[Objective] The active components of intracellular secondary metabolites from Monascus purpureus Mp-21 were studied. [Methods] The intracellular secondary metabolites were separated and purified by a variety of chromatographic separation methods, and the structure of the compounds was analyzed and identified using a variety of chromatographic data. Monomeric compounds were tested for antioxidant activity and hypoglycemia-related enzyme inhibitory activity. [Results] Three active compounds, namely baicalein, genistein and glycitein were isolated and identified. Baicalein was first discovered from Monascaceae whereas genistein and glycitein were first discovered from Monascus purpureus. In vitro antioxidant activity test and hypoglycemic- related enzyme activity test, baicalein had strong scavenging ability on 1,1-diphenyl-2-picrylhydrazyl (DPPH), O^2- and OH^- radical, and strong inhibitory effect on α-glucosidase and α-amylase, with IC₅₀ of 5.67, 36.40, 17.46, 30.94, 430.93 μg/mL, respectively. [Conclusion] Secondary metabolites from Monascus purpureus Mp-21 have the potential to be developed into functional food such as antioxidant and hypoglycemic agents.