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Application of PCSK9 inhibitor in preparation of products for promoting skin pigmentation

A technology of inhibitors and products, applied in the field of medicine, can solve the problems of patents and products for depigmentation diseases, and research reports on the effect of PCSK9, etc., and achieve the goals of small adverse reactions, significant curative effect, and good treatment methods Effect

Active Publication Date: 2022-01-04
陈敏
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there have been no research reports on the effect of PCSK9 on melanocytes, nor have there been any relevant literature, patents and products on the application of PCSK9 inhibitors in the treatment of depigmentation diseases

Method used

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  • Application of PCSK9 inhibitor in preparation of products for promoting skin pigmentation
  • Application of PCSK9 inhibitor in preparation of products for promoting skin pigmentation
  • Application of PCSK9 inhibitor in preparation of products for promoting skin pigmentation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Effect of embodiment 1PCSK9 gene knockout on mouse pigment growth

[0026] 1. Experimental method

[0027] 1.1 Experimental animals:

[0028] SPF grade C57BL / 6 (B6) mice, C57BL / 6-PCSK9- / - mice (use CRISPR gene editing technology, knock out Pcsk9 gene exon 2-3, establish Pcsk9 gene knockout mouse model), body weight ( 20±4.6)g, derived from SMOC.

[0029] 1.2 Animal grouping and modeling

[0030] Mice of different genotypes were divided into three groups: C57BL / 6 mouse blank control group, C57BL / 6 mouse model group and C57BL / 6-PCSK9- / - mouse model group, with 6 mice in each group, 3 males and 3 males. Remove the black hair in the area of ​​2cm×2cm on the back. Except for the blank control group, all other groups were smeared with 5% hydroquinone for depigmentation in the depilatory area, 0.5mL each time, twice a day, and the animals in the blank control group were smeared with the same amount of normal saline every day. After 30 days of continuous application, obviou...

Embodiment 2

[0052] Example 2 Effects of PCSK9 inhibitors on pigment growth in mice

[0053] 1. Experimental method

[0054] 1.1 Materials

[0055] (1) PCSK9 interfering RNA-1 sequence and modification

[0056] Gene 5'-3'Snese 5'-3'Antisense siPCSK9-1 GccuGGAGuuuAuucGGAAdT*dT UUCCgAAuAAACUCcAGGCdT*dT siPCSK9-2 AGGuGuAucuccuAGAcAcdT*dT GUGUCuAGGAGAuAcACCUdT*dT

[0057] Mix equal amounts of siPcsk9-1 and 2 and dilute to 20 μM with normal saline, take the diluted siRNA and mix evenly with lotion.

[0058] PCSK9 interference RNAi inhibitor-2: the RNA has the same sequence as Inclisran from Alnylam Company; PCSK9 interference RNAi inhibitor-3: the RNA has the same sequence as ALN-PCS from Affiris Company.

[0059] (2) PCSK9 small molecule compound inhibitor 1: R-IMPP from Selleck, chemical formula: C 24 h 27 N 3 o 2 , molecular weight: 389.49, structural formula: PCSK9 small molecule compound inhibitor 2: PF-06446846 from Selleck, chemical formula: C ...

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Abstract

The invention belongs to the technical field of medical biology, and particularly relates to an effect of proprotein convertase subtilisin / kexin type 9 (PCSK9) in promoting pigmentation and application of a PCSK9 inhibitor in preparing products for treating depigmentation diseases. The PCSK9 inhibitor is characterized in that the PCSK9 inhibitor is a PCSK9 small molecule compound or a PCSK9 interfering RNA or a PCSK9 monoclonal antibody or a PCSK9 mimic peptide or a PCSK9 mimic antibody protein or a PCSK9 antisense oligonucleotide or a PCSK9 vaccine, and the PCSK9 inhibitor is applied to preparation of the products for treating leucoderma and other skin depigmentation diseases. Systematic or external PCSK9 inhibitor products can be further developed and are used for treating skin depigmentation diseases. The products are remarkable in curative effect and small in adverse reaction.

Description

1. Technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the role of proprotein convertase Bacillus subtilis invertase (PCSK9) in promoting pigment production, and the application of PCSK9 inhibitors in the preparation of products for treating depigmentation diseases. 2. Background technology [0002] Vitiligo is a common acquired localized or generalized skin depigmentation disease, the prevalence of vitiligo worldwide is 1% to 2%. Depigmentation of the skin or mucous membranes caused by damage to melanocytes, characterized by discolored white spots, can occur in various parts of the body, such as backs of fingers, wrists, forearms, face, neck, and genitals. Most of the white spots are symmetrically distributed, and the initial stage is mostly from fingernails to coins, which are approximately round, oval or irregular. There are also punctate depigmentation spots at the onset of the disease, with more obvious borders,...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/7088A61K39/395A61P17/00
CPCA61K45/00A61K31/7088A61P17/00C07K16/40A61K2039/505Y02A50/30
Inventor 陈敏其他发明人请求不公开姓名
Owner 陈敏
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