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Tyrosinase polypeptide inhibitor

A technology of tyrosinase and inhibitors, which is applied in the field of tyrosinase inhibitors containing polypeptides, and can solve problems such as immediate effect and safety concerns

Inactive Publication Date: 2012-06-13
萧乃文
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] Although the Department of Health has announced that there are currently eight ingredients approved for use in whitening cosmetics, there are still doubts about the safety of some types. We must have correct expectations for whitening and should not have immediate results. In order to have healthy and fair skin , how to do an effective and safe whitening is an important topic in the field of whitening cosmetics

Method used

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  • Tyrosinase polypeptide inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0119] Embodiment 1: in vitro (In vitro) tyrosinase activity test

[0120] I. Drugs

[0121] Mushroom tyrosinase (Mushroom tyrosinase, 100U / ml), arbutin (Arbutin), tyrosine (L-tyrosine, 0.5mM), kojic acid (Kojic acid) and 2 to 5 short polypeptides of different sequences (0.5 mM). The short polypeptide sequence is R1n1-Xaa-R2n2-Yaa-R3n3, Xaa or Yaa is one of the five amino acids of tyrosine, cysteine, glycine, glutamic acid and arginine, and the substituents R1, R2 or The amino acids of R3 are divided into the following eight types according to their functional groups: glycine, aliphatic amino acids, aromatic amino acids, acidic amino acids, basic amino acids, hydroxyl amino acids, sulfur-containing amino acids and amide amino acids, choose one of each type, n1, n2 or n3 The number of substituents is equal to 0 or 1 respectively, and the above amino acids are cross-arranged to form short polypeptides with 2 to 5 different sequences.

[0122] II. Experimental steps

[0123] ...

Embodiment 2

[0149] Example 2: Results of Safety Tests for Short Peptides of Different Sequences

[0150] I. Drug source

[0151] 1. The peptide sequence is YD, YFR, GCY and YC

[0152] II. Experimental steps

[0153] Use the MTT test to determine whether the inhibitor contains cytotoxicity. The succinate dehydrogenase (succinate dehydrogenase) in the mitochondria of living cells can reduce the yellow MTT to purple crystals (formazan), and then add DMSO to the purple crystals. (formazan) was dissolved, and the absorbance value of this solution at OD 595nm was measured with a spectrophotometer, and the effect of the test substance on cell growth was estimated.

[0154] (1) Prepare MTT-containing culture medium first, and add 80 μl of MTT (original concentration: 5 mg / ml) to every 500 μl of culture medium.

[0155] (2) Aspirate all the cell culture medium, add 100 μl of MTT-containing medium to each 96-well plate (500 μl of MTT-containing medium in a 24-well plate), and incubate at 37° C....

Embodiment 3

[0159] Example 3: Analysis of melanin content in vivo (In vivo)

[0160] In this patent, there are some cis-reverse compounds whose inhibitory effect will not be different due to cis-reverse, but there are also some cis-reverse compounds whose inhibitory effects can differ by about 50%. On the other hand, Some compounds have color after being dissolved in the solution, so in order to eliminate the color may affect the high absorbance value, and confirm that the inhibitor designed in this study can also have the same good whitening effect in the human body, so we choose Some compounds YD, YFR, GCY, YC were analyzed for melanin content.

[0161] I. Drug source

[0162] 1. The peptide sequence is YD, YFR, GCY and YC

[0163] II. Experimental steps

[0164] Melanocytes were cultured in 24-well plates, and different inhibitors were cultured at concentrations of 1, 5, 10, 25, 50 and 100 μM for seven days. Seven days later, trypsin / EDTA (0.25% / 0.1% inphosphate bufferedsaline) was...

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Abstract

The invention relates to a tyrosinase polypeptide inhibitor, which consists of a polypeptide. In the polypeptide, one or more amino acids are further subjected to acetylation, amidation, formylation, hydroxylation, lipolyzation, methylation or phosphorylation modification. The tyrosinase inhibitor provided by the invention can be taken as a medical composition, comprises the polypeptide, and further comprises a pharmaceutically-acceptable supporting agent. The medicinal composition provided by the invention can be used for inhibiting the generation of black pigments under the action of activity inhibition of tyrosinase, and can be widely applied to cosmetics such as a whitening agent.

Description

technical field [0001] The present invention relates to a tyrosinase inhibitor, in particular to a tyrosinase inhibitor containing polypeptide. Background technique [0002] 1. The source and function of melanin [0003] During embryonic development, melanocytes differentiated from the neural crest are distributed in the skin (basal layer of the epidermis), eyes-retinal pigment epithelium, uveal tract, hair follicle stroma, ear-vascular striae ( strivascularis), mucous membranes and central nervous system - pia mater (leptomeninges). In melanocytes, there is a membrane-bound organelle called melanosomes that synthesize melanin. When melanin is synthesized, it will move from the dendrites of melanocytes to the adjacent keratinocytes. ), and then present the color of the skin, and the difference in skin color is mainly due to the different production and distribution of melanin. The main function of melanin is to absorb ultraviolet light (UV) in the sun, protect the skin fr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/062C07K5/087C07K5/093C07K5/083C07K5/11C07K5/107C07K5/103A61K8/64A61Q19/02A01N37/46A01N47/44A01N43/50A01P21/00
CPCC07K5/0812C07K5/0806C07K5/0606A61K8/64C07K5/0819C07K5/0808C07K5/081A61Q19/02
Inventor 萧乃文蔡耿彰
Owner 萧乃文
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