Antimalarial activity and nucleoside transport inhibitory activity of the triterpenic constituents of Cimicifuga spp.
The in vitro antimalarial activity against human malaria parasite (Plasmodium falciparum, FCR-3 strain) was examined using 59 triterpenoids obtained during studies on the triterpenic constituents of Cimicifuga spp. The 50% effective concentration values (EC50) of 25 active triterpenoids were 1.0-3.0 microM, and 19 of the compounds had a common 16, 23:23, 26:24, 25-triepoxy group in the side-chain moieties. Among the active triterpenoids, 9 also showed significant inhibition of nucleoside transport in mouse splenocytes. A relationship between the antimalarial activity and the inhibition of nucleoside transport involving these triterpenoids is discussed.
Takahira
M
M
Osaka University of Pharmaceutical Sciences, Takatsuki, Japan.
Kusano
A
A
Shibano
M
M
Kusano
G
G
Koizumi
K
K
Suzuki
R
R
Kim
H S
HS
Wataya
Y
Y
Takahara
M
M
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D006801:Humans; D007810:Lanosterol / Q000031:analogs & derivatives* / Q000494:pharmacology; D008214:Lymphocytes / Q000378:metabolism; D051379:Mice; D013329:Structure-Activity Relationship; D013936:Thymidine / Q000378:metabolism*
D000962:Antimalarials; D007810:Lanosterol; C031436:cimicifugoside; D013936:Thymidine