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6'-O-caffeoyl-arbutin and derivatives thereof, and application of compound prescription in preparing cosmetics or medicines

A technology for caffeoyl arbutin and cosmetics, which is applied in the field of medicine, can solve the problem of not finding melanin activity, etc., and achieve the effects of strong inhibitory effect, low acute toxicity effect, and strong inhibitory effect.

Inactive Publication Date: 2013-05-29
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 plant or the plant of the genus Hackwood, and did not find that 6'-O-caffeoyl arbutin had melanin-inhibiting activity or was prepared using it as a raw material before the present invention. There are no reports of cosmetics or pharmaceutical preparations, and there are no reports of the application in the preparation of whitening and freckle cosmetics or skin whitening and treatment of pigmentation diseases.

Method used

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  • 6'-O-caffeoyl-arbutin and derivatives thereof, and application of compound prescription in preparing cosmetics or medicines
  • 6'-O-caffeoyl-arbutin and derivatives thereof, and application of compound prescription in preparing cosmetics or medicines
  • 6'-O-caffeoyl-arbutin and derivatives thereof, and application of compound prescription in preparing cosmetics or medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The effect of 6'-O-caffeoyl-arbutin (6'-O-caffeoyl-arbutin) (abbreviation: KIBVA) on the inhibition of zebrafish melanin:

[0030] 1. The preparation of 6'-O-caffeoylarbutin (6'-O-caffeoyl-arbutin) (abbreviation: KIBVA): adopt the Chinese patent "patent number: ZL200710065956.X" authorized by the applicant, the method The obtained 6'-O-caffeoyl arbutin 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:

[0031] .

[0032] 2. Zebrafish selection:

[0033] The 6 hpf 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 hours after fertilization of zebrafish, such as 6 hpf refers to 6 hours after fertil...

Embodiment 2

[0051] Zebrafish Melanin Inhibition Recovery Assay:

[0052] 1. Zebrafish selection:

[0053] The 6 hpf 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.

[0054] 2. Compound treatment:

[0055] 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, that is, 0.1% dimethyl sulfoxide) 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.

[0056] For each treatment group, 30 6 hpf zebrafish with the same development were selected, and they were cultured in a 28°C incubator to 52 hpf and then photographed; KIBVA was removed 24 h after the photo...

Embodiment 3

[0061] Acute toxicity test of KIBVA:

[0062] 1. Zebrafish selection:

[0063] The 6 hpf 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.

[0064] 2. Compound treatment:

[0065] This experiment adopts hydrostatic test, and according to the pre-experimental results, 6 different concentrations of KIBVA and arbutin (both are respectively: 0 μM, 10 μM, 100 μM, 1 mM, 2 mM, 3 mM) were set, each 30 6 hpf zebrafish with the same concentration were put into 30 tails of 6 hpf zebrafish, which were cultured in a 28°C incubator in the dark, and the mortality rate of zebrafish was used as an evaluation index.

[0066] 3. Test results:

[0067] Through the test result recording and statistical analysis, it was found that:

[0068] (1) When zebrafish were treated with drugs up to 52 hpf, it was observed that the maximum non-lethal concentration of zebraf...

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Abstract

The invention relates to new application of 6'-O-caffeoyl-arbutin in the technical field of medicines for inhibiting melanin, particularly application of 6'-O-caffeoyl-arbutin or derivatives thereof, or a natural, synthetic or semisynthetic mixture containing the 6'-O-caffeoyl-arbutin, or a composition containing the 6'-O-caffeoyl-arbutin in preparing cosmetics for whitening skin and removing freckles or medicines for whitening skin and treating chromatodermatosis. The 6'-O-caffeoyl-arbutin can effectively inhibit and decompose melanin, thoroughly remove the melanin freckles, and have the effect of whitening skin and removing freckles; and the zebra fish acute toxicity test indicates that compared with arbutin, the 6'-O-caffeoyl-arbutin has the characteristics of lower toxicity, higher activity, higher efficiency and higher safety.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to the application of natural compound 6'-O-caffeoyl arbutin (6'-O-caffeoyl-arbutin) in the preparation of cosmetics or medicines, more specifically to 6'-O- Application of caffeoyl arbutin and its derivatives in the preparation of skin whitening and freckle removing cosmetics or skin whitening and treatment of 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 C...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/60A61K31/7034A61P17/00A61Q19/02
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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