Inhibition of both Trypanosoma brucei bloodstream form and related glycolytic enzymes by a new kolavic acid derivative isolated from Entada abyssinica.
A new kolavic acid derivative known from spectroscopic analyses as monomethyl ester-15-kolavic acid was isolated from the stem bark of Entada abyssinica, a plant traditionally used in West and East Africa for the management of sleeping sickness. The new derivative showed a strong and selective inhibitory activity on the GAPDH enzyme of Trypanosoma brucei with an IC50 value of 0.012 mM.
Nyasse
B
B
Laboratory of Bio-organic and Medicinal Chemistry, Department of Organic Chemistry, Faculty of Science, University of Yaounde I, Cameroon. bnyasse@uycdc.uninet.cm
Ngantchou
I
I
Tchana
E M
EM
Sonké
B
B
Denier
C
C
Fontaine
C
C
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000494:pharmacology; D004224:Diterpenes / Q000494:pharmacology*; D005987:Glyceraldehyde-3-Phosphate Dehydrogenases / Q000378:metabolism; D006019:Glycolysis / Q000187:drug effects*; D018314:Leishmania infantum / Q000187:drug effects / Q000254:growth & development; D009682:Magnetic Resonance Spectroscopy; D025221:Phosphofructokinases / Q000378:metabolism; D024301:Plant Bark / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry*; D011770:Pyruvate Kinase / Q000378:metabolism; D014346:Trypanosoma brucei brucei / Q000187:drug effects* / Q000201:enzymology* / Q000254:growth & development
D000962:Antimalarials; D000981:Antiprotozoal Agents; D004224:Diterpenes; C495288:monomethyl ester-15-kolavic acid; D005987:Glyceraldehyde-3-Phosphate Dehydrogenases; D025221:Phosphofructokinases; D011770:Pyruvate Kinase