Abstract: In order to research the effect of αspinasterol on the intestine transporters Pgp and PEPT1 when the tylenol tartrate was introduced as a substrate， 48 mice were equally divided into 4 treatment groups: αspinasterol group， tylenol tartrate group， mixed （αspinasterol and tylenol tartrate） group， and normal saline group which was used as control group. The formulations were administered by oral gavage with a dose of 0.2 mL·10 g-1 depending on body weight of mice. The small intestine samples of the dissected mice were excised at predetermined time intervals （1， 3， 5）. The expressions of Pgp and PEPT1 on the mice intestines were detected by immunohistochemical method at 1， 3, 5 d, respectively. The results showed that the protein expression of Pgp was distinctly reduced in αspinasterol and mixed groups， and the protein expression of PEPT1 was increased in these 2 groups compared with normal saline group. However， the protein expression of Pgp was increased and the protein expression of PEPT1 was decreased in tylenol tartrate group compared with normal saline group. The difference was more obvious with time pass by. In summary， αspinasterol had an obvious impact on intestine transporters， including inhibiting Pgp expression and inducing PEPT1 expression.

Key words: αspinasterol, mice, drug transporter, Pgp, PEPT1