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KMID : 0043320080310060679
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Archives of Pharmacal Research
2008 Volume.31 No. 6 p.679 ~ p.683
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Methylpiperate Derivatives from Piper longum and Their Inhibition of Monoamine Oxidase
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Lee Seon-A
Hwang Ji-Sang
Han Xiang-Hua
Lee Chul
Lee Min-Hee
Choe Sang-Gil
Hong Seong-Su
Lee Dong-Ho
Lee Myung-Koo
Hwang Bang-Yeon
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Abstract
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We have previously reported that piperine, a known piperidine alkaloid from Piper longum, competitively inhibited mouse brain MAO-A and MAO-B activities. Piperine also showed in vivo antidepressant-like activity against the tail suspension test. In the present study, we further expanded on the identification of MAO inhibitors from the fruit of P. longum. Activity-guided fractionation of a methylene chloride soluble extract led to the isolation of three known piperine-related compounds, methylpiperate (1), guineensine (2), and piperlonguminine (3). Of these, methylpiperate (1) and guineensine (2) showed significant MAO inhibitory activities with values of 3.6 and , respectively. Furthermore, methylpiperate (1) exhibited a selective inhibitory effect against MAO-B ( value: ) than MAO-A ( value: ). The kinetic study using the Lineweaver-Burk plots analysis suggested that methylpiperate (1) competitively inhibits MAO-A and MAO-B activities with the Ki values of 23.5 and , respectively.
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KEYWORD
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Piper longum, Piperaceae, Methylpiperate, Monoamine oxidase inhibitor
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