title: Activity of extracts and naphthoquinones from Kigelia pinnata against Trypanosoma brucei brucei and Trypanosoma brucei rhodesiense.
abstract: Dichloromethane extracts of the root bark and stem bark of Kigelia pinnata collected from Zimbabwe exhibited antitrypanosomal activity against Trypanosoma brucei brucei in vitro. Activity-guided fractionation led to the isolation of four naphthoquinones from both the root and stem bark of the plant. The compounds were identified as 2-(1-hydroxyethyl)-naphtho[2,3-b]furan-4,9-quinone (1), isopinnatal (2), kigelinol (3), and isokigelinol (4). Subsequently, the compounds were assessed for antitrypanosomal activity against T. brucei brucei and T. brucei rhodesiense bloodstream form trypomastigotes in vitro. Compound 1 with a furanonaphthoquinone structure was found to possess pronounced activity against both parasites with IC50 values of 0.12 and 0.045 microM, respectively, although it was less active than the standard drug pentamidine. Compounds 2, 3, and 4 also exhibited activity against the parasites, although to a lesser extent. The activities of the compounds were further assessed by comparison with the cytotoxic activities obtained against KB cell lines.
authors.affiliation: National Pharmaceutical Control Bureau, Jalan University, Petaling Jaya, Malaysia.
authors.forename: S V
authors.initials: SV
authors.lastname: Moideen
authors.forename: P J
authors.initials: PJ
authors.lastname: Houghton
authors.forename: P
authors.initials: P
authors.lastname: Rock
authors.forename: S L
authors.initials: SL
authors.lastname: Croft
authors.forename: F
authors.initials: F
authors.lastname: Aboagye-Nyame
mesh_terms: D000818:Animals; D006801:Humans; D015394:Molecular Structure; D009285:Naphthoquinones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000494:pharmacology*; D018547:Plant Stems; D010946:Plants, Medicinal; D014197:Trees; D014344:Trypanocidal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects* / Q000302:isolation & purification; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects*; D015030:Zimbabwe
chemical_list: D009285:Naphthoquinones; D010936:Plant Extracts; D014344:Trypanocidal Agents