Currently, black pepper commands the leading position among all the spices as a spice of handsome commercial importance in all the world trade and finds its way into the dietary habits of millions of people worldwide. Black pepper is biologically known as Piper nigrum and contains Piperine as the main active chemical constituent. This paper highlights various general methods for extracting Piperine from the crude drug: maceration extraction, Hydrotropic extraction, Accelerated solvent extraction, Thin layer chromatography, and extraction with ethanol & dichloromethane Ionic fluid-based ultrasonic-assisted extraction, etc. In this review, Piperine and its analogs exhibit numerous pharmacological activities and synthetic schemes of Insecticidal activity, Anti-cancer activity, Anti-inflammatory activity, Anti-diabetic activity, Anti-hyperlipidemic activity, Antifungal Activity, Narcotic Activity, etc. The biochemistry of Piperine also has been summarized in the presented article. This very exhaustive review details the complete information about Piperine, its derivatives, and further processing. Moreover, the current survey sums up the new writing identified with Piperine as a remedial specialist against a few illnesses.