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使用恶性疟原虫乳酸脱氢酶测定法对长叶刺蒺藜进行抗疟研究。

Antiplasmodial studies of Eurycoma longifolia Jack using the lactate dehydrogenase assay of Plasmodium falciparum.

作者信息

Chan Kit-Lam, Choo Chee-Yan, Abdullah Noor Rain, Ismail Zakiah

机构信息

School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang 11800, Malaysia.

出版信息

J Ethnopharmacol. 2004 Jun;92(2-3):223-7. doi: 10.1016/j.jep.2004.02.025.

Abstract

The roots of Eurycoma longifolia Jack have been used as traditional medicine to treat malaria. A systematic bioactivity-guided fractionation of this plant was conducted involving the determination of the effect of its various extracts and their chemical constituents on the lactate dehydrogenase activity of in vitro chloroquine-resistant Gombak A isolate and chloroquine-sensitive D10 strain of Plasmodium falciparum parasites. Their antiplasmodial activity was also compared with their known in vitro cytotoxicity against KB cells. Four quassinoids, eurycomanone (1), 13,21-dihydroeurycomanone (3), 13 alpha(21)-epoxyeurycomanone (4), eurycomalactone (6) and an alkaloid, 9-methoxycanthin-6-one (7), displayed higher antiplasmodial activity against Gombak A isolate but were less active against the D10 strain when compared with chloroquine. Amongst the compounds tested, 1 and 3 showed higher selectivity indices obtained for the cytotoxicity to antiplasmodial activity ratio than 14,15 beta-dihydroxyklaineanone (2), eurycomanol (5), 6 and 7.

摘要

长叶刺蒺藜草的根已被用作治疗疟疾的传统药物。对该植物进行了系统的生物活性导向分离,包括测定其各种提取物及其化学成分对体外氯喹抗性贡巴克A分离株和氯喹敏感D10株恶性疟原虫寄生虫乳酸脱氢酶活性的影响。还将它们的抗疟活性与其已知的对KB细胞的体外细胞毒性进行了比较。四种苦木素,刺蒺藜酮(1)、13,21-二氢刺蒺藜酮(3)、13α(21)-环氧刺蒺藜酮(4)、刺蒺藜内酯(6)和一种生物碱,9-甲氧基-6-酮基咔啉(7),对贡巴克A分离株显示出较高的抗疟活性,但与氯喹相比,对D10株的活性较低。在所测试的化合物中,1和3的细胞毒性与抗疟活性比值的选择性指数高于14,15β-二羟基克莱尼酮(2)、刺蒺藜醇(5)、6和7。

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