Hesperetin 7-O-neohesperidoside, a well-known flavanone glycoside widely found in citrus fruits, possesses various biological activities and has potential applications ranging from food ingredients to therapeutics. The aim of this manuscript is to provide a comprehensive overview of the chemical, biosynthetic, and pharmacokinetic profiles of neohesperidin, as well as its therapeutic effects and mechanisms on underlying diseases. This literature review covers the wide range of pharmacological responses elicited by neohesperidin, including neuroprotective, anti-inflammatory, antidiabetic, antibacterial, and anticancer activities, with a focus on the mechanisms of these pharmacological responses. In addition, compounds osteoporosis, anti-ulcer, cardioprotective and hepatoprotective actions were outlined. This review includes a detailed description of the biosynthesis, biopharmacokinetics, toxicology, and controlled release of neohesperidin. Neohesperidin exhibits broad therapeutic and biological activities in the treatment of various complex diseases, including neurodegenerative diseases, hepatic heart diseases, cancer, diabetes, obesity, infectious diseases, allergic diseases, and inflammatory diseases. Neohesperidin is a promising therapeutic candidate for the treatment of various diseases with complex etiology. However, further in vivo and in vitro mechanistic studies are needed to confirm the safety, bioavailability, and toxicity profile of neohesperidin before clinical trials. This review includes a detailed description of the biosynthesis, biopharmacokinetics, toxicology, and controlled release of neohesperidin. Neohesperidin exhibits broad therapeutic and biological activities in the treatment of various complex diseases, including neurodegenerative diseases, hepatic heart diseases, cancer, diabetes, obesity, infectious diseases, allergic diseases, and inflammatory diseases. Neohesperidin is a promising therapeutic candidate for the treatment of various diseases with complex etiology. However, further in vivo and in vitro mechanistic studies are needed to confirm the safety, bioavailability, and toxicity profile of neohesperidin before clinical trials. This review includes a detailed description of the biosynthesis, biopharmacokinetics, toxicology, and controlled release of neohesperidin. Neohesperidin exhibits broad therapeutic and biological activities in the treatment of various complex diseases, including neurodegenerative diseases, hepatic heart diseases, cancer, diabetes, obesity, infectious diseases, allergic diseases, and inflammatory diseases. Neohesperidin is a promising therapeutic candidate for the treatment of various diseases with complex etiology. However, further in vivo and in vitro mechanistic studies are needed to confirm the safety, bioavailability, and toxicity profile of neohesperidin before clinical trials. Neohesperidin exhibits broad therapeutic and biological activities in the treatment of various complex diseases, including neurodegenerative diseases, hepatic heart diseases, cancer, diabetes, obesity, infectious diseases, allergic diseases, and inflammatory diseases. Neohesperidin is a promising therapeutic candidate for the treatment of various diseases with complex etiology. However, further in vivo and in vitro mechanistic studies are needed to confirm the safety, bioavailability, and toxicity profile of neohesperidin before clinical trials. Neohesperidin exhibits broad therapeutic and biological activities in the treatment of various complex diseases, including neurodegenerative diseases, hepatic heart diseases, cancer, diabetes, obesity, infectious diseases, allergic diseases, and inflammatory diseases. Neohesperidin is a promising therapeutic candidate for the treatment of various diseases with complex etiology. However, further in vivo and in vitro mechanistic studies are needed to confirm the safety, bioavailability, and toxicity profile of neohesperidin before clinical trials. Neohesperidin is a promising therapeutic candidate for the treatment of various diseases with complex etiology. However, further in vivo and in vitro mechanistic studies are needed to confirm the safety, bioavailability, and toxicity profile of neohesperidin before clinical trials. Neohesperidin is a promising therapeutic candidate for the treatment of various diseases with complex etiology. However, further in vivo and in vitro mechanistic studies are needed to confirm the safety, bioavailability, and toxicity profile of neohesperidin before clinical trials.