Since the start of history, natural medicine has been of great interest and attention to humankind. A heap of empirical research indicates that spices have undoubtedly made our lives more interesting and may also make them longer. Capsicum is a highly regarded indispensable spice all over the globe for its umpteen culinary and medicinal facets. It has been used for more than 7000 years in Mexico and is believed to have originated in tropical Central America. Mainly, this botanical contains a good source of vitamin C, vitamin A, vitamin E, vitamin B5, potassium, magnesium, iron, calcium, phosphorus, and carotenoids. Interestingly, capsicum phenolic compounds are helpful in preventing and treating many ailments. So, it intends as a beneficial milestone in the pharmaceutical industry and a boon to humanity. This chapter highlights the tremendous pharmacological uses and health benefits of capsicum species and its active compounds in multifarious aspects.