Abstract: Objective: To study on bioative detetion and cell-based absorption mechanisms of gastrointestinal hydrolysis derived from bovine casein. It can further elucidate physiological mechanisms of food protein to humanbeing.Methods: Bovine milk casein was hydrolyzed in vitro simulating gastrointestinal digestion.The hydrolysate's antioxidant and antimicrobial activity were detected through the DPPH free radical clearance rate analysis and the bacteriostatic ring size determination. In addation, Caco-2 monolayer cell model was optimizated and established to simulate the membrane absorption of hydrolysate. RP-HPLC was used to analyze the digestive juices before and after across the membrane.Results: It showed the DPPH free radical clearance rates reached maximum, 46.40% of 2 h-Gastricand 56.7% of 2h-Gastroin-testinal digestions from bovine casein.At the same time, the inhibition activity on Escherichia coli and Staphylococcus aureus also achieve maximum. Experiment results showed that hydrolyzed 2 h stomach simulation peptide absorption nitrogen bioavailability of 7.79%, 2 h hydrolyzed imtestines simulation of 15.11%, after the flat.The peptide can be successfully absorb water into single cell layer under the side, but most hydrophobic peptide by not easily, easy degradation or stop.Conclusion: The gastrointestinal hydrolysate of casein can produce bioactive peptides as well as absorb by intestinal cell monolayer.