title: Antimalarial activity and nucleoside transport inhibitory activity of the triterpenic constituents of Cimicifuga spp.
abstract: 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.
authors.affiliation: Osaka University of Pharmaceutical Sciences, Takatsuki, Japan.
authors.forename: M
authors.initials: M
authors.lastname: Takahira
authors.forename: A
authors.initials: A
authors.lastname: Kusano
authors.forename: M
authors.initials: M
authors.lastname: Shibano
authors.forename: G
authors.initials: G
authors.lastname: Kusano
authors.forename: K
authors.initials: K
authors.lastname: Koizumi
authors.forename: R
authors.initials: R
authors.lastname: Suzuki
authors.forename: H S
authors.initials: HS
authors.lastname: Kim
authors.forename: Y
authors.initials: Y
authors.lastname: Wataya
authors.forename: M
authors.initials: M
authors.lastname: Takahara
mesh_terms: 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*
chemical_list: D000962:Antimalarials; D007810:Lanosterol; C031436:cimicifugoside; D013936:Thymidine