Review of Piperine as a Bio-enhancer

Piperine (1-peperoyl piperidine), a pungent alkaloid, is found in various Pipper species. Piperine produces antioxidant, antiplatelet, anti-inflammatory, antihypertensive, hepatoprotective, antithyroid, antitumor, antiasthmatic activities and also a fertility enhancer. Piperine enhances absorption from gastrointestinal tract by various mechanisms and reduces gut metabolism of drugs. Piperine modulates membrane dynamics and lipid environment and increases permeability at site of absorption Molecular structure of piperine is suitable for enzyme inhibition and it inhibits various metabolizing enzymes like cytochrome bs, NADPH cytochrome, CYP3A4, UDP-glucose dehydrogenase (UDP-GDH), aryl hydrocarbon hydroxylase (AAH) and UDP-glucuronyl transferase. Structural modification of piperine provides selective inhibitors of various cytochrome p450 enzymes. Inhibition of these enzymes by piperine results in enhanced bioavailability of drugs and nutrients like oxytetracyclin, metronidazole, ampicillin, norfloxacin, ciprofloxacin, acefotaxime, amoxicillin trihydrate, curcumin, beta-carotene, carbamazepine, gallic acid, nimesulide, tiferron, nevirapine, pentobarbitone, phenytoin, resveratrol, vasicine and sparteine by different mechanisms. Thus piperine is an absorption enhancer and a potent inhibitor of drug metabolism. Key words: Piperine, Metabolism inhibitor, Absorption enhancer, Bio-enhancer, bioavailability