Method for efficiently preparing cyclic depsipeptide, cyclic depsipeptide and application

A technology of cyclic depsipeptides and compounds, which is applied in the field of efficient preparation of cyclic depsipeptides, and can solve the problems of low yield of cyclic depsipeptides

Active Publication Date: 2021-05-14
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] At present, the yield of cyclic depsipeptides is low, and increasing th

Method used

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  • Method for efficiently preparing cyclic depsipeptide, cyclic depsipeptide and application
  • Method for efficiently preparing cyclic depsipeptide, cyclic depsipeptide and application
  • Method for efficiently preparing cyclic depsipeptide, cyclic depsipeptide and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1, Liquid Chromatography-Mass Spectrometry (LC-MS) Preliminary Analysis of Bat Feces Parasitic Fungus Amphichordaguana LC5815 Solid Fermentation

[0054] The bat feces parasitic fungus A.guana was inoculated on glucose agar medium (PDA) for strain activation, and the culture condition was 28°C for 5 to 7 days. Collect the spores of the activated bacterial strain with 0.1% (w / v) Tween-80, inoculate an appropriate amount of seed liquid to carry out solid fermentation, the medium used in the solid fermentation is composed of 20g rice and 30mL water, the culture conditions of the solid fermentation Incubate at 28°C for 7 days in the dark. For convenience of description, the culture medium composed of 30 mL of water per 20 g of rice can be called rice culture medium. The above experiments were repeated 3 times. Extract the fermentation product with ethyl acetate (specifically, extract three times with 7.5L ethyl acetate per 1kg of fermentation medium. After the fer...

Embodiment 2

[0060] Embodiment 2, separation and purification of active cyclic depsipeptide components

[0061] The preliminary analysis of the rice fermentation product of A.guana LC5815 by LC-MS in Example 1 has shown that it can produce abundant large molecular weight compounds. The bacterium was cultured in 20kg of rice culture medium (obtained by mixing 20kg of rice and 30L of water) for large-scale fermentation, and kept in the dark at 28°C for 30 days to obtain a rice fermentation culture. Ethyl acetate was added to the rice fermentation culture for extraction 3 times, soaked overnight each time to obtain an extract. Specifically, 7.5 L of ethyl acetate was used for extraction per 1 kg of rice, and ethyl acetate was directly added after the cultivation was completed. In the specific experiment, because the 250mL triangular flask used, each bottle of 20g rice, each bottle was extracted with 50mL ethyl acetate, repeated 3 times, a total of 150mL ethyl acetate was needed.

[0062] Th...

Embodiment 3

[0066] Example 3, verify the biological activity of the cyclic depsipeptide prepared in Example 2

[0067] 3.1, verify the anti-phytopathogenic fungal activity

[0068] Use a 90mm petri dish containing 10mL of PDA medium to measure its antifungal activity. Use the following three plant pathogenic fungi, Alternaria solani, Botrytis cinerea, and Fusarium oxysporum as indicator bacteria, and use PDA medium to cultivate plant pathogenic fungi. When the diameter grows to about 2cm Finally, a sterile blank filter paper sheet of the same size (diameter 0.625 cm) was placed 1 cm away from the edge of the mycelial colony. Distribution Dissolve the isaridin H, desmethylisaridin E, and isaridin E prepared in Example 2 with dimethyl sulfoxide (DMSO) to obtain samples with a final concentration of 1 mg / mL, respectively, and add 10 uL to the filter paper. in, Figure 6 Add isaridin H to sheet 1, add desmethylisaridin E to sheet 2, and isaridin E to sheet 3. Place the petri dish at 28°C a...

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Abstract

The invention relates to the field of preparation of medicinal compounds, in particular to a method for efficiently preparing cyclic depsipeptide, the cyclic depsipeptide and application. The method comprises the following steps: inoculating a culture medium with the parasitic fungus Amphihorda guana LC5815 from the bat feces, and fermenting, so as to obtain a fermentation culture; and performing separating from the fermentation culture to obtain the cyclic depsipeptide compound.

Description

technical field [0001] The present application relates to the field of preparation of pharmaceutical compounds, in particular to a method for efficiently preparing cyclic depsipeptides, cyclic depsipeptides and applications. Background technique [0002] Fungal insecticides are biologically active agents that use fungi as a means of biological control to control harmful insects in nature. At present, the main fungal insecticides are Beauveria bassiana, Metarhizium anisopliae, Paecilomyces lilacinus and so on. Although fungal insecticides have a wide insecticidal spectrum and have the advantages of being able to spread among target pests, the development of the fungal insecticide industry has been slow for a long time. In addition to issues such as industrial policies, application concepts, and industrial production, high-yield strains are also limited. important. [0003] It has been reported in many literatures that cyclic depsipeptide isariins compounds have insecticidal...

Claims

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Application Information

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IPC IPC(8): C12P21/04C12P21/02C12N1/14C07K7/06C07K11/02C07K1/14C07K1/16A01N43/72A01P3/00A01P1/00A01P7/04A01P15/00A61K38/08A61K38/15A61P31/04A61P31/10A61P29/00A61P33/06C12R1/645
CPCC12P21/02C12N1/14C07K11/02C07K7/06A01N43/72A61P31/04A61P31/10A61P29/00A61P33/06A61K38/00Y02A50/30
Inventor 尹文兵蔡磊梁敏李伟
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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