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Plants such as chamomile, echinacea, garlic, ginger, gingko, and black pepper are recognised for their medicinal properties and regular nutritious food intake. The knowledge of secondary metabolites present in this species that would be useful for producing natural products and disease diagnostic drugs that cure various diseases must be studied and improved. Black pepper (Piper nigrum L.) is called the “king of spices” and is a commonly used spice that adds flavour to sauces and enhances the taste of other ingredients. In Piper nigrum, several biological activities are reported, but the complete phytochemical profile is not known until the date. Black pepper is largely produced in countries like Vietnam, led by Indonesia, India, and Brazil. This chapter mainly discusses the important isolated phytochemicals from P. nigrum. Based on chemical structures, compounds are classified based on different biological activity.