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Alpha-pyrone compounds, and preparation method and application thereof

A compound, -OR technology, applied in the field of preparation of Candida albicans inhibitors, can solve problems such as drug resistance

Inactive Publication Date: 2011-05-25
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the abuse of drugs, Candida albicans has developed drug resistance and drug resistance to these drugs, which has become a major problem in clinical treatment. It is imminent to find anti-Candida albicans infection drugs with novel structures and high efficacy.

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] [Example 1] Fermentative production and separation and purification of compounds 1-3

[0028] 1 Fermentation production

[0029] Fermentation culture of production bacteria: According to the conventional method of cultivating microorganisms, take an appropriate amount of Nocardiopsis dassonvillei HR10-5 (Nocardiopsis dassonvillei HR10-5), inoculate it on the No. Cultured for 5 days. Get the right amount of Pseudo-Nocardia dassonville HR10-5 that was cultured on the slant for 5 days, inoculate into 150mL culture medium [substratum composition (%): glucose 2%, beef extract 0.3%, yeast extract 1%, soluble Starch 1%, peptone 1%, K 2 HPO 4 0.05%, MgSO 4 0.05%, CaCO 3 0.2%, artificial seawater 3.3%, pH 7.0] in 500mL Erlenmeyer flasks (400 bottles), loaded on a shaker at 28°C and 180 rpm for 8 days of production fermentation to obtain fermentation broth. The fermentation broth was extracted three times with an equal volume of ethyl acetate, and the combined ethyl acetate...

Embodiment 2

[0037] [Example 2] The test of anti-Candida albicans activity

[0038] 1 Experimental samples and experimental methods

[0039] Preparation of test sample and positive control drug solution: the test samples were pure compounds 1, 2, and 3 isolated and purified in Example 1 above, and pure positive control drug ketoconazole (Tokyo Kasei, Japan). Accurately weigh an appropriate amount of sample, and prepare a solution of the required concentration with methanol according to the double dilution method, namely 50 μg / mL, 25 μg / mL, 12.5 μg / mL, 6.25 μg / mL, 3.125 μg / mL, 1.5625 μg / mL, 0.78125μg / mL, 0.390625μg / mL, 0.1953125μg / mL for activity test.

[0040] Pathogenic bacterium Candida albicans cultivation: take a proper amount of frozen preserved Candida albicans, inoculate it on the slant of YPD medium for activation (the medium consists of 1% yeast extract, 2% glucose, 2% peptone, 2% agar, pH=7.0). Take an appropriate amount of Candida albicans cultured on the slant for 3 days, an...

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Abstract

The invention relates to alpha-pyrone compounds, and a preparation method and application thereof. The alpha-pyrone compounds with novel structure are prepared by nocardiopsis dassonvillei HR10-5 extracted from sea samples. Tests prove that the compounds can be used as a candida albicans inhibitor.

Description

Technical field: [0001] The present invention relates to a method for preparing α-pyrone compounds by using Nocardiopsis dassonvillei HR10-5 (Nocardiopsis dassonvillei HR10-5) (bacteria preservation number: CCTCC M 2010369, preservation date: December 28, 2010) Date, place of deposit: Wuhan, China, Wuhan University.); The present invention also relates to the use of such compounds in the preparation of Candida albicans inhibitors. Background technique: [0002] Candida albicans belongs to the Saccharomycetes, Saccharomycetes, and Candida genus, and is widely present on the skin surface, small intestine, cavity, and wet parts of the human body. It is the primary pathogen of fungal infections (Edwards JE Jr. Management of severe candidal infections: integration and review of current guidelines for treatment and prevention. Curr. Clin. Top. Infect. Dis. 2001, 21: 135-147; Klepser ME, Lewis RE, Pfaller MA. Therapy of Candida infections: susceptibility testing, resistance, and t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D309/38C12P17/06A61K31/366A61P31/10C12R1/04
Inventor 朱伟明付鹏王乂刘培培
Owner OCEAN UNIV OF CHINA
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