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Application of biphenyl compound in resisting clinical drug-resistant fungi

A technology of compounds and fungi, applied in the direction of antifungal agents, active ingredients of hydroxyl compounds, plant/algae/fungus/moss components, etc., can solve the problem of being unable to curb the spread of drug-resistant fungi, and achieve the effect of great application potential

Active Publication Date: 2021-09-21
INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, existing antifungal drugs fail to curb the spread of drug-resistant fungi

Method used

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  • Application of biphenyl compound in resisting clinical drug-resistant fungi
  • Application of biphenyl compound in resisting clinical drug-resistant fungi
  • Application of biphenyl compound in resisting clinical drug-resistant fungi

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1, the preparation of biphenyl compound

[0030] The preparation method of biphenyl compound is specifically as follows:

[0031] 1) Take 10kg of dried rowan suspension cells, extract by cold soaking with methanol at room temperature for 5 times, the amount of methanol is 20L / each time, the extraction time is 72h each time, combine the extracts, and decompress at 40°C and 0.08Mpa Concentrate the extract to obtain about 6 kg of extract;

[0032] 2) The obtained extract was dissolved in chloroform / methanol (1:1, v / v, 6L) and then adsorbed and mixed with 100-200 mesh silica gel (ca. Elution, followed by gradient washing with dichloromethane / methanol mixed solvent with a volume ratio of 100:0, 98:2, 95:5, 90:10, 80:20, 70:30, 50:50, 0:100 Take off, get 11 components, numbered as A 1 –A 11 ;

[0033] 3) The fifth component A 5 Further use normal phase silica gel column (filler is 100-200 mesh silica gel) to separate, the condition of separation is to adopt v...

Embodiment 2

[0039] Embodiment 2, antibacterial experiment

[0040] The compound shown in formula I obtained in Example 1 was used for MIC determination of a strain of clinical drug-resistant fungus, using the double dilution method, and the specific steps were as follows:

[0041] 1) Determination of MIC of clinical drug-resistant fungi: The obtained compound represented by formula I was prepared into a 10 mmol / mL stock solution with DMSO.

[0042]2) Prepare 500mL, 2×1640 medium, the specific operation is: take 10.4g RPMI Medium 1640powder (gibco, USA); 20g glucose (Shenggong, Shanghai); 34.53g MOPS (3-morpholinated propanesulfonic acid) dry powder (Shenggong, Shanghai); dissolve in 500mL distilled water; add 2.5g NaOH powder (Shenggong, Shanghai), and filter through a 0.22um membrane filter to sterilize. After filtration, it was stored at 4°C for use.

[0043] 3) Preparation of bacterial suspension: drug-resistant Candida glabrata (Candida glabrata) (preservation number: GDMCC NO: 6172...

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Abstract

The invention discloses application of a biphenyl compound in resisting clinical drug-resistant fungi, and belongs to the technical field of antibacterial activity research. The invention provides an application of a compound as shown in a formula I or pharmaceutically acceptable salt thereof in antibiosis. According to the invention, the compound represented by the formula I can effectively inhibit the growth of drug-resistant Candida glabrata under the condition of low concentration, and has a great application potential.

Description

technical field [0001] The invention relates to the technical field of antifungal activity research, in particular to the application of a biphenyl compound in anti-clinical drug-resistant fungi. Background technique [0002] The problem of fungal drug resistance is becoming more and more serious, posing a major threat to human life and health. Currently, existing antifungal drugs are unable to curb the spread of drug-resistant fungi. Therefore, the discovery and development of new anti-drug-resistant fungal drugs has become a major demand for innovative drug research in my country. [0003] In recent years, Candida infectious diseases have become more and more serious threats to human beings. In addition to Candida albicans, Candida glabrata has become the second most common invasive Candida in some countries and regions. Clinical isolates of Candida glabrata are highly resistant to first-line antifungal drugs, resulting in a mortality rate of up to 50%. It is imperativ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/05A61P31/10A61K36/73
CPCA61K31/05A61P31/10A61K36/73
Inventor 郭兰萍杨小龙江玉凤杨健高原
Owner INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI