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Aspergillus unguis bromo-depsidone compound and preparation method and application thereof

A technology of Aspergillus brominated depsipepsyl acid cyclic ether and depsipsipsic acid cyclic ether, which is applied in the field of microbial fermentation product extraction, can solve the problems of antibiotics losing curative effect, and achieve good antifungal properties, wide application prospects, and easy large-scale production Effect

Active Publication Date: 2017-05-10
GUANGDONG OCEAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, in clinical treatment, it is found that the drug resistance of pathogenic microorganisms is becoming stronger and stronger, especially methicillin-resistant Staphylococcus aureus (MRSA), Pseudomonas aeruginosa (commonly known as Pseudomonas aeruginosa) and Candida albicans (commonly known as albicans) are becoming more and more serious, and many traditional antibiotics have basically lost their efficacy, so it is necessary to find new antibiotics to meet this challenge

Method used

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  • Aspergillus unguis bromo-depsidone compound and preparation method and application thereof
  • Aspergillus unguis bromo-depsidone compound and preparation method and application thereof
  • Aspergillus unguis bromo-depsidone compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1 The preparation method of marine fungal brominated depsipepsyl acid cyclic ether compounds

[0048] 1. Fermentation

[0049] Aspergillus claw ( Aspergillus unguis ) CGMCC No.3372 was inoculated in the fungal liquid medium for static fermentation. After 2 days of fermentation, procaine solution with a final concentration of 1mM was added, and the fermentation was continued for 20 days, filtered, and the mycelia and fermentation broth were collected respectively.

[0050] Wherein, the formula of described fungal liquid culture medium is:

[0051] Each liter contains the following components: 500 mL of potato juice, 20 g of NaBr, 20 g of sucrose, and 500 mL of pure water or tap water.

[0052] 2. Rough extraction

[0053] The fermented liquid obtained in step 1 was extracted three times with ethyl acetate, concentrated under reduced pressure to obtain a concentrated liquid. At the same time, the mycelium obtained in step 1 was extracted three times with methano...

Embodiment 2

[0071] Example 2 Experiment of antifungal activity of brominated depsipphenolic acid cyclic ether compounds

[0072] 1. Candida albicans ( Candida albicans ) is a common opportunistic fungus that can invade many parts of the human body, causing skin candidiasis, mucosal candidiasis (thrush, angular cheilitis, and vaginitis are the most common) and visceral and central nervous candidiasis. Common fungal diseases. The clinical symptoms are intricate and varied in urgency and slowness. In recent years, with the high-dose application of antibiotics, hormones, and immunosuppressants, as well as the development of organ transplantation, the incidence of candidiasis has gradually increased, and can be life-threatening and cause serious consequences. This bacterium has become an important target for the development of antifungal drugs.

[0073] 2. Experimental method:

[0074] Use the international standard micro broth dilution method (National Committee for Clinical LaboratorySt...

Embodiment 3

[0079] Example 3 Anti-Gram-negative Bacteria Activity Experiment of Bromo-Depsipphenolic Acid Cyclic Ether Compounds

[0080] 1. Pseudomonas aeruginosa ( Pseudomonas aeruginosa ), also known as Pseudomonas aeruginosa, is an opportunistic pathogen and one of the main pathogens of nosocomial infection. Patients suffering from metabolic diseases, blood diseases and malignant tumors, as well as patients after surgery or certain treatments are susceptible to infection with this bacteria. The bacteria often cause postoperative wound infection, and can also cause bedsores, abscesses, and suppurative otitis media. The infected lesions caused by it can lead to hematogenous dissemination, and bacteremia and sepsis occur. Infection with Pseudomonas aeruginosa after burns can cause death. Moreover, with the widespread clinical use of broad-spectrum antibiotics, hormones, and immunosuppressants, Pseudomonas aeruginosa has rapidly developed resistance to a variety of antibiotics, making...

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Abstract

The invention discloses an aspergillus unguis bromo-depsidone compound and a preparation method and application thereof. The chemical structure formula of the aspergillus unguis bromo-depsidone compound is shown as the formula (I) in the accompanying drawing. The compound is obtained by inoculating aspergillus unguis DLEP2008001 into a fungus culture medium; performing still standing fermentation; extracting fermentation liquid by ethyl acetate; extracting mycelia by an organic solvent; after the merging, performing gradient silicagel column chromatography by an organic solvent; through the silicagel thin layer chromatography detection, continuously performing silicagel column and gel column chromatography on the elution fractions containing target subjects; performing normal phase preparation liquid chromatographic separation purification. The compound can be used for inhibiting fungus white candida, gram-negative bacterium pseudomonas aeruginosa and gram-positive bacterium methoxyl-resistant penicillin staphylococcus aureus and killing artemia larvae, and the potential purposes of antifungal antibiotics, antibacterial antibiotics or pesticides are realized.

Description

technical field [0001] The invention belongs to the technical field of extraction of microbial fermented products, and in particular relates to a marine fungus Aspergillus clawus brominated depsipaldehyde cyclic ether compound and its preparation method and application. Background technique [0002] At present, in clinical treatment, it is found that the drug resistance of pathogenic microorganisms is becoming stronger and stronger, especially methicillin-resistant Staphylococcus aureus (MRSA), Pseudomonas aeruginosa (commonly known as Pseudomonas aeruginosa) and Candida albicans (commonly known as albicans) are becoming more and more serious, and many traditional antibiotics have basically lost their efficacy. Therefore, it is necessary to find new types of antibiotics to meet this challenge. In addition, the excessive use of various chemically synthesized pesticides in agricultural production has caused serious food, soil and water pollution, and endangered human health an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D321/10C12P17/08A61P31/04A61P31/10A01N43/24A01P7/00C12R1/66
Inventor 张翼鲍海燕冯妍聂影影刘亚月杨文聪杨静明
Owner GUANGDONG OCEAN UNIVERSITY
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