Naringenin, a polyphenolic flavanone, exhibits diverse pharmacological and biological activities, including anti-inflammatory, antioxidant, anti-obesity, anticancer, antidiabetic, and antimicrobial effects. This review provides a comprehensive overview of the structural characteristics, extraction and synthesis methods, as well as the pharmacological actions of naringenin and its derivatives. The objective is to provide insights that may facilitate the rational design and practical application of naringenin-based therapeutics. Given its low aqueous solubility, nanoformulation strategies are recommended to enhance its bioavailability.