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Compounds and application of compounds in preparation of antituberculosis drug

A compound and anti-tuberculosis technology, applied in the field of medicine, can solve problems such as the difficulty of antibiotics

Inactive Publication Date: 2019-07-09
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

With the large number of compounds produced by Streptomyces being reported, the discovery of novel antibiotics has become increasingly difficult

Method used

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  • Compounds and application of compounds in preparation of antituberculosis drug
  • Compounds and application of compounds in preparation of antituberculosis drug
  • Compounds and application of compounds in preparation of antituberculosis drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1, application strain MS100137 production preparation compound

[0043] 1. Preparation of seed solution

[0044] 1. Spread MS100137 on a Ver01 solid plate and culture at 28°C for about 5 days until a single orange colony is formed.

[0045] The preparation method of plate medium: dissolve 10 grams of soluble starch, 10 grams of glucose, 10 grams of glycerin, 2.5 grams of corn steep liquor, 5 grams of peptone, 2 grams of yeast extract, 1 gram of sodium chloride, and 20 grams of agar powder in water, After adjusting the pH to 7.3, add 3 grams of calcium carbonate, dilute to 1 L, and sterilize at 115°C for 30 minutes.

[0046] 2. Divide the seed culture medium into 250 mL Erlenmeyer flasks (40 mL / bottle), pick a single colony of the bacterial species from the plate and inoculate it into the seed culture medium, shake and culture at 28° C. and 200 rpm for 5 days to obtain the seed liquid.

[0047] The preparation method of the seed medium: dissolve 10 grams of ...

Embodiment 2

[0079] Embodiment 2, anti-BCGMIC compound active test model

[0080] 7H9 medium (180ml): 0.94g 7H9 medium powder, 0.4mL glycerol, 0.1mL Tween80, sterilized at 121°C for 10min. Add 20 mL of filter-sterilized enrichment agent OADC just before use.

[0081] OADC (30 mL): NaCl 0.255g, BSA-V 1.5g, glucose 0.6g, sodium oleate 0.016g, catalase 0.0012g.

[0082] I.BCG cryopreservation tube live bacteria: Mycobacterium bovis Mycobacterium bovis attenuated strain bacillus Calmette-Guérin BCG (Pasteur 1137P2) is received in 10mL7H9 medium (adding filter-sterilized in the medium) OADC and 4 μL of 50 mg / mL kanamycin, the final concentration of kanamycin is 20 μg / ml), and cultured at 37°C and 110 rpm / min for 7-10 days (the culture time can be appropriately increased according to the growth of the bacterial solution).

[0083] II. Construction of MIC Compound Activity Test Model

[0084] The attenuated Mycobacterium bovis strain BCG was inoculated into a 250mL Erlenmeyer flask containing ...

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Abstract

This invention relates to compounds and an application of the compounds in preparation of an antituberculosis drug. The compounds have structures represented by a formula I or a formula II shown in the description, and the compounds represented by the formula I or the formula II can be prepared by performing fermentation culture on amycolatopsis methanolica MS100137. Another purpose of the invention is to provide the application of the compounds represented by the above formula I and formula II in the preparation of the antituberculosis drug. The compounds provided by the invention are obtained by a fermentation culture product of the amycolatopsis methanolica separated from an ocean, and have anti-BCG activity; the obtained compounds have important theoretical significance and practical application value; and the compounds have great significance to health cause of humans.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a compound and its application in preparing anti-tuberculosis drugs. Background technique [0002] Natural products of microbial origin are important sources of medicines. Since the discovery of penicillin, a large number of microbial secondary metabolites have been discovered as antibacterial drugs and used for the treatment of diseases, making great contributions to human health. [0003] However, in recent years, the number of newly discovered natural products has gradually decreased, and the number of new drugs on the market has also decreased year by year. At the same time, multidrug-resistant and highly resistant pathogenic bacteria continue to appear in the clinic, and the demand for novel antibiotics is increasing day by day. As the large number of compounds produced by Streptomyces has been reported, the discovery of novel antibiotics has become increasingly difficu...

Claims

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Application Information

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IPC IPC(8): C07D307/68A61K31/341A61P31/06C12P17/16C12R1/645
CPCA61P31/06C07D307/68C12P17/162
Inventor 张立新代焕琴谢峰李峥王秋水胡建森
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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