Essential structural factors of acetogenins, potent inhibitors of mitochondrial complex I.
To elucidate the role of the hydrophobic alkyl tail of acetogenins in the inhibitory action, we synthesized an acetogenin derivative possessing the shortest tail (i.e., methyl group) and examined its inhibitory activity against bovine heart mitochondrial complex I. Our results indicated that the alkyl tail, which is one of the common structural features of natural acetogenins, is not an essential structural factor required for the potent inhibition.
Motoyama
Tomoko
T
Division of Applied Life Sciences, Graduate School of Agriculture, Kyoto University, Sakyo-ku, 606-8502, Kyoto, Japan.
Yabunaka
Hiromi
H
Miyoshi
Hideto
H
D000818:Animals; D002417:Cattle; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D005663:Furans / Q000737:chemistry* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008929:Mitochondria, Heart / Q000187:drug effects / Q000201:enzymology* / Q000378:metabolism; D015394:Molecular Structure; D009097:Multienzyme Complexes / Q000378:metabolism; D009247:NADH, NADPH Oxidoreductases / Q000378:metabolism; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D005663:Furans; D009097:Multienzyme Complexes; C023107:NADH oxidase; D009247:NADH, NADPH Oxidoreductases