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白术内酯Ⅰ(B)、4,15-环氧羟基白术内酯(C)、白术内酯Ⅲ(D)28.0、56.0μmol/L能显著抑制大鼠离体回肠的自发运动,使收缩力降低(P<0.001),但对静息张力无明显影响(P>0.05)。B、C、D孵育后,可抑制由Ach、His所致大鼠离体回肠的痉挛作用,使Ach、His量效关系曲线右移,降低回肠的最大反应(P0.05). After incubation with B, C, and D, the ileal effects of Ach and His-induced ileum in rats were inhibited, and the Ach and His dose-response curves were shifted to the right and the ileal maximal response was reduced (P < 0.05). Non-competitive antagonism. B, C, D28.0, 56.0 μmol/L and Ver 0.28 μmol/L all inhibited the responses of rat ileum to CaCl 2 , showing significant differences. Co-incubation of B, C or D28.0.56 μmol/L with Atr 0.19 μmol/L had a synergistic effect, which reduced the ileal reactivity to Ach. B, C and D56.μmol/L could inhibit the rat ileum caused by Neo2.15μmol/L. The improved phenol red paste method proved that B, C and D 28.0mg/kg could significantly inhibit the gastrointestinal motility in mice. The results suggest that B, C, and D are effective ingredients for inhibiting gastrointestinal motility in Atractylodes macrocephala. The mechanism of action is related to inhibition of choline receptors and Ca 2+ .