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Active antibiotics dodeca peptide

A technology of dodecapeptide and antibiotics, which is applied in the field of a class of active dodecapeptide antibiotics, which can solve problems affecting the treatment of human infectious diseases, the expansion of bacterial numbers, and threats to human health.

Inactive Publication Date: 2003-10-08
高华 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the resistance of pathogenic bacteria to existing antibiotics has expanded rapidly, and what is more serious is the rapid expansion of the number of pathogenic bacteria resistant to multiple antibiotics. This situation has seriously affected the treatment of human infectious diseases and threatened human health.

Method used

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  • Active antibiotics dodeca peptide
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Experimental program
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Embodiment 1

[0019] 1. The amino acid sequence of the first dodecapeptide antibacterial drug designed according to the structural characteristics of the dodecapeptide described in this patent is:

[0020] A amino acid sequence expressed in Chinese:

[0021] arginine-valine-arginine-arginine-alanine-valine-arginine-arginine-valine-valine-arginine-valine

[0022] The amino acid sequence expressed by B in English abbreviation (international symbol) is:

[0023] Arg-Val-Arg-Arg-Ala-Val-Arg-Arg-Val-Val-Arg-Val This small peptide is named No. 1 dodecapeptide antibiotic.

[0024] C. Antibacterial activity test: We prepared the No. 1 dodecapeptide antibiotic according to the designed amino acid sequence with a peptide synthesizer, and conducted an in vitro antibacterial test to prove the correctness of the design idea. For this reason, we used Bactenecin, a natural dodecapeptide with strong antibacterial effect, as a positive control in the experiment. At the same time, we also design...

Embodiment 2

[0038] The amino acid sequence of the second dodecapeptide antibacterial drug designed according to the structural characteristics of the dodecapeptide described in this patent is: A The amino acid sequence expressed in Chinese:

[0039] Arginine-valine-arginine-arginine-alanine-valine-arginine-valine-valine-arginine-arginine-valine B in English The amino acid sequence expressed by the abbreviation (international symbol) is:

[0040] Arg-Val-Arg-Arg-Ala-Val-Arg-Val-Val-Arg-Arg-Val

[0041] This small peptide antibiotic is named No. 2 dodecapeptide antibiotic.

Embodiment 3

[0043] The amino acid sequence of the third dodecapeptide antibacterial drug designed according to the structural characteristics of the dodecapeptide described in this patent is: A The amino acid sequence expressed in Chinese:

[0044] Valine-arginine-valine-valine-arginine-arginine-valine-alanine-arginine-arginine-valine-arginine B in English The amino acid sequence expressed by the abbreviation (international symbol) is:

[0045] Val-Arg-Val-Val-Arg-Arg-Val-Ala-Arg-Arg-Val-Arg

[0046] This small peptide antibiotic is named as No. 3 dodecapeptide antibiotic.

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PUM

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Abstract

The present invention relates to the amino acid sequence with the structure characteristics of dodecapeptide. It features that the amino acid constituting dodecapeptide are divided into three parts; 4 amino acids at amino terminal, 4 central amino acids and 4 amino acids at carboxy termin, which can form stable alpha-helix and beta-angle to destroy the cell membrane, so playing its antibacterial role. It can also be used to synthesize relative isomer to increase its stability in human body and its possibility of using it as gastrointestinal medicine.

Description

field of invention [0001] Peptide antibiotics are ubiquitous in nature, and almost all animals, plants and microorganisms can produce one or more antimicrobial peptides. Thousands of antimicrobial peptides have been reported, for example, various antimicrobial peptides isolated from frog skin and mammalian neutrophils. [0002] Over the past decade, although there has been significant progress in the basic research of peptide antibiotics, there are many limitations in drug development. These limitations stem from traditional research and development methods: one is to directly isolate and extract antibacterial peptides from organisms, but since such natural antibacterial peptides generally have unpredictable side effects, it is difficult to directly act on animals; the other is to synthesize natural peptides Derivatives to improve its antibacterial activity or reduce side effects. However, because the law of chemical structure modification is difficult to predict, no satisfa...

Claims

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Application Information

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IPC IPC(8): A01N37/26A23L29/00A61K38/10A61P31/04A61P31/12C07K7/08
Inventor 高华张建华傅亚敏
Owner 高华
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