Piperine from the fruits of Piper longum with inhibitory effect on monoamine oxidase and antidepressant-like activity.
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 microM) and MAO-B (IC50 value: 7.0 microM). 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 microM and 3.19+/-0.5 microM, 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.
College of Pharmacy, Chungbuk National University, Cheongju, Korea.
Seon A
SA
Lee
Seong Su
SS
Hong
Xiang Hua
XH
Han
Ji Sang
JS
Hwang
Gab Jin
GJ
Oh
Kyong Soon
KS
Lee
Myung Koo
MK
Lee
Bang Yeon
BY
Hwang
Jai Seup
JS
Ro
D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D000928:Antidepressive Agents / Q000494:pharmacology*; D052117:Benzodioxoles; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D009043:Motor Activity / Q000187:drug effects; D031701:Piper / Q000737:chemistry*; D010880:Piperidines / Q000494:pharmacology*; D053284:Polyunsaturated Alkamides
D000470:Alkaloids; D000928:Antidepressive Agents; D052117:Benzodioxoles; D008996:Monoamine Oxidase Inhibitors; D010880:Piperidines; D053284:Polyunsaturated Alkamides; C008922:piperine