From ancient times, phytopharmaceuticals have played an important role in the management of human health. Piperine, an alkaloid with the piperidine nucleus was discovered and isolated by Hans Christian Ørsted, from the fruits of Piper nigrum. Piperine forms is slightly water soluble and forms monoclinic needles and possess a strong pungent taste. Piperine contains plentiful established health effects and beneficial therapeutic properties. Cells and enzymes are key elements in biotechnological processes to carry out a wide variety of very specific reactions under judicious conditions to produce piperine and their products. Piperine also serves as bio-enhancers in conjunction with drugs to stimulate drug molecules’ activity across different routes by improving the drug's bioavailability across the membrane, raising the drug's effect across conformational interaction, and working as a drug receptor. In recent years, there has been significant interest in the use of piperine to treat many illnesses, its health-beneficial effects, and its work as bio-enhancers. Due to their biological activity, piperine has the potential to be used in health and medicine.