title: In vitro antitrypanosomal activity of bis(bibenzyls)s and bibenzyls from liverworts against Trypanosoma brucei.
abstract: During the course of our screening program to discover new antitrypanosomal compounds, 17 known plant aromatic compounds [12 bis(bibenzyls)s and 5 bibenzyls] were evaluated for in vitro activity against Trypanosoma brucei brucei. Sixteen compounds were found to exhibit antitrypanosomal activity. In particular, three compounds, marchantin A (1), plagiochin A (5) and 2(R)-2-isopropenyl-6,7-dihydroxy-4-(2-phenylethyl)dihydrobenzofuran (16) demonstrated moderate selective and potent antitrypanosomal activities in vitro. We detail here the antitrypanosomal properties and cytotoxicities of the compounds in comparison with two commonly used therapeutic drugs, eflornithine and suramin. Our finding represents the first report of the promising trypanocidal activity of these compounds. The research also provides valuable insight into structure-activity relationships and the possible mode of action of the compounds.
authors.affiliation: Research Center for Tropical Diseases, Kitasato Institute for Life Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan. otoguro@lisci.kitasato-u.ac.jp
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Otoguro
authors.forename: Aki
authors.initials: A
authors.lastname: Ishiyama
authors.forename: Masato
authors.initials: M
authors.lastname: Iwatsuki
authors.forename: Miyuki
authors.initials: M
authors.lastname: Namatame
authors.forename: Aki
authors.initials: A
authors.lastname: Nishihara-Tukashima
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Kiyohara
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Hashimoto
authors.forename: Yoshinori
authors.initials: Y
authors.lastname: Asakawa
authors.forename: Satoshi
authors.initials: S
authors.lastname: Omura
authors.forename: Haruki
authors.initials: H
authors.lastname: Yamada
mesh_terms: D001632:Bibenzyls / Q000737:chemistry* / Q000494:pharmacology*; D035926:Hepatophyta / Q000737:chemistry*; D015394:Molecular Structure; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
chemical_list: D001632:Bibenzyls; D014344:Trypanocidal Agents