CN116236408A - Whitening composition derived from three traditional Chinese medicine active ingredients and application thereof - Google Patents
Whitening composition derived from three traditional Chinese medicine active ingredients and application thereof Download PDFInfo
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- A61K31/09—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
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Abstract
The invention discloses a whitening composition derived from three traditional Chinese medicine active ingredients, which consists of 24-82 parts of raspberry ketone glucoside, 16-41 parts of pterostilbene and 11-36 parts of senkyunolide A, wherein the whitening composition derived from the three traditional Chinese medicine active ingredients has good whitening effect by inhibiting tyrosinase activity, reducing tyrosinase expression level, scavenging free radicals, scavenging NO, inhibiting multi-dimensionality such as melanosome transportation and inhibiting melanin formation in multiple paths by utilizing the three effective ingredients derived from the natural traditional Chinese medicines, and has high market popularization value. The invention also discloses application of the whitening composition derived from the three traditional Chinese medicine active ingredients in preparation of medicines or cosmetics for treating and/or preventing the pigment increase diseases.
Description
Technical Field
The invention relates to a whitening composition derived from three traditional Chinese medicine active ingredients and application thereof.
Background
Under normal physiological conditions, melanin can protect human skin from ultraviolet rays, toxic chemicals, other environmental factors, and the like. However, excessive production and abnormal accumulation of melanin can cause pigment-increasing diseases such as freckle, chloasma, senile plaque, cyasma, coffee spot, sunburn, nevus, melanoma and other pigment-increasing skin diseases, seriously affect the appearance of patients, and cause great mental stress to the patients. Skin pigmentation is closely related to melanin production, tyrosinase is the rate-limiting enzyme for melanin production, and inhibition of tyrosinase production or tyrosinase activity is effective in inhibiting melanin production. It has been found that oxidative stress generated by free radicals during melanogenesis also promotes melanocyte production of melanin by activating a series of cell pathways; in addition, NO can increase melanin synthesis by melanocytes. Therefore, the antioxidant and the NO scavenger can synergistically enhance the whitening effect. Skin pigmentation is not only dependent on melanogenesis, but also is related to the distribution of melanin transport to keratinocytes, melanosomes are organelles of melanogenesis, storage and transport, and inhibition of melanosome transport is effective in exerting a whitening effect.
Disclosure of Invention
The invention aims to overcome the defects of the prior art, provides a whitening composition derived from three traditional Chinese medicine active ingredients and application thereof, utilizes the three active ingredients derived from natural traditional Chinese medicines, has good whitening effect by inhibiting tyrosinase activity, reducing tyrosinase expression level, scavenging free radicals, scavenging NO, inhibiting melanin formation by multiple dimensions and multiple paths such as melanosome transportation and the like, determines the optimal compatibility ratio of the three active ingredients for whitening effect, can be used in the fields of medicines and cosmetics, and has high market popularization value.
The technical scheme for achieving the purpose is as follows: a whitening composition derived from three traditional Chinese medicine active ingredients comprises, by weight, 24-82 parts of raspberry ketone glucoside, 16-41 parts of pterostilbene and 11-36 parts of senkyunolide A.
The whitening composition derived from the three traditional Chinese medicine active ingredients comprises the raspberry ketone glucoside, pterostilbene and senkyunolide A in a mass ratio of 0.54:0.25:0.21.
The whitening composition derived from the three traditional Chinese medicine active ingredients is prepared by chemical synthesis or natural animal and plant extraction and purification of raspberry ketone glucoside, pterostilbene and senkyunolide A.
The invention also provides application of the whitening composition derived from the three traditional Chinese medicine active ingredients in preparing medicines or cosmetics for treating and/or preventing the pigment increase diseases.
The application of the whitening composition derived from the three traditional Chinese medicine active ingredients, wherein the pigmentary diseases comprise freckles, chloasma, senile plaques, cyasma, coffee spots, sunburn, nevus and melanoma-associated skin diseases.
In the technical scheme of the whitening composition derived from three traditional Chinese medicine active ingredients and the application thereof, raspberry ketone glucoside (Raspberry ketone glucoside, RKG) is one of the effective ingredients of the traditional Chinese medicine raspberries, and has certain whitening, NO removal, antibacterial and other effects. Pterostilbene (Pterostilbene) is one of the effective components of the traditional Chinese medicine pterocarpus santalinus, also exists in plants such as blueberries, grapes and Pterocarpus marsupium, has the effects of resisting cancer, inflammation, oxidization and the like, has a certain whitening effect, and can effectively inhibit melanophore transport. The senkyunolide A (Senkyunolide A) is one of the effective components of the traditional Chinese medicine ligusticum wallichii, and has certain effects of whitening, antioxidation, pain relieving, antibiosis and the like.
According to the technical scheme of the whitening composition derived from three traditional Chinese medicine active ingredients and the application thereof, the three traditional Chinese medicine active ingredients are utilized, and the whitening composition derived from the three traditional Chinese medicine active ingredients can be used in the fields of medicines and cosmetics, and has high market popularization value by inhibiting tyrosinase activity, reducing tyrosinase expression level, scavenging free radicals, scavenging NO, inhibiting melanosome transportation and other multidimensional and multipath melanin formation, and has good whitening effect.
Drawings
FIG. 1 is a three-dimensional block diagram of a D-best design model construction;
fig. 2 is a graph showing the effect of whitening compositions derived from three traditional Chinese medicine active ingredients with different compatibility ratios on B16F10 cell melanogenesis;
FIG. 3 is a graph showing the effect of the whitening composition derived from three traditional Chinese medicine active ingredients with different compatibility ratios on B16F10 cell tyrosinase activity;
fig. 4 is a graph showing the effect of the whitening composition derived from three traditional Chinese medicine active ingredients with different compatibility ratios on the melanogenesis of zebra fish.
Detailed Description
In order to enable those skilled in the art to better understand the technical scheme of the present invention, the following detailed description is provided with reference to the accompanying drawings:
the whitening composition comprises, by weight, 24-82 parts of raspberry ketone glucoside, 16-41 parts of pterostilbene and 11-36 parts of senkyunolide A. The raspberry ketone glucoside, pterostilbene and senkyunolide A are prepared by chemical synthesis or natural animal and plant extraction and purification respectively. The raspberry ketone glucoside, pterostilbene and senkyunolide A can also be commercially available products.
The mass ratios of the raspberry ketone glucoside, pterostilbene and senkyunolide A in the whitening composition derived from the three traditional Chinese medicine active ingredients are shown in the following table:
table 1, different mass ratios between raspberry ketone glucoside, pterostilbene and senkyunolide a:
| name of the name | Mass |
| Compatibility proportion | |
| 1 | 0.4:0.3:0.3 |
| Compatibility ratio 2 | 0.98:0.01:0.01 |
| Compatibility ratio 3 | 0.3:0.4:0.3 |
| Compatibility ratio 4 | 0.4:0.4:0.2 |
| Compatibility ratio 5 | 0.01:0.01:0.98 |
| Compatibility ratio 6 | 0.6:0.2:0.2 |
| Compatibility ratio 7 | 0.2:0.2:0.6 |
| Compatibility ratio 8 | 0.3:0.2:0.5 |
| Compatibility ratio 9 | 0.2:0.1:0.7 |
| Proportion of compatibility 10 | 0.6:0.1:0.3 |
| Proportion of compatibility 11 | 0.01:0.98:0.01 |
Referring to fig. 1, on the premise of controlling the total amount of the whitening composition derived from the three traditional Chinese medicine active ingredients to be fixed, the effect activity change is associated by the change of the compatibility proportion of each component in the whitening composition derived from the three traditional Chinese medicine active ingredients by using a D-optimal design mathematical calculation method, and the compatibility proportion and the pharmacodynamic relationship of each component in the whitening composition derived from the three traditional Chinese medicine active ingredients are excavated by constructing a corresponding mathematical model, so that a three-dimensional structure diagram is constructed to predict the optimal compatibility proportion range and the optimal compatibility proportion. In fig. 1, a is the mass ratio of raspberry ketone glucoside; b is pterostilbene mass ratio; c is mass ratio of senkyunolide A. The three components of the whitening composition derived from the three traditional Chinese medicine active ingredients are subjected to coordination compatibility design from the digital-analog angle, and the optimal melanogenesis inhibition effect is achieved when the compatibility proportion of raspberry ketone glucoside, pterostilbene and senkyunolide A=0.54:0.25:0.21 is predicted.
And then carrying out biological evaluation on the whitening composition derived from the three traditional Chinese medicine active ingredients with different compatibility ratios from the cell and zebra fish level, and verifying the whitening effect of the whitening composition derived from the three traditional Chinese medicine active ingredients with the optimal compatibility ratio.
1. Effect of whitening composition derived from three Chinese medicinal active ingredients with different compatibility ratios on melanogenesis in B16F10 melanocytes
Referring to FIG. 2, B16F10 cells in good exponential growth phase were taken, digested, counted, and inoculated in 10cm cell culture dishes at a concentration of about 1X 10 5 The inoculation amount is 10 mL/dish, and the inoculation amount is placed at 37 ℃ and 5% CO 2 Culturing in an incubator for 24 hours; adding whitening composition derived from three traditional Chinese medicine active ingredients with different compatibility ratios, and culturing for 72h; collecting the cells after the administration treatment, adding 100 mu L of non-denaturing lysis solution (containing 1mM PMSF), and lysing at 4 ℃ for 20min; centrifuging at 12000r/min for 10min at 4deg.C to obtain melanin precipitate at the bottom of the centrifuge tube. 330. Mu.L NaOH (10% DMSO) was added, vortexed to facilitate sufficient lysis, and placed in a metal bath at 80℃for 2h to allow sufficient dissolution of the melanin precipitate. Vortex mixing, adding 100 μl of melanin solution into each well of 96-well plate, setting 3 multiple wells, and measuring OD value at 405 nm.
The effect of the whitening composition derived from the three traditional Chinese medicine active ingredients with different compatibility ratios on the melanogenesis in the B16F10 melanocyte is shown in fig. 2, and compared with the blank control group, the whitening composition derived from the three traditional Chinese medicine active ingredients with different compatibility ratios has different degrees of inhibition effects on the melanogenesis in the B16F10 melanocyte, wherein the optimal compatibility ratio group has the best inhibition effect (0.01, 0.001).
The experimental results show that: compared with a blank control group, the whitening composition derived from three traditional Chinese medicine active ingredients with different compatibility ratios can obviously inhibit the synthesis of B16F10 cell melanin, and the optimal compatibility ratio group, namely, the raspberry ketone glucoside, namely, pterostilbene, senkyunolide A=0.54:0.25:0.21 has obviously better effect on inhibiting the melanin in B16F10 cell than other compatibility ratio groups.
2. Effect of whitening composition derived from three Chinese medicinal active ingredients with different compatibility ratios on B16F10 melanocyte tyrosinase activity
Referring to FIG. 3, B16F10 cells in good exponential growth phase were taken, digested, counted, and inoculated in 10cm cell culture dishes at a concentration of about 1X 10 5 The inoculation amount is 10 mL/dish, and the inoculation amount is placed at 37 ℃ and 5% CO 2 Culturing in an incubator for 24 hours; adding whitening composition derived from three traditional Chinese medicine active ingredients with different compatibility ratios, and culturing for 72h; collecting the cells after the administration treatment, adding 100 mu L of non-denaturing lysis solution (containing 1mM PMSF), and lysing at 4 ℃ for 20min; centrifuging at 4deg.C and 12000r/min for 10min, and collecting supernatant as total cell protein extractive solution. After extraction of cellular proteins, 10. Mu.g of the total protein amount of the cell lysis supernatant was added to a centrifuge tube, and the supernatant was supplemented to 100. Mu.L with PBS (pH 6.8), and after sufficient mixing, 96-well plates were added, and then 0.1% L-DOPA was added to 100. Mu.L, 3 wells were set for each group, and incubated at 37℃for 1 hour in the absence of light. Absorbance values were determined at 475 nm. The higher absorbance value indicates higher tyrosinase activity.
The effect of the whitening composition derived from the three traditional Chinese medicine active ingredients with different compatibility ratios on the tyrosinase activity of the B16F10 melanocyte is shown in fig. 3, and compared with the blank control group, the whitening composition derived from the three traditional Chinese medicine active ingredients with different compatibility ratios has different degrees of inhibition effects on the tyrosinase activity of the B16F10 melanocyte, wherein the best compatibility ratio group has the best inhibition effect (less than 0.05, less than 0.01, less than 0.001).
Experimental results: compared with a blank control group, the whitening composition derived from the three traditional Chinese medicine active ingredients with different compatibility ratios can obviously inhibit the activity of B16F10 cell tyrosinase, and the optimal compatibility ratio group, namely, the raspberry ketone glucoside, namely, pterostilbene, and senkyunolide A=0.54:0.25:0.21 have obviously better inhibition effect on the activity of B16F10 cell tyrosinase than other compatibility ratio groups.
3. Effect of whitening composition derived from three Chinese medicinal active ingredients with different compatibility ratios on synthesis of zebra fish melanin
Referring to fig. 4, the experimental procedure used AB-line wild-type zebra fish. The zebra fish breeding method is carried out according to The zebrafish book. The water temperature for feeding is kept at about 28.5 ℃, the light is applied for 14 hours and the dark is applied for 10 hours each day, and the feed is fed once in the morning and evening. The day before embryo collection, 1 female fish and 2 male fish were placed in spawning jars and separated by a baffle and placed in a darkened environment. And (5) in the morning of the next day, the partition board is opened after the lamplight is started, and embryos are collected after spawning is completed. Embryos are placed in an eggwater and incubated in a light incubator at 28.5 ℃.
Collecting embryo at about 7-8hpf, thoroughly changing liquid to clean embryo, removing embryo in bad state, transferring to 6-well plate, placing 20 embryo in each hole, and adding whitening composition derived from three traditional Chinese medicine active ingredients with different compatibility ratio; when the strain is cultured to 54hpf in a light incubator at 28.5 ℃, the embryo state and melanin change of the zebra fish are observed, and a picture is taken by a split microscope. The effect of the whitening composition derived from the three traditional Chinese medicine active ingredients with different compatibility ratios on the synthesis of the zebra fish melanin is shown in figure 4.
The experimental results show that: compared with a blank control group, the whitening composition derived from the three traditional Chinese medicine active ingredients with different compatibility ratios can obviously inhibit the synthesis of the zebra fish melanin. And the optimal compatibility proportion group, namely, the inhibition effect on the generation of the black pigment of the zebra fish is obviously better than that of other compatibility proportion groups when the raspberry ketone glucoside is pterostilbene and senkyunolide A=0.54:0.25:0.21.
The biological evaluation of the whitening composition derived from the three traditional Chinese medicine active ingredients with different compatibility ratios from the cell and zebra fish level can confirm that the inhibition effect of the whitening composition derived from the three traditional Chinese medicine active ingredients on melanin and tyrosinase activity in B16F10 cells, which is formed by the three components, is obviously superior to other compatibility ratio groups, and the inhibition effect of the whitening composition derived from the three traditional Chinese medicine active ingredients on melanin of zebra fish is obviously superior to other compatibility ratio groups when pterostilbene and senkyunolide A=0.54:0.25:0.21. According to the technical scheme of the whitening composition derived from three traditional Chinese medicine active ingredients and the application thereof, the three traditional Chinese medicine active ingredients are utilized, and the whitening composition derived from the three traditional Chinese medicine active ingredients can be used in the fields of medicines and cosmetics, has good whitening effect by inhibiting tyrosinase activity, reducing tyrosinase expression level, scavenging free radicals, scavenging NO, inhibiting multi-dimensional and multi-path melanin formation such as melanosome transportation and the like, and has high market popularization value.
In conclusion, the whitening composition derived from three traditional Chinese medicine active ingredients and the application thereof provided by the invention have good whitening effect by utilizing the three active ingredients derived from natural traditional Chinese medicines, inhibiting tyrosinase activity, reducing tyrosinase expression level, scavenging free radicals, scavenging NO, inhibiting multi-dimensional and multi-path melanin formation such as melanosome transportation and the like, and the whitening composition derived from three traditional Chinese medicine active ingredients can be used in the fields of medicines and cosmetics and has high market popularization value.
It will be appreciated by persons skilled in the art that the above embodiments are provided for illustration only and not for limitation of the invention, and that variations and modifications of the above described embodiments are intended to fall within the scope of the claims of the invention as long as they fall within the true spirit of the invention.
Claims (5)
1. The whitening composition is characterized by comprising, by weight, 24-82 parts of raspberry ketone glucoside, 16-41 parts of pterostilbene and 11-36 parts of senkyunolide A.
2. The whitening composition derived from three traditional Chinese medicine active ingredients according to claim 1, wherein the mass ratio of raspberry ketone glucoside, pterostilbene and senkyunolide A is preferably 0.54:0.25:0.21.
3. The whitening composition derived from three traditional Chinese medicine active ingredients according to claim 1, wherein the raspberry ketone glucoside, pterostilbene and senkyunolide A are prepared by chemical synthesis or natural animal and plant extraction and purification.
4. Use of a whitening composition derived from three traditional Chinese medicine active ingredients according to any one of claims 1 to 3 in a medicament or cosmetic for the treatment and/or prevention of hyperchromic diseases.
5. The use of a whitening composition derived from three chinese medicinal active ingredients according to claim 4, wherein the pigmentary disorders include freckle, chloasma, senile plaque, cyasma, coffee, sunburn, nevus and melanoma-associated skin diseases.
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Citations (4)
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|---|---|---|---|---|
| US20040081631A1 (en) * | 2002-10-29 | 2004-04-29 | Kang-Tae Lee | Cosmetic composition for skin whitening comprising senkyunolide a as active ingredient |
| KR100681700B1 (en) * | 2005-12-28 | 2007-02-15 | 주식회사 코리아나화장품 | Cosmetic composition for skin whitening comprising senkyunolide a and gluconic acid as active ingredients |
| CN112451400A (en) * | 2020-11-28 | 2021-03-09 | 广州梦姿科技有限公司 | Water-in-oil type multi-effect whitening face cream |
| CN112545963A (en) * | 2020-12-30 | 2021-03-26 | 上海澄穆化妆品有限公司 | Composition with whitening effect, whitening compound preparation and preparation method of whitening compound preparation |
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|---|---|---|---|---|
| US20040081631A1 (en) * | 2002-10-29 | 2004-04-29 | Kang-Tae Lee | Cosmetic composition for skin whitening comprising senkyunolide a as active ingredient |
| KR100681700B1 (en) * | 2005-12-28 | 2007-02-15 | 주식회사 코리아나화장품 | Cosmetic composition for skin whitening comprising senkyunolide a and gluconic acid as active ingredients |
| CN112451400A (en) * | 2020-11-28 | 2021-03-09 | 广州梦姿科技有限公司 | Water-in-oil type multi-effect whitening face cream |
| CN112545963A (en) * | 2020-12-30 | 2021-03-26 | 上海澄穆化妆品有限公司 | Composition with whitening effect, whitening compound preparation and preparation method of whitening compound preparation |
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