irritants, antibacterial agents, anti-acne agents, antioxidants, colorants / pigments, moisturizers, emulsifiers, film-forming / retaining agents, fragrances, leave-on exfoliants, formula drugs, preservatives, scrub agents, silicones, skin-identical agents / skin-repairing agents, slip agents, sunscreen activators, surfactants / cleansing agents, penetration enhancers, and thickeners.

[0012] In certain embodiments, the composition of the present invention comprises pectolina ligenin and a preservative in an oil / water emulsion.

[0013] In certain embodiments, the composition of the present invention comprises pectolina ligenin in an oil / water emulsion, a solvent for solubilizing pectolina ligenin, and a preservative.

[0014] In certain embodiments, the composition of the present invention comprises pectolina ligenin in an oil / water emulsion, a solvent for solubilizing pectolina ligenin, a diluent, and a preservative.

[0015] In certain embodiments, the composition of the present invention comprises pectolina ligenin in an oil / water emulsion, a solvent for solubilizing pectolina ligenin, a thickener, a diluent if necessary, and a preservative.

[0016] In certain embodiments, the composition of the present invention comprises pectolina ligenin in an oil / water emulsion, a solvent for solubilizing pectolina ligenin, and one or more additives selected from the group consisting of diluents, absorbents, antioxidants, emollients, emulsifiers, thickeners, surfactants, and / or preservatives.

[0017] In certain embodiments, the additives included in the composition are: water, dimethyl isosorbide, glycerin, caprylic / capric triglyceride, propanediol, sunflower seed oil, ethoxydiglycol, squalane, sodium acrylate copolymer, cetearyl alcohol, phenoxyethanol, glyceryl stearate, capryloyl glycerin / sebacate copolymer, diheptyl succinate, naringenin, lecithin, decylene glycol, pentylene glycol, cetearyl glucoside, shea butter, palmitic acid, arachidyl alcohol, behenyl alcohol, arachidyl glucoside, phenethyl alcohol, 1,2-hexanediol, hydrogenated olive oil, olive (Olea europaea) fruit oil, olea The ingredients are unsponifiable europaea (olive) oil, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, citric acid, acetylated sodium hyaluronate, sodium hyaluronate crosspolymer, sodium phytate, hydrolyzed sodium hyaluronate, and / or ethylhexylglycerin.

[0018] In certain embodiments, the present invention provides that the compositions of the present invention are synergistic. The compositions provided by the present invention are beneficial because they enhance the stability of the components in the composition due to the synergistic effect, and have the resulting stability and efficacy. In certain embodiments, the present invention provides that the compositions of the present invention are more effective and stable compared to when administered or stored as individual components. The compositions of the present invention may also act synergistically when administered with other therapies for the treatment of the conditions described herein.

[0019] In certain embodiments of the present invention, a composition containing pectolinarigenin exhibits antioxidant activity. In certain embodiments, in the compositions of the present invention, the antioxidant activity of pectolinarigenin is demonstrated at a concentration of about 0.00005% w / w or higher. Advantageously, the compositions of the present invention containing pectolinarigenin that exhibits antioxidant activity are effective in treating and / or preventing oxidative damage. In certain embodiments, the compositions of the present invention containing pectolinarigenin that exhibits antioxidant activity are effective in treating skin and / or hair damaged by reactive oxygen species, and in protecting against other environmental aggressors that can damage the subject's skin. In certain other embodiments, the compositions of the present invention containing pectolinarigenin that exhibits antioxidant activity are effective in preventing skin and / or hair damage by reactive oxygen species, including damage caused by environmental aggressors.

[0020] In certain embodiments of the present invention, a composition comprising pectolinarigenin exhibits elastase enzyme inhibition. In certain embodiments, in the compositions of the present invention, the elastase enzyme inhibitory activity of pectolinarigenin is demonstrated at a concentration of about 0.005% w / w or higher. Advantageously, a composition comprising pectolinarigenin exhibiting elastase enzyme inhibitory activity is effective in promoting skin elasticity. In certain embodiments, the compositions of the present invention comprising pectolinarigenin exhibiting elastase enzyme inhibition are effective in reducing skin fine lines and / or wrinkles. In certain embodiments, the compositions of the present invention comprising pectolinarigenin exhibiting elastase enzyme inhibition are effective in preventing the formation of skin fine lines and / or wrinkles.

[0021] In certain embodiments of the present invention, a composition comprising pectolinarigenin exhibits glycation inhibition. In certain embodiments, in the compositions of the present invention, the glycation inhibitory activity of pectolinarigenin is demonstrated at a concentration of about 0.0005% w / w or higher. Advantageously, a composition comprising pectolinarigenin exhibiting glycation inhibitory activity is effective in supporting and promoting the resiliency of skin and / or hair.

[0022] In certain embodiments of the present invention, a composition comprising pectolinarigenin promotes skin lightening and / or brightening. In certain embodiments, a composition comprising pectolinarigenin at a concentration of at least 0.01% w / w has an L value (reflecting skin lightening) that is at least about 10% higher compared to skin treated with a corresponding composition without pectolinarigenin. In certain embodiments, a composition comprising pectolinarigenin at a concentration of at least 0.1% w / w has an L value that is about 4.6 units higher compared to skin treated with a corresponding composition without pectolinarigenin.

[0023] In certain embodiments of the present invention, a composition comprising pectolina ligenin modulates the expression of one or more genes related to a local condition. In certain embodiments, one or more genes are selected from the group consisting of (i) VCAN, (ii) COL1A2, (iii) MMP1, (iv) IL6, (v) IL23A, (vi) TLR2, and (vii) MMP3. In certain embodiments, administration of a composition comprising pectolina ligenin leads to upregulation of VCAN and / or COL1A2. In certain embodiments, administration of a composition comprising pectolina ligenin leads to downregulation of MMP1, MMP3, IL6, TLR2, and / or IL23A.

[0024] The VCAN gene plays a role in maintaining the skin barrier through interaction with extracellular matrix proteins. The COL1A2 gene is involved in regulating collagen expression. Increased collagen expression reduces wrinkles and sagging. The MMP1 gene is involved in regulating collagen degradation. Reduced collagen degradation improves the appearance of the skin. The IL6 gene plays a role in regulating inflammation, tissue atrophy, muscle loss, and / or melanin formation. Decreased IL6 expression reduces inflammation, tissue atrophy, muscle loss, and downregulates melanin formation. The IL23A gene plays a role in inflammation.

[0025] In certain embodiments, administration of a composition containing pectolina ligenin causes upregulation of one or more genes related to proteoglycans and collagen, which are barrier and extracellular matrix proteins. In certain embodiments of the present invention, administration of a composition containing pectolina ligenin leads to at least about 10-fold upregulation of one or more genes related to proteoglycans and collagen, which are barrier and extracellular matrix proteins.

[0026] In certain embodiments, administration of a composition containing pectolina ligenin induces downregulation of collagenase. In certain embodiments, administration of a composition containing pectolina ligenin leads to downregulation of many, or even about one-fifth, of one or more genes related to proteoglycans and collagen, which are barrier and extracellular matrix proteins.

[0027] In certain embodiments, administration of a composition containing pectolina ligenin downregulates the expression of inflammatory genes. In certain embodiments, administration of a composition containing pectolina ligenin leads to a downregulation of inflammatory gene expression to as little as 1 / 200th of its original level.

[0028] In certain embodiments, administration of a composition containing pectolina ligenin downmodulates proteins involved in the melaninogenesis signaling pathway. In certain embodiments, administration of a composition containing pectolina ligenin to a subject leads to the treatment or prevention of a local condition in the subject by modulation of the expression or activity levels of one or more genes that may be involved in the local condition. In certain embodiments, administration of a composition containing pectolina ligenin alters one or more functions associated with the modulated gene, where one or more functions are selected from the group consisting of (i) maintenance of the skin barrier, (ii) collagen expression, (iii) collagen degradation, (iv) inflammation, (v) tissue atrophy, (vi) muscle loss, and (vii) melanin production. [Brief explanation of the drawing]

[0029] [Figure 1A] Figure 1A is a photograph of a solution containing 0.5% w / w pectolina ligenin in an oil / water emulsion.

[0030] [Figure 1B] Figure 1B is a photograph of 1.03% w / w pectolina ligenin solubilized in dimethyl isosorbide.

[0031] [Figure 2]Figure 2 is a graph showing the stability of pectolina ligenin in dimethyl isosorbide.

[0032] [Figure 3] Figure 3 provides data on gene expression modulation. [Modes for carrying out the invention]

[0033] V. Detailed explanation Pectolinaligenin Pectolinarigenin is a flavone isolated from Cirsium (thistle). Pectolinarigenin is commonly used as an anti-inflammatory agent, acting as a COX-2 inhibitor and / or Nf-κB / Nrf2 pathway inhibitor. Feng et al., Pectolinarigenin Suppresses LPS-Induced Inflammatory Response in Macrophages and Attenuates DSS-Induced Colitis by Modulating the NF-κB / Nrf2 Signaling Pathway, Inflammation, 2022 Dec;45(6):2529-2543. The chemical structure of pectolinaligenin is provided below. [ka]

[0034] Pectolinaligenin can also be called 5,7-dihydroxy-6-methoxy-2-(4-methoxyphenyl)-4H-chromen-4-one.

[0035] The anti-inflammatory properties of pectolinarigenin have been evaluated, and the results indicate its potential use as a treatment for edema, allergic inflammation, and passive cutaneous anaphylaxis. Lim, et al. Anti-inflammatory activity of pectolinarigenin and pectolinarin isolated from Cirsium chanroenicum, Biol Pharm Bull. 2008 Nov;31(11):2063-2067.

[0036] Pectolinarigenin also exhibits protective properties in the nervous system. Acting as a neuroprotective agent, pectolinarigenin protects astrocytes from inflammatory toxicity. (Heimfarth et al., Neuroprotective and anti-inflammatory effect of pectolinarigenin, a flavonoid from Amazonian Aegiphila integrifolia (Jacq.), against lipopolysaccharide-induced inflammation in astrocytes via NFκB and MAPK pathways, Food Chem Toxicol. 2021 Nov; 157:112538.)

[0037] Furthermore, pectolinarigenin also induces apoptosis in melanoma cells and reduces melanoma metastasis by altering mitochondrial potential and altering the expression of apoptosis-related proteins. (Kumkarnjana et al., Anti-adipogenic effect of flavonoids from Chromolaena odorata leaves in 3T3-L1 adipocytes. J Integr Med., 2018 Nov;16(6):427-434.) Pectolinarigenin also inhibits tumor progression in osteosarcoma by inhibiting STAT3. (Zhang et al., Pectolinarigenin acts as a potential anti-osteosarcoma agent via mediating SHP-1 / JAK2 / STAT3 signaling. Biomed Pharmacother. 2022 Sep;153:113323.)

[0038] Pectolinarigenin also inhibits melanin synthesis and reduces SREBP-induced lipid biosynthesis, preventing fat accumulation in adipocytes and liver cancer cells. Lee et al., Pectolinarigenin, an aglycone of pectolinarin, has more potent inhibitory activities on melanogenesis than pectolinarin, Biochem Biophys Res Commun. 2017 Nov 4;493(1):765-772.

[0039] Pectolinaligenin composition In one embodiment, the present invention provides a composition comprising pectolinaligenin. In a particular embodiment, the present invention provides a composition comprising pectolinaligenin suitable for administration to the skin of a target.

[0040] The present invention recognizes that pectolinaligenin is poorly soluble or insoluble in water. The present invention also recognizes that pectolinaligenin is poorly soluble or insoluble in oils; for example, pectolinaligenin is insoluble in Helianthus annuus (sunflower) seed oil. The present invention recognizes that the solvent used to prepare the pectolinaligenin composition should be one of the solvents permitted for use in cosmetic formulations.

[0041] In certain embodiments, pectolinaligenin is 1,2-heptanediol, 1,2-hexanediol, 1,2-propanediol, butylene glycol, C 15~19 Alkanes, Capric / Caprylic Triglyceride, Dibutyl Adipate, Diisopropyl Adipate, Dimethyl Isosorbide, Dipropylene Glycol, Ethanol, Ethoxydiglycol, Isoamyl Laurate, Isohexadecane, Isopentyl Diol, Isopropyl Myristate, Isopropyl Lauroyl Sarcosinate, Jojoba Oil, Meadowfoam Seed Oil, Mineral Oil, Neopentyl Glycol Diethylhexanoate, Octyldodecanol, Oleyl Alcohol, Pentylene Glycol, Phenylpropanol, Polysorbate 20, Propanediol, Safflower Seed Oil, Squalene, Sunflower Oil, t-Butyl Alcohol, Tributyl Citrate, O-Acetyl Citrate Tributyl Citrate 15~19 It is soluble in a solvent selected from the group consisting of alkyl, triethyl citrate, triethyl O-acetylcitrate, and triisostearin.

[0042] In certain embodiments of the present invention, pectolina ligenin is dissolved in a solvent selected from the group consisting of dimethyl isosorbide, ethoxydiglycol, lauroyl sarcosinate isopropyl, pentylene glycol, propanediol, 1,2-hexanediol, and / or butylene glycol. In certain preferred embodiments, pectolina ligenin is dissolved in dimethyl isosorbide. Table 1 provides solubility data for pectolina ligenin in several solvents. [Table 1]

[0043] As is evident from the previously provided data, pectolina ligenin is soluble in dimethyl isosorbide. Figure 1B provides a photograph of a solution of pectolina ligenin dissolved in dimethyl isosorbide.

[0044] Therefore, in certain embodiments, the composition comprises an emulsion. Preferably, the emulsion is an oil / water emulsion. Figure 1B provides a photograph of pectolina ligenin formulated in an oil / water emulsion.

[0045] In certain embodiments, the composition further comprises dimethyl isosorbide. In certain embodiments, pectolina ligenin is dissolved in dimethyl isosorbide. The compositions of the present invention are stable under storage for at least three months. This is beneficial because the compositions of the present invention can be stored before being administered to a subject. In certain embodiments, the compositions of the present invention have less than about 20% degradation when stored at 4°C or 25°C for three months. In certain embodiments, the compositions of the present invention have less than about 30% degradation when stored at 40°C or 50°C for three months. Figure 2 provides data on the stability of pectolina ligenin dissolved in dimethyl isosorbide. The present invention beneficially provides that a pectolina ligenin solution dissolved in dimethyl isosorbide has increased solubility and storage stability. The increased solubility in dimethyl isosorbide is surprising and unexpected, as pectolina ligenin is insoluble in sunflower oil and other commonly used solvents.

[0046] In certain embodiments, the composition contains pectolinigenin at a concentration of about 5 nM to about 2500 nM. In certain embodiments, pectolinigenin is present in the composition of the present invention at a concentration of about 0.0001% w / w to about 5.0% w / w. In certain other embodiments, pectolinigenin is present at a concentration of 0.0005% w / w to about 2.0% w / w. In certain other embodiments, pectolinigenin is present at a concentration of 0.0007% w / w to about 1.0% w / w. In certain other embodiments, pectolinigenin is present at a concentration of 0.001% w / w to about 0.75% w / w. In certain other embodiments, pectolinigenin is present at a concentration of 0.001% w / w to about 0.75% w / w. In certain other embodiments, pectolinaligenin is present at a concentration of approximately 0.5% w / w.

[0047] In certain embodiments, the compositions of the present invention can be administered to the target skin as topical compositions. The compositions of the present invention may be included in any formulation suitable for topical administration. In certain embodiments, the compositions of the present invention are fluids, emulsions, capsules, suspensions, solids, semi-solids, jellies, pastes, gels, hydrogels, ointments, lotions, emulsions, creams, foams, mousses, liquids, sprays, suspensions, dispersions, powders, aerosols, colored cosmetics, and / or hair treatments. In certain embodiments, the compositions of the present invention also include additives. These additives may be selected from the group consisting of solvents, emulsifiers, preservatives, antioxidants, emollients, thickeners, penetration enhancers, surfactants, diluents, fillers, carriers, and / or pH control agents. In certain embodiments, the preservative in the composition is an antimicrobial preservative or a chelating agent. In certain embodiments, the solvent of the present invention is dimethyl isosorbide.

[0048] The compositions of the present invention can be prepared by a variety of methods. For example, the compositions can be prepared by dissolving or dispersing pectolina ligenin and optional additives provided herein in a carrier (e.g., water, saline solution, aqueous dextrose, glycerol, glycol, ethanol, or analogues) or solvent to form solutions, colloids, liposomes, emulsions, complexes (including inclusion complexes), coacervates, or suspensions. In certain embodiments, the compositions of the present invention may also contain auxiliary substances such as wetting agents, emulsifiers, cosolvents, solubilizers, pH buffering agents, and analogues (e.g., sodium acetate, sodium citrate, cyclodextrins and derivatives, sorbitan monolaurate, triethanolamine acetate, triethanolamine oleate, hydroxyethylpiperazine, and analogues). In certain embodiments, the compositions of the present invention may further include one or more additional additives selected from the group consisting of carriers, additives, or diluents, which include, but are not limited to, absorbents, anti-irritants, antibacterial agents, anti-acne agents, antioxidants, colorants / pigments, emollients (moisturizers), emulsifiers, film-forming / retaining agents, fragrances, leave-in exfoliants, formula drugs, preservatives, scrubs, silicones, skin homogenizers / skin repair agents, slippers, sunscreen activators, surfactants / cleansing agents, penetration enhancers, and thickeners.

[0049] Absorbents are substances added to topical products to absorb water-soluble and oil-soluble dissolved or finely dispersed substances. Topical absorbents can also be used as thickeners in a wide variety of formulations, including facial creams, lipsticks, shampoos, and calamine lotions. In some embodiments, the absorbent may include, but is not limited to, alcohols (ethyl alcohol, methanol, isopropyl alcohol, SD alcohol [especially denatured alcohol] and benzyl alcohol), alumina (aluminum oxide), aluminum chlorohydrate, aluminum hydroxide, magnesium aluminum silicate, aluminum silicate, aluminum starch octenyl succinate, aluminum sulfate, ammonium chloride, bentonite, bismuth oxychloride, boron nitride, calcium carbonate, carnauba wax, charcoal, china clay, clay, Copernicia cerifera wax, corn starch, fuller's earth, hydrolyzed corn starch, iron powder, kaolin, sodium lithium magnesium silicate, magnesium, magnesium carbonate, magnesium hydroxide, montmorillonite, nylon-12, rice starch, silica, silicate, silk powder, silt, sodium carbonate, sodium polyacrylate, and zeolite.

[0050] Anti-irritants are substances added to topical products to reduce inflammation, particularly inflammation resulting from the application of the product itself. Additives included as anti-irritants that perform the function of an anti-irritant or anti-inflammatory agent may have two or more functions. For example, many antioxidants also function as anti-irritants. In some embodiments, anti-irritants and / or antioxidants may include, but are not limited to, acacia senegal, acetylsalicylic acid, Achillea millefolium, adenosine, citric acid, adenosine triphosphate, Aloe barbadensis, Aloe barbadensis leaf juice extract, aloe extract, aloe juice, hydrogenated olive oil, hydrogenated palm oil glyceride, hydrolyzed silk, hydroquinone, aloe vera, and / or alpha-bisabolol.

[0051] In certain embodiments, the composition of the present invention may further include a humectant. Humidifiers (or moisturizers) are important cosmetic ingredients that prevent moisture loss and thereby retain the skin's natural moisture. Some humectants can also actively attract moisture. In certain embodiments, the humectant may be selected from the group consisting of sodium hyaluronate, acetylated sodium hyaluronate, hydrolyzed sodium hyaluronate, propylene glycol, hexylene glycol, and butylene glycol.

[0052] In certain embodiments, the composition of the present invention may further include a slip agent. The term “slip agent” is used to describe a variety of ingredients that can help other ingredients spread on the skin and penetrate the skin. Slip agents may also have moisturizing (hygroscopic) properties. In some embodiments, the slip agent may include amodimethicone, bis-PEG-18 methyl ether dimethylsilane, bis-phenylpropyl dimethicone, butylene glycol, cetyl dimethicone, cetyl dimethicone copolyol, cetyl PEG / PPG-10 / 1-dimethicone, cyclohexasiloxane, cyclomethicone, cyclopentasiloxane, cyclotetrasiloxane, decylene glycol, diisostearoyl trimethylolpropanesiloxysilicate, dimethicone, dimethicone copolyol, dimethicone crosspolymer, dimethiconol, dipropylene glycol, hexylene glycol, hydrolyzed silk, isododecane, methicone, methyl trimethicone, methylsilanol Nuronate, methylsilanol PEG-7 glyceryl cocoate, Good, PEG-10 dimethicone, PEG-10 dimethicone / vinyl dimethicone crosspolymer, PEG-12 dimethicone, PEG / PPG-18 / 18 dimethicone, PEG / PPG-20 / 15 dimethicone, pentylene glycol, phenyl trimethicone, polymethylsilsesquioxane, PPG-3 benzyl ether myristate, dimethylsilylated silica, silk powder, siloxane, simethicone, sorbitol, stearyl dimethicone, stearyl methicone, triethoxycaprylylsilane, trimethylsiloxysilicate, xylitol, and zinc stearate may be, but are not limited to, these.

[0053] In certain embodiments, the compositions of the present invention may further include diluents and / or carriers. Diluents and / or carriers may include, but are not limited to, polyethylene glycol (such as PEG200, PEG300, PEG400, PEG540, PEG600, PEG1450, or mixtures thereof) and coconut oil (such as propylene glycol dicaprate, coco-caprylate / caprate, propylene glycol dicaprylate / dicate, caprylic / capric acid triglyceride, caprylic / capric acid / laurate triglyceride, caprylic / capric acid / linoleic acid triglyceride, tricaprin, tricaprylin, glyceryl trioleate, neopentyl glycol dicaprylate / dicate, caprylic / capric acid / palmitic acid / stearic acid triglyceride (triglceride), or mixtures thereof).

[0054] In certain embodiments, the composition of the present invention may further include an emollient. An emollient is a flexible, waxy, lubricating, and thickening substance added to cosmetic / dermatological products that prevents moisture loss and has a softening and soothing effect on the skin. In some embodiments, the emollient may include 10-hydroxydecanoic acid, glyceryl acetylricinoleate, acetylated castor oil, acetylated hydrogenated cottonseed glyceride, acetylated lanolin, acetylated lanolin alcohol, acetylated palm kernel glyceride, agar, algal extract, algin, almond oil, squalane, squalene, α-glucan oligosaccharide, amodimethicone, Anacystis nidulans extract, apricot kernel oil, arachidic acid, arachidonic acid, arachidyl alcohol, arachidyl propionate, C 10~30 Cholesterol / lanosterol ester, C 12~15 Alkylbenzoate, C 12~18 Acid triglycerides, C 18~36Triglyceride, candelilla wax, Cannabis sativa L. oil, caprylic / capric triglyceride, caprylyl methicone, carrot oil, Carthamus tinctorius oil, Carya illinoensis oil, castor oil succinate isostearate, castor oil, Caulerpa taxifolia extract, and / or cephalin may be included, but are not limited thereto.

[0055] In certain embodiments, the compositions of the present invention can further include a film-forming / holding agent. A film-forming / holding agent is a substance added to cosmetic / dermatological products to help leave a flexible, adhesive, continuous film on the skin. This film has the property of binding to water and leaves a smooth feel on the skin. In some embodiments, the film-forming / holding agent includes acrylates, acrylate copolymers, acrylate / C 10~30Alkyl acrylate crosspolymer, acrylate / dimethicone copolymer, adipic acid / neopentyl glycol / trimellitic anhydride copolymer, allyl methacrylate crosspolymer, carnauba wax, cellulose gum, Copernicia cerifera wax, dextrin, diisopropyl adipate, glyceryl polymethacrylate, hydrolyzed wheat protein, hydroxyethylcellulose, locust bean, neopentyl glycol diheptanoate, PEG-40 hydrogenated castor oil, polyacrylamide, polyacrylate-17, polyglucuronic acid, polyglyceryl methacrylate, polyisobutene, polymethyl methacrylate, polyquaternium-10, polyquaternium compounds, polyvinyl alcohol, polyvinylpyrrolidone, propylene carbonate, P This may include, but is not limited to, VM / MA (polyvinyl methyl ether / maleic acid) decadien crosspolymer, PVP [poly(vinylpyrrolidone)] copolymer, PVP / dimethylaminoethyl methacrylate, sodium carbomer, sodium polyacrylate, styrene / acrylate copolymer, triethoxycaprylylsilane crosspolymer, VA (vinyl acetate) / crotonate, VA / crotonate copolymer, VP (vinylpyrrolidone) / eicosene copolymer, and VP / hexadecene copolymer.

[0056] In certain embodiments, the composition of the present invention may further include additives related to the fragrance of the formulation. The fragrance component is a single or blended volatile and / or fragrant vegetable oil (or synthetically derived oil) that imparts aroma and scent to the cosmetic / dermatological product. The level of fragrance used varies depending on the type of product. In some embodiments, the composition of the formulation may contain up to about 0.01% by weight of fragrance. In some embodiments, the fragrance (e.g., synthetic and fragrant plant extracts) may include: Acacia farnesiana extract, Aerocarpus santalinus, amyl cinnamate, amyl salicylate, amyris oil, Anethum graveolens, Angelica archangelica root oil, anisaldehyde, anise, balm mint extract, Peruvian balsam, bay leaf oil, bergamot oil, bitter orange blossom, bois de rose oil, bois oil, Boswellia carterii, butylphenyl methylpropional, cananga extract, Cananga odorata, cardamom, cedarwood, cherry extract, Citrus aurantifolia, Citrus aurantium, Citrus aurantium extract, Citrus medica limonium, clary oil, Commiphora myrrha extract, coriander, Cucurbitea Peponis, cyclamenaldehyde, dill extract, ethyl vanillin, eugenol, farnesol, farnesyl acetate, Ferula galbaniflua, fir needle oil, floral ozone, Foeniculum vulgare extract, frankincense extract, galbanum, Gardenia florida extract, grapefruit oil, guaiac wood, Guaiacum officinale, hedione, hexyl cinnamal, hyssop, Illicium vernum, Iris florentina extract, jasmine oil, Jasminium grandiflorum, jonquil extract, Laurus nobilis, lauryl lactate, lavandin oil, LavandulaThis may include, but is not limited to, angustifolia, Lavandula officinalis, lavender extract and oil, lemon, lemon balm, lemongrass oil, Levisticum officinale root extract, lime oil and extract, limonene, linalool, Litsea cubeba, mandarin orange oil or extract, marjoram, Melissa officinalis, Mentha piperita, Mentha spicata, Mentha viridis, menthol, menthone, menthoxypropanediol, and menthyl lactate.

[0057] In certain embodiments, the compositions of the present invention may further contain preservatives. Preservatives are substances that prevent bacterial, microbial, or fungal contamination of cosmetic / dermatological products, thereby increasing the shelf life of the product and consumer safety. Some of these agents also have stabilizing effects that can preserve the function of various active ingredients, including antioxidants (vitamins), emulsifiers, and surfactants. In some embodiments, preservatives include 1,2-hexanediol, benzoic acid, benzothonium chloride, borax, bronopol, butylparaben, caprylyl glycol, chlorophene, chloroxylenol, chlorphenesin, decylene glycol, dehydroacetic acid, diazolidinyl urea, DMDM ​​hydantoin, hydroxyacetophenone, ethylhexylglycerin, ethylparaben, formaldehyde-releasing preservatives, and Germaben. II may include, but is not limited to, thalene, imidazolidinyl urea, iodopropynyl butylcarbamate, isobutylparaben, methylchloroisothiazolinone, methyldibromoglutaronitrile, methylisothiazolinone, methylparaben, o-cymen-5-ol, phenoxyethanol, phenoxyisopropanol, phytosphingosine, polyaminopropyl biguanide, potassium sorbate, propylparaben, quaternium-15, sodium benzoate, sodium citrate, sodium dehydroacetate, sodium hexametaphosphate, sodium hydroxymethylglycinate, phenethyl alcohol, sodium lactobionate, sodium metabisulfite, sodium sulfite, sorbic acid, and styrax benzoin.

[0058] In certain embodiments of the present invention, the pharmaceutical composition is an emulsion. The emulsion composition of the present invention may further contain an emulsifier. An emulsifier is a substance added to cosmetic / dermatological products to help prevent dissimilar components (such as oil and water) from separating in the emulsion. There are two types of emulsifiers. Oil-in-water (o / w) emulsifiers trap oil droplets in water, while water-in-oil (w / o) emulsifiers trap water droplets in oil. W / O emulsifiers are used to create a fatty feel (e.g., night creams and sunscreens). O / W emulsifiers are often used in moisturizing products (e.g., body lotions and day creams).

[0059] In certain embodiments, the compositions of the present invention may further include surfactants. Surfactants are compounds that reduce surface tension or interfacial tension. By reducing surface tension, liquids spread more easily, while by reducing interfacial tension (interfacial tension meaning the space between two surfaces) between water and oil / lipids, they mix. Surfactants may be anionic, amphoteric, nonionic, and / or quaternary active substances. Surfactants may form the base of any personal cleansing product and may also have wetting, conditioning, degreasing, emulsifying, and thickening effects. In some embodiments, emulsifiers, surfactants, and detergents include ammonium laureth sulfate, ammonium lauryl sulfate, arachidyl glucoside, behenic acid, bis-PEG-18 methyl ether dimethylsilane, C 20~40Pareth-40, Cocamidopropyl Betaine, Cocamidopropyl Dimethylamine, Cocamidopropyl Hydroxysultaine, Coco-Glucoside, Coconut Oil, Decyl Glucoside, Dicetyl Phosphate, Dihydrocholeth-30, Disodium Cocoamphodiacetate, Disodium Cocoyl Glutamate, Disodium Lauraminopropionate, Glyceryl Behenate, Hydrogenated Vegetable Glycerides Citrate, Isohexadecane, Isostearamide DEA, Lauranhocarboxyglycinate, Laureth-23, Laureth-4, Laureth-7, Lauryl PEG-9 Polydimethylsiloxyethyl Dimethicone, Lauryl Alcohol, Lauryl Glucoside, Magnesium Laureth Sulfate, Magnesium Oleth Sulfate, Myristic Acid, Nonoxynol, Oleic Acid, Oleth-10, Palm Nucleic Acid, Palmitic Acid, PEG-60 Almond Glycerides, PEG-75 Shea Butter Glycerides, PEG 90M, PEG-10 Dimethicone, PEG-10 Dimethicone / Vinyl Dimethicone Crosspolymer, PEG-10 Rapeseed Sterol, PEG-100 Stearate, PEG-12 Dimethicone, PEG-120 Methyl Glucose Dioleate, PEG-20 Methyl Glucose Sesquistearate, PEG-40 Stearate, PEG-60 Hydrogenated Castor Oil, PEG-7 Glyceryl Cocoate, PEG-8, PEG-80 Sorbitan Laurate, PEG / PPG-17 / 6 Copolymer (Polyethylene Glycol / Polypropylene glycol-17 / 6 copolymer), PEG / PPG-18 / 18 dimethicone, PEG / PPG-20 / 15 dimethicone, poloxamer 184, poloxamer 407, poloxamer, polyglyceryl-3 beeswax, polyglyceryl-4 isostearate, polyglyceryl-6 isostearate, polysorbate 20, polysorbate 60, polysorbate 80, potassium cetyl phosphate, potassium hydroxide, potassium myristate, PPG-12 buteth-16, PPG-26 buteth-26, Salvia officinalis, Saponaria officinalis extract, soapwort, C 14~16This may include, but is not limited to, sodium olefin sulfonate, sodium cetearyl sulfate, sodium cocoamphoacetate, sodium cocoate, sodium cocoyl glutamate, sodium cocoyl isethionate, sodium dilauramidoglutamidolyninate, sodium hexametaphosphate, sodium hydroxide, sodium laureth sulfate, sodium laureth-13 carboxylate, sodium lauroamphoacetate, sodium lauroyl lactylate, sodium lauroyl sarcosinate, sodium lauryl glucose carboxylate, sodium lauryl sulfate, sodium cocoyl methyl taurate, sodium methyl taurate, sodium mireth sulfate, sodium palm nucleotide, sodium palmitate, sodium PEG-7 olive oil carboxylate, sodium trideceth sulfate, steareth-20, TEA lauryl sulfate (triethanolamine-lauryl sulfate), and tribehenin PEG-20 ester.

[0060] In certain embodiments, the composition of the present invention may further comprise one or more thickeners. Thickeners are substances added to cosmetic / dermatological products to enhance the consistency, volume, and viscosity of cosmetic products, thereby resulting in greater stability and better performance. While some thickeners also possess emulsifying or gelling properties, the majority of thickeners have the ability to retain moisture in the skin and therefore act as moisturizers. Thickeners may be entirely natural, such as waxes, but may also be synthetic or semi-synthetic. In some embodiments, the thickeners include acacia senegal, glyceryl acetylricinoleate, acetylated castor oil, hydrogenated acetylated cottonseed glyceride, acetylated palm kernel glyceride, acrylate / steareth-20 methacrylate copolymer, agar, Ahnfeltia concinna extract, Ahnfeltia extract, Alaria esculenta, algae, algal extract, algin, alkylamides, Althaea rosea, Althea officinalis, alumina, aluminum hydroxide, aluminum stearate, ammonium acryloyldimethyltaurate / VP copolymer, Anacystis nidulans extract, arachidic acid, arachidonic acid, arachidyl alcohol, arachidyl propionate, arrowroot, artemia extract, Ascophyllum nodosum, ascorbyl methylsilanol pectinate, Asparagopsis Armata extract, beeswax, behenic acid, behentrimonium chloride, behenyl alcohol, bis-diglyceryl polyacyladipate, bismuth oxychloride, C 12~15 Alkylbenzoate, C 12~18 Acid triglycerides, C 13~14 Isoparaffin, C 18~36Triglycerides, Candelilla wax, Caprylic / Capric triglycerides, Carbomer, Carbopol, Carnauba wax, Carrageenan, Caulerpa taxifolia extract, Cellulose, Cellulose gum, Cephalin, Cera Alba, Ceresin, Ceteareth-20, Cetearyl alcohol, Cetearyl ethylhexanoate, Cetearyl glucoside, Cetearyl octanoate, Cetyl alcohol, Cetyl dimethicone copolyol, Cetyl hydroxyethylcellulose, Cetyl palmitate, Cetyl PEG / PPG-10 / 1-dimethicone, Chlorella, Chondrus crispus, Cocamide DEA and MEA, Cocoglycerides, Codium tomentosum extract, Copernicia cerifera wax, Corallina This may include, but is not limited to, officinalis extract, Corallina, oleth-10 phosphate DEA, diethanolamine (DEA), di-PPG-3 myristyl ether adipate, dimethicone crosspolymer, dimethicone / vinyl dimethicone crosspolymer, polyacrylate crosspolymer, and / or dimer dilinoleyl dimer dilinoleate.

[0061] In certain embodiments, the composition of the present invention may further comprise one or more chelators. The chelating agent is one of a number of components that bind to metal ions or metal compounds, preventing them from adhering to surfaces (such as skin, hair, or clothing) or causing contamination, as in the case of trace amounts of iron. In some embodiments, the chelators may include, but are not limited to, tetrasodium EDTA, sodium phytate, and / or tetrahydroxypropylethylenediamine.

[0062] In certain embodiments, the additives included in the composition are: water, dimethyl isosorbide, glycerin, caprylic / capric triglyceride, propanediol, sunflower seed oil, ethoxydiglycol, squalane, sodium acrylate copolymer, cetearyl alcohol, phenoxyethanol, glyceryl stearate, capryloyl glycerin / sebacate copolymer, diheptyl succinate, naringenin, lecithin, decylene glycol, pentylene glycol, cetearyl glucoside, shea butter, palmitic acid, arachidyl alcohol, behenyl alcohol, arachidyl glucoside, phenethyl alcohol, 1,2-hexanediol, hydrogenated olive oil, olive (Olea europaea) fruit oil, olea The ingredients are europaea (olive) oil unsaponifiables, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, citric acid, acetylated sodium hyaluronate, sodium hyaluronate crosspolymer, sodium phytate, hydrolyzed sodium hyaluronate, and / or ethylhexylglycerin. Table 2 provides below a list of additives that may be used in exemplary compositions of the present invention, along with their approximate concentrations. [Table 2-1] [Table 2-2]

[0063] Pectolinaligenin for the treatment of local conditions

[0064] Advantageously, pectolinaligenin has been found to affect genes and signaling pathways involved in several local conditions. In one embodiment, the present invention provides a method of using compositions to treat, protect, and / or alter (e.g., improve) skin conditions and / or aesthetic appearance, including, for example, treating, preventing, improving, reducing and / or eliminating fine lines and / or wrinkles of the skin, and / or improving the aesthetic appearance of fine lines and / or wrinkles of the skin. In certain embodiments, the compositions of the present invention lead to increased resilience of skin and / or hair. In certain embodiments, the compositions of the present invention lead to increased elasticity of the skin. In certain embodiments, the compositions of the present invention prevent skin damage.

[0065] In one embodiment, the present invention comprises a composition for topical administration comprising an effective amount of pectolinaligenin. An effective amount of pectolinaligenin is an amount of pectolinaligenin that is effective in treating, improving or otherwise affecting the underlying condition of the skin.

[0066] In certain embodiments of the present invention, compositions comprising pectolina ligenin promote skin whitening and / or brightening. In certain embodiments, a composition comprising pectolina ligenin at a concentration of at least 0.01% w / w has an L value (reflecting skin whitening) at least about 10% higher than skin treated with a corresponding composition that does not contain pectolina ligenin. In certain embodiments, a composition comprising pectolina ligenin at a concentration of at least 0.1% w / w has an L value about 4.6 units higher than skin treated with a corresponding composition that does not contain pectolina ligenin.

[0067] In one embodiment, the present invention provides a method for skin whitening and / or brightening by administering a composition comprising pectolina ligenin. As demonstrated by the data provided in Example 2, skin tissue treated with compositions comprising 0.1% (w / w) and 0.01% (w / w) pectolina ligenin was 4.65 and 4.01, respectively, compared to tissue treated with a solvent. Therefore, compositions comprising pectolina ligenin are beneficial for skin whitening and / or brightening.

[0068] In certain embodiments of the present invention, compositions comprising pectolina ligenin exhibit antioxidant activity. In certain embodiments, the antioxidant activity of pectolina ligenin in the compositions of the present invention is demonstrated at concentrations of about 0.00005% w / w or higher. Advantageously, compositions of the present invention comprising pectolina ligenin exhibiting antioxidant activity are effective in treating and / or preventing oxidative damage. In certain embodiments, compositions of the present invention comprising pectolina ligenin exhibiting antioxidant activity are effective in treating skin and / or hair damaged by reactive oxygen species, as well as protecting the skin in question from other environmentally aggressive factors that may cause damage. In certain other embodiments, compositions of the present invention comprising pectolina ligenin exhibiting antioxidant activity are effective in preventing skin and / or hair damage caused by reactive oxygen species, including damage caused by environmentally aggressive factors.

[0069] As demonstrated by the data provided in Examples 3 and 4, compositions containing pectolina ligenin are effective in exhibiting robust antioxidant activity in both aqueous and organic solvent systems. The calculated IC50 values ​​of antioxidant activity in aqueous and organic solvent systems were 0.00027% w / w and 0.044%, respectively. These results demonstrate that compositions containing pectolina ligenin possess robust antioxidant activity.

[0070] In certain embodiments of the present invention, compositions comprising pectolina ligenin exhibit elastase enzyme inhibition. In certain embodiments, the elastase enzyme inhibitory activity of pectolina ligenin in the compositions of the present invention is demonstrated at concentrations of about 0.005% w / w or higher. As is evident from the data provided in Example 4, compositions comprising pectolina ligenin have robust elastase enzyme inhibitory activity. In fact, the calculated IC50 value for the elastase enzyme inhibitory activity of pectolina ligenin was 0.016%.

[0071] Advantageously, compositions containing pectolina ligenin exhibiting elastase enzyme inhibitory activity are effective in promoting skin elasticity. In certain embodiments, compositions of the present invention containing pectolina ligenin exhibiting elastase enzyme inhibitory activity are effective in reducing fine lines and / or wrinkles of the skin. In certain embodiments, compositions of the present invention containing pectolina ligenin exhibiting elastase enzyme inhibitory activity are effective in preventing the formation of fine lines and / or wrinkles of the skin.

[0072] In certain embodiments of the present invention, compositions containing pectolina ligenin exhibit glycation inhibition. In certain embodiments, the glycation inhibitory activity of pectolina ligenin in the compositions of the present invention is demonstrated at concentrations of about 0.0005% w / w or higher. As is evident from the data provided in Example 5, compositions containing pectolina ligenin have robust glycation inhibition. In fact, the IC50 for glycation inhibition by compositions containing pectolina ligenin was calculated. 50 The value is 0.002%. Advantageously, compositions containing pectolina ligenin, which exhibits glycation inhibitory activity, are effective in supporting and promoting the restorative power of skin and / or hair.

[0073] Modulation of gene expression and / or activity In certain embodiments of the present invention, a composition comprising pectolina ligenin modulates the expression of one or more genes related to a local condition. In certain embodiments, one or more genes are selected from the group consisting of (i) VCAN, (ii) COL1A2, (iii) MMP1, (iv) IL6, (v) IL23A, (vi) TLR2, and (vii) MMP3. In certain embodiments, administration of a composition comprising pectolina ligenin leads to upregulation of VCAN and / or COL1A2. In certain embodiments, administration of a composition comprising pectolina ligenin leads to downregulation of MMP1, MMP3, IL6, TLR2, and / or IL23A.

[0074] Advantageously, compositions containing pectolina ligenin have been found to affect the expression and / or activity of genes involved in pathways that maintain skin condition. In certain embodiments, administration of a composition containing pectolina ligenin affects the expression and / or activity of genes selected from the group consisting of (i) VCAN, (ii) COL1A2, (iii) MMP1, (iv) IL6, (v) IL23A, (vi) TLR2, and (vii) MMP3.

[0075] The VCAN (versican) gene plays a role in maintaining the skin barrier through interaction with extracellular matrix proteins. The VCAN gene is involved in the expression of the versican protein. Versican is a type of protein known as a proteoglycan, which means that multiple sugar molecules are bound to a protein. Versican is found in the extracellular matrix of many different tissues and organs. The extracellular matrix is ​​a complex lattice of proteins and other molecules formed in the intercellular space. Versican interacts with many proteins and molecules to promote the assembly of the extracellular matrix and ensure its stability. As demonstrated in the data provided in Figure 3, administration of pectolina ligenin resulted in an approximately 10-fold increase in VCAN expression. This upregulation of VCAN led to increased skin barrier strength, which demonstrates the anti-aging effect of pectolina ligenin.

[0076] The COL1A2 (Type I collagen alpha-2 chain) gene encodes a pro-alpha-2 chain of Type I collagen, whose triple helix contains two alpha-1 chains and one alpha-2 chain. Type I is the fibrogenic collagen found in most connective tissues and is abundant in bone, cornea, dermis, and tendons. The COL1A2 gene is involved in regulating collagen expression. Increased collagen expression reduces wrinkles and sagging. As demonstrated in the data provided in Figure 3, administration of pectolina ligenin resulted in an approximately 14-fold increase in COL1A2 expression. This upregulation of COL1A2 leads to increased collagen production, which is involved in maintaining skin strength and integrity.

[0077] MMP1 (matrix metallopeptidase 1) encodes a member of the M10 family of matrix metalloproteinases (MMPs). Proteins in this family are involved in the degradation of the extracellular matrix in normal physiological processes such as embryonic development, reproduction, and tissue remodeling, as well as in disease processes such as arthritis and metastasis. The encoded preproprotein is processed by proteolysis to produce a mature protease. This secreted protease degrades interstitial collagen, including types I, II, and III. This gene is part of the MMP gene cluster on chromosome 11. Therefore, MMP1 is involved in collagen degradation. A reduction in collagen degradation improves the appearance of the skin. As demonstrated in the data provided in Figure 3, administration of pectolina ligenin caused a reduction in MMP1 expression to approximately one-fifth. This reduction in MMP1 expression results in a decrease in the rate of collagen degradation, which is involved in maintaining skin strength and integrity.

[0078] MMP3 (matrix metallopeptidase 3) encodes matrix metalloproteinase-3, an enzyme involved in the degradation of type II, III, IV, IX, and X collagen, proteoglycans, fibronectin, laminin, and elastin. MMP3 is also a protein of the matrix metalloproteinase (MMP) family. Proteins of this family are involved in the degradation of the extracellular matrix in normal physiological processes such as embryonic development, reproduction, and tissue remodeling, as well as in disease processes such as arthritis and metastasis. The encoded preproprotein is processed by proteolysis to produce a mature protease. This secreted protease degrades interstitial collagen, including types I, II, and III. This gene is part of the MMP gene cluster on chromosome 11. Therefore, MMP3 is also involved in collagen degradation. As demonstrated by the data provided in Figure 3, administration of pectolina ligenin caused a reduction in MMP3 expression to approximately 1 / 20th. This decrease in MMP3 expression leads to a reduction in the rate of collagen degradation, which is involved in maintaining skin strength and integrity.

[0079] The IL6 (interleukin-6) gene encodes a cytokine that functions in inflammation and B cell maturation. In addition, the encoded protein has been shown to be an endogenous pyrogen that can induce fever in individuals with autoimmune diseases or infections. This protein is primarily produced at acute and chronic inflammation sites, where it is secreted into the serum and triggers a transcriptional inflammatory response via the interleukin-6 receptor alpha. This gene plays a role in regulating inflammation, tissue atrophy, muscle loss, and / or melanin formation. A decrease in IL6 expression reduces inflammation, tissue atrophy, muscle loss, and downregulates melanin formation. As demonstrated by the data provided in Figure 3, administration of pectolina ligenin caused a reduction in IL6 expression to approximately 1 / 200th. This reduction in IL6 expression leads to a decrease in the inflammatory activity of this gene. These results indicate that pectolina ligenin possesses potent anti-inflammatory activity.

[0080] The IL23A (interleukin-23 subunit alpha) gene also plays a role in inflammation. This gene encodes a subunit of the heterodimeric cytokine interleukin-23 (IL23). IL23 is composed of this protein and the p40 subunit of interleukin-12 (IL12B). The receptor for IL23 is formed by the beta-1 subunit of IL12 (IL12RB1) and the IL23-specific subunit, IL23R. Both IL23 and IL12 can activate the transcription activator STAT4 and stimulate the production of interferon-gamma (IFNG), in contrast to IL12, which primarily acts on naive CD4(+) T cells. As demonstrated by the data provided in Figure 3, administration of pectolina ligenin caused a reduction in IL23A expression to approximately one-quarter. This reduction in IL23A expression leads to a decrease in the inflammatory activity of this gene. These results indicate that pectolina ligenin possesses potent anti-inflammatory activity.

[0081] The TLR2 (Toll-like receptor 2) gene encodes a protein that is a member of the Toll-like receptor (TLR) family, which plays a fundamental role in pathogen recognition and activation of innate immunity. TLRs are highly conserved from Drosophila to humans and share structural and functional similarities. This protein is a cell surface protein that can form heterodimers with other TLR family members to recognize conserved molecules from microorganisms known as pathogen-associated molecular patterns (PAMPs). Activation of TLRs by PAMPs leads to upregulation of signaling pathways that modulate the host inflammatory response. Therefore, TLR2 is also involved in the inflammatory pathway. As demonstrated in the data provided in Figure 3, administration of pectolina ligenin caused a reduction in TLR2 expression to approximately one-fifth. This reduction in TLR2 expression leads to a decrease in the inflammatory activity of this gene. These results indicate that pectolina ligenin has potent anti-inflammatory activity.

[0082] In certain embodiments, administration of a composition containing pectolina ligenin causes upregulation of one or more genes related to proteoglycans and collagen, which are barrier and extracellular matrix proteins. In certain embodiments of the present invention, administration of a composition containing pectolina ligenin leads to at least about 10-fold upregulation of one or more genes related to proteoglycans and collagen, which are barrier and extracellular matrix proteins.

[0083] In certain embodiments, administration of a composition containing pectolina ligenin induces downregulation of collagenase. In certain embodiments, administration of a composition containing pectolina ligenin leads to downregulation of many, or even about one-fifth, of one or more genes related to proteoglycans and collagen, which are barrier and extracellular matrix proteins.

[0084] In certain embodiments, administration of a composition containing pectolina ligenin downregulates the expression of inflammatory genes. In certain embodiments, administration of a composition containing pectolina ligenin leads to a downregulation of inflammatory gene expression to as little as 1 / 200th of its original level.

[0085] In certain embodiments, administration of a composition containing pectolina ligenin downmodulates proteins involved in the melaninogenesis signaling pathway. In certain embodiments, administration of a composition containing pectolina ligenin to a subject leads to the treatment or prevention of a local condition in the subject by modulation of the expression or activity levels of one or more genes that may be involved in the local condition. In certain embodiments, administration of a composition containing pectolina ligenin alters one or more functions associated with the modulated gene, where one or more functions are selected from the group consisting of (i) maintenance of the skin barrier, (ii) collagen expression, (iii) collagen degradation, (iv) inflammation, (v) tissue atrophy, (vi) muscle loss, and (vii) melanin production.

[0086] Treatment of local conditions The present invention recognizes that compositions comprising pectolinaligenin are beneficial for treating, protecting, and / or improving the condition and / or aesthetic appearance of the skin. For example, compositions of the present invention may be effective in altering the aesthetic appearance of skin associated with or affected by fine lines and / or wrinkles caused, for example, cellular aging, environmental damage, or skin sunstroke, or in treating or preventing such fine lines and / or wrinkles on such skin. The present invention also provides methods for stimulating skin cell regeneration, increasing cell or tissue regeneration, promoting fibroblast proliferation, synthesizing elastin, collagen, proteoglycans, and / or new connective tissue, thereby reducing or improving the appearance of wrinkles and restoring skin elasticity, resilience, and / or suppleness.

[0087] The compositions of the present invention provided herein may be useful in improving the aesthetic appearance of the skin. Such improvements may include, but are not limited to, any externally visual and tactilely perceptible signs of skin aging and damage, as well as all other macro or micro effects. Such signs and effects may be induced or caused by internal and / or external factors, such as natural aging, environmental damage, climate, sun (UV) exposure, smoking, drugs, alcohol consumption, jet lag, night shifts, changes in circadian rhythms, pregnancy, menopause, genetic factors, nutritional factors and / or malnutrition, dehydration, stress, allergies (e.g., to plants, animals, drug therapy, and other substances), exposure to industrial and / or household chemicals, indoor heating and cooling, various disorders and diseases such as arteriosclerosis, diabetes, heart disease, liver disease, and obesity, thinning of the outer layer of skin, decrease in the number of pigment-containing cells, increase in the size of pigment-containing cells, changes in connective tissue, and decreased strength and elasticity of the skin.

[0088] The aesthetic appearance of the skin can be improved by improving the appearance of skin associated with or affected by one or more of the following: wrinkles, dry skin, sensitive skin, sagging, acne, vitiligo (a skin condition in which brown (pigmentation) is lost from certain areas of the skin), fine lines, sagging skin, dermal thinning, collagen fiber breakdown, loose skin, thinned skin, and skin exposed to ultraviolet radiation. In some embodiments, compositions of the present invention can improve the aesthetic appearance of the skin by reducing the appearance of fine lines on the skin, creating a more youthful skin appearance, reducing bag and / or ring around the eyes, increasing or repairing skin elasticity, resilience and / or suppleness, increasing the apparent thickness, elasticity, flexibility, radiance, glow and plumpness of the skin, improving skin texture, improving the appearance of wrinkled, linear, dry, scaly, aged and / or photodamaged skin, treating or preventing photodamaged skin, reducing signs of skin aging, reducing the appearance of hyperpigmentation, treating or preventing hyperpigmentation, treating or preventing skin pigmentation (e.g., caused by UV exposure), reducing the appearance of skin discoloration, and lightening and / or decolorizing the skin.

[0089] In certain embodiments, the composition can be used in facial or body skin care, treatment, cleansing, and / or protective products, anti-wrinkle or anti-aging compositions, skin-tightening compositions, skin-whitening compositions, compositions for rough skin, sunscreen compositions, self-tanning compositions or after-sun care compositions, scalp care compositions, shaving preparation compositions, hair removal compositions, or makeup products for facial or body skin.

[0090] In certain embodiments, compositions comprising pectolinaligenin are administered to alter the aesthetic appearance of skin associated with or affected by skin conditions / disorders (e.g., skin conditions / disorders involving loss of skin elasticity), or to treat or prevent such skin conditions / disorders.

[0091] In certain embodiments, compositions containing pectolinaligenin are administered to improve the skin's barrier function and viability.

[0092] In certain embodiments, a composition comprising pectolinaligenin is administered to alter the aesthetic appearance of skin associated with or affected by wrinkles, sagging, and / or loss of skin elasticity.

[0093] In certain embodiments, compositions comprising pectolinaligenin are administered to alter the aesthetic appearance of skin related to or affected by deterioration of skin viscoelasticity.

[0094] In certain embodiments, compositions comprising pectolinaligenin are administered to alter the aesthetic appearance of skin associated with or affected by one or more of the following: wrinkles and / or fine lines, sagging skin, loss of skin elasticity and / or tension, thinning of the dermis, breakdown of collagen fibers, sagging skin, thinned skin, and internal deterioration of the skin after exposure to ultraviolet radiation.

[0095] In certain embodiments, a composition containing pectolinaligenin is administered to reduce the appearance of fine lines and / or wrinkles on the skin.

[0096] In certain embodiments, a composition comprising pectolinaligenin is administered to reduce the appearance of sagging and / or dark circles around the eyes.

[0097] In certain embodiments, a composition containing pectolinaligenin is administered to reduce the appearance of hyperpigmentation.

[0098] In certain embodiments, a composition comprising pectolinaligenin is administered to improve or increase one or more of the thickness, elasticity, flexibility, radiance, luster, and fullness of the skin.

[0099] In certain embodiments, a composition containing pectolinaligenin is administered to improve the fineness of the skin texture.

[0100] In certain embodiments, compositions comprising pectolinaligenin are administered to improve the appearance of wrinkled, fringed, dry, scaly, aged, or photodamaged skin.

[0101] In certain embodiments, a composition comprising pectolinaligenin is administered to alter the aesthetic appearance of skin related to or affected by skin discoloration.

[0102] Method of administration In one embodiment, the present invention provides a method for administering a composition comprising pectolinaligenin. In a particular embodiment, the composition of the present invention is designed for topical administration.

[0103] In certain embodiments, the compositions of the present invention can be administered to the target skin as topical compositions. The compositions of the present invention may be included in any formulation suitable for topical administration. In certain embodiments, the compositions of the present invention may be fluids, emulsions, capsules, suspensions, solids, semi-solids, jellies, pastes, gels, hydrogels, ointments, lotions, emulsions, creams, foams, mousses, liquids, sprays, suspensions, dispersions, powders, aerosols, colored cosmetics, and / or hair treatments.

[0104] In certain other embodiments, compositions comprising pectolinaligenin may be prepared and used in the form of aerosol sprays, creams, emulsions, solids, liquids, dispersions, foams, oils, gels, lotions, mousses, ointments, powders, patches, pomades, solutions, pump sprays, sticks, wet wipes (towelettes), soaps, or other forms commonly used in the field of topical administration and / or cosmetic and skincare formulations. The compositions may also be in emulsion form. In addition, the compounds provided herein for use in the compositions provided herein may be used in colored cosmetic compositions such as foundation makeup, blush, eyeshadow, mascara, concealer, eyeliner, lip color, and nail color. Other cosmetic compositions may include perfumes, lipsticks, manicures and pedicures, eye makeup and face makeup, wet wipes, deodorants, hand sanitizers, baby products, bath oils, bubble baths, and butters.

[0105] In a particular embodiment, the composition containing pectolinaligenin is approximately 1.0 μg / cm³ 2 ~Approx. 100μg / cm 2 It is administered to the area.

[0106] In certain embodiments, the composition containing pectolinaligenin is administered over a period of time until the desired effect in improving or preventing a local condition is achieved. In certain embodiments, the composition containing pectolinaligenin contains an effective amount of pectolinaligenin. An effective amount of pectolinaligenin is the amount of pectolinaligenin that produces the desired result in the skin condition. In certain embodiments, the composition containing pectolinaligenin is administered once daily. In certain embodiments, the composition containing pectolinaligenin is administered twice daily. In certain embodiments, the composition containing pectolinaligenin is administered three times daily. In certain embodiments, the composition containing pectolinaligenin is administered once every two days. In certain embodiments, the composition containing pectolinaligenin is administered once every three days. [Examples]

[0107] (Example 1) Exemplary compositions containing pectolinaligenin Table 3 provides exemplary formulations of pectolinaligenin. [Table 3-1] [Table 3-2]

[0108] (Example 2) Preclinical analysis of the whitening and / or brightening effects of compositions containing pectolinaligenin.

[0109] This experiment was designed to evaluate the effects of compositions containing pectolina ligenin on skin whitening and / or brightening. In preclinical analyses performed in vitro on skin tissue, compositions containing pectolina ligenin resulted in skin whitening and / or brightening. [Table 4]

[0110] As is evident from the data provided in Table 4, skin tissues treated with compositions containing 0.1% and 0.01% pectolinaligenin scored 4.65 and 4.01, respectively, compared to skin tissue samples treated with the solvent.

[0111] (Example 3) ABTS Antioxidant Assay The 2,2'-azinobis[3-ethylbenzothiazoline-6-sulfonic acid]-diammonium salt (ABTS) antioxidant assay is designed to evaluate the antioxidant activity of compositions containing pectolina ligenin in an aqueous medium.

[0112] An ABTS+ solution was prepared as a free radical and used to measure the relative ability of the compound to capture the free radical. The decrease in absorbance at 734 nm was standardized against a solvent control as an indicator of ABTS+ capture. Table 5, provided below, shows the results of these experiments. [Table 5]

[0113] As is evident from the results provided in Table 5 above, compositions containing pectolina ligenin exhibit antioxidant activity at a low concentration of 0.00008% w / w in aqueous systems. Calculated IC 50 The value is 0.00027%w / w.

[0114] (Example 4) DPPH Antioxidant Activity Assay The 2,2-diphenyl-1-picrylhydrazyl (DPPH) antioxidant assay is designed to evaluate the antioxidant activity of compositions containing pectolina ligenin in organic media.

[0115] 2,2-diphenyl-1-picrylhydrazyl (DPPH) is a stable free radical used to evaluate the free radical scavenging ability of materials. DPPH is reduced in the presence of an antioxidant, thereby forming a colorless solution. The decrease in absorbance at 517 nm is standardized against a solvent control as an indicator of DPPH scavenging.

[0116] Table 6, provided below, provides antioxidant activity data. [Table 6]

[0117] As is evident from the results provided in Table 6 above, compositions containing pectolina ligenin exhibit antioxidant activity at a low concentration of 0.007% w / w in organic solvent systems. Calculated IC 50 The value is 0.0044%w / w.

[0118] (Example 5) Elastase enzyme inhibition This assay was performed to evaluate the elastase enzyme inhibitory activity of compositions containing pectolina ligenin.

[0119] Neutrophil infiltration and neutrophil elastase both increase in the skin in response to UV stress. Neutrophil elastase has been shown to activate MMP-1 and MMP-2 collagenases in response to low-dose UV exposure, damaging the extracellular matrix and contributing to photoaging and wrinkle formation. Elastase activity may be further upregulated in the presence of reactive oxygen species. Therefore, inhibition of this enzyme, especially in combination with antioxidant activity, is effective in delaying wrinkle formation and helping to maintain skin integrity. This assay can quantify 4-nitroaniline release from Me-Suc-Ala-Ala-Pro-Val-pNA by human neutrophil elastase at 405 nm by comparing it with a solvent control. Table 7 shows the elastase inhibitory activity of compositions containing pectolina ligenin. [Table 7-1] [Table 7-2]

[0120] As is evident from the data provided in Table 7, compositions containing pectolina ligenin inhibit elastase enzyme activity at a low concentration of 0.008% w / w. The calculated IC50 for elastase inhibitory activity was 0.016%.

[0121] (Example 6) Glycation inhibition assay This assay was performed to evaluate the glycation inhibitory activity of compositions containing pectolina ligenin.

[0122] Non-enzymatic glycation can occur when glucose reacts with proteins to form Schiff base intermediates, which then undergo Amadori rearrangement to form glycated proteins, which react with skin proteins to form advanced glycation end products (AGEs). AGE formation can lead to loss of skin elasticity and damage to cellular function. The glycation inhibitory activity of compounds is measured by the change in fluorescence at 360 nm / 420 nm excitation / emission relative to a solvent control.

[0123] Table 8 provides data on glycation inhibition. [Table 8]

[0124] As is evident from the data provided in Table 8, compositions containing pectolina ligenin inhibit glycation at a low concentration of 0.0007% w / w. The calculated IC for glycation inhibition 50 The value is 0.002%.

[0125] Embedding by reference Throughout this disclosure, references and citations are made to other documents, including patents, patent applications, patent publications, articles, books, papers, web content, and publicly available databases. All such documents are incorporated herein by reference in their entirety for any purpose.

[0126] Equal parts In addition to those shown and described herein, various modifications of the invention and many further embodiments will be apparent to those skilled in the art from the entirety of this document, including references to the scientific and patent documents cited herein. The subject matter of this specification includes important information, examples, and guidance that can be adapted to the practice of the invention in various embodiments and equivalents of the invention.

Claims

1. A composition for topical administration containing an effective amount of pectolinaligenin.

2. The composition according to claim 1, comprising an emulsion.

3. The composition according to claim 2, wherein the emulsion is an oil / water emulsion.

4. The composition according to claim 1, further comprising dimethyl isosorbide.

5. The composition according to claim 1, wherein the pectolinaligenin is dissolved in dimethyl isosorbide.

6. The composition according to claim 5, which is stable under storage conditions for at least three months.

7. The composition according to claim 5, which exhibits less than approximately 20% degradation when stored at 4°C or 25°C for three months.

8. The composition according to claim 5, which exhibits less than approximately 30% degradation when stored at 40°C or 50°C for three months.

9. The composition according to claim 1, wherein the pectolinaligenin is present in a concentration of about 0.0001% w / w to about 5.0% w / w.

10. The composition according to claim 1, wherein the pectolinaligenin is present in a concentration of about 0.0005% w / w to about 2.0% w / w.

11. The composition according to claim 1, wherein the pectolinaligenin is present at a concentration of 0.0007% w / w to about 1.0% w / w.

12. The composition according to claim 1, wherein the pectolinaligenin is present in a concentration of about 0.001% w / w to about 0.75% w / w.

13. The composition according to claim 1, wherein pectolinaligenin is present at a concentration of about 0.5% w / w.

14. The composition according to claim 1, selected from the group consisting of fluids, emulsions, capsules, suspensions, solids, semi-solids, jellies, pastes, gels, hydrogels, ointments, lotions, emulsions, creams, foams, mousses, liquids, sprays, suspensions, dispersions, powders, aerosols, colored cosmetics, hair treatments, and any combination thereof.

15. The composition according to claim 1, further comprising one or more additives selected from the group consisting of solvents, emulsifiers, preservatives, antioxidants, emollients, thickeners, penetration enhancers, surfactants, diluents, fillers, carriers, and / or pH control agents.

16. The composition according to claim 15, wherein the preservative is an antimicrobial preservative or a chelating agent.

17. The composition according to claim 15, wherein the solvent is dimethyl isosorbide.

18. Water, Dimethyl Isosorbide, Glycerin, Caprylic / Capric Triglyceride, Propanediol, Sunflower Seed Oil, Ethoxydiglycol, Squalane, Sodium Acrylate Copolymer, Cetearyl Alcohol, Phenoxyethanol, Glyceryl Stearate, Capryloyl Glycerin / Sebacate Copolymer, Diheptyl Succinate, Naringenin, Lecithin, Decylene Glycol, Pentylene Glycol, Cetearyl Glucoside, Shea Butter, Palmitic Acid, Arachidyl Alcohol, Behenyl Alcohol, Arachidyl Glucoside, Phenethyl Alcohol, 1,2-Hexanediol, Hydrogenated Olive Oil, Olea Europaea (Olive) Fruit Oil, Olea The composition according to claim 1, further comprising one or more additives selected from the group consisting of europaea (olive) oil unsaponifiables, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, citric acid, acetylated sodium hyaluronate, sodium hyaluronate crosspolymer, sodium phytate, hydrolyzed sodium hyaluronate, and ethylhexylglycerin.

19. The composition according to claim 1, comprising about 50% to about 70% (w / w) of water and about 10% to about 30% (w / w) of dimethyl isosorbide.

20. below: Table 9-1 Table 9-2 The composition according to claim 1.

21. A method for treating or preventing a local condition in a subject by administering a composition containing an effective amount of pectolinaligenin.

22. The method according to claim 21, wherein administration of the composition prevents wrinkles (lines) or wrinkles (wrinkles) in the skin of the subject.

23. The method according to claim 21, wherein administration of the composition leads to supporting the firmness and elasticity of the skin of the subject.

24. The method according to claim 21, wherein administration of the composition leads to the prevention of skin and hair damage caused by reactive oxygen species.

25. The method according to claim 21, wherein administration of the composition leads to protection of the skin from environmentally aggressive factors.

26. The method according to claim 21, wherein the administration of the composition leads to supporting skin elasticity.

27. The method according to claim 21, wherein the local state is glycation.

28. The method according to claim 21, wherein administration of the composition leads to an increase in the resilience of the skin and / or hair.

29. The method according to claim 21, wherein administration of the composition leads to an increase in skin elasticity.

30. The method according to claim 21, wherein the administration of the composition leads to the prevention of skin damage.

31. The method according to claim 21, wherein the composition is administered topically.

32. The method according to claim 21, wherein the composition comprises an emulsion.

33. The method according to claim 32, wherein the emulsion is an oil / water emulsion.

34. The method according to claim 21, wherein the composition further comprises dimethyl isosorbide.

35. The method according to claim 21, wherein the pectolinaligenin is dissolved in dimethyl isosorbide.

36. The method according to claim 35, wherein the composition is stable under storage conditions for at least three months.

37. The method according to claim 35, wherein the composition undergoes less than 20% degradation when stored at 4°C or 25°C for three months.

38. The method according to claim 35, wherein the composition undergoes less than 30% degradation when stored at 40°C or 50°C for three months.

39. The method according to claim 21, wherein the pectolinaligenin is present at a concentration of about 0.0001% w / w to about 5.0% w / w.

40. The method according to claim 21, wherein the pectolinaligenin is present at a concentration of about 0.0005% w / w to about 2.0% w / w.

41. The method according to claim 21, wherein the pectolinaligenin is present at a concentration of 0.0007% w / w to about 1.0% w / w.

42. The method according to claim 21, wherein the pectolinaligenin is present at a concentration of about 0.001% w / w to about 0.75% w / w.

43. The method according to claim 21, wherein the pectolinaligenin is present at a concentration of about 0.5% w / w.

44. The method according to claim 21, wherein the composition is selected from the group consisting of fluids, emulsions, capsules, suspensions, solids, semi-solids, jellies, pastes, gels, hydrogels, ointments, lotions, emulsions, creams, foams, mousses, liquids, sprays, suspensions, dispersions, powders, aerosols, colored cosmetics, and any combination thereof.

45. The method according to claim 21, wherein the composition further comprises one or more additives selected from the group consisting of solvents, emulsifiers, preservatives, antioxidants, emollients, thickeners, penetration enhancers, surfactants, diluents, fillers, carriers and / or pH control agents.

46. The method according to claim 45, wherein the preservative is an antimicrobial preservative.

47. The method according to claim 45, wherein the solvent is dimethyl isosorbide.

48. The composition contains water, dimethyl isosorbide, glycerin, caprylic / capric triglyceride, propanediol, sunflower seed oil, ethoxydiglycol, squalane, sodium acrylate copolymer, cetearyl alcohol, phenoxyethanol, glyceryl stearate, capryloyl glycerin / sebacate copolymer, diheptyl succinate, naringenin, lecithin, decylene glycol, pentylene glycol, cetearyl glucoside, shea butter, palmitic acid, arachidyl alcohol, behenyl alcohol, arachidyl glucoside, phenethyl alcohol, 1,2-hexanediol, hydrogenated olive oil, olive (Olea europaea) fruit oil, olive The method according to claim 21, further comprising one or more additives selected from the group consisting of europaea (olive) oil unsaponifiables, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, citric acid, acetylated sodium hyaluronate, sodium hyaluronate crosspolymer, sodium phytate, hydrolyzed sodium hyaluronate, and ethylhexylglycerin.

49. The method according to claim 21, wherein the composition comprises about 50% to about 70% (w / w) of water and about 10% to about 30% (w / w) of dimethyl isosorbide.

50. The composition is as follows: Table 10-1 Table 10-2 The method according to claim 21.

51. The composition according to claim 1, wherein it is an anhydrous substance.

52. The composition according to claim 1, comprising oil as the sole solvent.

53. The method according to claim 21, wherein the composition is an anhydrous substance.

54. The method according to claim 21, wherein the composition comprises oil as the sole solvent.

55. The method according to claim 21, wherein administration of the composition brings about whitening of the target skin.

56. The method according to claim 55, wherein the whitening effect is approximately 2 to 10 units higher than that of skin treated with a placebo.

57. The method according to claim 55, wherein the administration of a composition containing approximately 0.1% pectolinaligenin is greater than approximately 4 units compared to skin treated with placebo.

58. The method according to claim 55, wherein the dose of a composition containing approximately 0.1% pectolinaligenin is greater than approximately 4.65 units compared to skin treated with placebo.

59. The method according to claim 55, wherein the dose of a composition containing approximately 0.01% pectolinaligenin is greater than approximately 3 units compared to skin treated with placebo.

60. The method according to claim 55, wherein the dose of a composition containing approximately 0.01% pectolinaligenin is greater than approximately 4.01 units compared to skin treated with placebo.

61. A method for modulating the expression of one or more genes by administering a composition comprising pectolinaligenin, wherein at least one of the genes is related to a local condition.

62. The method according to claim 61, wherein the one or more genes are selected from the group consisting of (i) VCAN, (ii) COL1A2, (iii) MMP1, (iv) IL6, (v) IL23A, (vi) TLR2, and (vii) MMP3.

63. The method according to claim 61, wherein administration of the composition leads to the upregulation of VCAN and / or COL1A2.

64. The method according to claim 61, wherein administration of the composition leads to a downward adjustment of MMP1, MMP3, IL6, TLR2, and / or IL23A.

65. The method according to claim 61, wherein administration of the composition causes upregulation of one or more genes related to proteoglycans and collagen, which are barrier and extracellular matrix proteins.

66. The method according to claim 65, wherein administration of the composition further causes downregulation of collagenase.

67. The method according to claim 61, wherein administration of the composition downregulates the expression of inflammatory genes.

68. The method according to claim 61, wherein administration of the composition downregulates proteins involved in the melanin formation signaling pathway.

69. The method according to claim 61, wherein administering the composition to the subject leads to the treatment or prevention of a local condition of the subject.

70. The method according to claim 65, wherein administration of the composition leads to at least about tenfold upregulation of one or more genes related to proteoglycans and collagen, which are barrier and extracellular matrix proteins.

71. The method according to claim 66, wherein administration of the composition leads to a downregulation of one or more genes related to proteoglycans and collagen, which are barrier and extracellular matrix proteins, by at most about one-fifth.

72. The method according to claim 67, wherein administration of the composition leads to a downward regulation of inflammatory gene expression to at most about 1 / 200th.

73. The method according to claim 61, wherein administration of the composition alters one or more functions associated with the modulated gene, where one or more of the functions are selected from the group consisting of (i) maintenance of the skin barrier, (ii) collagen expression, (iii) collagen degradation, (iv) inflammation, (v) tissue atrophy, (vi) muscle loss, and (vii) melanin production.

74. The method according to claim 62, wherein the VCAN gene maintains the skin barrier through interaction with extracellular matrix proteins.

75. The method according to claim 62, wherein the COL1A2 gene regulates collagen expression.

76. The method according to claim 75, wherein the increase in collagen expression reduces wrinkles and sagging.

77. The method according to claim 62, wherein the MMP1 gene regulates collagen degradation.

78. The method according to claim 77, wherein the reduction in collagen breakdown improves the appearance of the skin.

79. The method according to claim 62, wherein the IL6 gene plays a role in regulating inflammation, tissue atrophy, muscle loss, and / or melanin formation.

80. The method according to claim 62, wherein the IL23A gene plays a role in inflammation.

81. The method according to claim 61, wherein the composition comprises about 5 nM to about 2500 nM of pectolinaligenin.

82. The method according to claim 61, wherein the composition further comprises a solvent.

83. The method according to claim 61, wherein the solvent is selected from the group consisting of dimethyl isosorbide, ethoxydiglycol, lauroyl sarcosinate isopropyl, pentylene glycol, propanediol, 1,2-hexanediol, and / or butylene glycol.

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