Application of Chukrasone B in preparation of medicines for resisting human body fungi

A technology against human fungi and drugs, applied in the directions of antifungal agents, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of digestive tract irritation, strong accumulation of toxicity, etc. active effect

Active Publication Date: 2013-10-30
煌途医药(无锡)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The spread of pathogenic bacteria and the enhancement of drug resistance seriously threaten human health and life. Antibacterial drugs have been widely used as routine drugs in the treatment of AIDS, organ transplantation and chronic wasting diseases (such as cancer, diabetes, uremia, etc.) Treatment, although antibacterial agents currently used clinically (such as ketoconazole, amikacin, gentamicin, vigorconazole, itraconazole, terbinafine, amphotericin, fluconazole, etc.) The curative effect on skin and superficial infection is good, but these antibacterial drugs have strong cumulative toxicity, often causing liver and kidney damage, gastrointestinal irritation, dizziness, allergies, etc. one of the hotspots

Method used

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  • Application of Chukrasone B in preparation of medicines for resisting human body fungi
  • Application of Chukrasone B in preparation of medicines for resisting human body fungi
  • Application of Chukrasone B in preparation of medicines for resisting human body fungi

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Embodiment 1: the preparation of the compound Chukrasone B tablet involved in the present invention:

[0014] Take 20 grams of compound Chukrasone B, add 180 grams of conventional excipients for tablet preparation, mix well, and make 1000 tablets with a conventional tablet press.

Embodiment 2

[0015] Embodiment 2: the preparation of the compound Chukrasone B capsules involved in the present invention:

[0016] Get 20 grams of compound Chukrasone B, add conventional auxiliary materials for preparing capsules such as 180 grams of starch, mix well, and pack into capsules to make 1000 tablets.

[0017] The following pharmacodynamic experiments will further illustrate its drug activity.

experiment example

[0018] Experimental example: Chukrasone B anti-fungal activity in humans

[0019] Anti-human fungus activity experiment is the method of concentration dilution, each determination is repeated three times, the test pathogens are Trichophyton rubrum, Microsporum lanoides and Trichophyton aureus, and the concentration of bacteria solution is 10 5 individual / mL. The initial concentration of Chukrasone B is 50.0 μg / mL (5% dimethyl sulfoxide DMSO), serially diluted to 0.098 μg / mL, the same volume of bacteria liquid and test samples are mixed and cultured in a 96-well plate, and the human fungal culture temperature 28 ℃ respectively, observe after 24 hours of incubation time, if no colony is found, it is the lowest anti-human fungal concentration of the sample, that is, the MIC value. The positive control of this experiment is ketoconazole, and the results of Chukrasone B against human fungi are shown in Table 1.

[0020] Table 1 Chukrasone B anti-human fungal MIC value (μg / mL)

...

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PUM

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Abstract

The invention relates to an application of Chukrasone B in the preparation of medicines for resisting human body fungi, and belongs to the field of medicines. The Chukrasone B has a very strong inhibition effect on trichophyton rubrum, microsporum lanosum or trichophyton tonsurans, therefore, the Chukrasone B can serve as a compound capable of resisting human body fungi and is expected to be applied in the preparation of related medicines. The application of the Chukrasone B in the preparation of the medicines for resisting the human body fungi is disclosed by the invention for the first time. As the skeleton type of the Chukrasone B belongs to a bran-new skeleton type and the Chukrasone B has unexpected strong inhibitory activity on human body fungi, the possibility that other compounds provide revelation does not exist. The Chukrasone B has prominently substantial characteristics and meanwhile has remarkably progressive significance when being used for preventing and treating the human body fungi infection.

Description

technical field [0001] The present invention relates to the application of Chukrasone B, in particular to the application of Chukrasone B in the preparation of antifungal drugs for human body. Background technique [0002] The spread of pathogenic bacteria and the enhancement of drug resistance seriously threaten human health and life. Antibacterial drugs have been widely used as routine drugs in the treatment of AIDS, organ transplantation and chronic wasting diseases (such as cancer, diabetes, uremia, etc.) Treatment, although antibacterial agents currently used clinically (such as ketoconazole, amikacin, gentamicin, vigorconazole, itraconazole, terbinafine, amphotericin, fluconazole, etc.) The curative effect on skin and superficial infection is good, but these antibacterial drugs have strong accumulation toxicity, often causing liver and kidney damage, gastrointestinal irritation, dizziness, allergies, etc. one of the hotspots. [0003] The compound Chukrasone B involv...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P31/10
Inventor 丁圣雨
Owner 煌途医药(无锡)有限公司
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