Application of Friedolanostanes in preparation of antihuman fungal medicines

An antifungal and drug technology, applied in antifungal agents, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of irritation, dizziness, allergy, strong accumulation of toxicity, etc. active effect

Inactive Publication Date: 2017-03-15
ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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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 the antibacterial agents currently used clinically have good curative effect on skin and superficial infection, but these antibacterial agents have strong cumulative toxicity and often cause liver and kidney damage, digestive tract irritation, dizziness, allergies, etc. New antibacterial drugs with unique mechanisms have become one of the hot spots in drug research and development today

Method used

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  • Application of Friedolanostanes in preparation of antihuman fungal medicines
  • Application of Friedolanostanes in preparation of antihuman fungal medicines
  • Application of Friedolanostanes in preparation of antihuman fungal medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Embodiment 1: the preparation of compound Friedolanostanes tablet involved in the present invention:

[0011] Take 5 grams of compound Friedolanostanes, add 195 grams of dextrin, mix well, and make 1000 tablets by conventional compression.

Embodiment 2

[0012] Embodiment 2: the preparation of compound Friedolanostanes capsules involved in the present invention:

[0013] Get 5 grams of compound Friedolanostanes, add 195 grams of starch, mix well, and pack into capsules to make 1000 capsules.

[0014] The following pharmacodynamic experiments will further illustrate its drug activity.

experiment example 1

[0015] Experimental Example 1: Antifungal activity of Friedolanostanes in humans

[0016] The anti-fungal activity experiment against human body adopts the method of concentration dilution, and each determination is repeated three times. The test pathogens include Trichomonas rubrum, Microsporum lanoides and Trichomonas clumps, and the concentration of bacteria solution is 105 / mL. The initial concentration of Friedolanostanes was 50.0 μg / mL (5% dimethyl sulfoxide DMSO), and it was serially diluted to 0.098 μg / mL. The equal volume of bacteria liquid and test samples were mixed and cultured in a 96-well plate, and the culture temperature of human fungi was respectively 28°C, observe after 24 hours of incubation time, if no colonies are 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 anti-fungal results of Friedolanostanes are shown in Table 1.

[0017] Table 1 Friedol...

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PUM

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Abstract

The invention relates to an application of Friedolanostanes in the preparation of antihuman fungal medicines, and belongs to the field of medicines. The Friedolanostanes have a very strong inhibition effect on Trichophyton rubrum, Microsporum lanosum or Trichophyton tonsurans, so the Friedolanostanes can be used as an antihuman fungal compound, and are hopeful to be applied to preparation of relevant medicines for the first time. The skeleton type of the Friedolanostanes is a brand new skeleton type, and the Friedolanostanes have high human fungus inhibition activity, have protruding practical characteristics, and have substantial progress in prevention and treatment of human fungus infection.

Description

technical field [0001] The present invention relates to the novel application of compound Friedolanostanes, in particular to the application of Friedolanostanes 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 the antibacterial agents currently used clinically have good curative effect on skin and superficial infection, but these antibacterial agents have strong cumulative toxicity and often cause liver and kidney damage, digestive tract irritation, dizziness, allergies, etc. New antibacterial drugs with unique mechanisms have become one of the hot spots in drug development today. [0003] The compound Friedolanostanes involved in t...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P31/10
CPCA61K31/56
Inventor 田丽华
Owner ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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