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Application of Scopariusins ??in preparation of antihuman fungal medicines

A technology against human fungi and drugs, applied in the direction of antifungal agents, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve problems such as allergies, strong accumulation of toxicity, irritation, etc., and achieve strong inhibitory activity and prominent substantive features Effect

Inactive Publication Date: 2014-01-01
SUZHOU CHENCAI TEXTILE RES & DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] 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, gastrointestinal irritation, dizziness, allergies, etc., so looking for unique mechanism of action New antibacterial drugs have become one of the hot spots in drug development today

Method used

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  • Application of Scopariusins ??in preparation of antihuman fungal medicines
  • Application of Scopariusins ??in preparation of antihuman fungal medicines
  • Application of Scopariusins ??in preparation of antihuman fungal medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Embodiment 1: the preparation of the compound Scopariusins ​​tablet involved in the present invention:

[0012] Take 5 grams of the compound Scopariusins, add 195 grams of dextrin, mix well, and make 1000 tablets by conventional compression.

Embodiment 2

[0013] Embodiment 2: the preparation of compound Scopariusins ​​capsules involved in the present invention:

[0014] Take 5 grams of the compound Scopariusins, add 195 grams of starch, mix well, and pack into capsules to make 1000 capsules.

[0015] The following pharmacodynamic experiments will further illustrate its drug activity.

experiment example 1

[0016] Experimental Example 1: Anti-human fungal activity of Scopariusins: The anti-human fungal activity experiment uses the method of concentration dilution, and each measurement is repeated three times. The test pathogens include Trichomonas rubrum, Microsporum lanoides and Phytophthora aureus. The concentration of the bacterial solution 105 / mL. The initial concentration of Scopariusins ​​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 results of Scopariusins ​​against human fungi are shown in Table 1.

[0017] Table 1 Scopariusins ​​anti-human fungal MIC...

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PUM

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Abstract

The invention relates to an application of Scopariusins in the preparation of antihuman fungal medicines, and belongs to the medicinal field. Scopariusins has a very strong Trichophyton rubrum, Microsporum lanosum or Trichophyton tonsurans inhibition effect, so the Scopariusins can be used as an antihuman fungal compound, and is expected to be applied in the preparation of related medicines. The skeleton type of the Scopariusins is a brand new skeleton type, and the Scopariusins has a strong human fungus inhibition activity, has prominent substantive characteristics, and is a substantial improvement in the prevention and treatment of human fungal infection.

Description

technical field [0001] The invention relates to a new application of the compound Scopariusins, in particular to the application of the Scopariusins ​​in the preparation of antifungal drugs for human body. Background technique [0002] 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, gastrointestinal irritation, dizziness, allergies, etc., so looking for unique mechanism of action New antibacterial drugs have become one of the hot spots in drug development today. [0003] The compound Scopariusins ​​involved in the present invention is published in 2013 (Min Zhou, et al., Scopariusins, A New Class of ent-Halimane Diterpenoids Isolated from Isodon scoparius, and Biomimetic Synthesis of Scopariusin A and Isoscoparin N.Organic Letters, 2013, 15 (2): 314–317.), this compound has a new type of skeleton, and the stu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/215A61P31/10
Inventor 高伟
Owner SUZHOU CHENCAI TEXTILE RES & DEV
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