Application of arbutin sugar ester derivative in preparation of cosmetics or drugs

A technology of arbutin sugar and derivatives, applied in the field of medicine, can solve the problems of undiscovered melanin activity of arbutin sugar ester derivatives, and achieve strong inhibitory effect, low acute toxicity, and strong inhibitory effect

Inactive Publication Date: 2013-08-21
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventors originally isolated it from the leaves of the Betula genus or Hackwood plant of the genus Silver Betula, and did not find that the arbutin sugar ester derivatives had melanin-inhibiting activity or were used as raw materials to prepare cosmetics or There are no reports on the preparation of pharmaceutical preparations, and there are no reports on the application in the preparation of whitening and freckle-removing cosmetics or medicines for skin whitening and treatment of pigmentation diseases

Method used

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  • Application of arbutin sugar ester derivative in preparation of cosmetics or drugs
  • Application of arbutin sugar ester derivative in preparation of cosmetics or drugs
  • Application of arbutin sugar ester derivative in preparation of cosmetics or drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The effect of 6'-O-caffeoyl-arbutin (6'-O-caffeoyl-arbutin) (abbreviation: KIBVA) on the inhibition of zebrafish melanin:

[0039] 1. The preparation of 6'-O-caffeoylarbutin (6'-O-caffeoyl-arbutin) (abbreviation: KIBVA): adopt the method of the Chinese patent "Patent No.: ZL200710065956.X" authorized by the applicant, The 6'-O-caffeoyl arbutin obtained by the method has high yield and high purity, simple and easy preparation process, short production cycle, and easy batch preparation and industrial production process. The prepared KIBVA structural formula is as follows:

[0040]

[0041] 2. Zebrafish selection:

[0042] The 6hpf AB line zebrafish were observed under a dissecting microscope, and the normal and consistent zebrafish were picked and transferred into 6-well microwell plates, with 30 fish per well. (Note: hpf=hour post fertilization in the present invention, Chinese refers to the number of hours after fertilization of zebrafish, such as 6hpf refers to 6 ...

Embodiment 2

[0060] Zebrafish Melanin Inhibition Recovery Assay:

[0061] 1. Zebrafish selection:

[0062] The 6hpf AB line zebrafish were observed under a dissecting microscope, and the normal and consistent zebrafish were picked and transferred into 6-well microwell plates, with 30 fish per well.

[0063] 2. Compound treatment:

[0064] Three experimental groups were set up in the experiment, namely A, B, and C groups, wherein A group was a blank control (control) treatment group containing 3 mL of aquaculture water; B group was a solvent (0.1% DMSO, i.e. 0.1% dimethyl methylene Sulfone) control treatment group, that is, 3 mL of aquaculture water containing 3 μL DMSO; group C is a 200 μM KIBVA treatment group, that is, a 200 μM KIBVA solution prepared with 3 mL of aquaculture water.

[0065] For each treatment group, 30 6hpf zebrafish with the same development were selected, and they were cultured in a 28°C incubator to 52hpf and then photographed; KIBVA was removed for 24 hours after ...

Embodiment 3

[0070] Acute toxicity test of KIBVA:

[0071] 1. Zebrafish selection:

[0072] The 6hpf AB line zebrafish were observed under a dissecting microscope, and the normal and consistent zebrafish were picked and transferred into 6-well microwell plates, with 30 fish per well.

[0073] 2. Compound treatment:

[0074] This experiment adopts hydrostatic test, and according to the pre-experimental results, 6 different concentrations of KIBVA and arbutin (both are respectively: 0μM, 10μM, 100μM, 1mM, 2mM, 3mM) were set respectively, and 30 tails were put into each concentration. The 6hpf zebrafish with the same development were placed in a 28°C incubator and cultured in the dark, and the mortality of the zebrafish was used as an evaluation index.

[0075] 3. Test results:

[0076] Through the test result recording and statistical analysis, it was found that:

[0077] (1) When zebrafish were treated with drugs to 52hpf, it was observed that the maximum non-lethal concentration of zeb...

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Abstract

The invention relates to an arbutin sugar ester derivative represented by a general formula I, a drug composition adopting the arbutin sugar ester derivative as an active component, and an application of the arbutin sugar ester derivative in preparation of skin whitening and spot removing cosmetics or drugs for skin whitening and pigmentation disease treatment. According to the present invention, with the arbutin sugar ester derivative, melanin can be effectively inhibited and decomposed so as to completely remove melanin spots and provide effects of whitening and spot removing; acute zebrafish toxicity test results show that the arbutin sugar ester derivative has characteristics of low toxicity, high activity, efficiency and safety compared with arbutin; and in the general formula I, R represents straight chain or branched chain saturated or unsaturated alkyl acyl, or trans or cis unsaturated aromatic acyl, R1 represents hydrogen atom, or straight chain or branched chain saturated or unsaturated alkyl acyl, or trans or cis unsaturated aromatic acyl, and R2 represents hydrogen atom, and/or hydroxy or methoxy or substituted acyl.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the application of natural arbutin sugar ester derivatives in the preparation of cosmetics or medicines, more specifically, to the application of arbutin sugar ester derivatives in the preparation of skin whitening and freckle-removing cosmetics or skin whitening and treatment Drug application in pigmentation diseases. Background technique: [0002] The depth of human skin color is regulated by many factors, but it mainly depends on the content and distribution of melanin. Therefore, people's whitening concept has turned to physiological whitening by melanin reduction. A large number of whitening skin care products have emerged on the market at present, and their safety and efficacy evaluations have naturally become the focus of attention of consumers and manufacturers. The natural active substances extracted from natural raw materials such as animals, plants, and Ch...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/203C07H1/00A61K8/60A61K31/7034A61K31/7048A61K36/258A61Q19/02A61P17/00
Inventor 张颖君李春启许敏劳乔聪赵平朱晓宇王东朱宏涛杨崇仁
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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