【摘要】 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（P<O.05）,属非竞争性拮抗。B、C、D28.0、56.0μmol/L及Ver0.28μmol/L均抑制离体大鼠回肠对CaCl₂的反应,具显著性差异。B、C或 D28.0.56.μmol/L与Atr0.19μmol/L共同孵育具有协同作用,可降低回肠对Ach的反应性。B、C、D56.μmol/L可抑制由Neo2.15μmol/L引起的大鼠回肠痉挛;改良酚红糊剂法证明B、C、D 28.0mg/kg可以显著抑制小鼠胃肠推进运动。结果提示B、C、D为白术中抑制胃肠运动的有效成分,其作用机理与胆碱受体及Ca²⁺”的抑制有关。更多还原

【Abstract】 Atractylenolide I (8,9-dehydroasterolide, B), 4,15-epoxy-8 β - hydroxyasterolide (C) and atractyleno-lide Ⅲ (8 β- hydroasterolide, D) from Atractylodes macrocephala Koidz, 28.0、56.0 μmol/L, inhibited the spontaneous movement of rat isolated ileum with contractile force decreased obviously (P <0.001), but the rest force not affected (P >0.05). B、C and D inhibited the spasm enhanced by Ach and His to rat ileum, rightly shifted the dose - response curves and reduced the maximal response (P <0.05). Pretreatment with B、C or D 28.0、56.0 μmol/L Ver 0.28 μmol/L significantly antagonized CaCl2-induced contraction of rat isolated ileum. Co bathing of B、C or D 56.0 μmol/L with Atr 0.19 μmol/L weakened the response of ileum to Ach. B、C or D 56.0 μmol/L restrained the spasm of ileum mediated by Neo 2.15 μmol/L. The modified Phenol Red Paste Model demonstrated that B、C or D in dose of 28.0 mg/kg inhibited the gastrointestinal prochoresis of mice significantly. These results suggested that B、C and D inhibit the gastrointestinal movement of rat and the spasm induced by the agonists. Their activities are related to the inhibition of cholinergic system and Ca2+.更多还原