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Indole alkaloid or pharmaceutically acceptable salt thereof, preparation method and applications thereof, and indole alkaloid pharmaceutical composition and applications thereof

A technology for indole alkaloids and compositions is applied in the field of indole alkaloids or their pharmaceutically acceptable salts and their preparation, and in the field of indole alkaloid pharmaceutical compositions, which can solve the problem of increased drug resistance of Candida albicans, patients and Heavy economic burden on society and other problems, to achieve the effect of strong drug resistance reversal activity, low cost, and wide source of raw materials

Active Publication Date: 2019-11-12
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Fluconazole, as the first-line antimicrobial drug currently used to treat deep fungus, has achieved good clinical therapeutic effects, but in recent years, with the wide application of fluconazole, the drug resistance of Candida albicans is increasing year by year, causing patients and a heavy economic burden on society

Method used

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  • Indole alkaloid or pharmaceutically acceptable salt thereof, preparation method and applications thereof, and indole alkaloid pharmaceutical composition and applications thereof
  • Indole alkaloid or pharmaceutically acceptable salt thereof, preparation method and applications thereof, and indole alkaloid pharmaceutical composition and applications thereof
  • Indole alkaloid or pharmaceutically acceptable salt thereof, preparation method and applications thereof, and indole alkaloid pharmaceutical composition and applications thereof

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preparation example Construction

[0039] The present invention provides the preparation method of indole alkaloid described in above-mentioned technical scheme, comprises the following steps:

[0040] mixing the dog's tooth flower and the extractant, extracting and concentrating to obtain the extract;

[0041] Adjusting the pH value to acidity, the first extraction, adjusting the pH value to alkalinity, the second extraction, silica gel column chromatography, reverse-phase chromatography separation and Sephadex LH-20 separation are carried out sequentially on the extract to obtain indole alkaloids;

[0042] The silica gel column chromatography adopts a gradient elution method, and the eluent used is a mixed solution of petroleum ether and acetone, and the volume ratio of the petroleum ether and acetone is 10:1 to 1:1;

[0043] The eluent used in the reverse-phase chromatographic separation is methanol and water, and the volume ratio of methanol and water is 30:70 to 70:30;

[0044] The solvent used for the Se...

Embodiment 1

[0068] 10kg of dried branches and leaves of Bermudagrass were heated to 68°C with 50L of methanol and refluxed for extraction 3 times, each time for 3 hours, the extracts were combined, and the methanol was recovered by distillation under reduced pressure to obtain the extract;

[0069] Mix the extract with 2000mL of 5% hydrochloric acid aqueous solution, and adjust the pH value to 2, respectively extract 3 times with 2000mL petroleum ether and 2000mL ethyl acetate, then adjust the pH value to 9 with saturated sodium carbonate solution, and use chloroform Extract to obtain the total base (70g); the total base is subjected to silica gel column chromatography, petroleum ether-acetone gradient elution (petroleum ether / acetone=30:1~10:1, v / v), and then reverse phase Chromatography C-18 separation (methanol / water=30:70~80:20, v / v) and Sephadex LH-20 (methanol) separation, obtain the indole alkaloid (0.04g, yield 0.0004%, purity 98%, colorless oil).

[0070] Structural characteriza...

Embodiment 2

[0082] Mix the indole alkaloid prepared in Example 1 and water for injection evenly, perform fine filtration, potting and sterilization in sequence to obtain the indole alkaloid injection.

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Abstract

The invention provides an indole alkaloid or a pharmaceutically acceptable salt thereof, a preparation method and applications thereof, and an indole alkaloid pharmaceutical composition and applications thereof, and belongs to the technical field of medicine. According to the present invention, the indole alkaloid or the pharmaceutically acceptable salt thereof does not have obvious inhibitory activity on Candida albicans fluconazole-resistant strains, and has a Candida albicans fluconazole-resistant strain inhibition rate of more than 99.2% when fluconazole and indole alkaloid co-act on Candida albicans fluconazole-resistant strains, such that the results show that the indole alkaloid can strongly inverse the drug-resistance of Candida albicans fluconazole-resistant strains, and is a potential candidate drug capable of inversing the drug resistance of Candida albicans fluconazole-resistant strains.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to an indole alkaloid or a pharmaceutically acceptable salt thereof, a preparation method and application thereof, an indole alkaloid pharmaceutical composition and an application thereof. Background technique [0002] Candida albicans is the main pathogenic fungus of nosocomial infection. With the widespread use of antifungal drugs, the cases of deep fungi caused by Candida albicans infection are increasing year by year. Fluconazole, as the first-line antimicrobial drug currently used to treat deep fungus, has achieved good clinical therapeutic effects, but in recent years, with the wide application of fluconazole, the drug resistance of Candida albicans is increasing year by year, causing patients and a heavy economic burden on society. In view of the complexity of the fluconazole resistance mechanism of Candida albicans and the seriousness of drug resistance forms, it is urgen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D498/22A61K31/55A61P31/10
CPCA61P31/10C07D498/22
Inventor 张于郝小江郭伶俐白雪
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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