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从不丹药用植物 Aconitum orochryseum 中提取的氯化阿替辛具有抗疟原虫活性。

Antiplasmodial activity of atisinium chloride from the Bhutanese medicinal plant, Aconitum orochryseum.

机构信息

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

出版信息

J Ethnopharmacol. 2010 Aug 9;130(3):559-62. doi: 10.1016/j.jep.2010.05.057. Epub 2010 Jun 2.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

The plant Aconitum orochryseum Stapf. (Ranunculaceae) is employed together with other plants in Bhutanese traditional medicine and is indicated for malaria-associated fever.

AIM OF THE STUDY

To study the in vitro antiplasmodial activity of atisinium chloride, the major alkaloid from Aconitum orochryseum.

MATERIALS AND METHODS

Atisinium chloride was extracted and purified from aerial parts of Aconitum orochryseum and its structure and absolute configuration confirmed by single crystal X-ray crystallography. The crude methanol extract, crude alkaloid fraction, and atisinium chloride were tested for in vitro antiplasmodial activity against the malarial Plasmodium falciparum strains TM4/8.2 (TM4; wild type) and K1CB1 (K1; chloroquine and antifolate resistant).

RESULTS

The diterpenoid alkaloid atisinium chloride was shown to have moderate antiplasmodial activities with IC(50) values of 4 microM and 3.6 microM, respectively against the TM4 strain and the K1 strain of Plasmodium falciparum.

CONCLUSIONS

Our studies provide the first evidence in support of one of the indicated treatments with Aconitum orochryseum in Bhutanese traditional medicine. This alkaloid also represents a potential new antimalarial structural lead.

摘要

民族药理学相关性

植物乌头(毛茛科)与其他植物一起被用于不丹传统医学中,用于治疗疟疾相关的发热。

研究目的

研究从乌头中提取的主要生物碱阿托辛的体外抗疟原虫活性。

材料和方法

从乌头的地上部分提取和纯化阿托辛,并通过单晶 X 射线晶体学确定其结构和绝对构型。对粗甲醇提取物、粗生物碱部分和阿托辛进行体外抗疟原虫活性测试,针对疟原虫恶性疟原虫株 TM4/8.2(TM4;野生型)和 K1CB1(K1;氯喹和抗叶酸耐药)。

结果

二萜生物碱阿托辛表现出中等的抗疟原虫活性,对 TM4 株和 K1 株恶性疟原虫的 IC50 值分别为 4 μM 和 3.6 μM。

结论

我们的研究首次为不丹传统医学中乌头的一种指示性治疗提供了证据。这种生物碱也代表了一种有潜力的新抗疟药物结构先导化合物。

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