Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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Antimalarial Activity of Cassane- and Norcassane-Type Diterpenes from Caesalpinia crista and Their Structure–Activity Relationship
Surya Kant KalauniSuresh AwaleYasuhiro TezukaArjun Hari BanskotaThein Zaw LinnPuji Budi Setia AsihDin SyafruddinShigetoshi Kadota
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2006 Volume 29 Issue 5 Pages 1050-1052

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Abstract

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 μM, more potent than the clinically used drug chloroquine (IC50, 0.29 μM). Based on the observed results, a structure–activity relationship has been established.

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© 2006 The Pharmaceutical Society of Japan
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