Antimalarial Activity of Cassane- and Norcassane-Type Diterpenes from Caesalpinia crista and Their Structure–Activity Relationship

Surya Kant Kalauni; Suresh Awale; Yasuhiro Tezuka; Arjun Hari Banskota; Thein Zaw Linn; Puji Budi Setia Asih; Din Syafruddin; Shigetoshi Kadota

doi:10.1248/bpb.29.1050

Notes

Antimalarial Activity of Cassane- and Norcassane-Type Diterpenes from Caesalpinia crista and Their Structure–Activity Relationship

Surya Kant Kalauni, Suresh Awale, Yasuhiro Tezuka, Arjun Hari Banskota, Thein Zaw Linn, Puji Budi Setia Asih, Din Syafruddin, Shigetoshi Kadota

Author information

Keywords: cassane-type diterpene, antimalarial activity, structure–activity relationship, norcassane-type diterpene, Caesalpinia crista

JOURNAL FREE ACCESS

2006 Volume 29 Issue 5 Pages 1050-1052

DOI https://doi.org/10.1248/bpb.29.1050

Details

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.

Corresponding author

Register with J-STAGE for free!