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Antifungal pharmaceutical compositions and uses thereof

A technology of antifungal drugs and compositions, applied in the directions of antifungal agents, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of research reports, there is no antifungal effect of Candida albicans, etc., and achieve reversal of drug resistance the effect of enhancing antibacterial activity

Active Publication Date: 2018-09-04
SHANDONG RES INST OF TUMOUR PREVENTION TREATMENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The research of domestic and foreign researchers on Rubescensine A mainly focuses on its anti-tumor effect and mechanism research, so there is no antifungal effect of Rubescensine A and triazole drugs on drug-resistant Candida albicans at present. research report

Method used

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  • Antifungal pharmaceutical compositions and uses thereof
  • Antifungal pharmaceutical compositions and uses thereof
  • Antifungal pharmaceutical compositions and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Determination of static effect of Oridonin A combined with triazoles against Candida albicans

[0036] 1. Materials

[0037] 1.1 Experimental strains

[0038] Quality control standard strain: Candida albicans (C.albicans, CA) standard strain CA (obtained from the American Type Culture Collection with the accession number ATCC 10231).

[0039] Experimental strain: Candida albicans isolated clinically. The Candida albicans used in the experiment were all samples submitted by clinical patients in the Laboratory Department of Shandong Cancer Hospital. The obtained Candida albicans strains were numbered CA173, CA195, CA2489 and CA3208 respectively, and according to the results of the drug susceptibility test, CA173 and CA195 were Candida albicans resistant to triazoles, while CA2489 and CA3208 were triazole-resistant Candida albicans. Azole-sensitive Candida albicans.

[0040] 1.2 Drugs and reagents

[0041] Fluconazole (FLC), itraconazole (ITR) and voriconazo...

Embodiment 2

[0083] Example 2: Determination of the dynamic effect of Oridonin A and triazole drugs combined against Candida albicans

[0084] 1. Materials

[0085] 1.1 Strains

[0086] The strain used in the experiment was clinically isolated triazole-resistant Candida albicans CA173, which was identified and confirmed by CHROMagar yeast identification medium, and subcultured on solid medium.

[0087] 1.2 Drugs and reagents

[0088] The bulk drug of ORI, FLC, ITR and VOR; Dimethyl sulfoxide DMSO; PBS damping fluid; 0.1mol / L NaOH solution; RPMI 1640; 1 is the same.

[0089] 1.3 Instruments

[0090] MMM constant temperature incubator, high temperature and high pressure sterilizer, biological safety cabinet (all the same as the above-mentioned embodiment 1); constant temperature oscillator (Germany GFL company).

[0091] 2. Content and method

[0092] In this experiment, the drug single-use and drug-combination action systems were established, and the culture was shaken at 35°C for 48h...

Embodiment 3

[0105] Example 3: Study on the mechanism of action of Rubescensine A combined with triazoles against Candida albicans

[0106] 1. Materials and Instruments

[0107] Experimental strain: clinically isolated Candida albicans CA173, thawed from -20°C refrigerator, subcultured on YPD solid medium for at least 3 times and recovered before use.

[0108] Medium: The preparation method of YPD liquid medium is as follows: Weigh 4g of yeast extract, 8g of peptone and 8g of glucose respectively, add an appropriate amount of distilled water and stir to dissolve it as much as possible, then add distilled water to 400ml, and stir well. Finally, autoclave at 121°C for 20 minutes, cool and store in a refrigerator at 4°C. YPD solid medium is a medium for daily inoculation culture, and its preparation method is the same as above.

[0109] Drug solution: Oridonin A mother solution was diluted to 32 μg / ml with RPMI 1640 medium (same as in Example 1 above), and set aside.

[0110] Reagents and ...

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Abstract

The invention provides application of oridonin and triazole compounds in preparation of antifungal medicines and an antifungal pharmaceutical composition containing the oridonin and the triazole compounds. Through combining triazole compounds serving as medicines such as fluconazole, itraconazole and / or voriconazole with oridonin, the antifungal pharmaceutical composition has a strong synergistic antifungal effect on fungi with resistance to existing triazole medicines, such as drug-resistant Candida albicans (C. albicans), and is capable of reversing the drug resistance of the drug-resistant C. albicans to the triazole medicines.

Description

technical field [0001] The present invention relates to antifungal pharmaceutical compositions and uses thereof, more specifically to the use of oridonin in combination with triazole compounds in the preparation of antifungal drugs and antifungal drugs comprising oridonin and triazole compounds combination. Background technique [0002] With the increasing number of cancer and AIDS patients, the general development of organ transplantation, catheter intubation and endoscopic technology, the wide use of high-efficiency broad-spectrum antibiotics, immunosuppressants and hormones, the incidence of deep fungal infections is increasing year by year, among which white Candida is the main pathogen causing clinical fungal infection. However, in recent years, the drug resistance of Candida albicans (C.albicans) has been increasing, and the mortality rate caused by deep infection of Candida albicans is high, which brings challenges to the successful clinical treatment of infections c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4196A61K31/496A61K31/506A61K31/352A61P31/10
CPCA61K31/352A61K31/4196A61K31/496A61K31/506A61K2300/00
Inventor 史文娜刘玉国李辉陈海生
Owner SHANDONG RES INST OF TUMOUR PREVENTION TREATMENT