Antitrypanosomal alkaloids from Polyalthia suaveolens (Annonaceae): their effects on three selected glycolytic enzymes of Trypanosoma brucei.
In continuation of our study on medicinal plants of Cameroon, stem barks of Polyalthia suaveolens were phytochemically studied. This investigation yielded a new indolosesquiterpene alkaloid, named polysin (1) and four hitherto known alkaloids (2-5). Polysin (1) appeared as a competitive reversible inhibitor (K(i)=10 microM) of phosphofructo kinase (PFK) of Trypanosoma brucei with respect to fructose-6-phosphate (K(i)/K(M)=0.05) and could be used in the design of new trypanocidal drugs. The other isolated compounds (2-5) also exhibited interesting inhibitory effects on selected glycolytic enzymes (PFK, glyceraldehyde-3-phosphate dehydrogenase and aldolase).
Ngantchou
Igor
I
Department of Organic Chemistry, Faculty of Sciences, University of Yaoundé I, Yaoundé, Cameroon. nwete@yahoo.fr
Nyasse
Barthélemy
B
Denier
Colette
C
Blonski
Casimir
C
Hannaert
Véronique
V
Schneider
Bernd
B
D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D002163:Cameroon; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006019:Glycolysis / Q000187:drug effects; D025221:Phosphofructokinases / Q000037:antagonists & inhibitors; D008517:Phytotherapy; D010946:Plants, Medicinal / Q000737:chemistry; D031044:Polyalthia / Q000737:chemistry*; D012717:Sesquiterpenes; D014344:Trypanocidal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects / Q000201:enzymology* / Q000378:metabolism
D000470:Alkaloids; D004791:Enzyme Inhibitors; D012717:Sesquiterpenes; D014344:Trypanocidal Agents; D025221:Phosphofructokinases