CN102860925A - Application of theaflavin to preparation of tyrosinase inhibitor - Google Patents
Application of theaflavin to preparation of tyrosinase inhibitor Download PDFInfo
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- CN102860925A CN102860925A CN2012103146006A CN201210314600A CN102860925A CN 102860925 A CN102860925 A CN 102860925A CN 2012103146006 A CN2012103146006 A CN 2012103146006A CN 201210314600 A CN201210314600 A CN 201210314600A CN 102860925 A CN102860925 A CN 102860925A
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- theaflavin
- tyrosinase
- preparation
- application
- liposome
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Abstract
The invention discloses an application of theaflavin to preparation of a tyrosinase inhibitor, which relates to the technical field of medicaments and daily chemical production, in particular to the technical field of production of an inhibitor of tyrosinase causing pigmentation diseases of a human body. The invention discloses a novel application of theaflavin, i.e., the theaflavin has an inhibiting function on tyrosinase, can be prepared into a novel potential medicament or cosmetic for preventing and treating the pigmentation diseases, and has the effects of preventing, improving and treating skin pigmentation diseases such as freckles, chloasma and age pigments.
Description
Technical field
The present invention relates to medicine, daily-use chemical industry production technical field, particularly to the production technical field of the inhibitor of the tryrosinase of the pigmentation disease that causes human body.
Background technology
Theaflavin (Theaflavin) structural formula is as follows, and its molecular formula is: C
29H
24O
12
The U.S. chemical abstract number of including (CASNo.): 4670-05-7; Be main component in the black tea, be described as " soft gold " in the Folium Camelliae sinensis, safe.Theaflavin not only plays decisive role to color, smell and taste and the quality of black tea, and has widely physiologically active and pharmacological action, such as anti-cardiovascular system diseases, antiinflammatory, immunomodulating, antitumor, antiviral, anti-diabetic etc.
Tryrosinase (Tyrosinase) is the synthetic key enzyme of organism melanin, and its unusual overexpression can cause the pigmentation disease of human body.Therefore, tyrosinase inhibitor can be treated at present common pigmentation disease such as freckle, chloasma, senile plaque etc., be widely used in cosmetics and pharmaceuticals industry, be tyrosinase inhibitor such as its brightening agent in the popular in the market skin-lightening cosmetic.As seen, efficient, safe tyrosinase inhibitor has broad application prospects.
Summary of the invention
The objective of the invention is to propose with theaflavin as the new purposes to tyrosinase inhibitory action.
The present invention proposes the application of theaflavin in the preparation tyrosinase inhibitor.
Through for a long time research, by lot of experiments, the inventor has proved theaflavin except having the existing purposes that it is found that, also has other new purposes---have tyrosinase inhibitory action, so proposed the present invention.
The theaflavin that the present invention relates to is a kind of chemical compound, can extract from Folium Camelliae sinensis, refining gained, also can buy in market to obtain, and be 98% theaflavin chemical compound (Theaflavin) etc. such as the purity of Jiangsu Kai Ji bio tech ltd production.
Theaflavin of the present invention is as the application of tyrosinase inhibitor in preparation cosmetics, pharmaceuticals or preparation for external application to skin.
The dosage form of described cosmetics, pharmaceuticals or preparation for external application to skin is: liposome, skin whitener, membrane, drop pill, ointment or nanometer formulation.
The present invention compared with prior art has following advantages: it is active that theaflavin has obvious restraint of tyrosinase, can form a kind of novel potential prevention, treatment pigmentation disease medicament or cosmetics, have the effect to prevention, improvement and the treatment of the cutaneous pigmentation diseases such as freckle, chloasma, senile plaque.
The present invention also provides and contains theaflavin as the pharmaceutical composition of the treatment pigmentation disease of effective ingredient, and this pharmaceutical composition also contains conventional pharmaceutical carrier and/or pharmaceutically acceptable excipient.
The specific embodiment
Embodiment one: the tyrosinase inhibitory activity test of theaflavin
1, experiment material
Theaflavin (CASNo.:4670-05-7) 98% purity, Jiangsu Kai Ji bio tech ltd provides; Tryrosinase (EC Number 1.14.18.1): be 3 933 U/mg than vigor, Sigma company buys; Other reagent are the AR level, the traditional Chinese medicines institutional purchase.
2, experimental procedure
2.1 operating procedure
Before the mensuration, accurately draw A, B, C, D group reaction liquid with volume shown in the pipettor according to the form below, every group parallel 3 times, place first 37 ℃ of water-baths to be incubated 5min, respectively with A, B, C and D four group reaction liquid mixings, and then add respectively 0.5ml tryrosinase solution, mixing to each group during mensuration, the beginning timing, 3min is transferred in the cuvette at 475nm place survey absorbance.
Table 1 reactant liquor forms
2.2 the calculating of tyrosinase activity suppression ratio
The suppression ratio of tyrosinase activity (%)=[(A
A-A
B)-(A
C-A
D)]/(A
A-A
B) * 100
In the formula: A
A: the absorbance of A pipe; A
B: the absorbance of B pipe; A
C: the absorbance of C pipe; A
D: the absorbance of D pipe.
2.3 the suppression ratio of tyrosinase activity---IC
50Calculating
Take the sample concentration logarithm as abscissa, take suppression ratio as vertical coordinate, curve plotting is obtained the IC of sample restraint of tyrosinase
50Value.
3, experimental result and summary
Experimental result shows, the IC of theaflavin
50Be 50.84 μ mol/L; The IC of positive control arbutin
50Be 3025.62 μ mol/L.
The IC of theaflavin
50The IC that obviously is better than the positive control arbutin
50
Experimental result is not difficult to find out that it is active that theaflavin has obvious restraint of tyrosinase, can form a kind of novel potential prevention, treatment pigmentation disease medicament or cosmetics.Theaflavin adopts conventional method to be prepared into various dosage forms as the restraint of tyrosinase active component with pharmaceutically acceptable excipient and/or pharmaceutical carrier.
Embodiment two: the preparation of theaflavin liposome
With 3g lecithin, 1g cholesterol and 0.1g theaflavin, solution is in the mixed solution (volume ratio of dehydrated alcohol and chloroform is 1:1, and cumulative volume is 15ml) of dehydrated alcohol and chloroform, and adding 2mg vitamin E obtains solution A.
An amount of folic acid 33mg is dissolved in must solution B in the 330 μ l dimethyl sulfoxines.
Solution A, B are mixed, and add the 9g lactose and get mixture C, this solution C desolventizing is obtained immobilized artificial membrane.
The gained immobilized artificial membrane is water-soluble, after aquation, obtain liposome, with this liposome by 0.2 μ m membrane filtration, with liposome solutions in high pressure homogenizer under pressure 200-400Mpa supercharging homogenizing 2h step by step, the liposome that obtains is the solution of clear and bright homogeneous.
With the liposome solutions lyophilization desolventizing that obtains, obtain the theaflavin liposome of lyophilizing.
The theaflavin liposome powder of lyophilizing is added distilled water jolting dissolving, and measure particle diameter with Ls-230 type laser light scattering particle size analyzer (U.S. Beckman Coulter company).The particle diameter of liposome is respectively 90.8nm ± 5.2nm(n=3).With sem observation gained liposome.Be ball at observed under electron microscope to liposome, size matches with result with particle size analyzer determination.Measuring liposome encapsulation with ultrafiltration is that 90.3%, 48h percolation ratio is 1.2%.
Conclusion: the liposome made from theaflavin has the function of restraint of tyrosinase activity.
Embodiment three: the preparation of theaflavin skin whitener
Get stearic acid 10.0g, spermol 4.5g, lanoline 1.0g mixing; Other gets theaflavin chemical compound 0.1g, propylene glycol 15.0g, triethanolamine 0.7g, sodium lauryl sulphate 0.5g, ethylparaben 0.1g, distilled water 68.1mL mixing, place respectively beaker to be heated to fusing or dissolving, be kept at about 70 ℃ and under the stirring oil phase joined aqueous phase, stir to condensation, namely get the theaflavin skin whitener.
Conclusion: the beauty functions that the skin whitener made from theaflavin has the restraint of tyrosinase activity.
Embodiment four: the preparation of theaflavin ointment
Getting stearic acid 12g, glyceryl monostearate 3.5g, white oil 6g, vaseline 5g, wool grease 5g is heated to the beaker and makes fusing fully about 80 ℃; Triethanolamine 0.5g, ethylparaben 0.1g, chemical compound theaflavin 0.1g and distilled water 73mL are heated to about 80 ℃, stir in the lower mixed liquor that is added to stearic acid etc., to emulsifying, namely get theaflavin ointment.
Conclusion: the ointment made from theaflavin has the function of restraint of tyrosinase activity.
Claims (3)
1. the application of theaflavin in the preparation tyrosinase inhibitor.
2. theaflavin as claimed in claim 1 is as the application of tyrosinase inhibitor in preparation cosmetics, pharmaceuticals or preparation for external application to skin.
3. application according to claim 2 is characterized in that the dosage form of described cosmetics, pharmaceuticals or preparation for external application to skin is: liposome, skin whitener, membrane, drop pill, ointment or nanometer formulation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012103146006A CN102860925A (en) | 2012-08-30 | 2012-08-30 | Application of theaflavin to preparation of tyrosinase inhibitor |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012103146006A CN102860925A (en) | 2012-08-30 | 2012-08-30 | Application of theaflavin to preparation of tyrosinase inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102860925A true CN102860925A (en) | 2013-01-09 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2012103146006A Pending CN102860925A (en) | 2012-08-30 | 2012-08-30 | Application of theaflavin to preparation of tyrosinase inhibitor |
Country Status (1)
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103083199A (en) * | 2013-01-23 | 2013-05-08 | 中华全国供销合作总社杭州茶叶研究所 | Application of theaflavin and skin care product containing theaflavin |
| CN103520372A (en) * | 2013-09-22 | 2014-01-22 | 浙江大学 | Method for extracting tyrosinase inhibitor from tea seed pulp |
| CN103520373A (en) * | 2013-09-22 | 2014-01-22 | 浙江大学 | Method for extracting tyrosinase inhibitor from tea peel |
| CN113545484A (en) * | 2021-07-26 | 2021-10-26 | 江苏德和生物科技有限公司 | Anti-saccharification whitening theaflavin composition and application thereof |
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| WO2003002134A1 (en) * | 2001-06-27 | 2003-01-09 | Unigen Pharmaceuticals, Inc. | Method for generating, screening and dereplicating natural product libraries for the discovery of therapeutic agents |
| WO2011124528A2 (en) * | 2010-04-06 | 2011-10-13 | Unilever Nv | A personal care composition |
| JP2012072084A (en) * | 2010-09-29 | 2012-04-12 | Kracie Home Products Ltd | Elastase inhibitor, and cosmetic composition and pharmaceutical composition comprising the same |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2003002134A1 (en) * | 2001-06-27 | 2003-01-09 | Unigen Pharmaceuticals, Inc. | Method for generating, screening and dereplicating natural product libraries for the discovery of therapeutic agents |
| WO2011124528A2 (en) * | 2010-04-06 | 2011-10-13 | Unilever Nv | A personal care composition |
| JP2012072084A (en) * | 2010-09-29 | 2012-04-12 | Kracie Home Products Ltd | Elastase inhibitor, and cosmetic composition and pharmaceutical composition comprising the same |
Non-Patent Citations (8)
| Title |
|---|
| ICHIRO SHIRASUGI等: "Novel Screening Method for Potential Skin- Whitening Compounds by a Luciferase Reporter Assay", 《BIOSCI.|BIOTECHNOL. BIOCHEM.》 * |
| PAYEL BANERJEE等: "Effect of Theaflavin, A Black Tea Extract on Ovarian Cancer Cell line", 《BOMBAY HOSPITAL JOURNAL》 * |
| TATYANA A.ZYKOVA等: "The signal transduction networks required for phosphorylation of STAT1 at Ser727 in mouse epidermal JB6 cells in the UVB response and inhibitory mechanisms of tea polyphenols", 《CARCINOGENESIS》 * |
| YUANYUAN WU等: "Evaluation of the antioxidant effects of four main theaflavin derivatives through chemiluminescence and DNA damage analyses", 《BIOMEDICINE & BIOTECHNOLOGY》 * |
| YURIKO YAMAOKA等: "Effect of Theaflavins on Melanin Biosynthesis in Mouse B16 Melanoma Cells", 《BIOSCI.|BIOTECHNOL. BIOCHEM.》 * |
| 林茂等: "姜黄素对正常人表皮黑素细胞黑素生成的影响", 《中国中西医结合皮肤性病学杂志》 * |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103083199A (en) * | 2013-01-23 | 2013-05-08 | 中华全国供销合作总社杭州茶叶研究所 | Application of theaflavin and skin care product containing theaflavin |
| CN103520372A (en) * | 2013-09-22 | 2014-01-22 | 浙江大学 | Method for extracting tyrosinase inhibitor from tea seed pulp |
| CN103520373A (en) * | 2013-09-22 | 2014-01-22 | 浙江大学 | Method for extracting tyrosinase inhibitor from tea peel |
| CN103520373B (en) * | 2013-09-22 | 2015-09-09 | 浙江大学 | A kind of method extracting tyrosinase inhibitor from tea peel |
| CN103520372B (en) * | 2013-09-22 | 2015-09-09 | 浙江大学 | A kind of method extracting tyrosinase inhibitor from the tea-seed dregs of rice |
| CN113545484A (en) * | 2021-07-26 | 2021-10-26 | 江苏德和生物科技有限公司 | Anti-saccharification whitening theaflavin composition and application thereof |
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Application publication date: 20130109 |