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Alpha-pyrone derivative, preparation method and application thereof

A technology of derivatives and pyrone is applied in the application field of preparing Candida albicans inhibitor, and can solve the problems such as no drugs.

Active Publication Date: 2017-07-21
NINGBO UNIV
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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 anti-Candida albicans activity of this compound, so there is no drug related to it on the market

Method used

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  • Alpha-pyrone derivative, preparation method and application thereof
  • Alpha-pyrone derivative, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] A kind of α-pyrone derivative structural formula is as shown in I:

[0024] (I).

Embodiment 2

[0026] The preparation method of the α-pyrone derivative shown in I formula specifically comprises the steps:

[0027] (1) Fermentation production

[0028] Penicillium ( Penicillium dipodomyicola DJ008) was resurrected by streaking, transferred to a 250mL Erlenmeyer flask containing 100mL PDB medium, and cultured at 28°C and 180 r / min for 4 days to obtain a seed culture solution; after that, the seed solution was inoculated with 10% inoculum Put it into a 1000mL Erlenmeyer flask filled with rice culture medium (dissolve 80g rice in 120ml seawater, soak overnight, then autoclave at 121°C for 20min), and culture at 28°C for 35 days to obtain the fermented product;

[0029] (2) Obtaining the extract

[0030] 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, repeat the extraction 3 times with 1L of ethyl acetate, combine the extracts obtained from the three extra...

Embodiment 3

[0038] Anti-Candida albicans activity test in vitro (96-well plate antibacterial method)

[0039] (1) Experimental samples

[0040] Preparation of 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 precisely weighed, and prepared into a solution with a required concentration with DMSO for testing the activity.

[0041] (2) Experimental method

[0042] 96-well plate anti-Candida albicans test method: The compound to be tested was serially diluted in 20% DMSO / saline, and transferred 10 µL to a 96-well flat-bottomed microplate. Under aerobic conditions, the Candida albicans strain was cultured on Sabouraud agar medium (SDA) at 30° C. for 16-20 hours. A series of compounds with different concentrations were added to RPMI1640 medium, and Candida albicans strains were inoculated, and cultured at 35°C for 46 hours. 8 μg / ml fluconazole was used as a positive control, and DMSO solution was use...

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Abstract

The invention discloses an alpha-pyrone derivative, a preparation method and application thereof. The alpha-pyrone derivative is characterized by having a structural formula shown as I. The preparation method includes the steps of: using penicillium dipodomyicola with a preservation number of CCTCC No. M2014087 to conduct fermentation culture so as to obtain a fermentation product containing new alpha-pyrone derivative, then conducting methanol soaking and ethyl acetate extraction on the fermentation product to obtain a crude extract, and carrying out pressure reduction silica gel column chromatography and reversed-phase semi-preparative high performance liquid chromatography separation and purification on the crude extract, thus obtaining the alpha-pyrone derivative. The alpha-pyrone derivative has anti-Candida albicans effect, and can be used as a new pharmaceutical component or lead compound of a Candida albicans inhibitor.

Description

technical field [0001] The present invention relates to an α-pyrone derivative, in particular to a method for preparing an α-pyrone derivative with marine Penicillium and the application of the compound in the preparation of Candida albicans inhibitors. Background technique [0002] α-pyrone is a class of six-membered ring lactones containing unsaturated bonds, which widely exist in many natural products and medicines. Studies have found that many compounds with α-pyrone rings have a variety of biological activities, such as anti-inflammatory, It plays an important role in antifungal, antitumor, antiviral treatment, Alzheimer's disease and other aspects. The inventor has studied and learned that the marine Penicillium Penicillium dipodomyicola The solid-fermented ethyl acetate extract of DJ008 (preserved in China Center for Type Culture Collection, preservation number: CCTCCNo: M2014087) has good anti-Candida albicans activity, and its active ingredients were studied. Ther...

Claims

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Application Information

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IPC IPC(8): C07D309/38C12P17/06A61P31/10C12R1/80
CPCC07D309/38C12P17/06
Inventor 丁立建何山原野
Owner NINGBO UNIV
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