Novel cytochalasin compound with function of antagonizing clinical drug-resistant bacteria and preparation method of novel cytochalasin compound

A technology of cytochalasin and compounds, which is applied in the field of biomedicine and can solve the problems reported by scholars on the antagonism of cytochalasin compounds

Active Publication Date: 2021-08-13
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In recent years, although new molecules that can antagonize clinical drug-resistant bacteria have been reported, few scholars have reported the antagonism of cytochalasin compounds against clinical drug-resistant bacteria.

Method used

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  • Novel cytochalasin compound with function of antagonizing clinical drug-resistant bacteria and preparation method of novel cytochalasin compound
  • Novel cytochalasin compound with function of antagonizing clinical drug-resistant bacteria and preparation method of novel cytochalasin compound
  • Novel cytochalasin compound with function of antagonizing clinical drug-resistant bacteria and preparation method of novel cytochalasin compound

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] A method for preparing a novel cytochalasin compound with the function of antagonizing clinical drug-resistant bacteria, comprising the following steps:

[0055] Step (1), the fermentation culture of Ascocystis aureus;

[0056] In step (2), methanol is used to extract the secondary metabolites obtained by the fermentation and cultivation of Ascocystis aureus, concentrated under reduced pressure to evaporate the solvent, washed with water, then extracted with ethyl acetate, and finally concentrated under reduced pressure to obtain a crude extract;

[0057] In step (3), the crude extract is wet-loaded to a silica gel column, and through silica gel column chromatography, gradient elution is performed with a mixed organic solvent of dichloromethane and methanol at a volume ratio of 100:1-1:1, and each sample is collected. The gradient eluate of the gradient was concentrated and monitored by TLC, and the same fractions were combined to obtain six groups of segments Fr.A-Fr.F...

Embodiment 2

[0066] A method for preparing a novel cytochalasin compound with the function of antagonizing clinical drug-resistant bacteria, comprising the following steps:

[0067] Step (1), the fermentation culture of Ascocystis aureus;

[0068] In step (2), methanol is used to extract the secondary metabolites obtained by the fermentation and cultivation of Ascocystis aureus, concentrated under reduced pressure to evaporate the solvent, washed with water, then extracted with ethyl acetate, and finally concentrated under reduced pressure to obtain a crude extract;

[0069] In step (3), the crude extract is wet-loaded to a silica gel column, and through silica gel column chromatography, gradient elution is performed with a mixed organic solvent of dichloromethane and methanol at a volume ratio of 100:1-1:1, and each sample is collected. The gradient eluate of the gradient was concentrated and monitored by TLC, and the same fractions were combined to obtain six groups of segments Fr.A-Fr.F...

Embodiment 3

[0083] A method for preparing a novel cytochalasin compound with the function of antagonizing clinical drug-resistant bacteria, comprising the following steps:

[0084] Step (1), the fermentation culture of Ascocystis aureus;

[0085] In step (2), methanol is used to extract the secondary metabolites obtained by the fermentation and cultivation of Ascocystis aureus, concentrated under reduced pressure to evaporate the solvent, washed with water, then extracted with ethyl acetate, and finally concentrated under reduced pressure to obtain a crude extract;

[0086] In step (3), the crude extract is wet-loaded to a silica gel column, and through silica gel column chromatography, gradient elution is performed with a mixed organic solvent of dichloromethane and methanol at a volume ratio of 100:1-1:1, and each sample is collected. The gradient eluate of the gradient was concentrated and monitored by TLC, and the same fractions were combined to obtain six groups of segments Fr.A-Fr.F...

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Abstract

The invention relates to a novel cytochalasin compound with a function of antagonizing clinical drug-resistant bacteria and a preparation method of the novel cytochalasin compound, and belongs to the technical field of biomedicine. The method comprises the following steps: firstly, carrying out fermentation culture on Cytospora chrysosperma; then extracting a secondary metabolite obtained by fermenting and culturing the Cytospora chrysosperma by using methanol, conducting extracting by using ethyl acetate, conducting concentrating under reduced pressure, carrying out gradient elution on the obtained crude extract to obtain six component segments, and carrying out gradient elution on the fourth component segment again to obtain four sub-component segments; and respectively carrying out sephadex chromatography separation and purification and high performance liquid chromatography separation and purification on the second subgroup segment and the fourth subgroup segment to obtain two novel cytochalasins. The two novel cytochalains have a very strong antagonistic effect on four clinical drug-resistant bacteria, namely carbapenem-resistant pseudomonas aeruginosa, methicillin-resistant staphylococcus aureus, multi-drug-resistant enterococcus faecalis and multi-drug-resistant enterococcus faecium, and are expected to be developed into novel drugs for resisting the clinical drug-resistant bacteria.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to a novel cytochalasin compound capable of antagonizing clinical drug-resistant bacteria and a preparation method thereof. Background technique [0002] Drug-resistant bacteria refer to those bacteria that are resistant to traditional antibacterial drugs. This is a special manifestation of bacteria in the process of survival. When antibiotics are used for a long time, most of the sensitive strains are constantly killed, and the drug-resistant strains Just a large number of reproduction, instead of sensitive strains, so that the resistance rate of bacteria to the drug continues to increase. Once drug resistance occurs, the therapeutic effect of the drug will obviously decline or even completely lose its therapeutic effect. In recent years, due to the abuse of antibiotics, a large number of drug-resistant bacteria have emerged around the world. As early as 2014, the Wo...

Claims

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Application Information

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IPC IPC(8): C07D491/20C07D209/96C12P17/18C12N1/14A61P31/04C12R1/645
CPCC07D491/20C07D209/96C12P17/18C12P17/182C12N1/14A61P31/04C07B2200/07Y02A50/30
Inventor 杨小龙牟青林王文静向婷
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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