期刊
BIOLOGICAL & PHARMACEUTICAL BULLETIN
卷 29, 期 5, 页码 1050-1052出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.29.1050
关键词
cassane-type diterpene; antimalarial activity; structure-activity relationship; norcassane-type diterpene; Caesalpinia crista
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 mu m, more potent than the clinically used drug chloroquine (IC50, 0.29 mu m). Based on the observed results, a structure-activity relationship has been established.
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