Plant active substances and their anti-pollution effects
A composition of bioactive molecules, including oxyresveratrol and tetrahydrocurcumin, effectively protects skin against UV radiation and environmental pollutants by reducing oxidative stress and inflammation, addressing the inadequacies of current skin care products.
Patent Information
- Application Number
- JP2022513211
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Priority Date
- 2019-08-26
- Filing Date
- 2020-08-26
- Publication Date
- 2025-05-19
- Estimated Expiration
- 2040-08-26
AI Technical Summary
Current skin care products are inadequate in protecting the skin against the harmful effects of UV radiation and environmental pollutants, which can lead to oxidative damage, inflammation, and premature aging.
A composition comprising one or more bioactive molecules selected from oxyresveratrol, tetrahydrocurcumin, oroxylin A, baicalein, chrysin, β-glucogallin, and total mucic acid gallate, which are topically administered to provide protection against UV radiation and environmental pollutants.
The composition effectively reduces oxidative stress, inflammation, and collagen degradation, while increasing antioxidant enzyme levels and reducing ROS and inflammatory markers, thereby protecting and rejuvenating the skin.
Smart Images

Figure 0007679359000028 
Figure 0007679359000029 
Figure 0007679359000030
Abstract
Description
Technical Field
[0001] Cross - Reference to Related Applications This is a PCT application claiming priority based on U.S. Provisional Application No. 62891913, filed on August 26, 2019, the subject matter of which is incorporated herein by reference. The present invention generally relates to the anti - pollution effects of natural bioactive molecules isolated from various plant sources. Specifically, the present invention relates to the use of plant active substances for protecting the skin against harmful UV radiation and environmental pollutants.
Background Art
[0002] The impact of air pollution on people's overall health is diverse. By causing several health problems, it affects our daily lives. One of the major effects of these pollutants appears on the skin, as they cause oxidative damage or interfere with the normal functions of cellular proteins, DNA, and lipids. The skin is exposed to various pollutants, which can lead to premature skin aging, pigmentation spots or acne, or more severe dermatological problems such as atopic dermatitis, psoriasis, and even skin cancer (English, J.S., R.S. Dawe, and J. Ferguson, Environmental effects and skin disease. Br Med Bull, 2003. 68: p. 129 - 42). The main sources of pollution include particulate matter, polycyclic aromatic hydrocarbons (PAH), volatile organic compounds (VOC), nitrogen and sulfur oxides, carbon monoxide, ozone and heavy metals (Baudouin, C., et al., Environmental pollutants and skin cancer. Cell Biol Toxicol, 2002. 18(5): p. 341-8). Toxic gases (CO2, CO, SO2, NO, NO2), low molecular weight hydrocarbons, persistent organic pollutants (e.g., dioxins), heavy metals (e.g., lead, mercury) and particulate matter (PM) form primary pollutants that are emitted from sources. Secondary pollutants, including ozone (O3), NO2, peroxyacetyl nitrate, hydrogen peroxide and aldehydes, are formed in the atmosphere through chemical and photochemical reactions involving primary pollutants (Kampa, M. and E. Castanas, Human health effects of air pollution. Environ Pollut, 2008. 151(2): p. 362-7). Some environmental pollutants of which benzo(a)pyrene (BaP) is a major component are potentially dangerous. BaP has been identified as a Group 1 carcinogen by the International Agency for Research on Cancer (IARC). BaP is metabolized into highly toxic peroxides, quinones, sulfur and nitrogen derivatives. The main sources of BaP are transport-related emissions (gasoline combustion, tar macadam, and tire wear, coal and wood). Other sources can be from uncontrolled fires, waste incineration and industrial emissions.
[0003] These contaminants coated with carbon particles and PAHs damage the skin, leading to alterations in the skin barrier, oxidative stress, inflammation, and cellular deterioration. These contaminants cause several specific skin-related problems such as hyperpigmentation, inflammation, collagen degradation, and elastin degradation. Environmental contaminants such as UVA upregulate the formation of matrix metalloproteinases (MMPs), enzymes that break down the elastin and collagen of matrix proteins, which, if not prevented, can lead to a significant decrease in skin elasticity and an increase in wrinkles (Risom, L., P. Moller, and S. Loft, Oxidative stress-induced DNA damage by particulate air pollution. Mutat Res, 2005. 592(1-2): p. 119-37; Moller, P. and S. Loft, Oxidative damage to DNA and lipids as biomarkers of exposure to air pollution. Environ Health Perspect, 2010. 118(8): p. 1126-36). UVA can penetrate deeper into the skin compared to UVB, contributing to photoaging, photocarcinogenesis, and photodermatosis, and increasing oxidative stress in fibroblasts and deeper cells within the skin. Blue light (light from mobile phones, TVs, laptop / desktop screens) has been reported to have similar effects (Godley et al., Blue Light Induces Mitochondrial DNA Damage and Free Radical Production in Epithelial Cells, The Journal Of Biological Chemistry, 2005, 280(22):21061-21066). The effects of various air pollutants on the skin are summarized in the following prior art documents. a. Araviiskaia et al., The impact of airborne pollution on skin, J Eur Acad Dermatol Venereol. 2019; 33(8): 1496-1505. b. Drakaki et al., Air pollution and the skin, Front. Environ. Sci., 2014; 2:1-6 c. Doris Day, The Impact of Pollution on The Skin, HCP live, The Impact of Pollution on The Skin, Source: hcplive.com / view / the-impact-of-pollution-on-the-skin, Accessed on August 20, 2020.
[0004] Anti-pollution products are thought to prevent the impact of various air pollutants by a. protecting skin tissue against harmful reactive oxygen species through antioxidant activity b. reducing inflammation and allergic reactions c. helping to stop cell death that occurs in the skin when exposed to pollutants
[0005] Plant-based products are currently attracting more attention due to their low toxicity. Essential oils and plant extracts such as turmeric, coconut, cocoa, basil, onion, green tea, perilla, licorice, rosemary, and aloe are used in skin care products (Aburjai & Natsheh, Plants used in cosmetics, Phytotherapy Research, 2003; 17(9), 987-1000. doi:10.1002 / ptr.1363). Tetrahydrocurcumin isolated from Curcuma longa (turmeric) has been reported for its skin whitening effect (Majeed et al., US Patent No. 6653327). Resveratrol and oxyresveratrol are also well-known for their skin care and skin whitening effects. The fruits of Oroxylum indicum (Sorizayano-ki) have also been reported to be good for the skin and are used in the treatment of skin diseases (Chauhan et al., Shyonak, Sona Patha (Oroxylum indicum) - Properties, benefits and dosage, Planet Ayurveda, planetayurveda.com / library / shyonak-oroxylum-indicum / , accessed August 22, 2020). The extract of Pterocarpus marsupium has also been reported for its skin whitening and anti-aging effects (Majeed et al., An Open-Label Single-Arm, Monocentric Study Assessing the Efficacy and Safety of Natural Pterostilbene (Pterocarpus marsupium) for Skin Brightening and Antiaging Effects, Clin Cosmet Investig Dermatol. 2020; 13: 105-116). However, it is common knowledge that not all products used for skin care and skin whitening are effective in protecting the skin against harmful contaminants.There still exists an unmet industrial need to discover a natural composition comprising one or more bioactive molecules isolated from plants that confers maximum protection against harmful pollutants. Further, the composition should be able to protect the skin from pollutants and also be able to purify and rejuvenate skin exposed to environmental pollutants. The present invention solves the above problems by disclosing a composition comprising one or more bioactive molecules selected from the group consisting of a composition comprising 95% by weight oxyresveratrol; 95% by weight tetrahydrocurcumin; at least 10% by weight β-glucogallin and at least 10% by weight total mucic acid gallate; and a composition comprising at least 10% by weight oroxylin A, at least 10% by weight baicalein and at least 2% by weight chrysin.
[0006] A primary object of the present invention is to disclose a method for protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants using a composition comprising one or more components selected from the group consisting of a composition comprising 95% by weight oxyresveratrol; 95% by weight tetrahydrocurcumin; at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate; and a composition comprising at least 10% by weight oroxylin A, at least 10% by weight baicalein and at least 2% by weight chrysin. Another object of the present invention is to disclose a method for purifying and rejuvenating mammalian skin exposed to environmental pollutants and UV radiation using a composition comprising one or more components selected from the group consisting of a composition comprising 95% by weight oxyresveratrol; 95% by weight tetrahydrocurcumin; 90% by weight pterostilbene; at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate; and a composition comprising at least 10% by weight oroxylin A, at least 10% by weight baicalein and at least 2% by weight chrysin. The present invention meets the above objectives and provides further related advantages.
Summary of the Invention
[0007] In the most preferred embodiment, the present invention is a method for protecting mammalian skin against the harmful effects of UV radiation and environmental contaminants, the method comprising the step of topically administering to a mammal in need of such protection a composition comprising one or more components selected from the group consisting of a composition comprising at least 10% by weight of oroxylin A, at least 10% by weight of baicalein and at least 2% by weight of chrysin; a composition comprising 95% by weight of oxyresveratrol; a composition comprising 95% by weight of tetrahydrocurcumin; a composition comprising 90% by weight of pterostilbene; and a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate.
[0008] In the most preferred embodiment, the present invention is a method for purifying and rejuvenating the skin of a mammal exposed to environmental contaminants and UV radiation, the method comprising the step of topically administering to a mammal in need of such an effect a composition comprising one or more components selected from the group consisting of a composition comprising at least 10% by weight of oroxylin A, at least 10% by weight of baicalein and at least 2% by weight of chrysin; a composition comprising 95% by weight of oxyresveratrol; a composition comprising 95% by weight of tetrahydrocurcumin; a composition comprising 90% by weight of pterostilbene; and a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate. Other features and advantages of the present invention will become apparent from the following more detailed description, which illustrates the principles of the invention by way of example.
Brief Description of the Drawings
[0009]
Figure 1
Figure 2a
Figure 2b
Figure 2c
Figure 3a
Figure 3b
Figure 4
Figure 5a
Figure 5b
Figure 5c
Figure 6a
Figure 6b
Figure 7
Figure 8a
Figure 8b
Figure 8c
Figure 9a
Figure 9b
Figure 10
Figure 11a
Figure 11b
Figure 11c
Figure 12a
Figure 12b
Mode for Carrying Out the Invention
[0010] In a most preferred embodiment, the present invention is a method for protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants, the method comprising the step of topically administering to a mammal in need of such protection a composition comprising at least 10% by weight of oroxylin A, at least 10% by weight of baicalein and at least 2% by weight of chrysin. In related embodiments, the composition further comprises one or more components selected from the group consisting of compositions comprising 95% by weight oxyresveratrol; 95% by weight tetrahydrocurcumin; 90% by weight pterostilbene; and at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate. In another related aspect, the environmental pollutants are selected from, but not limited to, the list comprising particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by increasing the levels of antioxidant enzymes, decreasing the ROS levels, and reducing the levels of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. In another related aspect, the inflammatory marker is IL-8.
[0011] In another most preferred embodiment, the present invention is a method for purifying and rejuvenating the skin of a mammal exposed to environmental pollutants and UV radiation, the method comprising the step of topically administering to a mammal in need of such an effect a composition comprising at least 10% by weight of oroxylin A, at least 10% by weight of baicalein and at least 2% by weight of chrysin. In a related embodiment, the composition further comprises one or more components selected from the group consisting of compositions comprising 95% by weight of oxyresveratrol; 95% by weight of tetrahydrocurcumin; 90% by weight of pterostilbene; and at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate. In another related aspect, the environmental pollutants are selected from, but not limited to, the list comprising particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by reducing collagenase activity, increasing the levels of antioxidant enzymes, reducing ROS levels, and decreasing the levels of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha and IL-8. In another related aspect, the inflammatory marker is IL-8.
[0012] In another most preferred embodiment, the present invention discloses a composition comprising 10% by mass or more of oroxylin A, 10% by mass or more of baicalein, and 2% by mass or more of chrysin for use in protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants. In a related aspect, the present invention discloses a composition comprising 10% by mass or more of oroxylin A, 10% by mass or more of baicalein, and 2% by mass or more of chrysin for use in purifying and rejuvenating the skin of a mammal exposed to environmental pollutants and UV radiation. In a related embodiment, the composition further comprises one or more components selected from the group consisting of compositions comprising 95% by mass oxyresveratrol; 95% by mass tetrahydrocurcumin; 90% by mass pterostilbene; and at least 10% by mass of β-glucogallin and at least 10% by mass of total mucic acid gallate. In another related aspect, the environmental pollutants are selected from, but not limited to, the list comprising particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by reducing collagenase activity, increasing the levels of antioxidant enzymes, decreasing ROS levels, and decreasing the levels of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. In another related aspect, the inflammatory marker is IL-8. In a related aspect, the composition is formulated with pharmaceutically / cosmetically acceptable excipients, adjuvants, bases, diluents, carriers, modifiers, antioxidants, bioavailability enhancers, and preservatives and / or incorporated into a formulation containing skin care components and topically administered in the form of creams, gels, lotions, powders, serums, oils, suspensions, ointments, soaps, scrubs, emulsions, and compacts.
[0013] In a most preferred embodiment, the present invention is a method for protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants, the method comprising the step of topically administering to a mammal in need of such protection a composition comprising 95% by weight oxyresveratrol. In related embodiments, the composition is a composition comprising 10% by weight or more of oroxylin A, 10% by weight or more of baicalein and 2% by weight or more of chrysin; 95% by weight tetrahydrocurcumin; 90% by weight pterostilbene; and further comprises one or more components selected from the group consisting of compositions comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate. In another related aspect, the environmental pollutants are selected from, but not limited to, the list comprising particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by increasing the levels of antioxidant enzymes, decreasing the ROS levels, and reducing the levels of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. In another related aspect, the inflammatory marker is IL-8.
[0014] In another most preferred embodiment, the present invention is a method for purifying and rejuvenating the skin of a mammal exposed to environmental pollutants and UV radiation, the method comprising the step of topically administering to a mammal in need of such an effect a composition comprising 95% by weight oxyresveratrol. In related embodiments, the composition is a composition comprising 10% by weight or more of oroxylin A, 10% by weight or more of baicalein and 2% by weight or more of chrysin; 95% by weight tetrahydrocurcumin; 90% by weight pterostilbene; and a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate. In another related aspect, the environmental pollutant is selected from, but not limited to, the list comprising particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by reducing collagenase activity, increasing the levels of antioxidant enzymes, reducing ROS levels, and decreasing the levels of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. In another related aspect, the inflammatory marker is IL-8.
[0015] In another most preferred embodiment, the present invention discloses a composition comprising 95% by weight of oxyresveratrol for use in protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants. In a related aspect, the present invention discloses a composition comprising 95% by weight of oxyresveratrol for use in purifying and rejuvenating the skin of a mammal exposed to environmental pollutants and UV radiation. In a related embodiment, the composition is a composition comprising 10% by weight or more of oroxylin A, 10% by weight or more of baicalein and 2% by weight or more of chrysin; 95% by weight of tetrahydrocurcumin; 90% by weight of pterostilbene; and a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate, and further comprises one or more components selected from the group consisting of. In another related aspect, the environmental pollutants are selected from, but not limited to, the list comprising particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by reducing collagenase activity, increasing the levels of antioxidant enzymes, reducing ROS levels, and decreasing the levels of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. In a related aspect, the composition is formulated with pharmaceutically / cosmetically acceptable excipients, adjuvants, bases, diluents, carriers, modifiers, antioxidants, bioavailability enhancers, and preservatives, and / or incorporated into a formulation containing skin care components, and is topically administered in the form of creams, gels, lotions, powders, serums, oils, suspensions, ointments, soaps, scrubs, emulsions, and compacts.
[0016] In a most preferred embodiment, the present invention discloses a method for protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants, the method comprising the step of topically administering to a mammal in need of such protection a composition comprising 95% by weight of tetrahydrocurcumin. In related embodiments, the composition is a composition comprising 10% by weight or more of oroxylin A, 10% by weight or more of baicalein and 2% by weight or more of chrysin; 95% by weight of oxyresveratrol; 90% by weight of pterostilbene; and a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate, and further comprises one or more components selected from the group consisting of. In another related aspect, the environmental pollutants are selected from, but not limited to, the list comprising particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by increasing the levels of antioxidant enzymes, decreasing the ROS levels, and reducing the levels of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. In another related aspect, the inflammatory marker is IL-8.
[0017] In another most preferred embodiment, the present invention discloses a method for purifying and rejuvenating the skin of a mammal exposed to environmental pollutants and UV radiation, the method comprising the step of topically administering to a mammal in need of such an effect a composition containing 95% by mass of tetrahydrocurcumin. In a related embodiment, the composition is a composition containing 10% by mass or more of oroxylin A, 10% by mass or more of baicalein and 2% by mass or more of chrysin; 95% by mass of oxyresveratrol; 90% by mass of pterostilbene; and further comprises one or more components selected from the group consisting of compositions containing at least 10% by mass of β-glucogallin and at least 10% by mass of total mucic acid gallate. In another related aspect, the environmental pollutants are selected from, but not limited to, the list containing particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by reducing collagenase activity, increasing the level of antioxidant enzymes, reducing ROS levels, and decreasing the level of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. In another related aspect, the inflammatory marker is IL-8.
[0018] In another most preferred embodiment, the present invention discloses a composition comprising 95% by weight of tetrahydrocurcumin for use in protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants. In a related aspect, the present invention discloses a composition comprising 95% by weight of tetrahydrocurcumin for use in purifying and rejuvenating the skin of a mammal exposed to environmental pollutants and UV radiation. In a related embodiment, the composition is a composition comprising 10% by weight or more of oroxylin A, 10% by weight or more of baicalein and 2% by weight or more of chrysin; 95% by weight of oxyresveratrol; 90% by weight of pterostilbene; and a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate, and further comprises one or more components selected from the group consisting of. In another related aspect, the environmental pollutants are selected from, but not limited to, the list comprising particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by reducing collagenase activity, increasing the levels of antioxidant enzymes, reducing ROS levels, and decreasing the levels of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. In a related aspect, the composition is formulated with pharmaceutically / pharmaceutically-cosmetically acceptable excipients, adjuvants, bases, diluents, carriers, regulators, antioxidants, bioavailability enhancers, and preservatives, and / or incorporated into a formulation containing skin care components, and is topically administered in the form of creams, gels, lotions, powders, serums, oils, suspensions, ointments, soaps, scrubs, emulsions, and compacts.
[0019] In a most preferred embodiment, the present invention is a method for protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants, the method comprising the step of topically administering to a mammal in need of such protection a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate. In related embodiments, the composition is a composition comprising 10% by weight or more of oroxylin A, 10% by weight or more of baicalein, and 2% by weight or more of chrysin; 95% by weight of oxyresveratrol; 90% by weight of pterostilbene; and / or one or more components selected from the group consisting of 95% by weight of tetrahydrocurcumin (Tetrahydrocurucmin). In another related aspect, the environmental pollutants are selected from, but not limited to, the list comprising particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by increasing the levels of antioxidant enzymes, decreasing the ROS levels, and reducing the levels of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. In another related aspect, the inflammatory marker is IL-8.
[0020] In another most preferred embodiment, the present invention is a method for purifying and rejuvenating the skin of a mammal exposed to environmental pollutants and UV radiation, the method comprising the step of topically administering to a mammal in need of such an effect a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate. In related embodiments, the composition is a composition comprising 10% by weight or more of oroxylin A, 10% by weight or more of baicalein and 2% by weight or more of chrysin; 95% by weight oxyresveratrol; 90% by weight pterostilbene; and one or more components selected from the group consisting of 95% by weight tetrahydrocurcumin. In another related aspect, the environmental pollutants are selected from, but not limited to, the list comprising particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by reducing collagenase activity, increasing the levels of antioxidant enzymes, reducing ROS levels, and decreasing the levels of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. In another related aspect, the inflammatory marker is IL-8.
[0021] In another most preferred embodiment, the present invention discloses a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate for use in protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants. In a related aspect, the present invention discloses a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallate for use in purifying and rejuvenating the skin of a mammal exposed to environmental pollutants and UV radiation. In a related embodiment, the composition is a composition comprising 10% by weight or more of oroxylin A, 10% by weight or more of baicalein and 2% by weight or more of chrysin; 95% by weight of oxyresveratrol; 90% by weight of pterostilbene; and / or one or more components selected from the group consisting of 95% of tetrahydrocurcumin. In another related aspect, the environmental pollutants are selected from, but not limited to, the list comprising particulate matter, polycyclic aromatic hydrocarbons (PAHs), volatile organic compounds (VOCs), surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. In yet another related aspect, the composition confers skin protection by reducing collagenase activity, increasing the levels of antioxidant enzymes, reducing ROS levels, and decreasing the levels of inflammatory markers. In another related aspect, the antioxidant enzymes are selected from the group consisting of glutathione peroxidase, superoxide dismutase and catalase. In another related aspect, the inflammatory markers are selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha and IL-8. In another related aspect, the inflammatory marker is IL-8. In a related aspect, the composition is formulated with pharmaceutically / cosmetically acceptable excipients, adjuvants, bases, diluents, carriers, modifiers, antioxidants, bioavailability enhancers, and preservatives and / or incorporated into a formulation containing skin care components and topically administered in the form of creams, gels, lotions, powders, serums, oils, suspensions, ointments, soaps, scrubs, emulsions, and compacts.
[0022] In related aspects, the one or more skin care components are selected from the group consisting of, but not limited to, alpha lipoic acid, beetroot extract, Boswellia serrata extract, beta boswellic acid, Boswellia serrata oil, Centella asiatica extract, triterpenes, Garcinia indica extract, anthocyanins, Cocos nucifera extract and juice, Coleus forskohlii extract, forskolin, Coleus forskohlii oil, tetrahydropiperine, ellagic acid, gall extract, polyphenols, galangal extract, glycyrrhizic acid, green tea extract, epigallocatechin gallate, licorice extract, glycyrrhizic acid monoammonium, limonoids, oleanolic acid, cosmetic peptides (oleanolic acid conjugated to Lys-Thr-Thr-Lys-Ser, oleanolic acid conjugated to Lys-Val-Lys), oleuropein, piperlongumine extract, piperine, ellagic acid, pomegranate extract (water-soluble), pterostilbene, resveratrol, Pterocarpus santalinus extract, rosemary extract, rosmarinic acid, amla extract, beta-glucogallin, tetrahydrocurcumin, Salvia Officinalis (sage) leaf extract, ursolic acid, saponins, Sesamum indicum (sesame) seed extract, sesamin and sesamolin, moringa oil, moringa seed extract, tochinoki extract, vitex oil, ximeninic acid, ethyl ascorbic acid, argan oil, lemon peel extract, turmeric oil, barley beta-glucan, coenzyme Q10, olive oil, avocado oil and cranberry oil.
[0023] In another related aspect, the one or more antioxidants and anti-inflammatory agents are selected from, but not limited to, vitamin A, D, E, K, C, B complex, rosmarinic acid, alpha-lipoic acid, ellagic acid, glycyrrhizic acid, epigallocatechin gallate, plant polyphenols, grabridine, moringa oil, oleanolic acid, oleuropein, carnosic acid, urocanic acid, phytoene, lipoid acid, lipoamide, ferritin, desferal, billirubin, billiverdin, melanin, ubiquinone, ubiquinol, ascorbyl palmitate, magnesium ascorbyl phosphate, ascorbyl acetate, derivatives such as tocopherol and vitamin E acetate, uric acid, alpha-glucosylrutin, calalase and superoxide dismutase, glutathione, selenium compounds, butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), sodium metabisulfite (SMB), propyl gallate (PG), and the amino acid cysteine. In another related aspect, the one or more bioavailability enhancers are selected from, but not limited to, the group consisting of piperine, tetrahydropiperine, quercetin, garlic extract, ginger extract, and naringin. This specification includes the following specific and illustrative examples that demonstrate the most preferred embodiments.
Example
[0024] (Example 1): Methodology Plant active substances A composition containing 10% by mass or more of oroxylin A, 10% by mass or more of baicalein, and 2% by mass or more of chrysin was obtained from the bark of Oroxylum indicum (Sorizaya no ki) according to the process outline of U.S. Patent No. 10,555,982. The composition is commercially available from Sami Labs Limited as Sabroxy (registered trademark). 95% by mass of oxyresveratrol was standardized from Artocarpus lakoocha (Lactipannoki) using a standardized internal process, which is also commercially available from Sami Labs Limited as Artonox (registered trademark). A phytochemical containing 95% by mass of tetrahydrocurcumin was isolated from Curcuma longa (Turmeric) using a commercially available process and is also available from Sami Labs Limited as Sabiwhite (registered trademark). A composition containing at least 10% by mass of β-glucogallin and at least 10% by mass of total mucic acid gallate was standardized from Emblica officinalis and is commercially available from Sami Labs Limited as Saberry (registered trademark). A 90% by mass pterostilbene composition was isolated and standardized from Pterocarpus marsupium using a standardized process and is also commercially available from Sami Labs Limited as Pterowhite (registered trademark).
[0025] ROS assay The cell-permeable non-fluorescent dye 2’,7’-dichlorofluorescein diacetate (DCFH-DA) enters the cells, the acetate groups of DCFH-DA are cleaved by cellular esterases, and non-fluorescent DCFH is trapped inside the cells. Subsequent oxidation by reactive oxygen species generated inside the cells results in the formation of fluorescent DCF, which is detectable at an Ex:Em wavelength of 485 / 520. The scavenging activity of the sample is indicated by the decrease in fluorescence when compared to a control without antioxidants.
Chemical formula
[0026] Human HaCaT keratinocyte cells / mouse fibroblasts were maintained in DMEM containing 25 mM glucose together with 10% heat-inactivated fetal bovine serum and antibiotics at 37 °C and 5% CO2. When the cells reached 70 - 80% confluence, they were trypsinized, washed, and seeded into 96-well plates at a density of 5x104 cells / well. The cells were allowed to adhere overnight. Prior to exposure to the contaminants, the cells were pretreated with various non-toxic concentrations of various plant bioactives for 60 minutes. The cells were then exposed to the following contaminants in the presence of the plant bioactives. UVA intensity of 15 joules / m2 for 60 minutes UV-B intensity of 4.6 joules / m2 for 10 minutes Heavy metals (0.25 mM each of cobalt chloride and lead nitrate) for 6 hours After a certain treatment period, freshly prepared DCFH-DA reagent was added to all wells at a concentration of 10 μg / well and incubated at 37 °C for 30 minutes to determine intracellular ROS. Fluorescence was recorded at a wavelength of 485:520 (Ex:Em) nm in a BMG FluoStar Optima microplate reader.
[0027] Protection against polycyclic aromatic hydrocarbons in the presence of UVA Polycyclic aromatic hydrocarbons (PAHs) are a class of environmental contaminants with mutagenic and tumorigenic properties. PAHs are widely present in the environment, being generated from the incomplete combustion of natural substances and tobacco smoke (Connell, D. W.; Hawker, D. W.; Warne, M. J.; Vowles, P. P.: Polycyclic aromatic hydrocarbons (PAHs). In Introduction into Environmental Chemistry (McCombs, K., and Starkweather, A. W., eds), 1997, pp. 205-217, CRC Press LLC, Boca Raton, FL. 2. Shaw, G. R.; Connell, D. W.: Prediction and monitoring of the carcinogenicity of polycyclic aromatic compounds (PACs). Rev. Environ. Contam. Toxic., 1994, 135, 1-62). PAHs themselves are biologically inert and require metabolic activation to exert genotoxicity. PAHs absorb light in the UVA range and react with oxygen or other molecules to generate reactive intermediates (Yu H, Xia Q, Yan J, et al. Photoirradiation of polycyclic aromatic hydrocarbons with UVA light - a pathway leading to the generation of reactive oxygen species, lipid peroxidation, and dna damage. Int J Environ Res Public Health.2006;3:348-354). Therefore, PAHs are "activated" by light irradiation and can cause photoinduced cytotoxicity. Thus, the photoirradiation of PAHs by UVA irradiation becomes a contaminant that causes cytotoxicity and DNA damage.
[0028] Human HaCaT keratinocyte cells were seeded in 96-well plates at a density of 1x104 cells / well. The cells were allowed to adhere overnight. These were pretreated with 50 μg / mL of benzo(a)pyrene as a PAH for 50 minutes and then exposed to UVA at an intensity of 17 J / m2 together with various concentrations of plant active substances. The cells were washed with sterile buffer, and fresh culture medium (2% FBS) was added together with each concentration of plant active substance, and then incubated at 37 °C for 24 hours in a CO2 incubator. Neutral red (25 μg / mL) (3-amino-7-dimethylamino-2-methylphenazine hydrochloride) was added to the cells for 3 hours. The cells were lysed, and the uptake of NR by the cells was determined by reading the absorbance at 540 nm with a Tecan microplate reader (TECAN Ltd, Mannedorf, Switzerland).
[0029] Antioxidant assay Cell antioxidants are depleted by pollutants. The ability of plant active substances to increase these antioxidant enzymes intracellularly was studied in vitro. Human HaCaT keratinocyte cells were seeded in 6-well plates at a density of 5x105 cells / well. The cells were pretreated with plant active substances for 1 hour and then exposed to UVA at an intensity of 17 J / m2 for 50 minutes. The cells were washed with sterile buffer, and fresh culture medium (2% FBS) was added together with each concentration of plant active substance, and then incubated at 37 °C for 24 hours in a CO2 incubator. Cell lysates were prepared and the superoxide dismutase (SOD) level and glutathione peroxidase (GPx) were estimated. Estimation of superoxide dismutase (SOD) activity As per the manufacturer's instructions (Elabsciences), the activity of SOD in cell lysates was measured by the WST-1 method. Xanthine oxidase (XO) can catalyze the WST-1 reaction with O2- to generate a water-soluble formazan dye. SOD can catalyze the disproportionation of superoxide anions, so this reaction can be inhibited by SOD, and the activity of SOD is negatively correlated with the amount of formazan dye. Therefore, the activity of SOD can be determined by colorimetric analysis of the WST-1 product.
[0030] Estimation of glutathione peroxidase (GPx) activity The activity of glutathione peroxidase was determined according to the method of Hafeman et al. (1974). Glutathione peroxidase decomposes H2O2 in the presence of glutathione (GSH), thereby depleting GSH. The remaining GSH was measured using DTNB, which gives a colored complex. To 100 μl of cell lysate, 0.2 mM GSH, 0.05 mM H2O2 and 1 mM NaN3 were added to a total volume of 250 μl with 1 M sodium phosphate buffer (pH 7.0). The reaction was incubated at 37 °C for 10 minutes and stopped by adding 50 μl of 25% TCA. The reaction mixture was centrifuged at 3000 rpm for 10 minutes, and to 0.1 ml of the supernatant, 0.1 ml of 0.4 M Na2HPO4 and 50 μl of 1 mM DTNB were added. After incubation at 37 °C for 10 minutes, the intensity of yellow formation was measured at 412 nm. The enzyme activity was expressed as units / mg protein. DPPH-free radical scavenging assay Reactive oxygen species (ROS), including superoxide, hydroxyl, peroxyl, and alkoxy radicals, are generated by normal metabolic processes. Under normal conditions, these free radicals are scavenged by cellular antioxidants to maintain an equilibrium state. Radiation, toxins, and pollutants increase ROS, which can induce oxidative damage to biomolecules such as lipids, nucleic acids, proteins, and carbohydrates. These ROS-induced damages cause skin irritation, inflammation, aging, cancer, and many other diseases. The α,α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging method is one of the first approaches for evaluating the antioxidant ability of compounds.
[0031] Materials Equipment: Tecan microplate reader (TECAN Ltd, Mannedorf, Switzerland) Reagents: 0.1 mM DPPH ethanol solution, 0.1 M phosphate buffered saline (pH 7.4) Microtiter plate: 96-well microtiter plate (Corning, USA) Procedure DPPH is a stable free radical in methanol solution with an absorbance at 520 nm. When the free radical is scavenged by an antioxidant molecule, the resulting solution appears yellow. The decolorization of the purple DPPH methanol solution was used to measure the hydrogen atom or electron donating ability of extracellular metabolites.
[0032] Various plant active substances at different concentrations were diluted with methanol. In the DPPH radical scavenging assay, 20 μL of samples at various concentrations were mixed with 180 μL of DPPH methanol in a 96-well plate according to the previously described method (Clarke et al., 2013). The plate was kept in the dark for 15 minutes, and then the absorbance of the solution was measured at 540 nm using a microplate reader (TECAN Ltd, Mannedorf, Switzerland). Blanks (DMSO, methanol) and standards (TBHQ methanol solution) were recorded simultaneously. Extracts were screened at varying concentrations to establish the inhibitory concentration (IC50, the concentration that reduces the DPPH absorbance by 50%). The free radical scavenging activity was calculated as follows. (B - C)-(S - C) % Scavenging activity = ----------- X 100 (B - C) Wherein, B = Absorbance of the reference solution (OD of DPPH) C = Absorbance of the reference solution blank (OD of methanol only) S = Absorbance of the test solution C = Absorbance of the test solution blank
[0033] Anti - inflammatory activity IL8 in the assay supernatant was measured using a Duoset ELISA kit (R&D systems, catalog number DY208). Anti - collagenase activity Collagenase is a type of matrix metalloprotease that digests collagen and other components of the extracellular matrix (ECM). The ECM functions as a scaffold for stabilizing skin structure and also aids in skin cell proliferation and metabolic functions. Loss of collagen leads to skin wrinkles and sagging. The principle of the collagenase inhibition assay is based on the fact that the substrate DQ (trademark) gelatin is conjugated to a fluorescein - fluorescent compound. Fluorescence is quenched in DQ (trademark) gelatin. DQ (trademark) gelatin is efficiently digested by collagenase, yielding a measurable fluorescent compound. The increase in fluorescence is proportional to the enzyme activity. In the presence of an anti - collagenase compound, the amount of fluorescence should decrease for a given enzyme and substrate concentration.
[0034] Materials Equipment - BMG FLUOstar Optima (fluorescence microplate reader) Reagents: Phosphate buffer (pH 7.4) Collagenase enzyme assay kit (Enzchek (registered trademark) collagenase, gelatinase assay kit, Invitrogen, USA) Microtiter plate - 96 - well microtiter plate (black) - Corning, USA. The assay was performed using a 96-well black microtiter plate. Type IV from Clostridium histolyticum with DQ gelatin as the substrate was used in the assay. Various concentrations of various plant active substances were pre-incubated with 20 μl of the gelatin substrate (12.5 μg / ml). 100 μl of the collagenase enzyme solution (final concentration - 0.4 U / ml) was added, and the fluorescence intensity was measured at Em: 485 nm and Ex: 520 nm after 30 minutes. The enzyme activity of the control (buffer) was recorded.
[0035] The percent inhibition was calculated as follows. (B - BC) - (T - C) Percent inhibition = -------------- X 100 (B - BC) B - Fluorescence in the presence of the enzyme BC - Fluorescence in the absence of enzyme activity T - Fluorescence of enzyme activity in the presence of the inhibitor TC - Fluorescence of the inhibitor alone
[0036] (Example 2): Anti - contamination effect of a composition containing oroxylin A, baicalein, and chrysin Protection against UVA and BaP Compositions containing oroxylin A, baicalein, and chrysin at concentrations of 3.12 - 25 μg / ml conferred dose - dependent protection against UVA + BaP (Figure 1). Similarly, the compositions reduced ROS generated by exposure to heavy metals (Figure 2a), UVA (Figure 2b), and UVB (Figure 2c). Normalization of antioxidant enzyme activity Exposure to UV reduced the superoxide dismutase concentration and increased the glutathione peroxidase activity. The compositions restored normal enzyme activity in keratinocytes (Figures 3a and 3b).
[0037] Inhibition of pollutant - induced inflammatory cytokines The composition containing oroxylin A, baicalein and chrysin inhibited the generation of IL-8 induced by pollutants (Table 1).
Table 1
[0038] Antioxidant activity The composition containing oroxylin A, baicalein and chrysin showed excellent antioxidant activity by inhibiting DPPH radicals in a dose-dependent manner with an IC50 of 5.1 μg / ml (Table 2).
Table 2
[0039] Anti-collagenase activity Harmful pollutants damage the skin by decomposing collagen. The composition containing oroxylin A, baicalein and chrysin inhibited collagen degradation by inhibiting the enzyme collagenase (Table 3).
Table 3
[0040] (Example 3): Anti-pollution effect of β-glucogallin composition Protection against UVA and BaP The β-glucogallin composition at a concentration of 3.12 - 25 μg / ml conferred dose-dependent protection against UVA + BaP (Figure 4). Similarly, the composition reduced ROS generated by exposure to heavy metals (Figure 5a), UVA (Figure 5b) and UVB (Figure 5c). Normalization of antioxidant enzyme activity Exposure to UV decreased the superoxide dismutase concentration and increased the glutathione peroxidase activity. The composition restored normal enzyme activity in keratinocytes (Figure 6a and 6b).
[0041] Inhibition of Inflammatory Cytokines Induced by Pollutants β-Glucogallin inhibited the production of IL-8 induced by pollutants (Table 4). [Table 4] Antioxidant Activity The β-glucogallin composition showed excellent antioxidant activity by inhibiting DPPH radicals in a dose-dependent manner with an IC50 of 4.34 μg / ml (Table 5). [Table 5]
[0042] Anticollagenase Activity The β-glucogallin composition inhibited collagen degradation by inhibiting the enzyme collagenase (Table 6). [Table 6]
[0043] (Example 4): Anti-Pollution Effect of 95% Tetrahydrocurcumin Protection against UVA and BaP Tetrahydrocurucmin at concentrations of 1.25 - 10 μg / ml conferred dose-dependent protection against UVA + BaP (Figure 7). Similarly, the composition reduced ROS generated by exposure to heavy metals (Figure 8a), UVA (Figure 8b), and UVB (Figure 8c). Normalization of Antioxidant Enzyme Activity Exposure to UV decreased the superoxide dismutase concentration and increased the glutathione peroxidase activity. Tetrahydrocurucmin restored normal enzyme activity in keratinocytes (Figures 9a and 9b).
[0044] Inhibition of Inflammatory Cytokines Induced by Pollutants Tetrahydrocurucmin inhibited the production of IL-8 induced by pollutants (Table 7). [Table 7]
[0045] Antioxidant activity Tetrahydrocurucmin showed excellent antioxidant activity by inhibiting DPPH radicals in a dose-dependent manner with an IC50 of 2.29 μg / ml (Table 8). [Table 8]
[0046] Anticollagenase activity Tetrahydrocurucmin inhibited collagen degradation by inhibiting the enzyme collagenase (Table 9). [Table 9]
[0047] (Example 4) Anti-pollution effect of 95% oxyresveratrol Protection against UVA and BaP Oxyresveratrol at concentrations of 3.12 - 12.5 μg / ml conferred dose-dependent protection against UVA+BaP (Figure 10). Similarly, the composition reduced ROS generated by exposure to heavy metals (Figure 11a), UVA (Figure 11b), and UVB (Figure 11c). Normalization of antioxidant enzyme activity Exposure to UV decreased the concentration of superoxide dismutase and increased the activity of glutathione peroxidase. Oxyresveratrol restored normal enzyme activity in keratinocytes (Figures 12a and 12b).
[0048] Inhibition of Inflammatory Cytokines Induced by Pollutants Oxyresveratrol inhibited the production of IL-8 induced by pollutants (Table 10). [Table 10]
[0049] Antioxidant Activity Oxyresveratrol showed excellent antioxidant activity by inhibiting DPPH radicals in a dose-dependent manner with an IC50 of 0.61 μg / ml (Table 11). [Table 11]
[0050] Anticollagenase Activity Oxyresveratrol inhibited collagen degradation by inhibiting the enzyme collagenase (Table 12). [Table 12]
[0051] (Example 5): Anti-Pollution Effect of Combinations of Bioactive Compositions The effects of combinations of bioactive compositions were evaluated by their ability to protect HaCaT cells against UVA-benzo(a)pyrene. The results are summarized in Table 13 below. [Table 13]
[0052] The activities of the individual active substances are referred to in Table 14. [Table 14] The results indicate that the combination with oroxylin, baicalein, and chrysin compositions exhibits synergistic activity and may be incorporated into formulations either alone or in combination with other anti-fouling agents. Compositions containing oroxylin, baicalein, and chrysin compositions together with various plant active substances were further evaluated for their protective ability against UVA-BaP exposure and the elimination of UVA and heavy metal-induced ROS. The results are summarized in the following tables.
[0053] Protection against UV-A BaP exposure [Table 15]
[0054] [Table 16]
[0055] [Table 17]
[0056] [Table 18]
[0057] Reduction of UVA-induced ROS [Table 19]
[0058] [Table 20]
[0059] [Table 21]
[0060] [Table 22]
[0061] Reduction of heavy metal-induced ROS
Table 23
[0062]
Table 24
[0063]
Table 25
[0064]
Table 26
[0065] The results showed that compositions containing oroxylin, baicalein, and chrysin compositions, together with various phytochemicals, exhibited a synergistic increase in their protective ability against UVA-BaP exposure and the elimination of UVA and heavy metal-induced ROS. Although the invention has been described with reference to preferred embodiments, it will be clearly understood by those skilled in the art that the invention is not limited thereto. Rather, the scope of the invention should be construed only in conjunction with the appended claims. Another aspect of the present invention may be as follows. 〔1〕A method for protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants, the method comprising the step of topically administering to a mammal in need of such protection a composition comprising 10% by mass or more of oroxylin A, 10% by mass or more of baicalein, and 2% by mass or more of chrysin. 〔2〕The method according to 〔1〕 above, wherein the composition further comprises one or more components selected from the group consisting of compositions comprising 95% by mass of oxyresveratrol; 95% by mass of tetrahydrocurcumin; 90% by mass of pterostilbene; and at least 10% by mass of β-glucogallin and at least 10% by mass of total mucic acid gallate. 〔3〕The method according to 〔1〕 above, wherein the environmental pollutant is selected from the group consisting of particulate matter, polycyclic aromatic hydrocarbons, volatile organic compounds, surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. 〔4〕The method according to 〔1〕 above, wherein the composition confers skin protection by increasing the level of antioxidant enzymes, decreasing the ROS level, and decreasing the level of inflammatory markers. 〔5〕The method according to 〔4〕 above, wherein the antioxidant enzyme is selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. 〔6〕The method according to 〔4〕 above, wherein the inflammatory marker is selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. 〔7〕The method according to 〔4〕 above, wherein the inflammatory marker is IL-8. 〔8〕A method for purifying and rejuvenating the skin of a mammal exposed to environmental pollutants and UV radiation, the method comprising the step of topically administering to a mammal in need of such an effect a composition comprising 10% by mass or more of oroxylin A, 10% by mass or more of baicalein, and 2% by mass or more of chrysin. The method according to [8], wherein the composition further comprises one or more components selected from the group consisting of compositions containing 95% by mass of oxyresveratrol; 95% by mass of tetrahydrocurcumin; 90% by mass of pterostilbene; and at least 10% by mass of β-glucogallin and at least 10% by mass of total mucic acid gallate. The method according to [8], wherein the environmental pollutant is selected from the group consisting of particulate matter, polycyclic aromatic hydrocarbons, volatile organic compounds, surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals. The method according to [8], wherein the composition confers skin protection by reducing collagenase activity, increasing the level of antioxidant enzymes, reducing the ROS level, and decreasing the level of inflammatory markers. The method according to
[11] , wherein the antioxidant enzyme is selected from the group consisting of glutathione peroxidase, superoxide dismutase, and catalase. The method according to
[11] , wherein the inflammatory marker is selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8. The method according to
[11] , wherein the inflammatory marker is IL-8.
Claims
1. Use of oroxylin A, baicalein and chrysin in the manufacture of a composition for protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants, wherein the composition comprises one or more components selected from the group consisting of 95% by weight oxyresveratrol; 95% by weight tetrahydrocurcumin; and 90% by weight pterostilbene, together with 10% by weight or more of oroxylin A, 10% by weight or more of baicalein and 2% by weight or more of chrysin.
2. 2. The use of claim 1, wherein the composition further comprises a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallates.
3. 2. The use according to claim 1, wherein the environmental pollutants are selected from the group consisting of particulate matter, polycyclic aromatic hydrocarbons, volatile organic compounds, surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals.
4. 2. The use according to claim 1, wherein the composition provides protection to the skin by increasing the levels of antioxidant enzymes, decreasing the levels of ROS and lowering the levels of inflammatory markers.
5. 5. The use according to claim 4, wherein the antioxidant enzyme is selected from the group consisting of glutathione peroxidase, superoxide dismutase and catalase.
6. The use according to claim 4, wherein the inflammatory marker is selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha and IL-8.
7. The use according to claim 4, wherein the inflammatory marker is IL-8.
8. 1. Use of oroxylin A, baicalein and chrysin in the manufacture of a composition for cleansing and rejuvenating mammalian skin exposed to environmental pollutants and UV radiation, wherein the composition comprises one or more ingredients selected from the group consisting of 95% oxyresveratrol by weight; 95% tetrahydrocurcumin by weight; and 90% pterostilbene by weight, together with 10% or more oroxylin A, 10% or more baicalein by weight, and 2% or more chrysin by weight.
9. 9. The use of claim 8, wherein the composition further comprises a composition comprising at least 10% by weight of β-glucogallin and at least 10% by weight of total mucic acid gallates.
10. 9. The use according to claim 8, wherein the environmental pollutants are selected from the group consisting of particulate matter, polycyclic aromatic hydrocarbons, volatile organic compounds, surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals.
11. 9. The use according to claim 8, wherein the composition confers protection to the skin by decreasing collagenase activity, increasing the levels of antioxidant enzymes, decreasing ROS levels and decreasing the levels of inflammatory markers.
12. 12. The use according to claim 11, wherein the antioxidant enzyme is selected from the group consisting of glutathione peroxidase, superoxide dismutase and catalase.
13. The use according to claim 11, wherein the inflammatory marker is selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha and IL-8.
14. The use according to claim 11, wherein the inflammatory marker is IL-8.
15. A composition for protecting mammalian skin against the harmful effects of UV radiation and environmental pollutants, comprising one or more ingredients selected from the group consisting of oxyresveratrol; tetrahydrocurcumin; and pterostilbene, together with at least 10% by weight of oroxylin A, at least 10% by weight of baicalein, and at least 2% by weight of chrysin, the composition being administered topically to a mammal in need of such protection.
16. 16. The composition of claim 15, further comprising a composition comprising β-glucogallin and total mucic acid gallate.
17. 16. The composition of claim 15, wherein the environmental pollutants are selected from the group consisting of particulate matter, polycyclic aromatic hydrocarbons, volatile organic compounds, surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals.
18. 16. The composition of claim 15, which provides protection to the skin by increasing levels of antioxidant enzymes, decreasing ROS levels, and lowering levels of inflammatory markers.
19. 19. The composition of claim 18, wherein the antioxidant enzyme is selected from the group consisting of glutathione peroxidase, superoxide dismutase and catalase.
20. 19. The composition of claim 18, wherein the inflammatory marker is selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8.
21. The composition of claim 18, wherein the inflammatory marker is IL-8.
22. A composition for cleansing and rejuvenating mammalian skin exposed to environmental pollutants and UV radiation, comprising one or more ingredients selected from the group consisting of oxyresveratrol; tetrahydrocurcumin; and pterostilbene, together with at least 10% by weight of oroxylin A, at least 10% by weight of baicalein, and at least 2% by weight of chrysin, the composition being administered topically to a mammal in need of such benefit.
23. 23. The composition of claim 22, further comprising a composition comprising β-glucogallin and total mucic acid gallate.
24. 23. The composition of claim 22, wherein the environmental pollutants are selected from the group consisting of particulate matter, polycyclic aromatic hydrocarbons, volatile organic compounds, surfactants, nitrogen and sulfur oxides, carbon monoxide, ozone, and heavy metals.
25. 23. The composition of claim 22, wherein the composition confers protection to the skin by decreasing collagenase activity, increasing levels of antioxidant enzymes, decreasing ROS levels, and decreasing levels of inflammatory markers.
26. 26. The composition of claim 25, wherein the antioxidant enzyme is selected from the group consisting of glutathione peroxidase, superoxide dismutase and catalase.
27. 26. The composition of claim 25, wherein the inflammatory marker is selected from the group consisting of interleukin (IL)-1 alpha, IL-1 beta, tumor necrosis factor (TNF)-alpha, and IL-8.
28. The composition of claim 25, wherein the inflammatory marker is IL-8.
Citation Information
Patent Citations
Composition for cosmetic or dermatic use containing combination of tetrahydrocurcuminoid and amide oil
JP2003300815A
Skin lightening compositions and methods
US20080305059A1
Protective Compositions for Dermal Papilla Cells
US20110033565A1
Compositions including sesamin, methods of making and using the same in skin Anti-aging and skin lightening applications
US20160287505A1