title: Antiprotozoal activity of drimane and coloratane sesquiterpenes towards Trypanosoma brucei rhodesiense and Plasmodium falciparum in vitro.
abstract: The extracts and 12 sesquiterpenes obtained from the East African medicinal plant Warburgia ugandensis Sprague (Canellaceae) were assessed for their antiplasmodial activity against the chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum and antitrypanosomal activity against Trypanosoma brucei rhodesiense. The dichloromethane extract displayed strong antiplasmodial and antitrypanosomal activities with IC(50) values of 8.10 and 1.10 µg/mL against K1 strain of the malaria parasite and STlB900 strain of T. b. rhodesiense, respectively. Among the compounds evaluated for inhibition of trypomastigotes, both drimane and coloratane sesquiterpenes possessing aldehyde groups at positions 8 and 9 were found to show most antitrypanosomal activity with IC(50) values in the range 0.56-6.4 µM. The antiplasmodial assays also revealed that the six coloratane and six drimane sesquiterpenes isolated from this extract exhibited significant antitrypanosomal activity with IC(50) values ranged from 0.45 to ?114 µM. Among the compounds tested against the malarial parasite P. falciparum 11?-hydroxymuzigadiolide (3) was most active with an IC(50) value of 6.40 µM.
authors.affiliation: Department of Pharmacognosy, Institute of Pharmaceutical Sciences, Karl-Franzens University Graz, Universitaetsplatz 4/1, A-8010 Graz, Austria.
authors.forename: Abraham Abebe
authors.initials: AA
authors.lastname: Wube
authors.forename: Franz
authors.initials: F
authors.lastname: Bucar
authors.forename: Simon
authors.initials: S
authors.lastname: Gibbons
authors.forename: Kaleab
authors.initials: K
authors.lastname: Asres
authors.forename: Lauren
authors.initials: L
authors.lastname: Rattray
authors.forename: Simon L
authors.initials: SL
authors.lastname: Croft
mesh_terms: D000981:Antiprotozoal Agents / Q000302:isolation & purification / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D019684:Magnoliopsida / Q000737:chemistry; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D024301:Plant Bark / Q000737:chemistry; D010936:Plant Extracts / Q000494:pharmacology; D010946:Plants, Medicinal / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects*; D000081223:Polycyclic Sesquiterpenes; D012717:Sesquiterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects*
chemical_list: D000981:Antiprotozoal Agents; D010936:Plant Extracts; D000081223:Polycyclic Sesquiterpenes; D012717:Sesquiterpenes; C437376:drimane