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A kind of preparation method and application of amicoumacin isocoumarin compound

An isocoumarin and compound technology, which is applied in the field of pesticides and achieves the effects of high compound content, good reproducibility, and good activity against crop pathogens

Active Publication Date: 2021-04-02
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation method of the amicoumacin isocoumarin compound involved in the present invention and its anti-crop pathogenic bacteria activity have not been seen so far at home and abroad have any relevant patents or literature reports

Method used

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  • A kind of preparation method and application of amicoumacin isocoumarin compound
  • A kind of preparation method and application of amicoumacin isocoumarin compound
  • A kind of preparation method and application of amicoumacin isocoumarin compound

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Experimental program
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Effect test

Embodiment 1

[0020] Embodiment 1: Fermentative production and separation and purification of the compound of formula I

[0021] 1 Fermentation production

[0022] Fermentation culture of production bacteria: Paenibacillus sp.xy-2 is transferred from an inclined plane to a triangular flask equipped with a liquid medium after resuscitating (the composition of each bottle of medium: starch 1.0%, yeast extract 0.4%, peptone 0.2 %, add water to make up to 150mL), shake culture at 180rpm on a shaker at 28°C for 2-3 days, and use it as a seed culture solution. Then seed liquid is inoculated into the Erlenmeyer flask containing fresh, sterilized liquid culture medium (substrate composition as above) by 5~10% inoculum amount, under 28 ℃ 180rpm shaker culture 5 days, obtains fermentation culture fluid altogether About 30L.

[0023] 2 Obtaining of crude extract

[0024] The fermentation broth was centrifuged at 6000rpm to obtain mycelium and fermentation broth. Add HP20 macroporous resin (20g / L) ...

Embodiment 2

[0027] Embodiment 2: the antibacterial experiment of formula I compound to rice blast, corn stalk rust and cucumber downy mildew:

[0028] a. In vitro spore germination assay: the compound was dissolved in methanol as the test solution. Under sterile conditions, the test solution and rice blast fungus spore suspension were respectively added to a 96-well plate, and the 96-well plate was placed in a constant temperature incubator, and the inhibition of the compound on spore germination was detected after 24 hours. The inhibitory rate of the compound to the pathogenic bacteria is represented by 0-100%. The inhibitory rate of 0% means that the spore germination rate of the infection pathogenic bacteria group has no difference from that of the blank control group. The inhibitory rate of 100% means that the germination of the spores can be completely inhibited.

[0029] b. In vivo spray protection assay: Dissolve the compound in 2mL of acetone, add water containing 0.05% Tween-80 t...

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Abstract

The invention belongs to the technical field of pesticides, and relates to a preparation method for a natural amicoumacin isocoumarin compound PM-94128 and an application of the compound. The compoundhas a chemical structure shown in a formula I in the description. The invention provides the method for preparing the compound from fermented products of Paenibacillus sp. strains and the applicationof the compound in crop fungicide preparation. Experimental research shows that the compound has different-degree antibacterial effects on rice pyricularia oryzae, maize puccinia polysra, and cucumber pseudoperonospora cubenis, and the application of the compound in crop fungicide preparation can be developed.

Description

technical field [0001] The invention belongs to the technical field of pesticides, and relates to a preparation method of an amicoumacin isocoumarin compound PM-94128 extracted and separated from a fermentation product of endophytic bacteria Paenibacillus sp.xy-2 and its use in the preparation of agricultural fungicides. Background technique [0002] Amicoumacin isocoumarins are a class of microbial secondary metabolites with unique chemical structures and significant biological activities. At present, there are more than 40 such compounds found in nature, and most of them are found in marine bacteria of the genus Bacillus. According to literature reports, these compounds have significant anti-ulcer, anti-tumor, anti-bacteria and other medical biological activities. In particular, PM-94128, which was originally isolated from the fermentation broth of marine bacteria Bacillus sp., can inhibit DNA and protein synthesis (IC on DNA 50 = 2.5 μM, IC for protein 50 =0.1μM), has ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/76A01N43/16A01P3/00
CPCA01N43/16C07D311/76
Inventor 白皎潘华奇孙克华会明裴月湖卞西清
Owner SHENYANG PHARMA UNIVERSITY
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