Blueberry anthocyanins are well known for their beneficial biological activities. However, the poor bioavailability of anthocyanins limits their functional capacity in vivo. Our current study aimed to detect the effects of α-casein on the absorption of blueberry anthocyanins and their metabolites in rats. Blueberry anthocyanins with and without α-casein were intragastrically administered to two groups of rats and their blood samples were collected within 24 h. Results illustrated that rapid absorption of anthocyanins was observed in the rat plasma, but their concentration was relatively low. With the complexation of α-casein, the maximum concentration (Cmax) of bioavailable anthocyanins and metabolites could increase by 1.5-10.1 times (P < 0.05 or P < 0.01). The promotional effect on the plasma absorption of malvidin-3-O-galactoside and vanillic acid was outstanding with the Cmax increasing from 0.032 to 0.323 and from 0.360 to 1.902 μg/mL, respectively (P < 0.01). Besides, the molecular docking models presented that anthocyanins could enter the structural cavity and interact with amino acid residues of α-casein, which was in accordance with the improved bioavailability of anthocyanins. Therefore, α-casein could assist more blueberry anthocyanins and their metabolites to enter blood circulation.
Keywords: blueberry anthocyanins; metabolites; pharmacokinetic analysis; plasma absorption; α-casein.