Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
Piperine from the Fruits of Piper longum with Inhibitory Effect on Monoamine Oxidase and Antidepressant-Like Activity
Seon A LeeSeong Su HongXiang Hua HanJi Sang HwangGab Jin OhKyong Soon LeeMyung Koo LeeBang Yeon HwangJai Seup Ro
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2005 Volume 53 Issue 7 Pages 832-835


A bioassay-guided isolation of the ethanol extract from the fruits of Piper longum yielded a known piperidine alkaloid, piperine, as a monoamine oxidase (MAO) inhibitor. Piperine showed an inhibitory effect against MAO-A (IC50 value: 20.9 μM) and MAO-B (IC50 value: 7.0 μM). Kinetic analyses by a Lineweaver–Burk plot clearly indicated that piperine competitively inhibited MAO-A and MAO-B with Ki values of 19.0±0.9 μM and 3.19±0.5 μM, respectively. The inhibition by piperine was found to be reversible by dialysis of the incubation mixture. In addition, the immobility times in the tail suspension test were significantly reduced by piperine, similar to that of the reference antidepressant fluoxetine, without accompanying changes in ambulation when assessed in an open-field. These results suggest that piperine possesses potent antidepressant-like properties that are mediated in part through the inhibition of MAO activity, and therefore represent a promising pharmacotherapeutic candidate as an antidepressant agent.

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© 2005 The Pharmaceutical Society of Japan
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