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In vitro antitrypanosomal activity of plant terpenes against Trypanosoma brucei
Authors:Otoguro Kazuhiko  Iwatsuki Masato  Ishiyama Aki  Namatame Miyuki  Nishihara-Tukashima Aki  Kiyohara Hiroaki  Hashimoto Toshihiro  Asakawa Yoshinori  Omura Satoshi  Yamada Haruki
Affiliation:aResearch Center for Tropical Diseases, Kitasato Institute for Life Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan;bLaboratory of Biochemical Pharmacology for Phytomedicine, Kitasato Institute for Life Sciences & Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan;cFaculty of Pharmaceutical Sciences, Tokushima Bunri University, Yamashiro-cho, Tokushima 770-8514, Japan;dKitasato Institute for Life Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan
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.
Keywords:In vitro   Antitrypanosomal   Terpenes   Plant products
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