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- W2273197701 abstract "Previous reports have documented that 1,4‐naphthoquinones act as inhibitors of the monoamine oxidase ( MAO ) enzymes. In particular, fractionation of the extracts of cured tobacco leafs has led to the characterization of 2,3,6‐trimethyl‐1,4‐naphthoquinone, a non‐selective MAO inhibitor. To derive structure–activity relationships for MAO inhibition by the 1,4‐naphthoquinone class of compounds, this study investigates the human MAO inhibitory activities of fourteen structurally diverse 1,4‐naphthoquinones of natural and synthetic origin. Of these, 5,8‐dihydroxy‐1,4‐naphthoquinone was found to be the most potent inhibitor with an IC 50 value of 0.860 μ m for the inhibition of MAO ‐B. A related compound, shikonin, inhibits both the MAO ‐A and MAO ‐B isoforms with IC 50 values of 1.50 and 1.01 μ m , respectively. It is further shown that MAO ‐A and MAO ‐B inhibition by these compounds is reversible by dialysis. In this respect, kinetic analysis suggests that the modes of MAO inhibition are competitive. This study contributes to the discovery of novel MAO inhibitors, which may be useful in the treatment for disorders such as P arkinson's disease, depressive illness, congestive heart failure and cancer." @default.
- W2273197701 created "2016-06-24" @default.
- W2273197701 creator A5030450621 @default.
- W2273197701 creator A5051406131 @default.
- W2273197701 creator A5079529603 @default.
- W2273197701 date "2016-01-12" @default.
- W2273197701 modified "2023-10-15" @default.
- W2273197701 title "Evaluation of Natural and Synthetic 1,4‐naphthoquinones as Inhibitors of Monoamine Oxidase" @default.
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- W2273197701 doi "https://doi.org/10.1111/cbdd.12708" @default.
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