TY - JOUR
T1 - Antimalarial activity of cassane- and norcassane-type diterpenes from Caesalpinia crista and their structure-activity relationship
AU - Kalauni, Surya Kant
AU - Awale, Suresh
AU - Tezuka, Yasuhiro
AU - Banskota, Arjun Hari
AU - Linn, Thein Zaw
AU - Asih, Puji Budi Setia
AU - Syafruddin, Din
AU - Kadota, Shigetoshi
PY - 2006/5
Y1 - 2006/5
N2 - 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.
AB - 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.
KW - Antimalarial activity
KW - Caesalpinia crista
KW - Cassane-type diterpene
KW - Norcassane-type diterpene
KW - Structure-activity relationship
UR - http://www.scopus.com/inward/record.url?scp=33646461692&partnerID=8YFLogxK
U2 - 10.1248/bpb.29.1050
DO - 10.1248/bpb.29.1050
M3 - 学術論文
C2 - 16651745
AN - SCOPUS:33646461692
SN - 0918-6158
VL - 29
SP - 1050
EP - 1052
JO - Biological and Pharmaceutical Bulletin
JF - Biological and Pharmaceutical Bulletin
IS - 5
ER -
