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Application of indolyl diketopiperazine compound in preparation of antifungal medicines

A technology of antifungal drugs and compounds, applied in the field of medicine and biology

Inactive Publication Date: 2016-08-17
GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Compound 1,2,3,4-tetrahydro-2-methyl-3-methylene-1,4-dioxopyrazino[1,2-a]indole structure and literature "Wan-Ling Liang, Xiu Le, Hou-Jin Li, et al. Exploring the chemodiversity and biological activities of the secondary metabolites from the marine fungus Neosartorya pseudofischeri [J]. MarDrugs, 2014, 12(11): 5657-5676." Consistent reports on an indole diketopiperazine compound , but so far, there is no report on the antifungal activity of 1,2,3,4-tetrahydro-2-methyl-3-methylene-1,4-dioxopyrazino[1,2-a]indole at home and abroad

Method used

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  • Application of indolyl diketopiperazine compound in preparation of antifungal medicines
  • Application of indolyl diketopiperazine compound in preparation of antifungal medicines
  • Application of indolyl diketopiperazine compound in preparation of antifungal medicines

Examples

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Embodiment 1

[0016] The effect of compound 1,2,3,4-tetrahydro-2-methyl-3-methylene-1,4-dioxopyrazino[1,2-a]indole on Candida albicans, Trichoderma viride, Aspergillus niger or Aspergillus antibacterial activity.

[0017] The compound 1,2,3,4-tetrahydro-2-methyl-3-methylene-1,4-dioxopyrazino[1,2-a]indole was dissolved in DMSO and diluted to a concentration of 2 mg / mL.

[0018] Take Candida albicans in the logarithmic growth phase and prepare them with physiological saline to a concentration of 10 6 CFU / mL bacterial solution; other fungi prepared to spore number of 10 6 spore suspension per mL, draw 1 mL of the prepared bacterial liquid or spore suspension into a petri dish, pour it into the PDA medium that has been cooled to a suitable temperature, mix well, and use sterile tweezers to pick up 1.5 mm thick, A filter paper piece with a diameter of 6 mm was placed on the bacteria-containing plate, and 5 μL of the extract was added dropwise on the filter paper as a sample group, DMSO was use...

Embodiment 2

[0023] The effect of compound 1,2,3,4-tetrahydro-2-methyl-3-methylene-1,4-dioxopyrazino[1,2-a]indole on Candida albicans, Trichoderma viride, Aspergillus niger, The minimum inhibitory concentration of Aspergillus.

[0024] Compound 1,2,3,4-tetrahydro-2-methyl-3-methylene-1,4-dioxopyrazino[1,2-a]indole or nystatin were diluted to 200, 100, 80, 60, 40, 20, 10 μg / mL. The absorption concentration is 10 6 CFU / mL of Candida albicans solution or 10 6 Put 1mL of other fungal spore suspensions / mL into the plate, pour into the PDA medium that has been cooled to an appropriate temperature, and mix well. Use sterile tweezers to pick up a filter paper sheet with a thickness of 1.5 mm and a diameter of 6 mm and place it on a plate containing bacteria, and at the same time add the above-mentioned concentration of compound 1,2,3,4-tetrahydro-2-methyl-3 to the filter paper sheet respectively -methylene-1,4-dioxopyrazino[1,2-a]indole or nystatin 5 μL, cultured in a 28°C incubator for 72 hou...

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Abstract

The invention discloses an application of an indolyl diketopiperazine compound in preparation of antifungal medicines. According to the application, the discovered compound, i.e., 1,2,3,4-tetrahydro-2-methyl-3-methylene-1,4-dioxopyrazino[1,2-a]indole has a very high inhibiting effect on Candida albicans, Trichoderma viride, Aspergillus niger and Aspergillus flavus, so that the compound, i.e., 1,2,3,4-tetrahydro-2-methyl-3-methylene-1,4-dioxopyrazino[1,2-a]indole has very good antifungal activity and has a good application development prospect. Therefore, the invention provides candidate drugs for researching and developing novel antifungal medicines and provides a scientific basis for developing and utilizing marine fungus derived natural active substances.

Description

technical field [0001] The invention belongs to the field of medical biotechnology, in particular to compound 1,2,3,4-tetrahydro-2-methyl-3-methylene-1,4-dioxopyrazino[1,2-a]indole in the preparation of antifungal drugs and as antifungal Application of active ingredients in fungal medicines. Background technique: [0002] Due to the massive development and application of terrestrial microbial active substances, it is becoming more and more difficult to find new species or special traits of microorganisms and new antibacterial and anti-tumor drugs produced by their metabolism. Therefore, people are turning their attention to microorganisms in the special marine environment . Marine fungi are an important part of marine microorganisms. These fungi not only have many types and are widely distributed, but also live in unique environments such as low temperature, high pressure, high salinity, high cold, and oligotrophic conditions. They will inevitably produce some different met...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4985A61P31/10
CPCA61K31/4985
Inventor 李浩华范震章卫民孙章华刘洪新叶伟
Owner GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY
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