Klaivanolide, an antiprotozoal lactone from Uvaria klaineana.
Bioguided-fractionation of a CH(2)Cl(2) extract of the stems of Uvaria klaineana (Annonaceae) led to isolation of klaivanolide, a novel bisunsaturated 7-membered lactone (5-acetoxy-7-benzoyloxymethyl-7H-oxepin-2-one), together with benzyl benzoate. Klaivanolide showed potent in vitro antileishmanial activity against both sensitive and amphotericin B-resistant promastigote forms of Leishmania donovani with IC(50) values of 1.75 and 3.12 microM, respectively. The compound also showed in vitro trypanocidal activity against trypomastigote forms of Trypanosoma brucei brucei GVR 35. Its structure was established by 1D and 2D NMR and other spectroscopic techniques.
Akendengue
Blandine
B
Département de Chimie-Biochimie, Faculté de Médecine et des Sciences de la Santé, B.P. 4009, Libreville, Gabon.
Roblot
François
F
Loiseau
Philippe M
PM
Bories
Christian
C
Ngou-Milama
Edouard
E
Laurens
Alain
A
Hocquemiller
Reynald
R
D000818:Animals; D029061:Annonaceae / Q000737:chemistry*; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007783:Lactones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007893:Leishmania donovani / Q000187:drug effects*; D009682:Magnetic Resonance Spectroscopy; D021261:Parasitic Sensitivity Tests; D014344:Trypanocidal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
D000981:Antiprotozoal Agents; D007783:Lactones; D014344:Trypanocidal Agents; C465329:klaivanolide