CN104983602A - Whitening agent combining water-soluble glabridin and endothelin antagonist - Google Patents
Whitening agent combining water-soluble glabridin and endothelin antagonist Download PDFInfo
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- CN104983602A CN104983602A CN201510487946.XA CN201510487946A CN104983602A CN 104983602 A CN104983602 A CN 104983602A CN 201510487946 A CN201510487946 A CN 201510487946A CN 104983602 A CN104983602 A CN 104983602A
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- glabridin
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Abstract
The invention relates to a whitening agent combining water-soluble glabridin and endothelin antagonist. The water-soluble glabridin which can inhibit the activity of three kinds of enzyme, namely, tyrosinase, hallachrome interconvertible enzyme and DHICA oxidase, in the melanin synthetic process and inhibit the activation effect of melanocyte stimulating hormone on melanophores, and native protein enzymolysis multidimensional peptide which can inhibit the cell differentiation of endothelin on the melanophore and the activation effect of tyrosinase activity are used in a combine mode, the whitening effect is improved, and the whitening agent combining water-soluble glabridin and endothelin antagonist is applied to whitening and sun block products.
Description
Technical field
The present invention relates to a kind of by the whitening additive of water solublity glabridin and endothelin antagonist compound use.
Background technology
Research shows, in melanic biosynthesis, tryrosinase, dopachrome interconvertible enzyme (Dopachrometautomerase) and DHICA oxidase (DHICA oxidase) take part in reaction simultaneously.Therefore, when exploitation whitening agent and skin-lightening cosmetic, this three kinds of enzymes must be considered simultaneously.
The beginning of the nineties in last century, the people such as the Imokawa of Japan find, under ultraviolet radiation, horn cell discharges a kind of basic element of cell division, after it is accepted by the receptor of melanocyte, meeting stimulation melanin cell proliferation, differentiation, and activate the activity of tryrosinase, improve melanic synthetic quantity (Jiang Zhijie, Zhu Yuxin, Wu Qiying, Zhang Fengxiang. the new ideas of melanin formation mechenism and the application [J] of composite whitening agent. household chemicals science .1998 (04): 3-5).
Glabridin extracts from the Radix Glycyrrhizae of certain species, is to generally acknowledge the most effective natural whiting agent in the world at present.The activity of its not only restraint of tyrosinase, dopachrome interconvertible enzyme and the oxidasic activity of DHICA can be suppressed again simultaneously, it is a kind of quick, efficient, green whitening cosmetics additive, there is the ability of the scavenging activated oxygen similar to SOD (superoxide dismutase), and the Ability of antioxygen free radicals close with vitamin E, also there is the effect of anti-inflammation, antioxidation, defying age, absorption ultraviolet, the bright skin of whitening, speckle dispelling.The glabridin of reported in literature 0.0002% can suppress melanotropin to the activation of melanocyte, its restraint reaches 41% (Zhou Mei, Xiao Jun, Xu Yizhao, Zeng Hong. the white-skinned face function evaluation of composite " three enzyme one elements " inhibitor. Perspective of China Washing Product Industry .2011 (2): 71-74).
After the enzymolysis hybrid peptide with the native protein of Endothelin antagonism enters the receptors bind of epidermis and melanocyte, make melanocyte no longer by the impact of Endothelin, and allow melanic aggregate velocity in each melanocyte be reduced to the genetic factor of this organism itself and the normal level of regulatory factor defined.
People's reports such as Zhu Yuxin, Sun Donghai are by Glycyrrhiza glabra L. warp or without water extraction or extraction, by organic solvent extraction or reflux, extract, concentrate, obtain the glabridin of concentrate or≤40% purity, directly adsorb with macromolecule resin with ultrafilter membrane ultrafiltration or without ultrafiltration, with water, ethanol, acetone or their mixed liquor drip washing, concentrated dissolving-recrystallization, obtain purity be greater than 90% high-purity glabrene (Zhu Yuxin, Sun Donghai. the production method .ZL200510023860.8 of high-purity glabrene).
The people such as Cui Zhaoyun, Jiang Zhijie, by the licoflavone of various purity and cyclodextrin in dehydrated alcohol, cyclodextrin bag is made to connect licoflavone, again after ethanol removed in vacuo, inclusion compound is soluble in water, filter out decontamination, obtain water solublity licoflavone (Cui Zhaoyun, Jiang Zhijie, Yao Wei. the production method of water solublity licoflavone, CN102140144 A).
Summary of the invention
The object of the invention is according to melanin formation mechenism, a kind of whitening additive simultaneously suppressing three kinds of enzymatic activitys, melanotropin and Endothelin effect is provided.
Whitening additive involved in the present invention is a kind of by water solublity glabridin, endothelin antagonist and the antiseptic mixture according to the weight ratio of 90 ~ 99:10 ~ 1:0-50, recommends weight ratio to be followed successively by the whitening product of the compound use of 96.7:3.3:5.
Above-mentioned water solublity glabridin is that it contains the cyclodextrin parcel glabridin aqueous solution of 2.0%-2.5% weight, and water solublity light Radix Glycyrrhizae is that cyclodextrin parcel glabridin can be dissolved in the water.
Its nitrogen content of endothelin antagonist involved in the present invention is 8%-15%, the enzymolysis hybrid peptide dry powder of molecular weight≤2000, and it is by pearl protein lyophilizing gained after papain enzymolysis.Through B16 melanoma cell model discrimination, the enzymolysis hybrid peptide of the tool Endothelin antagonism of acquisition.
Described antiseptic is pentanediol, phenoxyethanol or hexanediol.
Endothelin antagonist involved in the present invention is that pearl protein is carried out enzymolysis through papain by one, obtains the enzymolysis hybrid peptide with Endothelin antagonism.
Above-mentioned whitening additive preparation method of the present invention, is the aqueous solution of the glabridin wrapped up by hybrid peptide dry powder and the cyclodextrin containing 2.0%-2.5% weight, filters or add activated carbon filtration, removes impurity, adds or do not add antiseptic; Wherein the enzymolysis hybrid peptide of glabridin aqueous solution, native protein and the weight ratio of antiseptic are 90 ~ 99:10 ~ 1:0 ~ 50.
Described enzymolysis hybrid peptide is obtained by following method: when 10-80 DEG C and pH value are 2-10, pearl protein papain is carried out enzymolysis 10 minutes-12 hours, ultrafilter membrane ultrafiltration or again drying become powder, during enzymolysis, the ratio of albumen and water is 1:5-1:120, and described enzyme and the ratio of albumen are 1:10 to 1:1000.
Whitening additive of the present invention may be used for whitening articles for use.Be a kind of effective skin-whitening and sunscreen product, effectively can reduce the calmness that UVB irradiates rear skin pigment, skin can be protected and improve skin whiteness.
Detailed description of the invention
To contribute to understanding the present invention by following embodiment, but content of the present invention can not be limited.
Embodiment 1:
Go 88% lactic acid 0.3L to stir and add purified water 1.2L, mix homogeneously, the gradation of 100g Margarita powder is joined in lactic acid solution, filtration after question response completes, removing filtrate stays filter cake, is taken off by filter cake and puts into 1L distilled water water, add 1.5g papain, 1g cysteine hydrochloride, 1gEDTA disodium salt be uniformly mixed, enzymolysis 5 hours in 40 DEG C of water-baths, crosses and filters filter cake, stay enzymolysis solution.This enzymolysis solution is carried out ultrafiltration with the film of 2000 molecular cut offs, and ultrafiltrate is concentrated into 100mL, and carry out lyophilization subsequently and obtain dry powder 6.3g, nitrogen content is 10.55%, is required endothelin antagonist.
Embodiment 2:
Get the water solublity glabridin aqueous solution that 90g content is 2.0%, add 10g endothelin antagonist under stirring, add 1g active carbon drainage until completely dissolved, a small amount of insoluble matter of elimination.Add 5g pentanediol in the solution of filtering as antiseptic, obtain composite whitening agent.
Embodiment 3:
Get the water solublity glabridin aqueous solution that 93g content is 2.0%, add 7g endothelin antagonist under stirring, add 1g active carbon drainage until completely dissolved, a small amount of insoluble matter of elimination.Add 5g pentanediol in the solution of filtering as antiseptic, obtain composite whitening agent.
Embodiment 4:
Get the water solublity glabridin aqueous solution that 97g content is 2.0%, add 3g endothelin antagonist under stirring, add 1g active carbon drainage until completely dissolved, a small amount of insoluble matter of elimination.Add 5g pentanediol in the solution of filtering as antiseptic, obtain composite whitening agent.
Embodiment 5:
Deionized water 99g heated and boiled leaves standstill after 30 minutes and is cooled to room temperature, gets 0.1g endothelin antagonist stirring and dissolving, a small amount of insoluble matter of elimination.Add 5g pentanediol in the solution of filtering as antiseptic, obtain endothelin antagonist test fluid.
Embodiment 6:
The composite whitening agent 3g (containing water solublity glabridin 0.0582g, endothelin antagonist 0.09g) that Example 4 is obtained, adds mix homogeneously in the cooling purified water after 97g boiling sterilization, and obtained composite whitening agent content is the whitening test fluid of 3%.
Embodiment 7:
Deionized water 97.1g heated and boiled leaves standstill after 30 minutes and is cooled to room temperature, gets the water solublity glabridin aqueous solution stirring and dissolving that 2.9g content is 2.0%, a small amount of insoluble matter of elimination.Add 5g pentanediol in the solution of filtering as antiseptic, obtain water solublity glabridin test fluid.
Embodiment 8:
U.S. AMA test result: blank is carried out in three pieces of regions respectively by choosing at 30 Fitzpatrick Ш type skin volunteer back skin surface, UV smears the process of whitening test fluid after irradiating and not treating process and UV irradiation.Through 56 days test proofs, embodiment 5 gained composite whitening agent was a kind of effective skin-whitening product, effectively can reduce the calmness that UVB irradiates rear skin pigment simultaneously.The improvement of skin whiteness and two test blocks---the reduction of the undosed pigment with smearing the test block that composite whitening agent treatment processes has statistical significance, further statistical analysis is pointed out, after composite whitening agent treatment process is smeared in test section, also there is statistical significance compared with the test section data without irradiation treatment process.
Table one:
Table two:
Embodiment 9:
Example 4 gained endothelin antagonist test fluid, by carrying out Pigmented reduction test at 30 Fitzpatrick Ш type skin volunteer back skin surface, test result contrasts with embodiment 8 gained composite whitening agent test result and shows: the effect that composite whitening agent reduces for cutaneous pigmentation will be much better than single endothelin antagonist.
Table three:
Embodiment 10:
Example 7 gained water solublity glabridin test fluid, improve test by carrying out skin brightness at 30 Fitzpatrick Ш type skin volunteer back skin surface, test result contrasts with embodiment 8 gained composite whitening agent test result and shows: composite whitening agent will be much better than single water solublity glabridin test fluid for the improvement effect of skin brightness.
Table four:
Claims (6)
1. a whitening additive for water solublity glabridin and endothelin antagonist compound use, is characterized in that the enzymolysis hybrid peptide of glabridin aqueous solution, native protein and the antiseptic weight ratio according to 90 ~ 99:10 ~ 1:0-50 is to mixture;
Described glabridin aqueous solution is the aqueous solution of the water solublity glabridin containing 2.0%-2.5% weight;
The enzymolysis hybrid peptide of described native protein is by the endothelin antagonist of pearl protein lyophilizing gained after papain enzymolysis;
Described antiseptic is pentanediol, phenoxyethanol or hexanediol.
2. whitening additive as claimed in claim 1, is characterized in that described water solublity glabridin is the glabridin of cyclodextrin parcel.
3. whitening additive as claimed in claim 1, is characterized in that described enzymolysis hybrid peptide to be nitrogen content is the endothelin antagonist dry powder of 8%-15%, molecular weight≤2000.
4. a whitening additive preparation method as claimed in claim 1, it is characterized in that the aqueous solution of the glabridin wrapped up as claim 1 hybrid peptide dry powder and the cyclodextrin containing 2.0%-2.5% weight, filter or add activated carbon filtration, add or do not add antiseptic; Wherein the enzymolysis hybrid peptide of glabridin aqueous solution, native protein and the weight ratio of antiseptic are 90 ~ 99:10 ~ 1:0 ~ 50.
5. whitening additive preparation method as claimed in claim 41, it is characterized in that described enzymolysis hybrid peptide is obtained by following method: when 10-80 DEG C and pH value are 2-10, pearl protein papain is carried out enzymolysis 10 minutes-12 hours, ultrafilter membrane ultrafiltration or again drying become powder, during enzymolysis, the ratio of albumen and water is 1:5 ~ 1:120, and described enzyme and the ratio of albumen are 1:10 to 1:1000.
6. whitening additive as claimed in claim 1 is used for whitening and sun-proof articles.
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| CN201510487946.XA CN104983602A (en) | 2015-08-11 | 2015-08-11 | Whitening agent combining water-soluble glabridin and endothelin antagonist |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106619148A (en) * | 2017-01-17 | 2017-05-10 | 上海应用技术大学 | Water-soluble glabridin microcapsule and preparation method thereof |
| CN108618992A (en) * | 2018-06-25 | 2018-10-09 | 亿利耐雀生物科技有限公司 | A kind of glabridin composition and preparation method thereof |
| CN109730006A (en) * | 2019-03-19 | 2019-05-10 | 西华大学 | The method for improving Animal melanin content |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004107284A (en) * | 2002-09-20 | 2004-04-08 | Naris Cosmetics Co Ltd | Cosmetic |
| CN1680386A (en) * | 2005-02-05 | 2005-10-12 | 上海奥利实业有限公司 | Production of high-purity glabrene |
| CN1908183A (en) * | 2006-08-16 | 2007-02-07 | 上海奥利实业有限公司 | Enzyme medium hybrid peptide of native protein with endothelin antagonism |
| CN104688652A (en) * | 2015-03-17 | 2015-06-10 | 欧诗漫生物股份有限公司 | Cosmetic composition for skin whitening and preparation method thereof |
-
2015
- 2015-08-11 CN CN201510487946.XA patent/CN104983602A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004107284A (en) * | 2002-09-20 | 2004-04-08 | Naris Cosmetics Co Ltd | Cosmetic |
| CN1680386A (en) * | 2005-02-05 | 2005-10-12 | 上海奥利实业有限公司 | Production of high-purity glabrene |
| CN1908183A (en) * | 2006-08-16 | 2007-02-07 | 上海奥利实业有限公司 | Enzyme medium hybrid peptide of native protein with endothelin antagonism |
| CN104688652A (en) * | 2015-03-17 | 2015-06-10 | 欧诗漫生物股份有限公司 | Cosmetic composition for skin whitening and preparation method thereof |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106619148A (en) * | 2017-01-17 | 2017-05-10 | 上海应用技术大学 | Water-soluble glabridin microcapsule and preparation method thereof |
| CN108618992A (en) * | 2018-06-25 | 2018-10-09 | 亿利耐雀生物科技有限公司 | A kind of glabridin composition and preparation method thereof |
| CN109730006A (en) * | 2019-03-19 | 2019-05-10 | 西华大学 | The method for improving Animal melanin content |
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