The microbial production of pinocembrin (PIN) is becoming increasingly necessary in light of the potential therapeutic applications heralded in many published papers in recent years, such as neuroprotective, cardiovascular, anti-inflammatory, antioxidant, antitumor, antifibrotic, and antimicrobial activities. The chapter is structured in four parts as follows: (i) chemical structure and characterization of PIN; (ii) biological production; (iii) biological activity; and (iv) potential applications of PIN in the food industry. After covering some aspects related to PIN’s structure and chemical characteristics, the second part contains two sections on plant and microbial syntheses of this compound. The third part describes the molecular targets and potential therapeutic applications, as well as several considerations on the biological activities of this flavonoid (neuroprotective, anti-inflammatory, antifibrotic, antitumor, antioxidant and antimicrobial activities, wound healing properties). The last section focuses on the possible uses of PIN in the industry linked to recent research. As researchers have started to create clinical studies for deciphering the clinical impact of this compound, the results so far support its vast potential in the therapy of severe diseases, including central nervous system disorders and infections.