Bioactive alkaloid of pepper Abstract: Piperine, a bioactive alkaloid of pepper, has been considered for its medicinal properties and received significant attention from pharmaceutical scientists for its bioavailability enhancement action to develop novel formulations. Piperine has shown numerous health effects and therapeutic properties; however, its pharmacological actions are limited due to its poor aqueous solubility. Numerous reports have been published which depicted the potential of piperine in pharmaceuticals development and the treatment of various ailments. The present review is emphasized upon the different methods for isolation of piperine from natural resources, synthesis of piperine, chemistry, quality control aspects of piperine in bulk drug, and formulation, the usefulness of piperine in pharmaceutical formulations, its biological activities, and clinical studies. The detailed