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[email protected] Open Chemistry Journal, 2016, 3, 75-96 75 Open Chemistry Journal Content list available at: www.benthamopen.com/CHEM/ DOI: 10.2174/1874842201603010075 REVIEW ARTICLE Piperine and Its Various Physicochemical and Biological Aspects: A Review Bhawna Chopra1,2,*, Ashwani Kumar Dhingra1,2, Ram Prakash Kapoor1 and Deo Nandan Prasad3 1Guru Gobind Singh College of Pharmacy, Yamuna Nagar -135001, Haryana, India 2I.K Gujral Punjab Technical University, Kapurthala-144603, Punjab, India 3Shivalik College of Pharmacy, Nangal 140124, Punjab, India Received: September 07, 2015 Revised: May 11, 2016 Accepted: August 11, 2016 Abstract: Piper nigrum L. is examined as the king of species worldwide by virtue of its principle piperine. In Ayurveda, since from the ancient times, it is known as “Yogvahi”. It is one of the important alkaloids of Pepper fruits (Family Piperaceae) and has been found to have numerous medicinal properties such as antioxidant, antiplatelet, anti-inflammatory, antihypertensive, hepatoprotective, antithyroid, antitumor, antiasthmatic activity and also have significant role as fertility enhancer. The present review discusses the biosynthetic pathway, extraction process, chemistry and various analytical methods of piperine. It also describes the structural modification of piperine and its various effects on biological system. The utility of piperine as a bioenhancer for certain antibacterial- antibiotics and a potent inhibitor of drug metabolism are also discussed. Thus, review provides knowledgeable erudition on the piperine which paves way for further work. Keywords: Piperine, Bioenhancer, Biological activity, Piper nigrum. 1. INTRODUCTION Piperine is an interesting compound because it is a good biomarker together with other pure bioactive components or their derivatives or with drug molecules and hence proves to be potential drug compound.