The bioactive compounds of bee pollen have been demonstrated through the years to have antioxidant, antibacterial, and antitumor potential. Phenolic compounds are considered the main active ingredients having these biological activities, but research studies were carried out with the aim of characterizing samples from various countries, seeking to identify those with greater biological potential and the varieties that influence this potential. Recently, some researchers have focused on in vivo studies with the inclusion of this food source in the diet of humans and animals, and in the formulation of medications with a bee pollen base. Latest studies with results of in vitro and in vivo studies of the antibacterial, antioxidant and antitumor activity of bee pollen are presented, as well as factors that influence the biological potential of this product. Recently, the biological activity of bee pollen has been complemented with studies demonstrating hepatoprotective and antidiabetic activity, as well as immunomodulatory, anti-inflammatory, and antiradiation activity, which are reviewed in this chapter.