Modified berberine and protoberberines from Enantia chlorantha as potential inhibitors of Trypanosoma brucei.
Phytochemical study of the stem bark of Enantia chlorantha resulted in the isolation of two protoberberines 1 and 2. These alkaloids as well as commercially available berberine were modified chemically and tested in vitro against Typanosoma brucei proliferation as well as on three targeted glycolytic enzymes. The inhibitory activities observed were in the range of 20 microM (ED50 values).
Nyasse
B
B
Department of Organic Chemistry, Faculty of Science, University of Yaoundé I, Cameroon. bnyasse@uycdc.uninet.cm
Nkwengoua
E
E
Sondengam
B
B
Denier
C
C
Willson
M
M
D000818:Animals; D001599:Berberine / Q000494:pharmacology*; D001600:Berberine Alkaloids / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005987:Glyceraldehyde-3-Phosphate Dehydrogenases / Q000037:antagonists & inhibitors / Q000378:metabolism; D007202:Indicators and Reagents; D025221:Phosphofructokinases / Q000037:antagonists & inhibitors / Q000378:metabolism; D010735:Phosphoglycerate Kinase / Q000037:antagonists & inhibitors / Q000378:metabolism; D019441:Plant Epidermis / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry*; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects* / Q000201:enzymology
D001600:Berberine Alkaloids; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D014344:Trypanocidal Agents; D001599:Berberine; C009090:protoberberine; D005987:Glyceraldehyde-3-Phosphate Dehydrogenases; D025221:Phosphofructokinases; D010735:Phosphoglycerate Kinase