Antiplasmodial activity of Uvaria klaineana.
Crude extracts of Uvaria klaineana Engler and Diels (Annonaceae) stems showed in vitro activity against chloroquine-resistant K1 strain of Plasmodium falciparum. The most active extract was the basic dichloromethane extract containing crude alkaloids (IC50 = 3.55 microg/mL). The bioassay-guided fractionation of this extract led to the isolation of the major alkaloid crotsparine (1) which showed an antiplasmodial activity against the chloroquine-sensitive Thai strain of P. falciparum and the chloroquine-resistant K1 and FcB1 strains of P. falciparum. Two minor alkaloids were also identified as crotonosine (2) and zenkerine (3). Their structures were elucidated using 2D-NMR techniques.
Akendengue
B
B
Ngou-Milama
E
E
Roblot
F
F
Laurens
A
A
Hocquemiller
R
R
Grellier
Ph
P
Frappier
F
F
D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D029061:Annonaceae; D000962:Antimalarials / Q000494:pharmacology*; D001681:Biological Assay; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance; D005681:Gabon; D016488:Medicine, African Traditional; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018547:Plant Stems / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects*
D000470:Alkaloids; D000962:Antimalarials; D010936:Plant Extracts; C455069:crotonosine; C455068:crotsparine; C455070:zenkerine; D002738:Chloroquine