1-methyl-2-undecyl-4(1H)-quinolone as an irreversible and selective inhibitor of type B monoamine oxidase.
The inhibitory compound of monoamine oxidase (MAO) activity was isolated from the CH(2)Cl(2) fraction of the fructus of Evodia rutaecarpa and identified as 1-methyl-2-undecyl-4(1H)-quinolone (1). Compound 1 showed a selective inhibition of type B MAO (MAO-B) activity with the IC(50) value of 15.3 microM using a substrate kynuramine, but did not inhibit type A MAO (MAO-A) activity. The kinetic analysis using Lineweaver-Burk plots indicated that compound 1 competitively inhibited MAO-B activity with the K(i) value of 9.91 microM. The inhibition of MAO-B by compound 1 was found to be irreversible by dialysis of the incubation mixture. These results suggest that compound 1 is a potent irreversible inhibitor of MAO-B, and may regulate catecholamine content in the neurons.
Lee
Myung Koo
MK
College of Pharmacy, Chungbuk National University, Cheongju 361-763, Korea.
Hwang
Bang Yeon
BY
Lee
Seon A
SA
Oh
Gab Jin
GJ
Choi
Woo Hoi
WH
Hong
Seong Su
SS
Lee
Kyong Soon
KS
Ro
Jai Seup
JS
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000201:enzymology; D032086:Evodia; D005638:Fruit; D051379:Mice; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D015363:Quinolones / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*
C000618672:1-methyl-2-undecyl-4(1H)-quinolone; D008996:Monoamine Oxidase Inhibitors; D010936:Plant Extracts; D015363:Quinolones; D008995:Monoamine Oxidase