Aurones interfere with Leishmania major mitochondrial fumarate reductase.
A series of aurones was analyzed for the ability to inhibit respiratory functions of mitochondria of Leishmania parasites. The aim of this study was to find a rational explanation for the activity of certain aurones and auronols as novel antiprotozoal compounds of plant origin. In a cell-free assay mitochondrial fumarate reductase from L. donovani was inhibited in a concentration-dependent manner. The most active compounds were 4',6-dihydroxyaurone and 6-methoxyaurone which inhibited parasite enzyme activity at 25 nM by over ninety percent.
Kayser
Oliver
O
Freie Universität Berlin, Institut für Pharmazie, Pharmazeutische Biotechnologie, Germany. kayser@zedat.fu-berlin.de
Chen
Ming
M
Kharazmi
Arsalan
A
Kiderlen
Albrecht F
AF
D000818:Animals; D001572:Benzofurans / Q000494:pharmacology*; D002851:Chromatography, High Pressure Liquid; D007700:Kinetics; D018320:Leishmania major / Q000201:enzymology*; D009682:Magnetic Resonance Spectroscopy; D008928:Mitochondria / Q000201:enzymology*; D010101:Oxygen Consumption / Q000187:drug effects; D013329:Structure-Activity Relationship; D013385:Succinate Dehydrogenase / Q000037:antagonists & inhibitors / Q000378:metabolism*
D001572:Benzofurans; D013385:Succinate Dehydrogenase