Journal
CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 53, Issue 7, Pages 832-835Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.53.832
Keywords
Piper longum; piperine; monoamine oxidase inhibitor; antidepressant agent
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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 mu m) and MAO-13 (IC50 value: 7.0 mu m). Kinetic analyses by a Lineweaver-Burk plot clearly indicated that piperine competitively inhibited MAO-A and MAO-B with K-i values of 19.0 +/- 0.9 mu m and 3.19 +/- 0.5 mu m, 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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