Objective:To observe uptake process of shikonin（SKN） in Caco-2 cell.Method: The concentration of SKN in cells was detected by HPLC and the mechanism of SKN absorption in cells was explored by studying the influencing of time

pH

drug concentration and inhibitors on the uptake of SKN in cells.Result: SKN in Caco-2 cells uptake was time-dependent;SKN at 0.2-3.2 mg · L-1 concentration range of uptake increased linearly

which was consistent with passive diffusion process.The drug intake amount（0.350±0.004）mg · g-1 under pH 8.0 was significantly lower than pH 5.0（0.450±0.008）mg · g-1

（P<0.01）.Compared with the control group

SKN cell uptake was significantly higher after addition of verapamil[（0.320±0.007）mg · g-1

P<0.01]

sodium azide [（0.340±0.003）mg · g-1

P<0.05]and 2

4-dinitrophenol[（0.260±0.007）mg ·g-1

P<0.01].Conclusion: The mechanism of SKN absorption in cells mainly is passive transport and P-glycoproteins does not participate in the conveying process of SKN in Caco-2 cells.