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Trichothecene compound as well as preparation method and application thereof

A technology of trichothecenes and compounds, which is applied in the field of trichothecenes and their preparation, and can solve problems such as no drugs

Active Publication Date: 2018-11-13
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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  • Trichothecene compound as well as preparation method and application thereof
  • Trichothecene compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] A trichothecene compound, structural formula as shown in I:

[0022] (Ι).

Embodiment 2

[0024] The preparation method of the trichothecene compound shown in the formula I of embodiment 1 specifically comprises the steps:

[0025] (1) Fermentation production

[0026] Fusarium ( Fusarium sp.) Strain revival, inoculated into PDB solid medium, activated in a 28°C incubator for 3 days, picked a colony from the slope with an inoculation needle and inoculated it into PDB liquid medium, at 28°C, at a speed of Shake culture on a shaker at 180rpm for 3 days to obtain seed liquid, then inoculate the seed liquid with an inoculation amount of 10% by volume into PDB liquid medium, and culture on a shaker with a speed of 180rpm at 28°C for 12 days to obtain strains Fermented product, the strain fermented product is separated by gauze filtration to obtain mycelium and fermented liquid;

[0027] (2) Obtaining extract

[0028] Add the mycelium obtained in step (1) into methanol and ultrasonically break it, then extract it with equal volume of ethyl acetate for 3 times, and eva...

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 product of the compound isolated and purified in the above-mentioned Example 1, an appropriate amount of sample is accurately weighed, and a solution of the required concentration is prepared with methanol for testing the activity. The indicator bacteria used in this experiment was Vibrio harveii, a common aquatic pathogen.

[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, and then use it to activate the bacteria. Vibrio harveyi was inoculated on LB solid medium and cultured at 37°C for 24 hours. Inoculate the strains in the LB solid medium into the LB liquid medium, and incubate at 37°C for 12 hours. The bacteria suspension was added to a 96-well plate, and each gradient com...

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Abstract

The invention discloses a trichothecene compound as well as a preparation method and application thereof. The trichothecene compound is characterized in that the structural formula of the trichothecene compound is shown as I. The preparation method comprises the following steps: preparing a leavening of a trichothecene compound from fusarium of which the collection number is CGMCC No. 14121 by microorganism fermenting and culturing, and performing filtration through gauze in order to separate a mycelium from a fermentation liquid; then, adding the mycelium into methyl alcohol for performing ultrasonic smashing, performing isovolumetric extraction with ethyl acetate for 3 times, and evaporating an extractant with a rotary evaporator to dryness to obtain a thallus extract; performing extraction on the fermentation liquid with the isovolumetric ethyl acetate for 3 times, combining and collecting an ethyl acetate phase, evaporating the ethyl acetate phase with the rotary evaporator to dryness to obtain a bacteria solution extract, and combining the thallus extract and the bacteria solution extract to obtain a main rough extract; lastly, dissolving the main rough extract with acetonitrile, and performing separation and purification with a semi-prepared reverse phase efficient liquid chromatograph. The trichothecene compound has the advantage of capability of restraining aquatic pathogenic bacteria of vibrio harveyi.

Description

technical field [0001] The invention relates to a trichothecene compound, in particular to a trichothecene compound and a preparation method and use thereof. Background technique [0002] The reported trichothecene compounds 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 as Biological activities such as biological herbicides and insecticides. The inventors have learned from research that the liquid fermentation product of marine fungi is extracted with ethyl acetate, and the extract has good antibacterial activity, so the active ingredients have been studied. There is no report on the structure of the compound and its anti-Harveylia activity, so there is no drug related to it in the market. Contents of the invention [0003] The technical problem to be solved by the present invention is to provide a trichothecene c...

Claims

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Application Information

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Patent Type & Authority Applications(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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