Anti-aging polypeptide component for activating ppar pathway and application thereof
Patent Information
- Application Number
- CN202410031284.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2024-01-09
- Publication Date
- 2026-09-25
- Estimated Expiration
- 2044-01-09
AI Technical Summary
然而,单一成分的使用可能限制了其抗衰老效果,因为衰老过程涉及多个生化途径
[0116]本发明的主要优点包括:
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Abstract
Description
Technical Field
[0001] This invention relates to the fields of biomedicine and cosmetics, specifically to an anti-aging polypeptide component that activates the PPAR pathway and its applications. Background Technology
[0002] With increasing focus on beauty and anti-aging, the cosmetics industry is constantly seeking to develop more effective skincare products. The anti-aging cosmetics market has become a highly competitive sector, with consumer demand for products that can slow down signs of skin aging continuing to grow. Therefore, researchers are constantly seeking new active ingredients and compositions to provide superior anti-aging effects.
[0003] Currently, a wide variety of anti-aging cosmetics are available on the market, typically containing various active ingredients such as vitamin C, hyaluronic acid, and collagen. These ingredients can improve the appearance of the skin to some extent, reducing fine lines and wrinkles. However, the use of a single ingredient may limit its anti-aging effect, as the aging process involves multiple biochemical pathways. Therefore, it is necessary to develop compositions with synergistic activities to more effectively combat signs of aging.
[0004] Therefore, there is an urgent need in the field to develop active ingredients and cosmetic compositions with functions such as anti-aging and / or wrinkle reduction. Summary of the Invention
[0005] The purpose of this invention is to provide active ingredients with anti-aging and anti-wrinkle functions and their applications.
[0006] In a first aspect, the present invention provides the use of a short peptide for preparing an agent or composition that promotes PPAR expression, wherein the short peptide is selected from the group consisting of ZPC-1, ZPC-2, or combinations thereof;
[0007] The structure of ZPC-1 is shown in Equation I:
[0008]
[0009] The structure of ZPC-2 is shown in Formula II:
[0010]
[0011] In another preferred embodiment, the short peptide is ZPC-1:
[0012]
[0013] In another preferred embodiment, the short peptide is ZPC-2:
[0014]
[0015] In another preferred embodiment, the formulation or composition includes cosmetics for the preparation of anti-wrinkle, anti-aging, and firming effects.
[0016] In another preferred embodiment, the formulation or composition is used to enhance the expression of collagen and / or elastin-related genes.
[0017] In another preferred embodiment, the collagen-related and / or elastin genes are selected from the group consisting of COL1A1, COL3A1, ELN, HAS2, IL17A, or combinations thereof.
[0018] In another preferred embodiment, the short peptide is used to prepare a formulation or composition that promotes PPAR expression in skin cells.
[0019] In another preferred embodiment, the skin cells are human fibroblasts.
[0020] In a second aspect, the present invention provides a formulation or composition comprising...
[0021] (a) A short peptide, said short peptide being selected from the group consisting of ZPC-1, ZPC-2, or combinations thereof;
[0022] The structure of ZPC-1 is shown in Equation I:
[0023]
[0024] The structure of ZPC-2 is shown in Formula II:
[0025]
[0026] and (b) a cosmetically acceptable carrier or excipient.
[0027] In another preferred embodiment, the cosmetically acceptable carrier or excipient is selected from the group consisting of: moisturizers, antioxidants, UV protectants, preservatives, film-forming agents, oil-soluble gelling agents, organically modified clay minerals, resins, antibacterial agents, fragrances, salts, pH adjusters, chelating agents, cooling agents, anti-inflammatory agents, skin-beautifying ingredients, vitamins, amino acids, inclusion compounds, or combinations thereof.
[0028] In another preferred embodiment, the cosmetically acceptable carrier or excipient is water.
[0029] In another preferred embodiment, the concentration of the short peptide in the cosmetic composition is 0.1 to 5000 ppm, preferably 1 to 1000 ppm, more preferably 5 to 500 ppm, for example 50 ppm.
[0030] In another preferred embodiment, the cosmetic composition further includes additional components selected from the group consisting of whitening or spot-reducing ingredients, anti-inflammatory ingredients, antioxidant ingredients, anti-UV ingredients, or combinations thereof.
[0031] In another preferred embodiment, the dosage form of the cosmetic composition is a solid dosage form, a semi-solid dosage form, or a liquid dosage form, such as a solution, gel, cream, lotion, ointment, paste, cake, powder, patch, etc.
[0032] In another preferred embodiment, the cosmetic composition is used for: anti-wrinkle, anti-aging, anti-oxidation, anti-inflammation, moisturizing, hydrating, and skin tone conditioning.
[0033] A third aspect of the present invention provides a method for preparing an formulation or composition as described in the second aspect of the present invention, comprising the following steps:
[0034] (i) Provides a short peptide, said short peptide being selected from the group consisting of ZPC-1, ZPC-2, or combinations thereof;
[0035] The structure of ZPC-1 is shown in Equation I:
[0036]
[0037] The structure of ZPC-2 is shown in Formula II:
[0038]
[0039] (ii) The short peptide from step (i) is mixed with a cosmetically acceptable carrier to obtain a formulation or composition that promotes PPAR expression.
[0040] In a fourth aspect, the present invention provides a method for promoting PPAR expression in vitro, comprising the steps of:
[0041] Skin cells are cultured in the presence of a short peptide to promote the expression of PPAR in the cells, wherein the short peptide is selected from the group consisting of ZPC-1, ZPC-2, or a combination thereof.
[0042] The structure of ZPC-1 is shown in Equation I:
[0043]
[0044] The structure of ZPC-2 is shown in Formula II:
[0045]
[0046] In another preferred embodiment, the concentration of the short peptide is 0.1 to 5000 ppm, preferably 1 to 1000 ppm, more preferably 5 to 500 ppm, for example 50 ppm.
[0047] In another preferred embodiment, the skin cells are human fibroblasts.
[0048] In another preferred embodiment, the culture is carried out in DMEM complete medium for 24 hours.
[0049] In another preferred embodiment, the method is non-diagnostic and non-therapeutic.
[0050] In a fifth aspect, the present invention provides a method for promoting the expression of collagen-related protein genes in vitro, comprising the steps of:
[0051] In the presence of short peptides, skin cells are cultured to promote the expression of collagen-related protein and / or elastin genes in the cells, wherein the short peptides are selected from the group consisting of ZPC-1, ZPC-2, or combinations thereof.
[0052] The structure of ZPC-1 is shown in Equation I:
[0053]
[0054] The structure of ZPC-2 is shown in Formula II:
[0055]
[0056] Furthermore, the collagen-related protein and / or elastin genes are selected from the group consisting of COL1A1, COL3A1, ELN, HAS2, IL17A, or combinations thereof.
[0057] In another preferred embodiment, the concentration of the short peptide is 0.1 to 5000 ppm, preferably 1 to 1000 ppm, more preferably 5 to 500 ppm, for example 50 ppm.
[0058] In another preferred embodiment, the skin cells are human fibroblasts.
[0059] In another preferred embodiment, the culture is carried out in DMEM complete medium for 24 hours.
[0060] In another preferred embodiment, the method is non-diagnostic and non-therapeutic.
[0061] It should be understood that, within the scope of this invention, the above-described technical features of this invention and the technical features specifically described below (such as in the embodiments) can be combined with each other to form new or preferred technical solutions. Due to space limitations, they will not be described in detail here. Attached Figure Description
[0062] Figure 1 This showed that PPAR agonist peptide affects PPAR gene expression levels.
[0063] Figure 2 The study showed that PPAR agonist peptides affect the expression levels of collagen and elastin-related genes. Detailed Implementation
[0064] Through extensive and in-depth research and screening, the inventors unexpectedly discovered for the first time that certain short peptides (such as ZPC-1 and ZPC-2) can efficiently increase PPAR gene expression, and therefore can be used as PPAR agonist peptides. The PPAR agonist peptides of this invention (hereinafter referred to as "the agonist peptides of this invention") can be used in cosmetics and pharmaceutical products, possessing functions such as anti-wrinkle and wrinkle reduction, promotion of collagen and / or elastin synthesis, antioxidant properties, skin tone conditioning, and skin moisturizing and hydrating. This invention was completed based on these findings.
[0065] the term
[0066] To facilitate understanding of the invention, certain technical and scientific terms are specifically defined below. Unless otherwise expressly defined herein, all other technical and scientific terms used herein have the meanings commonly understood by one of ordinary skill in the art to which this invention pertains. Before describing the invention, it should be understood that the invention is not limited to the specific methods and experimental conditions described, as such methods and conditions can vary. It should also be understood that the terminology used herein is intended only to describe particular embodiments and is not intended to be restrictive; the scope of the invention will be limited only by the appended claims.
[0067] As used herein, "formulation of the present invention" refers to a formulation containing the active compound of the present invention.
[0068] As used herein, the term “comprising” or its variations such as “including” or “comprising” are understood to include the said element or component without excluding other elements or other components.
[0069] PPAR
[0070] PPAR stands for peroxisome proliferator-activated receptor. It is a class of nuclear receptor proteins that play a wide range of regulatory roles in the human body, involving biological processes such as lipid metabolism, energy metabolism, glucose metabolism, and inflammation.
[0071] PPAR receptors are divided into three subtypes:
[0072] PPARα (alpha type): Primarily involved in the regulation of lipid and energy metabolism, particularly in the liver, regulating fatty acid oxidation. Drugs such as fibrates are PPARα agonist peptides used to treat dyslipidemia symptoms such as high cholesterol and high triglycerides.
[0073] PPARβ / δ (β / δ type): Involved in various cellular processes, including cell proliferation, anti-inflammatory effects, and muscle metabolism. Currently, no drugs targeting PPARβ / δ have been approved for marketing, but research is ongoing.
[0074] PPARγ (γ-type): Primarily functions in adipocytes, regulating lipid metabolism, insulin sensitivity, and glucose metabolism. Some antidiabetic drugs, such as meglitazone and rosiglitazone, are PPARγ agonists used to treat type 2 diabetes.
[0075] PPAR agonist peptide
[0076] As used herein, "PPAR agonist peptide of the present invention," "active ingredient of the present invention," and "agonist peptide of the present invention" are used interchangeably and all refer to the following short peptides of the present invention that can efficiently increase PPAR gene expression: ZPC-1, ZPC-2, or combinations thereof. It should be understood that the terms also include physiologically acceptable salts or esters of the said short peptides.
[0077] The ZPC-1 polypeptide of this invention is Pal-His-D-Phe-Arg-NH2, and its structural formula is shown in Formula I.
[0078]
[0079] The ZPC-2 polypeptide of this invention is TFA-Val-Tyr-Val-OH, and its structural formula is shown in Formula II.
[0080]
[0081] In the PPAR agonist peptide ZPC-1 of the present invention, D-Phe is a D-type amino acid, while the other amino acids are L-type amino acids.
[0082] The PPAR agonist peptide of the present invention can be prepared using conventional synthetic methods.
[0083] The PPAR agonist peptide of this invention can be used in skin care products. PPARs are a type of nuclear receptor that participate in a variety of biological processes within cells, including cell differentiation, lipid metabolism, and inflammation regulation.
[0084] The PPAR agonist peptide of this invention can activate PPAR receptors, thereby altering related biological processes and gene expression.
[0085] Taking cosmetics as an example, the main applications of the PPAR agonist peptide of this invention in cosmetics include (but are not limited to):
[0086] (1) Anti-wrinkle and anti-aging
[0087] PPAR agonist peptides are widely used in cosmetics for anti-wrinkle and anti-aging products. They improve skin elasticity and reduce the appearance of wrinkles and fine lines by promoting the synthesis of collagen and / or elastin. This is because PPAR activation can regulate genes related to cell differentiation and matrix synthesis, thereby improving skin texture and appearance.
[0088] (2) Antioxidant effect
[0089] PPAR agonists also possess antioxidant properties, helping to protect the skin from free radicals and oxidative damage. They can increase skin's resistance and reduce the damage caused by oxidative stress, thus helping to maintain youthful and healthy skin.
[0090] (3) Adjust skin tone
[0091] PPAR agonists also play a role in improving skin tone. They can reduce pigmentation, improve uneven skin tone, and make the skin tone more even and bright. This helps to improve uneven skin tone and reduce problems such as dark spots.
[0092] (4) Anti-inflammatory effect
[0093] PPAR agonist peptides are highly valued in skincare products due to their anti-inflammatory properties in cosmetics. They help reduce skin inflammation and sensitivity, soothe redness and discomfort, and leave skin feeling more comfortable and healthy.
[0094] (5) Moisturizing and hydrating
[0095] PPAR agonists can also enhance the skin's moisturizing properties, helping to lock in moisture, prevent water loss, and keep the skin hydrated and smooth. This is crucial for maintaining the skin's barrier function and preventing dryness.
[0096] Pharmaceutical compositions and health product compositions
[0097] The present invention also provides compositions containing the agonist of the present invention, such as pharmaceutical compositions, health product compositions, etc.
[0098] The pharmaceutical compositions of the present invention comprise (a) the PPAR agonist peptide of the present invention; and (b) a pharmaceutically acceptable carrier or excipient. Furthermore, the pharmaceutical compositions also include health supplement compositions.
[0099] Taking pharmaceutical compositions as an example, the PPAR agonist peptides of the present invention can be prepared into pharmaceutical compositions, such as tablets, capsules, powders, microparticles, solutions, lozenges, gels, creams, liniments, suspensions, tinctures, poultices, liniments, lotions, and aerosols. The pharmaceuticals can be prepared using commonly known manufacturing techniques, and suitable pharmaceutical additives can be added to the pharmaceuticals.
[0100] Examples of pharmaceutical additives include excipients, binders, disintegrants, lubricants, flow aids, suspending agents, emulsifiers, stabilizers, heat-retaining (wetting) agents, preservatives, solvents, solubilizers, flavoring agents, sweeteners, dyes, fragrances, propellants, etc. These pharmaceutical additives can be selected and added in appropriate amounts without affecting the effects of the present invention.
[0101] Cosmetic Composition
[0102] The present invention also provides cosmetic compositions containing the agonist of the present invention. The cosmetic compositions of the present invention comprise (a) the PPAR agonist peptide of the present invention; and (b) a cosmetically acceptable carrier or excipient.
[0103] The PPAR agonist peptides of the present invention can be prepared into various cosmetic compositions, such as emulsions, liquids, ointments, creams, pastes, cakes, powders, etc., using conventional methods.
[0104] Within the scope that does not impair the effects of the present invention, other ingredients commonly used in cosmetics may be added to the cosmetics of the present invention, such as film-forming agents, oil-soluble gelling agents, organically modified clay minerals, resins, moisturizers, preservatives, antibacterial agents, fragrances, salts, antioxidants, pH adjusters, chelating agents, cooling agents, anti-inflammatory agents, skin beautifying ingredients (whitening agents, cell activators, skin roughness improvers, blood circulation promoters, skin astringents, anti-seborrheic agents, etc.), vitamins, amino acids, nucleic acids, hormones, inclusion compounds, etc.
[0105] Oil-soluble gelling agents are selected from metal soaps such as aluminum stearate, magnesium stearate, and zinc myristate; amino acid derivatives such as N-lauroyl-L-glutamic acid and α,γ-di-n-butylamine; cyclodextrin fatty acid esters such as cyclodextrin palmitate, cyclodextrin stearate, and cyclodextrin 2-ethylhexanoate palmitate; sucrose fatty acid esters such as sucrose palmitate and sucrose stearate; benzylidene derivatives of sorbitol such as benzylidene sorbitol and dibenzylidene sorbitol; and organically modified clay minerals such as dimethylbenzyl dodecylammonium montmorillonite clay and dimethyl octadecylammonium montmorillonite clay. One, two, or more can be used as needed.
[0106] Moisturizers include: glycerin, sorbitol, propylene glycol, dipropylene glycol, 1,3-butanediol, glucose, xylitol, maltitol, polyethylene glycol, hyaluronic acid, chondroitin sulfate, pyrrolidone carboxylate, polyoxyethylene methyl glucoside, polyoxypropylene methyl glucoside, etc.
[0107] Antibacterial and preservative agents include: alkyl p-hydroxybenzoate, benzoic acid, sodium benzoate, sorbic acid, potassium sorbate, phenoxyethanol, etc. Antibacterial agents include: benzoic acid, salicylic acid, carbolic acid, sorbic acid, alkyl p-hydroxybenzoate, p-chloro-m-cresol, hexachlorophenol, benzalkonium chloride, chlorhexidine chloride, trichloro-N-carbonylaniline, triclosan, photosensitizer, phenoxyethanol, etc.
[0108] Antioxidants include: tocopherol, butylated hydroxyanisole, butylated hydroxytoluene, phytic acid, etc.; pH adjusters include: lactic acid, citric acid, glycolic acid, succinic acid, tartaric acid, dl-malic acid, potassium carbonate, sodium bicarbonate, ammonium bicarbonate, etc.; chelating agents include: alanine, sodium ethylenediaminetetraacetate, sodium polyphosphate, sodium metaphosphate, phosphoric acid, etc.; cooling agents include: L-menthol, camphor, etc.; anti-inflammatory agents include: allantoin, glycyrrhetinic acid, glycyrrhizic acid, tranexamic acid, azulene, etc.
[0109] Skin-beautifying ingredients include: whitening agents such as placental extract, arbutin, glutathione, and saxifrage extract; cell activators such as royal jelly, photosensitizers, cholesterol derivatives, and calf blood extract; skin roughness improvers; blood circulation promoters such as valeramide nonanoate, benzyl nicotinate, β-butoxyethyl nicotinate, capsaicin, gingerone, cantharides tincture, ichthammol, caffeine, tannic acid, α-borneol, nicotinic acid tocopherol, hexanicotinic acid inositol ester, cyclic mandelic acid ester, cinnarizine, tolazoline, acetylcholine, verapamil, senna extract, and γ-oryzanol; skin astringents such as zinc oxide and tannic acid; anti-seborrheic agents such as sulfur; and vitamins such as vitamin A oil, rosin oil, rosin acetate oil, and rosin palmitic acid oil; riboflavin, riboflavin butyrate, and flavin adenine nucleotide. Vitamins include: B2; B6 (such as pyridoxine hydrochloride, pyridoxine dicaprylate, and pyridoxine tripalmitate); B12 and its derivatives; B15 and its derivatives; L-ascorbic acid, L-ascorbic acid dipalmitate, L-ascorbic acid-2-sulfate sodium, and L-ascorbic acid phosphate dipotassium; D (such as ergocalciferol and cholecalciferol); E (such as α-tocopherol, β-tocopherol, γ-tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol niacin, and dl-α-tocopherol succinate); H; P; niacin derivatives (such as niacin, benzyl nicotinate, and nicotinamide); pantothenic acid derivatives (such as calcium pantothenate, D-panthenol, pantothenicotinyl ethyl ether, and acetylpantothenicotinyl ethyl ether); and biotin.
[0110] Amino acids include: glycine, valine, leucine, isoleucine, serine, threonine, phenylalanine, arginine, lysine, aspartic acid, glutamic acid, cystine, cysteine, methionine, tryptophan, etc.
[0111] Preferred examples of cosmetics of the present invention include: skin care cosmetics, makeup cosmetics, and UV protection cosmetics. Examples include basic cosmetics such as lotions, creams, serums, sunscreens, mask ingredients, facial cleansers, and essences; and makeup cosmetics such as foundations, face powders, and blushes.
[0112] There are no particular restrictions on the form of the product; it can be liquid, emulsion, cream, solid, paste, gel, powder, multi-layered, mousse, spray, etc.
[0113] The present invention also provides a skin care method comprising the steps of: applying the PPAR agonist peptide of the present invention, or a cosmetic or care product containing the agonist peptide of the present invention, to an individual in need.
[0114] In another preferred embodiment, the effective concentration range of the PPAR agonist peptide is 1 to 500 ppm.
[0115] In another preferred embodiment, the method is for anti-wrinkle, firming, and anti-aging purposes.
[0116] The main advantages of this invention include:
[0117] (1) For the first time, PPAR agonist peptides ZPC-1 and ZPC-2 that can significantly promote PPAR expression were provided.
[0118] (2) The agonist peptide of the present invention has anti-wrinkle, firming and anti-aging functions, and therefore can be used in the development of cosmetics or drugs.
[0119] The present invention will be further illustrated below with reference to specific embodiments. It should be understood that these embodiments are for illustrative purposes only and are not intended to limit the scope of the invention. Experimental methods in the following embodiments, unless otherwise specified, are generally performed under conventional conditions, such as those described in Sambrook et al., Molecular Cloning: A Laboratory Manual (New York: Cold Spring Harbor Laboratory Press, 1989), or as recommended by the manufacturer. Unless otherwise stated, percentages and parts are weight percentages and parts by weight.
[0120] Example
[0121] I. Cell Treatment
[0122] Using HFF cells (human fibroblasts), at a ratio of 2 × 10⁶ cells per well. 5 Cells were seeded at a density of 1000 cells / well in 6-well plates and incubated at 37°C in a 5% CO2 incubator for 24 hours.
[0123] The experimental groups consisted of eleven groups (each with three replicates): negative control group, positive control group (Pioglitazone hydrochloride, TGF-β), Creasend 011P group Repairs 012P group Eyelash 006P set Eyelash 001P set Melanopep 090P group Collagen 045P group Wrinklend 008P group, ZPC-1 group, ZPC-2 group.
[0124] Table 1 shows the experimental groups and drug administration regimens.
[0125]
[0126]
[0127] Except for the control group, the other 11 experimental groups were added with the predetermined concentrations of the analytes shown in Table 1 and cultured for another 24 hours. Afterwards, the supernatant was removed, and lysis agents were added to the cells to obtain cell lysates (for gene content detection).
[0128] II. Detection of PPAR agonist peptide gene content and PPAR agonist peptide-related genes promoting collagen and / or elastin.
[0129] 2.1 Method
[0130] 1. RNA extraction
[0131] (1) Add 1 / 5 volume of chloroform to the cell lysis buffer, mix well, let stand for 5 min, centrifuge at 12,000 x g, 4 °C for 15 min.
[0132] (2) Take the supernatant, add isopropanol, mix well, refrigerate for 10 min, centrifuge at 12,000 x g, 4 °C for 10 min, and retain the precipitate;
[0133] (3) Wash with 75% ethanol solution, centrifuge at 7,500 x g, 4°C for 5 min. Retain the precipitate and air dry at room temperature;
[0134] (4) Add an appropriate amount of RNase-free ddH2O to dissolve the precipitate.
[0135] (5) Measure RNA concentration.
[0136] 2. qPCR detection
[0137] (1) Preparation of reverse transcription reaction system
[0138] Prepare the reverse transcription reaction system according to Table 2.
[0139] Table 2. Preparation of Reverse Transcription Reaction System
[0140]
[0141] (2) Setting up the reverse transcription program
[0142] Table 3 Reverse Transcription Procedure
[0143]
[0144] (3) Preparation of qPCR reaction system.
[0145] (4) After adding the sample, centrifuge the reaction plate at 1000 rpm for 1 min.
[0146] (5) qPCR reaction program settings.
[0147] Table 4. qPCR reaction procedure table
[0148]
[0149] The expression levels of genes COL1A1, COL3A1, ELN, HAS2, and IL17A were detected. The composition of the quantitative real-time PCR reaction system is shown in Table 5; the PCR amplification primers are shown in Table 6.
[0150] Table 5 PCR reaction system
[0151] upstream primer 1 10μM Downstream primer 1 10μM 2×TransStart Top Green qPCR SuperMix 10.4 2× Sterile ultrapure water 4.6 - cDNA template 3 10ng / μl total 20 -
[0152] Table 6 Primers
[0153]
[0154] Data processing was performed using Graphpad Prism 8.0.2 statistical software, and T-tests (and non-parametric tests) were conducted for statistical analysis; *** represents P<0.001, ** represents P<0.01, and * represents P<0.05.
[0155] III. Results
[0156] The results showed that the positive control group had a significant increase compared with the negative control group (P<0.05), indicating that the experimental system was effective.
[0157] like Figure 1 As shown, among the many test substances, ZPC-1 and ZPC-2 significantly increased the PPAR gene expression in HFF cells (P<0.005).
[0158] like Figure 2 As shown, compared with the blank control, ZPC-1 and ZPC-2 significantly increased the expression of collagen genes COL1A1 and COL3A1 and elastin gene ELN (P<0.01), with the increase being comparable to that of the positive control TGF-β.
[0159] The above results indicate that ZPC-1 and ZPC-2 can promote the production of collagen and elastin, thereby achieving anti-wrinkle, firming, and anti-aging effects.
[0160] discuss
[0161] The results showed that ZPC-1 and ZPC-2 significantly increased the expression of the PPAR gene, and also significantly enhanced the expression levels of COL1A1 (type I collagen), COL3A1 (type III collagen), and ELN (elastin). Therefore, ZPC-1 and ZPC-2 can effectively promote the production of collagen and elastin, thus helping to reduce signs of aging such as fine lines, wrinkles, and fine lines. Through anti-wrinkle and firming effects, ZPC-1 and ZPC-2 can achieve the goal of delaying aging. This invention provides strong scientific evidence for the development of novel anti-aging skincare products.
[0162] All documents mentioned in this invention are incorporated herein by reference as if each document were individually incorporated by reference. Furthermore, it should be understood that after reading the foregoing teachings of this invention, those skilled in the art can make various alterations or modifications to this invention, and these equivalent forms also fall within the scope defined by the appended claims.
Claims
1. The use of a short peptide in the preparation of formulations or compositions that promote PPAR expression, characterized in that, The short peptide is selected from the group consisting of ZPC-1, ZPC-2, or combinations thereof; The structure of ZPC-1 is shown in Equation I: (I); The structure of ZPC-2 is shown in Formula II: (II)。 2. The use as described in claim 1, characterized in that, The short peptide is ZPC-1: (I)。 3. The use as described in claim 1, characterized in that, The short peptide is ZPC-2: (II)。 4. The use as described in claim 1, characterized in that, The formulations or compositions include cosmetics for anti-wrinkle, anti-aging, and firming purposes.
5. The use as described in claim 1, characterized in that, The formulation or composition is used to enhance the expression of collagen and / or elastin-related genes.
6. The use as described in claim 5, characterized in that, The collagen-related and / or elastin genes are selected from the following group: COL1A1 , COL3A1 , ELN , HAS2 , IL17A , or combinations thereof.
7. The use as described in claim 1, characterized in that, The short peptide is used to prepare formulations or compositions that promote PPAR expression in skin cells.
8. The use as described in claim 7, characterized in that, The skin cells are human fibroblasts.
9. The use as described in claim 1, characterized in that, The formulation or composition contains: (a) A short peptide, said short peptide being selected from the group consisting of ZPC-1, ZPC-2, or combinations thereof; The structure of ZPC-1 is shown in Equation I: (I); The structure of ZPC-2 is shown in Formula II: (II); and (b) a cosmetically acceptable carrier or excipient.
10. The use as described in claim 9, characterized in that, The cosmetically acceptable carrier or excipient is selected from the group consisting of: moisturizers, antioxidants, UV protectants, preservatives, film-forming agents, oil-soluble gelling agents, organically modified clay minerals, resins, antibacterial agents, fragrances, salts, pH adjusters, chelating agents, cooling agents, anti-inflammatory agents, skin-beautifying ingredients, vitamins, amino acids, inclusion compounds, or combinations thereof.
11. The use as described in claim 9, characterized in that, A method for preparing the formulation or composition includes the following steps: (i) Provides a short peptide, said short peptide being selected from the group consisting of ZPC-1, ZPC-2, or combinations thereof; The structure of ZPC-1 is shown in Equation I: (I); The structure of ZPC-2 is shown in Formula II: (II); (ii) The short peptide from step (i) is mixed with a cosmetically acceptable carrier to obtain a formulation or composition that promotes PPAR expression.
12. A method for promoting PPAR expression in vitro for non-disease therapeutic purposes, characterized in that, Including the following steps: Skin cells are cultured in the presence of a short peptide to promote the expression of PPAR in the cells, wherein the short peptide is selected from the group consisting of ZPC-1, ZPC-2, or a combination thereof. The structure of ZPC-1 is shown in Equation I: (I); The structure of ZPC-2 is shown in Formula II: (II)。 13. The method as described in claim 12, characterized in that, The concentration of the short peptide is 0.1~5000ppm.
14. The method as described in claim 12, characterized in that, The concentration of the short peptide is 1~1000ppm.
15. The method as described in claim 12, characterized in that, The concentration of the short peptide is 5~500ppm.
16. A method for promoting the expression of collagen-related proteins and / or elastin genes in vitro for non-disease therapeutic purposes, characterized in that, Including the following steps: In the presence of a short peptide, skin cells are cultured to promote the expression of collagen-related protein genes in the cells, wherein the short peptide is selected from the group consisting of ZPC-1, ZPC-2, or a combination thereof. The structure of ZPC-1 is shown in Equation I: (I); The structure of ZPC-2 is shown in Formula II: (II); Furthermore, the collagen-related protein and / or elastin genes are selected from the following group: COL1A1 , COL3A1 , ELN , HAS2 , IL17A , or combinations thereof.
17. The method as described in claim 16, characterized in that, The concentration of the short peptide is 0.1~5000ppm.
18. The method as described in claim 16, characterized in that, The concentration of the short peptide is 1~1000ppm.
19. The method as described in claim 16, characterized in that, The concentration of the short peptide is 5~500ppm.
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