Quassinoids Exhibit Greater Selectivity Against Plasmodium Falciparum Than Against Entamoeba Histolytica, Giardia Intestinalis Or Toxoplasma Gondii In Vitro
Quassinoids Exhibit Greater Selectivity Against Plasmodium Falciparum Than Against Entamoeba Histolytica, Giardia Intestinalis Or Toxoplasma Gondii In Vitro
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在体外，Quassinoids 对恶性疟原虫的选择性高于对溶组织内阿米巴、肠贾第虫或弓形虫的选择性
DOI：
10.1111/j.1550-7408.1993.tb04910.x
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发表时间：
1993
影响因子：
2.2
通讯作者：
Hernan R. Chang
中科院分区：
文献类型：
--
作者：
C. Wright;Margaret L. M. Anderson;David Allen;J. Phillipson;G. C. Kirby;D. Warhurst;Hernan R. Chang
摘要。比较了一系列拟瓜素对恶性疟原虫、溶组织内阿米巴、肠贾第虫和刚地弓形虫的体外抑菌活性及其对人鼻咽部表皮样癌细胞的体外细胞毒作用。所有化合物对KB细胞的毒性均大于对肠芽孢杆菌的毒性，但4种化合物（臭椿苷酮、马钱子碱D、brusatol和青红素）对KB细胞的毒性略低于对溶组织芽孢杆菌的毒性。青红素酮对胞内弓形虫的毒性同样大于对KB细胞的毒性，但臭椿素酮的选择性更强（对弓形虫的毒性是KB细胞的36倍）。所有化合物对恶性疟原虫的毒性均大于对KB细胞的毒性；结果表明，最具选择性的拟assinoone （glaucarubinone）、bruceine D、ailanthinone和brusatoi)的毒效比分别为285、76、48和32。这些结果表明，拟西番莲对恶性疟原虫具有选择性作用。进一步的研究正在阐明其基础。
ABSTRACT. The in vitro activities of a series of quassinoids against Plasmodium falciparum, Entamoeba histolytica, Giardia intestinalis and Toxoplasma gondii have been compared with their in vitro cytotoxic effects against KB cells (human epidermoid carcinoma of the nasopharynx). All of the compounds tested were more toxic to KB cells than to G. intestinalis, but four (ailanthinone, bruceine D, brusatol and glaucarubinone) were slightly less toxic to KB cells than to E. histolytica. Glaucarubinone was similarly more toxic to intracellular T. gondii than to KB cells but ailanthinone was more selective (36 times more toxic to T. gondii than to KB cells). All of the compounds were more toxic to P. falciparum than to KB cells; the most selective quassinoids—glaucarubinone, bruceine D, ailanthinone and brusatoi—were found to have toxicity/activity ratios of 285, 76, 48 and 32 respectively. These results suggest that quassinoids have a selective action on P. falciparum. Further studies to elucidate the basis for this are in progress.