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Application of salidroside derivative in external preparation for skin whitening

一种皮肤美白、外用剂的技术，应用在护肤品领域，能够解决破坏黑色素细胞、黑色素细胞不足等问题，达到增强美白活性的效果

Active Publication Date: 2021-04-30
SHANGHAI CHENGMU IND DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, excessive inhibition of melanin synthesis will seriously damage the existing melanocytes, resulting in insufficient melanocytes, which will make the skin color abnormally white and cause vitiligo. Of course, scientifically inhibiting melanin will not endanger the health of the body.

Method used

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  • Application of salidroside derivative in external preparation for skin whitening
  • Application of salidroside derivative in external preparation for skin whitening
  • Application of salidroside derivative in external preparation for skin whitening

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 : Preparation of 1-(3,5-dihydroxyphenyl)ethyl-β-D-glucoside

[0046]

[0047] step one:

[0048]

[0049] 1.18g of 3,5-dihydroxyphenylacetic acid and 8.4ml of BH3.THF (1.0M in THF) were dissolved in 20ml of THF and reacted at room temperature for 4 hours. After the reaction was completed, the solvent was removed by rotary evaporation to obtain a crude product. Purified by column chromatography to obtain 1.05 g of product with a yield of 97%.

[0050] Step two:

[0051]

[0052] Add 16.9g of intermediate 2, 6.9mL of benzyl chloride and 200mL of acetone in sequence in the reaction flask, stir to dissolve, add 8.3g of potassium carbonate and 0.8g of potassium iodide, and monitor the reflux reaction by TLC for 18h. The solvent was evaporated, the residue was poured into 200 mL of water, hydrochloric acid was added dropwise to adjust the pH to 7, and extracted with ethyl acetate. The organic phase was evaporated under reduced pressure and then recrystal...

Embodiment 2

[0063] Example 2 : Effects of β-D-glucoside derivatives on melanin biosynthesis in melanocytes in vitro

[0064] a. Detection of activity of β-D-glucoside derivatives on inhibition of melanin production

[0065] Detection method:

[0066] In this part of the experiment, two kinds of tool cells, human melanocytes and instrumental melanocytes, were used for experiments. Human and instrumental melanocytes were seeded in 96-well plates with a plating density of 5000 cells / well. After the cells adhered to the wall, the culture medium was induced by adding nerve factors and induced by UV to simulate the production of melanin in vivo. Subsequently, the β-D-glucoside derivatives to be determined were added to the cells at a co-concentration of 100 μM to incubate the cells, and each group was set up with 3 replicates, and the cells were incubated at 37°C, 5% CO 2 The constant temperature and humidity incubator continued to cultivate for 60h. The cells were washed with pre-cooled p...

Embodiment 3

[0084] Example 3 : SP-037 Safety Evaluation

[0085] a. Mouse skin long-term toxicity test

[0086] experiment method:

[0087] In this part of the experiment, Kunming rats were used to carry out experiments. SP-037 was prepared with physiological saline, and the concentrations were 2.5% (mass volume ratio), 5% (mass volume ratio), and 10% (mass volume ratio). A control group, a 2.5% dose group, a 5% dose group and a 10% dose group were respectively set up. There was one mouse in the blank group, and two mice in each experimental group. Treatment with back skin smearing: first, use depilatory cream to remove the back hair of the mouse, apply the drug of corresponding concentration on the exposed part of the depilated skin every day, and administer the drug continuously for 3 months. During the experiment, take pictures regularly and record the weight of the mice, and observe Whether it can cause white spots, other skin irritation damage or poisoning.

[0088] Results and...

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Abstract

The invention provides an application of a salidroside derivative in an external preparation for skin whitening, and belongs to the technical field of skin care products. The whitening activity of salidroside can be enhanced, the protection effect of salidroside sugar rings is fully utilized, salidroside-plus (SP-037), namely 1-(3, 5-dihydroxyphenyl) ethyl-beta-Dglucoside and / or salt thereof, is obtained by modifying phenol residues of salidroside, and the whitening effect of the product is detected through series experiments.

Description

[0001] This application is a divisional application of the following application, the application number is 201911367032.4; the invention name is a salidroside derivative, its preparation method and its application in whitening cosmetics; the application date is 2019-12-26. technical field [0002] The invention belongs to the technical field of skin care products, and in particular relates to the application of salidroside derivatives in skin whitening external preparations. Background technique [0003] The content and distribution of melanin in the skin determine the color of human skin. The production of melanin is inseparable from tyrosine, tyrosinase, active oxygen and melanosomes: external stimuli such as ultraviolet radiation lead to activation of tyrosinase, Then tyrosine is oxidized to dopa under the action of tyrosinase, and then oxidized to melanin, which is then transferred to the skin surface, showing the phenomenon of dull complexion and local spots, and finall...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/60A61Q19/02C07H15/18C07H1/00
CPCC07H15/18C07H1/00A61K8/602A61Q19/02A61P17/00A61K31/31
Inventor 朱才彬李俊翔
Owner SHANGHAI CHENGMU IND DEV CO LTD
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