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Natural products provide cornucopia of heterocyclic systems. The nucleus of 2- phenyl chromane is one of the important and well-known heterocycles found in the natural products. Naringenin, a plant-derived flavanone (2-phenyl chroman-4-one) belongs to the family of flavanoids. It possesses diverse biologic activities such as antidiabetic, antiatherogenic, antidepressant, antiandrogenic, antiestrogenic, immunomodulatory, antitumor, antimicrobial, anti-inflammatory, antiviral, hypolipidemic, antihypertensive, antioxidant, neuroprotective, anti-obesity, anti-Alzheimer, and memory enhancer activity. It has the potential to be used as an active pharmacophore. There have been reports of a number of molecular mechanisms underlying their beneficial activities. With emerging interest in traditional medicine and exploiting their potential based on a variety of health care systems, naringenin literature was thought to be explored. Further, this review aims to provide a new era of flavonoid-based therapeutic agents with new insights into naringenin and its derivatives as a lead compound in drug design.