title: In vitro antitrypanosomal activity of plant terpenes against Trypanosoma brucei.
abstract: During the course of screening to discover antitrypanosomal compounds, 24 known plant terpenes (6 sesquiterpenes, 14 sesquiterpene lactones and 4 diterpenes) were evaluated for in vitro antitrypanosomal activity against Trypanosoma brucei brucei. Among them, 22 terpenes exhibited antitrypanosomal activity. In particular, α-eudesmol, hinesol, nardosinone and 4-peroxy-1,2,4,5-tetrahydro-α-santonin all exhibited selective and potent antitrypanosomal activities in vitro. Detailed here in an in vitro antitrypanosomal properties and cytotoxicities of the 24 terpenes compared with two therapeutic antitrypanosomal drugs (eflornithine and suramin). This finding represents the first report of promising trypanocidal activity of these terpenes. Present results also provide some valuable insight with regard to 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: Masato
authors.initials: M
authors.lastname: Iwatsuki
authors.forename: Aki
authors.initials: A
authors.lastname: Ishiyama
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: D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000518:Eflornithine / Q000494:pharmacology; D010944:Plants / Q000737:chemistry; D013329:Structure-Activity Relationship; D013498:Suramin / Q000494:pharmacology; D013729:Terpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
chemical_list: D004224:Diterpenes; D013729:Terpenes; D014344:Trypanocidal Agents; D013498:Suramin; D000518:Eflornithine