Antimalarial activity of cassane- and norcassane-type diterpenes from Caesalpinia crista and their structure-activity relationship.

Abstract

Malaria is one of the most life-threatening infectious diseases worldwide and claims millions of people's lives 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 microM, more potent than the clinically used drug chloroquine (IC50, 0.29 microM). Based on the observed results, a structure-activity relationship has been established.

• Authors: Surya Kant Kalauni, Suresh Awale, Yasuhiro Tezuka, Arjun Hari Banskota, Thein Zaw Linn, Puji Budi Setia Asih, Din Syafruddin, Shigetoshi Kadota
• Journal: Biological & pharmaceutical bulletin (Biol Pharm Bull) Vol. 29 Issue 5 Pg. 1050-2 (May 2006) ISSN: 0918-6158 [Print] Japan
• PMID: 16651745 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antimalarials
• Diterpenes
• Chloroquine

Topics

• Animals
• Antimalarials (pharmacology)
• Caesalpinia (chemistry)
• Chloroquine (pharmacology)
• Diterpenes (chemistry, pharmacology)
• Erythrocytes (parasitology)
• Humans
• In Vitro Techniques
• Indonesia
• Myanmar
• Plasmodium falciparum (drug effects)
• Structure-Activity Relationship