• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    Disclosed is the cosmeceutical potential of 3,5-dimethoxy-4'-hydroxystilbene with respect to its melanogenesis-inhibiting and photoprotective activities. Also disclosed is a topical melanogenesis inhibiting composition comprising from 0.01% to 50% by weight of 3,5-dimethoxy-4'-hydroxystilbene.
    公开号:AT510867A2
    申请号:T9089/2010
    申请日:2010-05-21
    公开日:2012-07-15
    发明作者:
    申请人:Sami Labs Ltd；Majeed Muhammed；
    IPC主号:
    专利说明:

    1 «« * I * · * · »» * * «··« · • * «4 t ·« · ··· «* · * ··· ····« · · · · · «» «» • # * »· * ·« · ·
    Melanogenesis inhibition by 3, 5-dimethoxy-4 1-hydroxystilbene and cosmeceutical compositions thereof
    b CROSS-REFERENCE TO RELATED APPLICATIONS
    This application claims the benefit of US Patent Application No. 12 / 408,808, filed March 23, 2009, in the United States Patent and Trademark Office, the contents of which are incorporated herein by reference in their entireties.
    BACKGROUND OF THE INVENTION
    FIELD OF THE INVENTION
    The invention relates generally to 3,5-dimethoxy-4'-hydroxystilbene. More particularly, the invention discloses the potential of 3, 5-dimethoxy-4'-hydroxystilbene (Pteros-2C tilben) in terms of its melanogenesis-inhibiting and photoprotective activities and compositions thereof.
    DESCRIPTION OF THE PRIOR ART Pterostilbene is a stilbenoide, which belongs to a phytoalexi-called group of compounds produced by plants in response to stress. It is considered to be the key compound found mainly in blueberries and grapes, which is known to have anti-cancer, anti-hypercholesterolemia, anti-cancer
    Hypertriglyceridamie, antidiabetic and anti-fungal potential has. • • • • 2 • * ·
    It is the primary object of the present invention to disclose novel melanogenesis-inhibiting activity of pterostilbene. It is another object of the present invention to disclose a melanogenesis-inhibiting composition comprising 3,5-dimethoxy-41-hydroxystilbene, which compositions have been disclosed from about 0.01% to about 50% of 3,5-dimethoxy-41-hydroxystilbene. 10
    It is yet another object of the present invention to disclose the use of 3,5-dimethoxy-4'-hydroxystilbene in the manufacture of a medicament for treating skin hyperpigmentation. 15
    Furthermore, the present invention also discloses a method of treating skin hyperpigmentation.
    The present invention achieves the above objects and provides further similar advantages.
    SUMMARY OF THE INVENTION
    The invention relates to the kosmezeutisehe potential of 3,5-25 dimethoxy-4'-hydroxystilbene in view of its Melsnoge-nese -emnende and photoprotective activities. Also disclosed is a topical melanogenesis inhibiting composition comprising from 0.01% to 50% by weight of 3,5-dimethoxy-4'-hydroxystilbene. who
    Other features and advantages of the present invention will be apparent from the more detailed description which follows.
    visually, which exemplifies the principle of the invention. DESCRIPTION OF THE PREFERRED EMBODIMENT o
    In another most preferred embodiment, the present invention relates to a melanogenesis inhibiting composition comprising 3,5-dimethoxy-41-hydroxystilbene as reported by STR # 1, wherein the composition is from about 0.01% to about 10% by weight 50% 3,5-dimethoxy-4'-hydroxystilbene.
    In yet another most preferred embodiment, the present invention relates to the use of 3,5-15 dimethoxy-4'-hydroxystilbene, represented by STR # 1, in the manufacture of a medicament for treating skin hyperpigmentation.
    In yet another most preferred embodiment, the present invention provides a method of treating skin hyperpigmentation, which method comprises topical application of a composition comprising, by weight, from about 0.01% to about 50% 3,5-dimethoxy-4 '- hydroxystilbene, represented by STR # 1, on affected areas of the skin requiring such treatment.
    In yet another, most preferred embodiment, the present invention relates to a method of treating skin hyperpigment: erur.g, which method comprises topical application of a composition comprising, by weight, from about 0.01% to about 50% of 3,5-dimethoxy 4'-hydroxystilbene, represented by STR # 1, on the affected area of the chew that require such treatment, said "" * * + * ·· "· · *« · 4 «« • * + · · · «· · *« · 4
    f »· * M« · · · * · · * «• # · ♦ · ·
    Stilbene is obtained from Pterocarpus marsupium extract in commercially significant purity of at least 90%. The stilbene 3,5-dimethoxy-4r-hyroxystilbene was obtained by solvent extraction ιοη of Pterocarpus marsupium. The solvents used were ethyl acetate and hexane. Other solvents of similar polarity may be used. Supercritical carbon dioxide, scC02 / can also be used to remove non-polar constituents of Pterocarpus marsupium. Alternatively, pterostilbene can be obtained by synthesis, as shown by way of example in US Patent 7,253,324.
    STR # 1
    OH
    15 EXAMPLE I
    The fungal tyrosinase inhibitory activity of 3,5-dimethoxy-4'-hydroxystilbene was determined by incubating different concentrations of the sample with 400 U / ml fungal tyrosinase and then adding 3.53 mM L-tyrosine substrate in one Microplate examined. The absorbance at the 10th reaction minute was read in a Fluostar Optima microplate reader at 4 92 r.m. 3,5-Dinethoxy-4'-hydroxystyrene showed a significant inhibition of fungal tyrsinase with an IC50 of 7 25 pg / ml. EXAMPLE II 3-O-Dimethoxy-4'-hydroxystyrene was tested for melanogenesis inhibition in a BlGF1 mouse melanoma cell line. *** " 5 B16F1 cells were induced with 0.5 nM MSH (melanocyte stimulating horirion) and then treated with different concentrations of the sample. The sample was treated three times after every 72 hours. On the 9th day of treatment, the melanin was extracted from the cells with IN NaOH and absorbance read at 405 nm in a Fluostar Optima microplate reader. 3,5-Dimethoxy-4'-hydroxystilbene showed a significant inhibition of melanogenesis with an IC50 value of C, 5 pg / ml. Surprisingly, 3,5-dimethoxy-41-hydroxystilbene showed about 6 times higher potential than glabridin. 15
    EXAMPLE III 3,5-Dimethoxy-4 1-hydroxystyrene. Iben was examined for UV protection in Swiss 3T3 mouse fibroblast cells. Swiss 3T3 Fib-20 roblet cell monolayers were exposed to UV A (0.5 J / cm 2) and UV B (0.05 J / cm 2) in the presence and absence of sample treatment at different concentrations. After ÜV-Expcsition the lines in the. C02 ~ incubator was incubated for 72 hours and cell viability was determined by SRB (Sulp-25 horhodomin B) staining. UV protection is determined as the increased percentage of live sample-treated cells compared to the untreated lines after UV exposure. 3, b-dimethoxy-4'-hydroxystilbene exhibited a significant JV protease of 32% compared to the 30 untreated cells. 5 »·» »6
    EXAMPLE IV PTEROSTILED COMPOSITIONS OF THE PRESENT INVENTION (ILLUSTRATIVE EXAMPLES)
    Prototype formulation for depigmenting cream
    Ingredients% w / w Function A Glyceryl monostearate qs Emulsifier Isopropylpyrimate qs Plasticizer PEG 100 Stearate qs Plasticizer Stearic acid qs Emulsifier Caprin-capryl-crlglyceride qs Plasticizer Propylparaben Preservative 3 Propyler.cl ykol qs Humectant Tetrasodium EDTA qs Complexing agent Imidurea f qs Preservative Methylparaben qs Preservative Demmcral Water to 100 Solvents C Pterost: Iben 0, 1 active substance arbutin 1.0 active substance licorice 40% CA 0.1 active substance ethanol qa solvent D 20% sodium hydroxide solution qs neutralizing agent (if necessary to adjust the pH) DC 3 021. qs Silicone Salcare SC 91 qs Viscosity modifying agent E Perfume qs Perfume
    Properties:
    Appearance: pH:
    Light brown colored emulsion 5.5-7.5 10
    Alternative formulation
    Ceteareth-25-2.0%
    Glyceryl stearate 4.0%
    Stearyl alcohol 2.0%
    Ethylhexyl-8.5%
    Caprylic / capric triglyceride 5.5%
    Water 75.0%
    Kathon CG-2-3 Tr Pterostilbene (90%) - 1% While the invention has been described in terms of a preferred embodiment, it will be 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.
    权利要求:
    Claims (6)
    [1]
    Claims 1. A melanogenesis-inhibiting composition comprising 3,5-dimethoxy-4'-hydroxystyrene represented by STR # 1, wherein 5 is the composition by weight of about zero , 01% to 50% has 3,5-dimethoxy-4'-hydroxystilbene.

    OH STR # 1
    [2]
    2. Use of 3,5-drmethoxy-4'-hydroxystilbene, represented by 3TR # 1, in the manufacture of a medicament for treating skin hyperpigmentation.


    [3]
    A method of treating skin hyperpigmentation, wherein the method comprises topically applying a collagen composition comprising, by weight, from about 0.01% to 50% of 3,5-dimethoxy-41-hydroxystilbene, represented by STR # 1, to be 9 * * • * affected areas of the skin in need of such treatment. 9 * * • *


    [4]
    A melanogenesis inhibiting composition comprising 3,5-dimethoxy-4'-hydroxystilbene according to claim 1, wherein 3,5-dimethoxypterostilber is obtained from Pterocarpus marsupium at purity levels above 50% w / w.

    _L
    [5]
    5. Use of 3,5-dimethoxy-4'-hydroxystilbene according to claim 2, wherein 3, 5-dimethoxy-4'-hydroxystilbene is obtained from Pterocarus marsupium in purity degrees above 50% w / w * • · 10 * • · 10

    OH STR # 1
    [6]
    6. Use of 3,5-dimethoxy-4'-hydroxystilbene according to An-5 spoke 3, wherein Pterocar-pus marsupium 3,5-dimethoxy-4'-hydroxystilbene is obtained in purities above 50% w / w.

    STR # 1 OH 10
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    AU4084599A|1998-05-18|1999-12-06|Oklahoma Medical Research Foundation|Resveratrol inhibition of myeloperoxidase|
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    US8716355B2|2007-06-20|2014-05-06|Kent State University|Hydroxylated tolans and related compounds in the treatment of a cancer|EP2322159A1|2009-10-30|2011-05-18|Green Molecular, S.L.|Use of pterostilbeneas medicament for prevention and/or treatment of skin diseases, damages or injures or as cosmetic|
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    CN103393579B|2013-08-08|2014-10-22|珀莱雅化妆品股份有限公司|Preparation method for whitening and repairing lipid nanoparticle emulsion|
    WO2016014529A1|2014-07-21|2016-01-28|Wisys Technology Foundation, Inc.|Skin lightening compounds|
    US9980924B2|2014-09-04|2018-05-29|The Regents Of The University Of California|Topical pterostilbene compositions for use in treating UV-induced loss of barrier function in skin|
    WO2018034327A1|2016-08-17|2018-02-22|香港友池有限公司|Composition for internal use that includes pterostilbene glycoside|
    CN106755133B|2017-01-20|2021-05-25|深圳大学|Method for preparing o-phenol compound by enzyme method|
    法律状态:
    2016-05-15| REJ| Rejection|Effective date: 20160515 |
    优先权:
    申请号 | 申请日 | 专利标题
    US12/408,808|US20100240767A1|2009-03-23|2009-03-23|Melanogenesis inhibitiuon by 3,5-dimethoxy-4'-hydroxystilbenes and cosmeceutical compositions thereof|
    PCT/US2010/035766|WO2010111719A2|2009-03-23|2010-05-21|Melanogenesis inhibition by 3, 5-dimethoxy-4'-hydroxystilbenes and cosmeceutical compositions thereof|
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