Marine fungus derived azaphilones dimer compound and application thereof in anti-tuberculosis medicaments

A technology of marine fungi and compounds, applied in fungi, antibacterial drugs, microorganism-based methods, etc., can solve the problems of limited species and anti-tuberculosis activity, and achieve the effect of strong inhibitory activity and broad application prospects.

A technology of marine fungi and compounds, applied in fungi, antibacterial drugs, microorganism-based methods, etc., can solve the problems of limited species and anti-tuberculosis activity, and achieve the effect of strong inhibitory activity and broad application prospects.

CN111423987AActive Publication Date: 2020-07-17HEBEI UNIVERSITY
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  • Marine fungus derived azaphilones dimer compound and application thereof in anti-tuberculosis medicaments
  • Marine fungus derived azaphilones dimer compound and application thereof in anti-tuberculosis medicaments
  • Marine fungus derived azaphilones dimer compound and application thereof in anti-tuberculosis medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049](1) Cultivation of the marine fungus HBU-135 strain

[0050] The medium used for the culture of marine fungus HBU-135 contains 1.0wt% glucose, 0.1wt% yeast extract, 0.2wt% peptone, 1.0wt% agar, 3.0wt% coarse sea salt, and the rest is water. It is made into a test tube when used For slant, the marine fungus strain HBU-135 was grown at 28°C for 3 days.

[0051] (2) Fermentation of marine fungus HBU-135

[0052] The fermentation medium used for the fermentation culture of the marine fungus HBU-135 is that each 1000mL Erlenmeyer flask contains 100g of potatoes (boiled in water for 20 minutes to remove the potato dregs), 20g of glucose, and CaCl 2 33g and 500mL of water, the strain was fermented and cultured on a shaking table at 28°C for 14 days to obtain a fermented product; a total of 20 1000mL Erlenmeyer flasks were used for fermentation.

[0053] (3) Separation and analysis of Azaphilones dimers

[0054] Take the fermented product obtained in step (2), extract 3 time...

Embodiment 2

[0059] (1) Cultivation of the marine fungus HBU-135 strain

[0060] The medium used for the culture of the marine fungus HBU-135 contains 10wt% of glucose, 4.0wt% of yeast extract, 4.0wt% of peptone, 6.0wt% of agar, 10wt% of coarse sea salt, and the rest is water. Fungal strains were grown at 35°C for 5 days.

[0061] (2) Fermentation and cultivation of marine fungus HBU-135

[0062] The fermentation medium used for the fermentation culture of the marine fungus HBU-135 is that each 1000mL Erlenmeyer flask contains 120g of potatoes (boiled in water for 20 minutes to remove the potato dregs), 30g of glucose, and CaCl 2 40g, 600mL of water; the fermentation conditions are 20 days at 35°C on a shaking table to obtain a fermented product.

[0063] (3) Separation and analysis of Azaphilones dimer compounds

[0064]Take the fermented product obtained in step (2), extract 4 times with ethyl acetate, combine the ethyl acetate extracts and concentrate under reduced pressure to obtai...

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Abstract

The invention provides a marine fungus derived azaphilones dimer compound and an application thereof in anti-tuberculosis medicaments, wherein the structural formula of the compound is shown in formula 1 or formula 2. Fermenting culture is carried out on an HBU-135 strain of pleosporales sp., and the compound is isolated from the fermentation product. Proved by verification, the compound providedby the invention has high inhibitory activity on multi-drug-resistant mycobacterium tuberculosis (MDR-TB), can be used as an anti-tuberculosis medicament, and has a wide application prospect.

Description

technical field [0001] The invention relates to the field of marine natural medicinal chemistry, in particular to a marine fungus-derived azaphilones dimer compound and its application in anti-tuberculosis drugs. Background technique [0002] Mycobacterium tuberculosis, the causative bacterium of tuberculosis, has potentially infected about one-third of the world's population. Among them, 5%-10% of the infected people will eventually develop the disease, and the number of new infections is 9 million every year, and the death toll is about 2 million. At present, tuberculosis has become the eighth leading cause of death in low- and middle-developing countries, and among the population aged 15-59, tuberculosis has become the third leading cause of death after AIDS and ischemic heart disease. In recent years, due to the emergence of multidrug-resistant Mycobacterium tuberculosis (MDR-TB), the treatment of tuberculosis is facing great challenges. Finding new lead compounds for a...

Claims

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Application Information

Patent Timeline
17 Jul 2020
Publication
CN111423987A
IPC
C12N1/14; C07D311/96; C07D311/76; C12P17/16; A61P31/06; A61K31/352; C12R1/645
CPC
C07D311/96; C07D311/76; C12P17/162; A61P31/06; C12R2001/645; C12N1/145; Y02A50/30
Inventors
曹飞; 刘云凤