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目的:探讨小檗碱对平滑肌肌球蛋白功能及胃肠平滑肌收缩性的影响。方法:以平滑肌肌球蛋白Mg2+-ATPase活性、肌球蛋白磷酸化以及胃与肠道平滑肌的收缩振幅为指标,考察小檗碱对平滑肌肌球蛋白Mg2+-ATPase活性和肌球蛋白磷酸化程度的影响,及其对离体小肠与胃平滑肌条收缩性的影响。结果:(1)在肌球蛋白轻链的Ca2+依赖性磷酸化反应中,小檗碱能抑制磷酸化肌球蛋白Mg2+-ATPase活性;(2)在肌球蛋白轻链的Ca2+依赖性磷酸化反应中,小檗碱可显著抑制磷酸化肌球蛋白轻链磷酸化程度;(3)小檗碱对大鼠离体小肠及胃平滑肌条收缩性均具有抑制作用。且均呈剂量依赖性。结论:小檗碱可通过抑制平滑肌肌球蛋白的功能,抑制胃肠道平滑肌的收缩性。
Objective: To investigate the effect of berberine on smooth muscle myosin function and gastrointestinal smooth muscle contraction. Methods: The effects of berberine on the activity of myosin Mg2 + -ATPase and myosin phosphorylation of smooth muscle were investigated with the activity of myosin Mg2 + -ATPase, myosin phosphorylation and the amplitude of gastric and intestinal smooth muscle contraction Effect, and its impact on contractility of isolated small intestine and gastric smooth muscle strips. RESULTS: (1) Berberine inhibited phosphorylation of myosin Mg2 + -ATPase in the Ca2 + -dependent phosphorylation of myosin light chain; (2) Ca2 + -dependent phosphorylation of myosin light chain In the reaction, berberine could significantly inhibit the phosphorylation of myosin light chain phosphorylation; (3) Berberine inhibited the contractility of isolated rat small intestine and gastric smooth muscle strips. And all in a dose-dependent manner. Conclusion: Berberine can inhibit the contraction of gastrointestinal smooth muscle by inhibiting the function of smooth muscle myosin.