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体外和体内抗疟活性及吉尔氏三蕊苣苔叶、根皮和茎皮提取物和馏分的细胞毒性。

In vitro and in vivo antimalarial activity and cytotoxicity of extracts and fractions from the leaves, root-bark and stem-bark of Triclisia gilletii.

机构信息

Faculty of Pharmaceutical Sciences, University of Kinshasa, Kinshasa XI, Democratic Republic of Congo.

出版信息

J Ethnopharmacol. 2013 Sep 16;149(2):438-42. doi: 10.1016/j.jep.2013.06.043. Epub 2013 Jul 19.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

To evaluate the in vitro antiplasmodial activity and cytotoxicity, and the in vivo activity of extracts and fractions from the leaves, root-bark and stem-bark of Triclisia gilletii (De Wild) Staner (Menispermaceae), used in traditional medicine against malaria.

MATERIALS AND METHODS

The aqueous and 80% MeOH extracts, and a series of fractions and subfractions from the leaves, stem and root-bark of Triclisia gilletii were tested in vitro for their antiplasmodial activity against a Congolese-sensitive strain of Plasmodium falciparum, against the chloroquine and pyrimethamine-resistant K1 strain of Plasmodium falciparum, for cytotoxicity against MRC-5 cells, and in vivo in mice infected with Plasmodium berghei berghei.

RESULTS

Many samples from the three plant parts exhibited pronounced activity against the Congolese chloroquine-sensitive strain of Plasmodium falciparum with some IC50 values <0.02 µg/ml, and against the K1 strain, with some IC50 <0.25; the selectivity was higher against the Congolese strain. At oral doses of 200 and 400mg/kg body weight in infected mice, the aqueous, 80% methanol and total alkaloid extracts from the three plant parts produced more than 65% and 75% chemosuppression, respectively. The antiplasmodial activity of these three plant parts of Triclisia gilletii can at least in part be attributed to bisbenzylisoquinoline alkaloids, and supports its use for the treatment of uncomplicated malaria in traditional medicine.

摘要

民族药理学相关性

评估三齿拉雷亚(Menispermaceae)叶、根皮和茎皮提取物和馏分的体外抗疟活性和细胞毒性,以及体内活性,用于传统医学治疗疟疾。

材料和方法

用刚果敏感株恶性疟原虫、氯喹和乙胺嘧啶耐药株恶性疟原虫 K1 株对三齿拉雷亚叶、茎和根皮的水提物和 80%甲醇提取物以及一系列馏分和亚馏分进行了体外抗疟活性测试,对 MRC-5 细胞的细胞毒性,以及在感染疟原虫伯氏疟原虫的小鼠体内进行了测试。

结果

三个植物部分的许多样品对刚果氯喹敏感株恶性疟原虫表现出明显的活性,一些 IC50 值<0.02μg/ml,对 K1 株的活性,一些 IC50<0.25;对刚果株的选择性更高。在感染小鼠中以 200 和 400mg/kg 体重的口服剂量,三种植物部分的水提物、80%甲醇提取物和总生物碱提取物分别产生了超过 65%和 75%的化学抑制作用。三齿拉雷亚这三个植物部分的抗疟活性至少部分归因于双苄基异喹啉生物碱,支持其在传统医学中用于治疗单纯性疟疾。

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