CN103142435B - Lightening compositions of multimachine reason restraint of tyrosinase activity and products thereof - Google Patents
Lightening compositions of multimachine reason restraint of tyrosinase activity and products thereof Download PDFInfo
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- CN103142435B CN103142435B CN201310080919.1A CN201310080919A CN103142435B CN 103142435 B CN103142435 B CN 103142435B CN 201310080919 A CN201310080919 A CN 201310080919A CN 103142435 B CN103142435 B CN 103142435B
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Abstract
The present invention proposes lightening compositions of a kind of multimachine reason restraint of tyrosinase activity and products thereof, relate to household chemicals field.The lightening compositions of this multimachine reason restraint of tyrosinase activity contains the active matter of three kinds of restraint of tyrosinase active mechanisms: the active matter playing the active matter of Competitive assays effect, the active matter of non-competitive inhibition and linear hybrid competitive inhibition.The present invention uses three kinds of suppression mechanism to draw novel composite inhibiting, thus improve whitening working substance and combination press down enzyme effect, improve the biological effect of whitening and reduce and possible use zest; Broad covered area, the suitability is comparatively strong and have good whitening and speckle dispelling effect; And the products such as essence, day cream late frost, facial film, cleansing milk can be designed in cosmetic product.
Description
Technical field
The present invention relates to a kind of lightening compositions, be specifically related to a kind of different inhibiting mechanism generating rate-limiting enzyme-tryrosinase for melanin, the lightening compositions of Combinatorial Optimization comprising competitiveness, noncompetitive and linear hybrid competitive inhibition mechanism.
Background technology
Asia women especially focuses on pale U.S. of skin.For this demand, a large amount of cosmetics companies and researcher drop into the research and development that manpower and materials carry out skin-whitening effective ingredient.Existing many skin-whitening agents come out, if early stage pure chemistry thing hydroquinone, the fruit acid in mid-term and tissue extract placenta cream and recent natural plant extracts are as arbutin, Vc derivant and Radix Glycyrrhizae extract etc. at present.The appearance of these skin-whitening agents, meets the demand of consumers in general to a certain extent, have stimulated the development in skin-lightening cosmetic market.But we also should recognize clear-headedly, the whitening effect of pure chemistry thing is better, but side effect is larger; Though pure natural plant extract side effect is little, whitening effect is little or uncertain.
Current most skin-whitening agents works mainly in melanogenic rate-limiting enzyme-tryrosinase, existing research is known, and tyrosine → DOPA acid → DOPA quinone → dopachrome (or dihydroxy indole acid) → melanin oligomer → melanin is followed in the generation of dermal melanin.Arrive epidermis cell by melanocyte dendritic processes to epithelial cells transfer after melanin granule generates, thus cause skin darkening.For the research of skin-whitening or spot-removing function, mainly for the inhibitory action of tryrosinase, as patent CN101080215A, CN101357114A, CN102614094A etc., have an effect as target spot for tyrosinase activity.
Although more than research can suppress tyrosinase activity, but effect fails to reach expection in actual product, mainly there is several deficiency: 1) fail to study further for the mechanism of restraint of tyrosinase activity, not yet study whitening agent or which kind of mechanism restraint of tyrosinase activity of combination; 2) even if some whitening agent or composition known to tryrosinase inhibiting mechanism, but not yet for various inhibiting mechanism as competitive inhibition, Noncompetition inhibition and linear Noncompetition inhibition mechanism carry out the combination of working substance; 3) fail to carry out for different inhibiting mechanism the screening of whitening working substance or combination, and make the test of corresponding inhibition of enzyme activity.The existing whitening agent for tryrosinase suppression or combination, often only single consideration is to the Competitive assays effect of tryrosinase, and this action target spot is single, therefore there is effect deficiency, the required whitening agent dosage deficiencies such as releasing stimulus greatly in actual use.
Summary of the invention
The present invention is directed to the deficiency of the research of existing tryrosinase inhibiting mechanism and technical scheme, comprehensively different mechanism is suppressed to tyrosinase activity, select the competitive native tyrosine enzyme inhibitor of the suppression of competitive tryrosinase, Noncompetition inhibition and linear hybrid, carry out screening design whitening working substance and combine; The effect of comprehensive three kinds of suppressor modes, thus improve whitening working substance and combination press down enzyme effect, improve the biological effect of whitening and reduce and possible use zest.
Technical scheme of the present invention is achieved in that
A kind of lightening compositions of multimachine reason restraint of tyrosinase activity, it contains the active matter of three kinds of restraint of tyrosinase active mechanisms: the active matter playing the active matter of Competitive assays effect, the active matter of non-competitive inhibition and linear hybrid competitive inhibition, wherein, the active matter playing Competitive assays effect is at least one in ligustrazine, Morin, Radix Scutellariae extract; Playing the active matter of non-competitive inhibition is at least one in hesperidin, Folium Ginkgo extract, Radix Rhodiolae extract; The active matter of linear mixing competitive inhibition is Aloe cortex portion's extract or paeonol.
Competitive assays action character is: the analog of a competitive inhibitor zymolyte often; B inhibitor is identical with the binding site of substrate and enzyme with the binding site of enzyme; C inhibitor concentration is larger, then inhibitory action is larger; But increasing concentration of substrate can make suppression degree reduce; D kinetic parameter: Km value increases, and Vm value is constant.
Non-competitive inhibition feature is: a inhibitor can be combined with the different parts of enzyme with substrate simultaneously; B must have substrate to exist, and inhibitor could produce inhibitory action to enzyme; C kinetic parameter Km value is constant, and Vm reduces.
As preferably, its composition and percentage by weight are: ligustrazine 20 ~ 40%; Morin 10 ~ 30%; Hesperidin 20 ~ 40%; Paeonol 30 ~ 40%.
As preferably, its composition and percentage by weight are: Morin 20 ~ 30%; Radix Scutellariae extract 10 ~ 30%; Radix Rhodiolae extract 20 ~ 40%; Aloe cortex portion extract 20 ~ 30%.
As preferably, its composition and percentage by weight are: Morin 20 ~ 30%; Hesperidin 10 ~ 20%; Folium Ginkgo extract 20 ~ 40%; Aloe cortex portion extract 20 ~ 30%.
A kind of cold cream, its formula and mass parts as follows:
Component A: join osamine base stearate 12.0 parts; Spermol lactate 10.0 parts; 5.0 parts, white liquid paraffin; The Polyethylene Glycol of cetostearyl alcohol 2.5 parts; Ceryl alcohol 1.0 parts;
B component: propylene glycol 5.0 parts; Spermol lactate 60 is 3.0 parts; Distilled water 55.5 parts;
Component C: Kazon 0.5 part; 0.5 part, essence
D component: lightening compositions 5.0 parts.
A preparation method for cold cream, comprises the following steps: component A mixed, be heated to 80 DEG C; Again B component is mixed, be heated to 80 DEG C; In stirring, component A is added in B component, when temperature is down to 45 DEG C, adds lightening compositions and essence, continue to be cooled to 25 ~ 28 DEG C, packaging.
A kind of cream pack, its formula and mass parts as follows: polyvinyl acetate emulsion 15.0 parts; Polyvinyl alcohol 10.0 parts; 3.0 parts, olive oil; Glycerol 5.0 parts; Zinc oxide 8.0 parts; Kaolin 7.0 parts; Ethanol 5.0 parts; Purified Water 40.0 parts; Lightening compositions 6.0 parts; Spice 0.5 part; Kazon 0.5.
Then and Kaolin a preparation method for cream pack, comprises the following steps: by polyvinyl alcohol 3.0 parts of ethanol wet, zinc oxide, Purified Water mixes, and is heated to 70 DEG C of stirrings, leaves standstill and after being cooled to 45 DEG C, by spice, antiseptic, olive oil and remaining ethanol mixing, then and glycerol, lightening compositions, polyvinyl acetate emulsion add in the above-mentioned solution prepared together, stir into pasty state.
A kind of clean skin cleansing milk, its formula and mass parts as follows: Polyquaternium-10 is 1.0 parts; Cetearyl alcohol is 2.0 parts; Isopropyl palmitate is 6.0 parts; Cosmetic grade white oil is 0.5 part; Glycerol is 5.0 parts; Polysorbate-60 is 0.5 part; Glyceryl stearate is 0.5 part; Sodium lauryl sulfate is 0.3 part; Deionized water; 78.6 parts; Lightening compositions 5.0 parts; Kazon 0.1 part; 0.5 part, essence.
A preparation method for clean skin cleansing milk, is characterized in that comprising the following steps: by cetearyl alcohol, isopropyl palmitate, cosmetic grade white oil, glyceryl stearate, glycerol, polysorbate-60, sodium lauryl sulfate, after deionized water mixing, adds Polyquaternium-10, heat to 85 DEG C of mixing and emulsifyings, be cooled to 50 DEG C, add lightening compositions, Kazon, essence, stir and obtain product.
A kind of fair complexion cream, its formula and mass parts as follows:
Component A: 6.0 parts, Cera Flava; Hexadecanol 5.0 parts; Hydrogenated lanolin 8.0 parts; Squalane 37.5 parts; Fatty acid glyceride 4.0 parts;
B component: hydrophilic glyceryl monostearate 2.0 parts; Polysorbate-20 is 2.0 parts; Cysteine 0.25 part; Propylene glycol 5.0 parts; Kazon 0.4 part; Propyl gallate 0.1 part; Distilled water 23.75 parts;
Component C: 1.0 parts, essence;
D component: lightening compositions 5.0 parts.
A manufacture method for fair complexion cream, comprises the following steps: component A mixed, be heated to 75 DEG C, under agitation, component A added B component, to be cooledly add lightening compositions and essence to when 45 DEG C, packaging.
The beneficial effect that the present invention compared with prior art has is: the different suppression mechanism for tyrosinase inhibitor carry out screening and the combination of whitening working substance, use three kinds of suppression mechanism to draw novel composite inhibiting simultaneously, thus improve whitening working substance and combination press down enzyme effect, improve the biological effect of whitening and reduce and possible use zest; Broad covered area, the suitability is comparatively strong and have good whitening and speckle dispelling effect; And the products such as essence, day cream late frost, facial film, cleansing milk can be designed in cosmetic product.
Detailed description of the invention
Embodiment 1
Composition and the percentage by weight of the lightening compositions of the multimachine reason restraint of tyrosinase activity of the present embodiment are as follows:
| Active matter or extract | Proportioning (%) | To the tryrosinase mechanism of action |
| Ligustrazine | 20～40 | Competitive assays effect |
| Morin | 10～30 | Competitive assays effect |
| Hesperidin | 10～30 | Noncompetitive inhibition effect |
| Paeonol | 30～40 | The effect of linear hybrid Competitive assays |
Embodiment 2
Composition and the percentage by weight of the lightening compositions of the multimachine reason restraint of tyrosinase activity of the present embodiment are as follows:
| Active matter or extract | Proportioning (%) | To the tryrosinase mechanism of action |
| Morin | 20～30 | Competitive assays effect |
| Radix Scutellariae extract | 10～30 | Competitive assays effect |
| Radix Rhodiolae extracting solution | 20～40 | Noncompetitive inhibition effect |
| Aloe cortex portion extract | 20～30 | The effect of linear hybrid Competitive assays |
Embodiment 3
Composition and the percentage by weight of the lightening compositions of the multimachine reason restraint of tyrosinase activity of the present embodiment are as follows:
| Active matter or extract | Proportioning (%) | To the tryrosinase mechanism of action |
| Morin | 20～30 | Competitive assays effect |
| Hesperidin | 10～20 | Noncompetitive inhibition effect |
| Folium Ginkgo extract | 20～40 | Noncompetitive inhibition effect |
| Aloe cortex portion extract | 20～30 | The effect of linear hybrid Competitive assays |
Embodiment 4
A kind of cold cream, its formula and mass parts as follows:
Component A: join sugared amino stearic acid ester 12.0 parts; Spermol lactate 10.0 parts; 5.0 parts, white liquid paraffin; The Polyethylene Glycol of cetostearyl alcohol 2.5 parts; Ceryl alcohol 1.0 parts;
B component: propylene glycol 5.0 parts; Spermol lactate 60 is 3.0 parts; Distilled water 55.5 parts;
Component C: Kazon 0.5 part; 0.5 part, essence
D component: the lightening compositions of embodiment 1 5.0 parts.
Component A mixes by [method for making], is heated to 80 DEG C; Again B component is mixed, be heated to 80 DEG C; In stirring, component A is added in B component, when temperature is down to 45 DEG C, adds lightening compositions and the essence of embodiment 1, continue to be cooled to 25 ~ 28 DEG C, packaging.
[characteristic] this product pH value is 6.0, and close to the acid-base value of application on human skin, therefore suitable people use, and can produce well moisten and whitening effect skin.
Embodiment 5
A kind of cream pack, its formula and mass parts as follows: polyvinyl acetate emulsion 15.0 parts; Polyvinyl alcohol 10.0 parts; 3.0 parts, olive oil; Glycerol 5.0 parts; Zinc oxide 8.0 parts; Kaolin 7.0 parts; Ethanol 5.0 parts; Purified Water 40.0 parts; The lightening compositions of embodiment 1 6.0 parts; Spice 0.5 part; Kazon 0.5.
[method for making] is by polyvinyl alcohol 3.0 parts of ethanol wet, and Kaolin then, zinc oxide, Purified Water mixes, be heated to 70 DEG C of stirrings, to leave standstill and after being cooled to 45 DEG C, by spice, antiseptic, olive oil and the mixing of remaining ethanol, again and glycerol, the lightening compositions of embodiment 1, polyvinyl acetate emulsion add in the above-mentioned solution prepared together, stir into pasty state.
Fine moisturizing function is had to skin of face after [characteristic] this cream pack often uses, and can the generation of effective check melanin, reach the good result of whitening and speckle dispelling.
Embodiment 6:
A kind of clean skin cleansing milk, its formula and mass parts as follows:
Polyquaternium-10 is 1.0 parts; Cetearyl alcohol is 2.0 parts; Isopropyl palmitate is 6.0 parts; Cosmetic grade white oil is 0.5 part; Glycerol is 5.0 parts; Polysorbate-60 is 0.5 part; Glyceryl stearate is 0.5 part; Sodium lauryl sulfate is 0.3 part; Deionized water; 78.6 parts; The lightening compositions of embodiment 2 5.0 parts; Kazon 0.1 part; 0.5 part, essence.
A preparation method for clean skin cleansing milk, is characterized in that comprising the following steps: by cetearyl alcohol, isopropyl palmitate, cosmetic grade white oil, glyceryl stearate, glycerol, polysorbate-60, sodium lauryl sulfate, after deionized water mixing, adds Polyquaternium-10, heat to 85 DEG C of mixing and emulsifyings, be cooled to 50 DEG C, add lightening compositions, Kazon, the essence of embodiment 2, stir and obtain product.
Embodiment 7
A kind of fair complexion cream, its formula and mass parts as follows:
Component A: 6.0 parts, Cera Flava; Hexadecanol 5.0 parts; Hydrogenated lanolin 8.0 parts; Squalane 37.5 parts; Fatty acid glyceride 4.0 parts;
B component: hydrophilic glyceryl monostearate 2.0 parts; Polysorbate-20 is 2.0 parts; Cysteine 0.25 part; Propylene glycol 5.0 parts; Kazon 0.4 part; Propyl gallate 0.1 part; Distilled water 23.75 parts;
Component C: 1.0 parts, essence;
D component: the lightening compositions of embodiment 3 5.0 parts.
Component A mixes by [method for making], is heated to 75 DEG C, under agitation, component A is added B component, lightening compositions and the essence to adding embodiment 3 when 45 DEG C to be cooled, packaging.
[characteristic] this frost has good moisture-keeping functions, and can the effectively generation of check melanin in skin.
Above-mentioned composition is carried out to the Tyrosinase inhibition assays of cell-free system and cell system:
1, lightening compositions is to the inhibition test of tryrosinase:
In the test system of 0.25mol/L phosphate buffer (pH6.8), respectively with the L-DOPA of L-Tyr, 1.0mmol/L of 2.5mmol/L for substrate, add lightening compositions and the enzyme liquid of variable concentrations respectively, end reaction system is 1.0mL, enzyme concentration is 100U/mL, take arbutin as positive control, deionized water is as experiment blank; Optical density value D (λ) 475nm of 475nm is measured during reaction 25min.With the relative surplus vigor of enzyme, sample concentration is mapped, try to achieve IC
50value.
2, lightening compositions suppresses tryrosinase vitality test in mouse melanin cell:
B16 melanocyte is inoculated in 96 orifice plates, every hole 100uL, puts after 24h is educated in cultivation in incubator and add medicine.Take arbutin as positive control, sterilizing deionized water is blank.Abandoning supernatant after drug effect 3d, rinse twice with the PBS of pH6.8, it is ultrasonication in the PBS ice bath of the Tritonx-100 of 1% that every hole adds 90uL containing volume fraction, every hole adds the L-Dopa of 10uL10mmoL/L, hatch 60min for 37 DEG C, in 475nm place colorimetric, survey each hole absorbance by after blank well zeroing.
Suppression ratio=(1-medicine group mean absorbance values ÷ matched group mean absorbance values) × 100%.
3, finally result is suppressed:
According to suppression result, no matter lightening compositions suppresses vigor all good than the arbutin of single component at the tryrosinase of acellular system or cell line.Especially show on the Tyrosinase inhibition assays to B16 melanocyte, composition contained by said composition has better through cell performance than single arbutin, therefore to the tryrosinase suppression efficiency of B16 melanocyte, also there is better performance, imply that it is better than the interpolation of one-component arbutin to the effect of human body whitening and speckle dispelling in various cosmetics add.
The foregoing is only preferred embodiment of the present invention, not in order to limit the present invention, within the spirit and principles in the present invention all, any amendment done, equivalent replacement, improvement etc., all should be included within protection scope of the present invention.
Claims (7)
1. the lightening compositions of a multimachine reason restraint of tyrosinase activity, it is characterized in that it contains the active matter of three kinds of restraint of tyrosinase active mechanisms: the active matter playing the active matter of Competitive assays effect, the active matter of non-competitive inhibition and linear hybrid competitive inhibition, wherein, the active matter playing Competitive assays effect is at least one in ligustrazine, Morin, Radix Scutellariae extract; Playing the active matter of non-competitive inhibition is at least one in hesperidin, Folium Ginkgo extract, Radix Rhodiolae extract; The active matter of linear mixing competitive inhibition is Aloe cortex portion's extract or paeonol;
Its composition and percentage by weight are: ligustrazine 20 ~ 40%; Morin 10 ~ 30%; Hesperidin 20 ~ 40%; Paeonol 30 ~ 40%.
2. a lightening compositions for multimachine reason restraint of tyrosinase activity, is characterized in that, its composition and percentage by weight are: Morin 20 ~ 30%; Radix Scutellariae extract 10 ~ 30%; Radix Rhodiolae extract 20 ~ 40%; Aloe cortex portion extract 20 ~ 30%.
3. a lightening compositions for multimachine reason restraint of tyrosinase activity, is characterized in that, its composition and percentage by weight are: Morin 20 ~ 30%; Hesperidin 10 ~ 20%; Folium Ginkgo extract 20 ~ 40%; Aloe cortex portion extract 20 ~ 30%.
4. a kind of cold cream of the lightening compositions containing multimachine according to claim 1 reason restraint of tyrosinase activity, it is characterized in that its formula and mass parts as follows:
Component A: join osamine base stearate 12.0 parts; Spermol lactate 10.0 parts; 5.0 parts, white liquid paraffin; The Polyethylene Glycol of cetostearyl alcohol 2.5 parts; Ceryl alcohol 1.0 parts;
B component: propylene glycol 5.0 parts; Spermol lactate 60 is 3.0 parts; Distilled water 55.5 parts;
Component C: Kazon 0.5 part; 0.5 part, essence;
D component: lightening compositions 5.0 parts.
5. a kind of cream pack of the lightening compositions containing multimachine according to claim 1 reason restraint of tyrosinase activity, is characterized in that, its formula and mass parts as follows: polyvinyl acetate emulsion 15.0 parts; Polyvinyl alcohol 10.0 parts; 3.0 parts, olive oil; Glycerol 5.0 parts; Zinc oxide 8.0 parts; Kaolin 7.0 parts; Ethanol 5.0 parts; Purified Water 40.0 parts; Lightening compositions 6.0 parts; Spice 0.5 part; Kazon 0.5.
6. the clean skin cleansing milk of one of the lightening compositions containing multimachine according to claim 2 reason restraint of tyrosinase activity, is characterized in that, its formula and mass parts as follows: Polyquaternium-10 is 1.0 parts; Cetearyl alcohol is 2.0 parts; Isopropyl palmitate is 6.0 parts; Cosmetic grade white oil is 0.5 part; Glycerol is 5.0 parts; Polysorbate-60 is 0.5 part; Glyceryl stearate is 0.5 part; Sodium lauryl sulfate is 0.3 part; Deionized water; 78.6 parts; Lightening compositions 5.0 parts; Kazon 0.1 part; 0.5 part, essence.
7. a kind of fair complexion cream of the lightening compositions containing multimachine according to claim 3 reason restraint of tyrosinase activity, is characterized in that, its formula and mass parts as follows:
Component A: 6.0 parts, Cera Flava; Hexadecanol 5.0 parts; Hydrogenated lanolin 8.0 parts; Squalane 37.5 parts; Fatty acid glyceride 4.0 parts;
B component: hydrophilic glyceryl monostearate 2.0 parts; Polysorbate-20 is 2.0 parts; Cysteine 0.25 part; Propylene glycol 5.0 parts; Kazon 0.4 part; Propyl gallate 0.1 part; Distilled water 23.75 parts;
Component C: 1.0 parts, essence;
D component: lightening compositions 5.0 parts.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310080919.1A CN103142435B (en) | 2013-03-13 | 2013-03-13 | Lightening compositions of multimachine reason restraint of tyrosinase activity and products thereof |
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Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103845271A (en) * | 2014-02-13 | 2014-06-11 | 上海珍馨化工科技有限公司 | Whitening skin care product |
| CN103845237A (en) * | 2014-02-13 | 2014-06-11 | 上海珍馨化工科技有限公司 | Whitening body lotion |
| CN104434618B (en) * | 2014-08-28 | 2017-06-09 | 济南臻雅化妆品有限公司 | Have whitening, nti-freckle concurrently and print nine grass green frosts of effect and preparation method thereof |
| WO2017035775A1 (en) * | 2015-09-01 | 2017-03-09 | 拉芳家化股份有限公司 | Product containing rhodiola rosea extract and ginkgo biloba extract, preparation method therefor, and use thereof |
| CN105362088B (en) * | 2015-12-22 | 2019-05-17 | 深圳市维琪医药研发有限公司 | A kind of peptide composition for the light spot of whitening skin lightening |
| CN105686975A (en) * | 2016-03-13 | 2016-06-22 | 佛山市芊茹化妆品有限公司 | Cleansing ointment and preparation method thereof |
| CN105943445B (en) * | 2016-06-17 | 2019-07-09 | 云南天美天康生物科技有限公司 | A kind of foodcare liquid and preparation method thereof |
| CN106074227A (en) * | 2016-08-19 | 2016-11-09 | 陈家泓 | A kind of antibacterial facial milk cleanser |
| CN111388367B (en) * | 2020-03-25 | 2021-09-24 | 江南大学 | Composition for inhibiting melanin at multiple target points, preparation method and application of composition in cosmetics |
| CN111514054A (en) * | 2020-06-08 | 2020-08-11 | 云南菊开生物科技有限公司 | Composition for inhibiting tyrosinase activity, preparation method thereof and cosmetic |
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| 植物美白提取物的筛选及作用机理探索;王鹏;《中国优秀硕士学位论文全文数据库》;20101215;前言部分第1-4页 * |
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Effective date of registration: 20170309 Address after: 510000 Guangdong province Guangzhou Science City Economic and Technological Development Zone No. 31 Southern China Ke Feng Lu new materials innovation park building G1 No. 422 Patentee after: Guangzhou huan'ao axiata Biotechnology Co. Ltd. Address before: 510000 Conghua, Taiping Economic Development Zone, Guangzhou, Fuk Road, No. 18, No. Patentee before: Guangzhou Tianwen Jiaoyan Cosmetics Co., Ltd. |
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