Azaphilones compounds in marine fungus HK1-6 and application of azaphilones compounds as MRSA-resistant drug

A technology of marine fungi and compounds, applied in antibacterial drugs, microorganism-based methods, medical preparations containing active ingredients, etc., can solve problems such as threats to patients' lives

Active Publication Date: 2018-06-01
YANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Once MRSA shows widespread resistance to antibiotics, it will seriously threaten the lives of patients

Method used

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  • Azaphilones compounds in marine fungus HK1-6 and application of azaphilones compounds as MRSA-resistant drug
  • Azaphilones compounds in marine fungus HK1-6 and application of azaphilones compounds as MRSA-resistant drug
  • Azaphilones compounds in marine fungus HK1-6 and application of azaphilones compounds as MRSA-resistant drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] (1) Cultivation of the marine fungus Penicillium sp.HK1-6

[0040] The medium used for the culture of the fungus Penicillium sp. (HK1-6) is to add in every 1000mL of water: boil 200g of potatoes to extract the juice, 20g of glucose, 30g of coarse sea salt, and 15g of agar; Media plates. The fungal strains were inoculated on medium plates and cultured on a shaker at 20°C for 3 days.

[0041] (2) Fermentation of marine fungus Penicillium sp.HK1-6

[0042] The fermentation medium used in the fermentation culture of the fungus Penicillium sp.HK1-6 is as follows: add 200g of potatoes to boil for juice, 20g of glucose, and 30g of coarse sea salt for every 1000mL of water; when used, divide them into Erlenmeyer flasks. The fungal strain is inoculated in the culture medium of the Erlenmeyer flask, and cultured statically at 15-20° C. for 28 days.

[0043] (3) Preliminary separation of components in the fermented product

[0044] Get 10L of the fermented product obtained in ...

Embodiment 2

[0058] (1) Culture of marine fungus Penicillium sp. (HK1-6)

[0059] The medium used for the culture of the fungus Penicillium sp. (HK1-6) contains 0.1% glucose (percentage by weight, the same below), 5% yeast extract, 0.01% peptone, 0.1% agar, 10% coarse sea salt, and the rest are Water, made into a test tube slant when used, and the fungal strains were cultivated at 25°C for 5 days.

[0060] (2) Fermentation of marine fungus Penicillium sp. (HK1-6)

[0061] The fermentation medium used for the fermentation culture of the fungus Penicillium sp. (HK1-6) contains glucose 0.1% (weight percentage, the same below), yeast extract 0.01%, peptone 5%, coarse sea salt 0.05%, appropriate amount of water, fungal strain Cultivate at 15-20°C for 21 days.

[0062] (3) Preliminary separation of components in the fermented product

[0063] Get 30L of the fermented product obtained in step (2), separate the fermented liquid from the thalline, extract the fermented liquid 3 times with ether,...

Embodiment 3

[0067] (1) Cultivation of the marine fungus Penicillium sp.HK1-6

[0068] The medium used for the culture of the fungus Penicillium sp.HK1-6 contains 10% glucose (percentage by weight, the same below), 0.01% yeast extract, 5% peptone, 3% agar, 0.05% coarse sea salt, and the rest is Water, made into a test tube slant when used, and the fungal strains were cultured at 30°C for 7 days.

[0069] (2) Fermentation of marine fungus Penicillium sp.HK1-6

[0070] The fermentation medium used for the fermentation culture of the fungus Penicillium sp.HK1-6 contains 10% of glucose (percentage by weight, the same below), 5% of yeast extract, 0.01% of peptone, 5% of coarse sea salt, and the rest is water. Cultivate for 35 days at 25-32°C.

[0071] (3) Preliminary separation of components in the fermented product

[0072] Get 50L of the fermented product obtained in step (2), separate the fermented liquid from the thalline, extract the fermented liquid 5 times with ether, and concentrate ...

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Abstract

The invention relates to azaphilones compounds in marine fungus HK1-6 and an application of the azaphilones compounds as an MRSA-resistant drug, in particular to secondary metabolites 1-4 produced bymarine fungus Penicillium sp.HK1-6 or pharmaceutically acceptable salt. The compounds 1-4 show very high antibacterial activity for MRSA (such as S. aureus ATCC4330 and S. aureus ATCC33591) and VER (such as E. faecalis ATCC51299), MIC is smaller than or equal to 12.5 mu g/mL, the MIC of a compound 2 for E. faecalis ATCC51299 is one times higher than that of positive drug vancomycin, and the compounds have good prospects to be developed into drugs resisting drug-resistant bacteria, lead compounds of drugs and candidate drugs.

Description

technical field [0001] The invention belongs to the field of secondary metabolites of marine fungi, in particular to an azaphilones compound derived from marine fungi. The present invention also relates to the above-mentioned azaphilones compound, its preparation method and its application as an anti-drug-resistant bacteria drug. The azaphilones compound of the present invention shows good activity against drug-resistant bacteria, especially methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecalis (VER). Background technique [0002] Methicillin-resistant Staphylococcus aureus (MRSA) is the primary pathogenic bacteria of clinical infection, which is widely prevalent in the world and has the characteristics of high infection rate and high fatality rate, and the infection rate continues to increase year by year. high. MRSA can cause various infections in the body, and it brings great difficulties to clinical treatment due to its multi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/76A61K31/352A61P31/04C12P17/06C12R1/80
CPCC07D311/76C12P17/06
Inventor 陈敏沈南星陈芷杞
Owner YANGZHOU UNIV
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