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来自不丹传统药用植物紫堇的抗疟生物碱。

Antimalarial alkaloids from a Bhutanese traditional medicinal plant Corydalis dubia.

机构信息

School of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia.

出版信息

J Ethnopharmacol. 2012 Aug 30;143(1):310-3. doi: 10.1016/j.jep.2012.06.037. Epub 2012 Jul 14.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Corydalis dubia is used in Bhutanese traditional medicine as a febrifuge and for treating infections in the blood, liver and bile which correlate to the signs and symptoms of malarial and microbial infections.

AIM OF THE STUDY

To validate the ethnopharmacological uses of the plant and to discover potential new therapeutic drug leads.

MATERIALS AND METHODS

C. dubia was collected from Bhutan and the alkaloids were obtained using acid-base fractionation and separation by repeated column and preparative plate chromatography. The alkaloids were identified from analysis of their physiochemical and spectroscopic data and were tested for antiplasmodial, antimicrobial and cytotoxicity activities.

RESULTS

A systematic extraction and isolation protocol yielded one new natural product, dubiamine, and seven known isoquinoline alkaloids, scoulerine, cheilanthifoline, protopine, capnoidine, bicuculline, corydecumbine and hydrastine. Among the four alkaloids tested, scoulerine showed the best antiplasmodial activity with IC(50) values of 5.4μM and 3.1μM against the antifolate sensitive and the multidrug resistant P. falciparum strains: TM4/8.2 and K1CB1, respectively. None of the alkaloids tested showed significant antimicrobial or cytotoxicity activities.

CONCLUSIONS

The antiplasmodial test results, of the isolated alkaloid components, are commensurated with the ethnopharmacological uses of this plant.

摘要

民族药理学相关性

在不丹传统医学中,紫堇属植物被用作退烧药,并用于治疗血液、肝脏和胆汁中的感染,这与疟疾和微生物感染的症状相对应。

研究目的

验证该植物的民族药理学用途,并发现潜在的新治疗药物。

材料和方法

从不丹采集紫堇属植物,通过酸碱分步提取和反复柱层析及制备薄板层析分离得到生物碱。根据其理化和光谱数据分析鉴定生物碱,并测试其抗疟原虫、抗菌和细胞毒性活性。

结果

系统的提取和分离方法得到了一种新的天然产物,即 dubiamine,以及七种已知的异喹啉生物碱,即石杉碱、 cheilanthifoline、普罗托品、 capnoidine、bicuculline、 corydecumbine 和 hydrastine。在所测试的四种生物碱中,石杉碱对叶酸敏感和多药耐药性 P. falciparum 株 TM4/8.2 和 K1CB1 的 IC50 值分别为 5.4μM 和 3.1μM,显示出最好的抗疟原虫活性。

结论

分离的生物碱成分的抗疟原虫试验结果与该植物的民族药理学用途相符。

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