In vitro antitrypanosomal activity of plant terpenes against Trypanosoma brucei

• Published in: Phytochemistry (Oxford) Vol. 72; no. 16; pp. 2024 - 2030
• Main Authors: Otoguro, Kazuhiko, Iwatsuki, Masato, Ishiyama, Aki, Namatame, Miyuki, Nishihara-Tukashima, Aki, Kiyohara, Hiroaki, Hashimoto, Toshihiro, Asakawa, Yoshinori, Ōmura, Satoshi, Yamada, Haruki
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 01.11.2011; Elsevier
• Subjects: Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiparasitic agents; Antitrypanosomal; Biological and medical sciences; Chemical constitution; Diterpenes - chemistry; Diterpenes - isolation & purification; Diterpenes - pharmacology; Eflornithine - pharmacology; Fundamental and applied biological sciences. Psychology; In vitro; Medical sciences; Pharmacology. Drug treatments; Plant physiology and development; Plant products; Plants - chemistry; Structure-Activity Relationship; Suramin - pharmacology; Terpenes; Terpenes - chemistry; Terpenes - isolation & purification; Terpenes - pharmacology; Trypanocidal Agents - chemistry; Trypanocidal Agents - isolation & purification; Trypanocidal Agents - pharmacology; Trypanosoma brucei; Trypanosoma brucei brucei; Trypanosoma brucei brucei - drug effects; Plant products; Antitrypanosomal; Terpenes; In vitro; Kinetoplastida; Protozoa; Terpene; Plant origin; Chemical structure; Parasiticide; Trypanosoma brucei; Biological activity
• ISSN: 0031-9422; 1873-3700
• DOI: 10.1016/j.phytochem.2011.07.015

The antitrypanosomal activity of 24 known plant terpenes was evaluated against Trypanosoma brucei brucei. Among them, α-eudesmol, hinesol, nardosinone and 4-peroxy-1,2,4,5-tetrahydro-α-santonin exhibited selective and potent antitrypanosomal activities. [Display omitted] ► The antitrypanosomal activity of 24 terpenes was evaluated against Trypanosoma brucei. ► Among them, 22 plant terpenes exhibited some level of the activity. ► α-Eudesmol and hinesol exhibited most selective and potent activities. ► Nardosinone and 4-peroxy-1,2,4,5-tetrahydro-α-santonin also showed potent activities. 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.