Piperine (94-62-2) is a natural product isolated from black pepper that has myriad biological effects. Piperine has recently been shown to increase the metabolic rate of resting muscle (fast twitch skeletal fibers) without effecting slow twitch or cardiac fibers via destabilization of the super-relaxed state of myosin heads.1 This is proposed as a mechanism for the mitigation of obesity and type 2 diabetes by piperine. Piperine is an agonist at the TRPV1 receptor (EC50 = 38 µM).2 Piperine has various effects on drug metabolism3, inhibits human P-glycoprotein and CYP3A44 as well as UDP-glucose dehydrogenase and glucuronidation5.
1) Nogara et al. (2016), Piperine’s mitigation of obesity and diabetes can be explained by its up-regulation of the metabolic rate of resting muscle; Proc. Natl. Acad. Sci. USA; 113 13009
2) McNamara et al. (2005), Effects of piperine, the pungent component of black pepper, at the human vanilloid receptor (TRPV1); Br. J. Pharmacol., 144 781
3) Atal et al. (1985), Biochemical basis of enhanced drug bioavailability by piperine: evidence that piperine is a potent inhibitor of drug metabolism; J. Pharmacol. Exp.Ther., 232 258
4) Bhardwaj et al. (2002), Piperine, a major constituent of black pepper, inhibits human P-glycoprotein and CYP3A4; J. Pharmacol. Exp. Ther., 302 645
5) Reen et al. (1993), Impairment of UDP-glucose dehydrogenase and glucuronidation activities in liver and small intestine of rat and guinea pig in vitro by piperine; Biochem. Pharmacol., 46 229