title: In vitro antitrypanosomal activities of quassinoid compounds from the fruits of a medicinal plant, Brucea javanica.
abstract: The medicinal plant Brucea javanica (L.) Merr. (Simaroubaceae) is widely distributed throughout Asia where its bitter fruits have been used in traditional medicine for various ailments. Fifteen C-20 quassinoids were isolated from the fruits of B. javanica and examined for their in vitro antitrypanosomal activities against trypomastigotes of Trypanosoma evansi. Bruceine A, bruceantinol, bruceine C, brusatol, and bruceine B showed strong antitrypanosomal activities with IC(50) values in the range of 2.9-17.8nM, which compared well with the standard trypanocidal drugs diminazene aceturate (IC(50)=8.8nM) and suramin (IC(50)=43.2nM). However, dehydrobruceine A, dehydrobruceine B, and dehydrobrusatol were about 2100, 900, and 1200 times less active, respectively, than bruceine A, bruceine B, and brusatol. The relationship of the structure and antitrypanosomal activity of these quassinoid compounds suggested that the presence of a diosphenol moiety in ring A and the nature of the C-15 side chain are important for their activities against T. evansi. This is the first report on the antitrypanosomal activity of isolated quassinoids.
authors.affiliation: Laboratory of Parasitology, Department of Disease Control, Graduate School of Veterinary Medicine, Hokkaido University, Sapporo 060-0818, Japan.
authors.forename: Saw
authors.initials: S
authors.lastname: Bawm
authors.forename: Hideyuki
authors.initials: H
authors.lastname: Matsuura
authors.forename: Ahmed
authors.initials: A
authors.lastname: Elkhateeb
authors.forename: Kensuke
authors.initials: K
authors.lastname: Nabeta
authors.lastname: Subeki
authors.forename: Nariaki
authors.initials: N
authors.lastname: Nonaka
authors.forename: Yuzaburo
authors.initials: Y
authors.lastname: Oku
authors.forename: Ken
authors.initials: K
authors.lastname: Katakura
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D032269:Brucea / Q000737:chemistry*; D005638:Fruit / Q000737:chemistry*; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry; D036702:Quassins / Q000737:chemistry / Q000494:pharmacology*; D014345:Trypanosoma / Q000187:drug effects*
chemical_list: D000981:Antiprotozoal Agents; D010936:Plant Extracts; D036702:Quassins