Application of polypeptide and polypeptide derivative in prevention and treatment of fibrotic diseases

A technology for fibrotic diseases and peptide derivatives, applied in skin diseases, sensory diseases, bone diseases, etc., can solve the problems of low solubility, affecting the druggability of peptides, poor stability, etc., to inhibit inflammation and fibrosis, prevent and treat diseases Treatment of fibrotic diseases, the effect of reducing inflammatory cell infiltration

Active Publication Date: 2017-06-20
CHENGDU HUITAI BIOMEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the actual application process, the peptide has the problems of low solubility and poor stability, which greatly affects the druggability of the peptide. In the application of preparing drugs for the prevention and treatment of fibrosis, it is necessary to improve its physical and chemical properties.

Method used

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  • Application of polypeptide and polypeptide derivative in prevention and treatment of fibrotic diseases
  • Application of polypeptide and polypeptide derivative in prevention and treatment of fibrotic diseases
  • Application of polypeptide and polypeptide derivative in prevention and treatment of fibrotic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Example 1 Polypeptide and Rat Pulmonary Fibrosis Model

[0080] 1. Main experimental materials and animals

[0081] Bleomycin was produced by Nippon Kayaku Co., Ltd. (batch number 650472); Shutai 50 anesthetic was produced by France Vic Co., Ltd.

[0082] Peptides N2 and N3 were synthesized by Chengdu Capgemini Biomedical Technology Development Co., Ltd. The N2 sequence is: Tyr-Arg-Val-Arg-Phe-Leu-Ala-Lys-Glu-Asn-Val-Thr-Gln-Asp-Ala-Glu-Asp (the sequence is shown in SEQID NO: 2 in the sequence listing) . The N3 sequence is: PEG2-Tyr-Arg-Val-Arg-Phe-Leu-Ala-Lys-Glu-Asn-Val-Thr-Gln-Asp-Ala-Glu-Asp (PEG2 is connected to the N-terminal of the polypeptide by an amide bond , the sequence is shown in SEQ ID NO: 3 in the sequence listing)

[0083] SPF grade SD rats were purchased from Chongqing Daping Hospital, male, weighing 200-250 g.

[0084] 2. Rat model of pulmonary fibrosis

[0085] Weigh before administration, intramuscularly inject Shutai anesthesia solution, the ...

Embodiment 2

[0087] Example 2 Detecting the lung coefficient of rats

[0088] Take the rats in Example 1, weigh the body weight and kill the rats by overdose anesthesia, remove the lung tissues on both sides of the rats, carefully remove the connective tissue around the lung tissues, wash them with normal saline and dry them with filter paper, weigh them with an electronic balance The whole lung is wet and heavy. After weighing the wet weight of the whole lung with an electronic balance, calculate the lung coefficient according to the formula, lung coefficient=lung mass (mg) / body weight (g) (results see figure 1 ). The results showed that: compared with the rats in the blank control group, the PBS control group and the drug control group, the lung coefficients of the left lung, right lung and whole lung of the rats in the bleomycin group were significantly increased (*: P<0.01), suggesting that Lesions occurred in the lung tissue of the rats; compared with the rats in the bleomycin group...

Embodiment 3

[0089] Example 3 HE staining of pathological section of rat lung tissue

[0090] Get the lung tissue of the rat in Example 1 and fix it with 4% paraformaldehyde and embed it in paraffin, slice the largest cross-section of the wax block embedding the lung tissue, and observe the pathological changes of the lung tissue by hematoxylin-eosin (HE) staining. Observe the pathological changes of the lung tissue under an optical microscope (low magnification) with a magnification of 100 times (for the results, see figure 2 ). The results showed that the alveolar morphology of the rats in the PBS control group and the drug control group was normal, the alveolar walls were slender, and there was a very small amount of inflammatory cell infiltration in the interstitium; The alveolar wall in the N2 and N3 treatment groups was compared with the model group, and the alveolar structure of the lung tissue of the rats in the N2 and N3 treatment groups was significantly increased. It is relat...

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Abstract

The invention belongs to the technical field of medicines, relates to the field of prevention and treatment of fibrotic diseases and discloses application of a polypeptide fragment, a polypeptide fragment derivative and a polypeptide derivative in preparation of medicines for preventing and treating the fibrotic diseases. The invention relates to a product obtained by carrying out amino acid deletion, addition and substitution on the polypeptide and a product obtained through various chemical modification, a composition of the polypeptide fragment, the polypeptide fragment derivative and the polypeptide derivative, a pharmaceutically acceptable carrier and dose form and application of the polypeptide fragment, the polypeptide fragment derivative and the polypeptide derivative in preparation of medicines for preventing and treating the fibrotic diseases. By utilizing the polypeptide fragment, the polypeptide fragment derivative and the polypeptide derivative, the inflammation and fibrotic development of tissues and organs can be effectively inhibited, and the polypeptide fragment, the polypeptide fragment derivative and the polypeptide derivative have ideal new medicine development values.

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to the field of prevention and treatment of fibrotic diseases, and specifically relates to the application of polypeptides and derivatives thereof in the preparation of drugs for preventing and / or treating fibrotic diseases. Background technique [0002] Protein is the material basis of the body and the main bearer of life activities, involving physiological processes such as growth, development, immune regulation, and metabolism. The abnormality of protein and the signal transduction it participates in is the root cause of the occurrence and development of diseases. It is the essential idea of ​​biomedicine to use the body's own regulation to prevent and treat diseases. Therefore, protein is not only the source of drug targets, but also an important category of biomedicine , and protein functional fragments provide a guarantee for precision medicine. Peptides are active fragments of pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/10A61P29/00A61P19/02A61P11/00A61P1/16A61P13/12A61P19/08A61P9/00A61P17/02A61P9/14A61P27/06A61P27/12A61P27/02A61P9/10
CPCA61K38/10
Inventor 韦德李小梅俞雯陈晓红陈瑞肖玲金琨琪陈玲
Owner CHENGDU HUITAI BIOMEDICINE CO LTD
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