A kind of trichothecene compound and its preparation method and application

A technology for trichothecenes and compounds, which are applied in the field of trichothecenes and their preparations, and can solve problems such as unseen drugs and the like

Active Publication Date: 2021-02-05
NINGBO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report on the structure of the compound and its anti-Harveylia activity, so there is no drug related to it on the market

Method used

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  • A kind of trichothecene compound and its preparation method and application
  • A kind of trichothecene compound and its preparation method and application
  • A kind of trichothecene compound and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021]A trichothecenes compound, the structural formula is as shown in Ι:

[0022](Ι).

Embodiment 2

[0024]The preparation method of trichothecenes as shown in the formula I in Example 1, specifically includes the following steps:

[0025](1) Fermentation production

[0026]The Fusarium with the deposit number CGMCC No. 14121 (Fusarium sp.) Bacteria were resurrected by streaking, inoculated into PDB solid medium, and activated in a 28℃ incubator for 3 days. Use an inoculating needle to pick a colony from the slope and inoculate it into the PDB liquid medium. Shake culture on a shaker at 180 rpm for 3 days to obtain a seed solution. Then, the seed solution was inoculated into the PDB liquid medium at a volume ratio of 10%, and cultured at 28°C on a shaker at 180 rpm for 12 days to obtain a strain Fermented product, strain fermented product is filtered through gauze to obtain mycelium and fermentation broth;

[0027](2) Obtaining extract

[0028]The mycelium obtained in step (1) was added to methanol to be ultrasonically broken, and then extracted three times with equal volume of ethyl acetate....

Embodiment 3

[0037]In vitro antibacterial activity test (96-well plate antibacterial test)

[0038](1) Experimental samples

[0039]Preparation of the test sample solution: The test sample is the pure compound separated and purified in the above-mentioned Example 1. An appropriate amount of the sample is accurately weighed, and a solution of the required concentration is prepared with methanol to test the activity. The indicator bacteria used in this experiment is the common aquatic pathogen Vibrio harveyi.

[0040](2) Experimental method

[0041]96-well plate antibacterial test method: After preparing the medium, sterilize it for about two hours, dry and cool it to activate the bacteria. Vibrio harveyi was inoculated into LB solid medium and cultured at 37°C for 24 hours. The bacteria in the LB solid medium were inoculated into the LB liquid medium and cultured at 37°C for 12 hours. The cell suspension was added to a 96-well plate, and each gradient of the compound to be tested was added. The solvent used ...

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Abstract

The invention discloses a trichothecene compound and its preparation method and application, and is characterized in that the structural formula of the trichothecene compound is shown in I, and the preparation method steps include the preservation number of CGMCC No.14121 The Fusarium fungus is fermented by microbial fermentation to obtain trichothecene compounds, and the mycelium is separated from the fermentation broth by gauze filtration; then the mycelium is added to methanol for ultrasonic crushing, and then ethyl acetate, etc. The volume was extracted 3 times, and the extract was evaporated to dryness with a rotary evaporator to obtain a bacterial extract; the fermentation broth was extracted 3 times with an equal volume of ethyl acetate, and the ethyl acetate phase was combined and collected, and the ethyl acetate phase was extracted with a rotary evaporator. Evaporate to dryness to obtain the bacterial liquid extract, combine the bacterial cell extract and the bacterial liquid extract to obtain the total crude extract; finally dissolve the total crude extract with acetonitrile, and use semi-preparative reversed-phase high-performance liquid chromatography to separate and purify it. Advantages It has an inhibitory effect on the aquatic pathogen Vibrio harveylius.

Description

Technical field[0001]The invention relates to a trichothecenes compound, in particular to a trichothecenes compound and a preparation method and application thereof.Background technique[0002]The reported trichothecenes have various biological activities, including anti-tumor, anti-HIV, antibacterial, anti-malarial, anti-leukemia, inhibition of protein synthesis, inhibition of DNA and RNA synthesis, immunosuppression, and use as Biological activity such as biological herbicides and pesticides. The inventor learned that the liquid fermentation product of marine fungi was extracted with ethyl acetate, and the extract had good antibacterial activity, so the active ingredients were studied. There is no report on the structure of the compound and its anti-Vibrio harveyi activity, so there are no related drugs on the market.Summary of the invention[0003]The technical problem to be solved by the present invention is to provide a trichothecenes compound which has a certain inhibitory effect ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/22C12P17/18A61P31/04C12R1/77
CPCA61P31/04C07D493/22C12P17/181
Inventor 丁立建何山刘勇贺小平金海晓斯拉瓦·爱泼斯坦
Owner NINGBO UNIV
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