文章基本信息

标题：Antimalarial Activity of Cassane- and Norcassane-Type Diterpenes from Caesalpinia crista and Their Structure–Activity Relationship
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作者：Surya Kant Kalauni ; Suresh Awale ; Yasuhiro Tezuka 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2006
卷号：29
期号：5
页码：1050-1052
DOI：10.1248/bpb.29.1050
出版社：The Pharmaceutical Society of Japan
摘要：Malaria is one of the most life-threatening infectious diseases worldwide and claims the millions of peoples life each year. The appearance of drug-resistance Plasmodium falciparum has made the treatment of malaria increasingly problematic, and thus, it is a dire need to search the new alternatives of current drugs. In the present study, 44 cassane- and norcassane-type diterpenes isolated from Caesalpinia crista of Myanmar and Indonesia were evaluated for their antimalarial activity against the malaria parasite Plasmodium falciparum FCR-3/A2 clone in vitro . Most of the tested diterpenes displayed antimalarial activity, and norcaesalpinin E (28) showed the most potent activity with an IC₅₀ value of 0.090 μ M , more potent than the clinically used drug chloroquine (IC₅₀, 0.29 μ M ). Based on the observed results, a structure–activity relationship has been established.
关键词：cassane-type diterpene;antimalarial activity;structure–activity relationship;norcassane-type diterpene;Caesalpinia crista