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Furanone compound, preparation method and application thereof

A compound, the technology of furanone, which is applied in the field of furanone compounds, can solve problems such as drugs that have not yet been seen

Active Publication Date: 2017-03-22
宁波顾德生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are no reports on the chemical structure and antifungal activity of this compound, so there are no related drugs on the market.

Method used

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  • Furanone compound, preparation method and application thereof
  • Furanone compound, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] A kind of furanone compound structural formula is as shown in I:

[0023] (I).

Embodiment 2

[0025] The preparation method of the furanone compound shown in formula I specifically comprises the steps:

[0026] (1) Fermentation production

[0027] Aspergillus versicolor ( Aspergillus versicolor DJ013) was revived by streaking, inoculated on PDA solid slant medium, and cultured in a 28°C incubator for 5 days; all the colonies obtained from slant culture were inoculated into solid medium (dissolve 80g rice in 120ml seawater, soak overnight, Autoclave at 121°C for 20 minutes), then ferment at 28°C for 40 days to obtain the fermented product;

[0028] (2) Obtaining the extract

[0029] Soak the above-mentioned fermented product in 4L of methanol for 3 times, then concentrate and evaporate the methanol extract to dryness, redissolve it in 1L of water, and then extract it with 1L of ethyl acetate for 3 times, combine the extracts obtained from the three extractions and concentrate under reduced pressure to remove ethyl acetate ester to obtain crude extract;

[0030] (3) ...

Embodiment 3

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

[0038] (1) Experimental samples

[0039] Preparation of the test sample solution: the test sample is the pure compound I isolated and purified in Example 1 above, and an appropriate amount of sample is accurately weighed, and prepared into a solution of the required concentration with DMSO for testing the activity. The indicator bacteria used in this experiment were Cryptococcus neoformans and Candida albicans.

[0040] (2) Experimental method

[0041] 96-well plate antifungal test method: The test compound was serially diluted in 20% DMSO / saline, and transferred 10 µL to a 96-well flat-bottomed microplate. Under aerobic conditions, the two bacterial indicator strains were cultured on Sabouraud agar medium (SDA) at 30° C. for 16-20 hours. A series of different concentrations of compounds were added to RPMI1640 medium, and fungal strains were inoculated. Cryptococcus neoformans was cultured at 35...

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Abstract

The invention discloses a furanone compound, a preparation method and application thereof. The furanone compound is characterized by having a structural formula shown as formula I. The preparation method includes the steps of: conducting fermentation culture on aspergillus versicolor with a preservation number of CCTCC No. M2014089 to obtain a fermentation product containing a new furanone compound, then soaking the fermentation product with methanol, and performing extraction with ethyl acetate to obtain a crude extract, subjecting the crude extract to decompression silica gel column chromatography and conducting reversed-phase semi-preparative high performance liquid chromatography separation and purification, thus obtaining the product. The furanone compound has antifungal effect, and can be used as an antifungal new drug component or lead compound.

Description

technical field [0001] The invention relates to a furanone compound, in particular to a furanone compound, a preparation method thereof and the application of the compound in the preparation of antifungal drugs. Background technique [0002] With the extensive use and irrational use of antibiotics and the acceleration of microbial mutation, the drug resistance of pathogenic microorganisms is gradually increasing, and it is urgent to find new antibiotics. Marine fungi have attracted increasing attention from researchers because of their complex metabolic pathways and rich metabolites. The types and quantities of reported marine fungal secondary metabolites are rapidly increasing, and many of these metabolites have strong antibacterial, antiviral, antitumor and enzyme inhibitory activities. The inventor has studied and learned that marine fungi Aspergillus versicolor DJ013 (preserved in China Center for Type Culture Collection, preservation number: CCTCC No. M2014089) solid...

Claims

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Application Information

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IPC IPC(8): C07D307/60A61P31/10C12P17/04C12R1/66
CPCC07D307/60C12P17/04
Inventor 丁立建何山严小军
Owner 宁波顾德生物科技有限公司
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