Display omitted •Comprehensive nutrients profiling of bee pollen with various botanical and geographic origins were reviewed.•Active natural plant metabolites from bee pollen and their in vivo metabolic pathways were summarized.•The nutritional values of bee pollen and its potential bioactivities for human health were updated.•The safety of bee pollen as a food supplement was highlighted. Bee pollen is a mixture of plant pollen pellet with nectar and honeybee secretions. Due to its active natural metabolites with extensive nutritional and therapeutic properties, it is recommended as a treasure trove of human nutrition. The nutritional components in bee pollen include carbohydrates, proteins, lipids, vitamins, minerals, polyphenols, and a small percentage of other components. Previous studies demonstrated that bee pollen exhibit antioxidant, antibacterial, anti-inflammatory, anticarcinogenic, and antiallergic properties. This comprehensive review focused on the nutritional properties and potentially active phytometabolites (polyphenolic acids and flavonoids) of bee pollen and its therapeutic health benefits. We also covered the food safety and guidelines for the consumption with future industrial challenges of bee pollen.