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Fusarielin M and application of derivative and pharmaceutically acceptable salt thereof

A derivative and pharmaceutical technology, applied in the pharmaceutical field, can solve the problem of weakening the ability of Mtb to infect guinea pigs

Active Publication Date: 2021-04-09
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

MptpB is also a non-essential gene for Mtb growth in vitro, and the deletion of MptpB did not affect the growth of Mtb in culture medium, but severely inhibited the proliferation of Mtb in IFN-γ-activated macrophages and impaired the ability of Mtb to infect guinea pigs

Method used

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  • Fusarielin M and application of derivative and pharmaceutically acceptable salt thereof
  • Fusarielin M and application of derivative and pharmaceutically acceptable salt thereof
  • Fusarielin M and application of derivative and pharmaceutically acceptable salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] 1. Isolation and identification of Fusarielin M

[0030] The compound Fusarielin M is a natural metabolic active product isolated from the cell of the marine fungus Fusarium graminearum SYSU-MS5127. The marine fungus is isolated from Laishizhou sea anemone in Shenzhen City, Guangdong Province, and is preserved in Guangdong Microbial Culture Collection Center with the preservation number GDMCC NO:60964. The separation method of compound Fusarielin M is as follows:

[0031] (1) Strains

[0032] Fusarium graminearum SYSU-MS5127, stored in PDA slant medium at 4°C.

[0033] (2) culture medium

[0034] Seed medium: 200g of potatoes, 20g of glucose, 1L of double distilled water.

[0035] Fermentation medium: rice 6000g, sea salt 180g, double distilled water 6L.

[0036] (3) Strain activation and shake flask culture

[0037] The bacteria were picked out from the storage slant, inoculated on the seed culture medium, placed on a constant temperature shaker at 28°C (rotation...

Embodiment 2

[0089] 1. Determination of in vitro anti-tuberculosis growth activity of compound Fusarielin M

[0090] In this experiment, resazurin was used as an indicator reagent for bacterial growth, and the effect of compound Fusarielin M on 4 strains of mycobacteria (M.smegmatis, M.marinum, M.bovis, M.tuberculosis), 1 strain of Staphylococcus aureus) and an Escherichia coli strain (Escherichia coli) in vitro, and the minimum inhibitory concentration (MIC) was used as an index to evaluate the antibacterial activity of the compound.

[0091] (1) strain

[0092] Mycobacteria: M. tuberculosis H 37 Ra, M. bovis BCG, M. smegmatis mc 2 155, M.marinumBAA-535, cultured in 7H9 (containing 0.2% glycerol, 0.05% Tween-80, 10% OADC) liquid medium (BD).

[0093] Staphylococcus aureus (Staphylococcus aureus ATCC6538) and Escherichia coli (Escherichiacoli ATCC25922) were cultured in LB medium.

[0094] (2) Resazurin (aladdin) was used as an indicator of bacterial growth to detect the antibacterial ...

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Abstract

The invention relates to the field of pharmacy, and particularly relates to Fusarielin M and application of a derivative and a pharmaceutically acceptable salt thereof. The compound Fusarielin M has strong inhibitory activity on mycobacterium tuberculosis tyrosine phosphatase B, and the IC50 of the compound Fusarielin M is 1.05 + / - 0.08 microns. The compound Fusarielin M can effectively inhibit the dephosphorylation activity of the mycobacterium tuberculosis tyrosine phosphatase B, is low in cytotoxicity, has an obvious inhibitory effect on proliferation of mycobacteria in macrophages, and has clinical application potential in tuberculosis treatment. In addition, the compound Fusarielin M is a natural metabolic active small molecule product separated from microorganisms, the structure of the compound Fusarielin M is analyzed, the compound Fusarielin M can be produced through large-scale fermentation separation, the source is rich, the production cost is low, and the possibility of patent medicine is high.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to the application of Fusarielin M, its derivatives and pharmaceutically acceptable salts. [0002] technical background [0003] Tuberculosis is a chronic infectious disease caused by Mycobacterium tuberculosis (Mtb), and it is one of the most deadly infectious diseases in the world. According to the World Health Organization's 2019 Global Tuberculosis Control Report, in 2018, there were 10 million new cases and about 1.2 million deaths from tuberculosis (TB). my country is a country with a high burden of tuberculosis and drug-resistant tuberculosis. Coupled with the continuous emergence of drug-resistant bacteria, the research and development of anti-tuberculosis drugs is imminent! [0004] Mycobacterium tuberculosis protein tyrosinephosphatase B (Mycobacterium tuberculosis protein tyrosinephosphatase, MptpB), is a secreted virulence factor necessary for Mycobacterium tuberculosis to infec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/19A61P31/06
CPCA61K31/19A61P31/06
Inventor 陈冬妮陆勇军陈森华刘岚
Owner SUN YAT SEN UNIV