Effect of Epoxyaurapten on the Function of Myosin and the Contractility of Intestinal Smooth Muscle

XU Zhi-li1; ZHANG Ying2; TAO Xiao-jun1; YAN Yu-hui1

doi:10.13422/j.cnki.syfjx.2012.08.063

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Effect of Epoxyaurapten on the Function of Myosin and the Contractility of Intestinal Smooth Muscle

更新时间：2024-09-23

- Effect of Epoxyaurapten on the Function of Myosin and the Contractility of Intestinal Smooth Muscle
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 18, Issue 8, Pages: 170-174(2012)
- 作者机构：
  
  1. 辽宁中医药大学药学院
  2. 大连市儿童医院
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2012.08.063
  CLC： R285.5
- Published：2012
- 稿件说明：
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[1]徐志立,张莹,陶小军,闫宇辉.环氧橙皮油素对平滑肌肌球蛋白功能及肠平滑肌收缩性的影响[J].中国实验方剂学杂志,2012,18(08):170-174.

XU Zhi-li1, ZHANG Ying2, TAO Xiao-jun1, et al. Effect of Epoxyaurapten on the Function of Myosin and the Contractility of Intestinal Smooth Muscle[J]. Chinese journal of experimental traditional medical formulae, 2012, 18(8): 170-174.
[1]徐志立,张莹,陶小军,闫宇辉.环氧橙皮油素对平滑肌肌球蛋白功能及肠平滑肌收缩性的影响[J].中国实验方剂学杂志,2012,18(08):170-174. DOI： 10.13422/j.cnki.syfjx.2012.08.063.

XU Zhi-li1, ZHANG Ying2, TAO Xiao-jun1, et al. Effect of Epoxyaurapten on the Function of Myosin and the Contractility of Intestinal Smooth Muscle[J]. Chinese journal of experimental traditional medical formulae, 2012, 18(8): 170-174. DOI： 10.13422/j.cnki.syfjx.2012.08.063.

摘要

目的:探讨环氧橙皮油素对平滑肌肌球蛋白功能及肠平滑肌收缩性的影响。方法:在纯化的蛋白体系中进行平滑肌肌球蛋白Ca2+依赖性磷酸化反应

采用甘油聚丙烯酰胺凝胶电泳测定肌球蛋白轻链磷酸化程度

孔雀绿法测定肌球蛋白Mg2+-ATPase活性。以平滑肌肌球蛋白Mg2+-ATPase活性、肌球蛋白磷酸化以及在克氏液中孵育的肠平滑肌收缩振幅为指标

考察环氧橙皮油素对平滑肌肌球蛋白Mg2+-ATPase活性和肌球蛋白磷酸化程度的调节作用

以及环氧橙皮油素对大鼠离体小肠平滑肌收缩性的影响。结果:在肌球蛋白轻链的Ca2+依赖性磷酸化反应中

在40～320μmol·L-1浓度内环氧橙皮油素能抑制磷酸化肌球蛋白Mg2+-ATPase活性及其轻链磷酸化程度（P<0.01）

这种抑制作用与1-（5-氯-1-萘-磺酰）-六氢-1

4-二氮杂卓（ML-9）具有协同作用;40～320μmol·L-1浓度内环氧橙皮油素可剂量依赖性抑制大鼠离体小肠平滑肌收缩

且可拮抗新斯的明、乙酰胆碱引起的促进收缩作用

相加阿托品引起的抑制收缩作用（P<0.01）。结论:环氧橙皮油素可通过抑制平滑肌肌球蛋白的功能

抑制胃肠平滑肌的收缩性。

Abstract

Objective:To investigate the effects of epoxyaurapten on the function of smooth muscle myosin and the contractility of isolated intestinal smooth muscle strips.Method: Mg2+-ATPase activity and phosphorylation of myosin and contractility of isolated intestinal smooth muscle strips were chosen to determine the effects of epoxyaurapten on the activity of smooth muscle myosin and smooth muscle contractility.Result: Epoxyaurapten（40-320 μmol·L-1） exerted inhibitory effects on myosin Mg2+-ATPase activity in the presence of Ca2+/calmodulin and in a dose-dependent manner;and epoxyaurapten（40-320 μmol·L-1） exerted inhibitory effects on myosin phosphorylation in the presence of Ca2+/calmodulin and in a dose-dependent manner.Epoxyaurapten inhibited the muscle contraction of isolated rat intestinal strips in a dose-dependent manner

antagonized the stimulation induced by neostigmine and acetylcholine.Synergy inhibition on contractile activity was induced by concurrent use of atropine.Conclusion: Epoxyaurapten has prominent inhibition on the contractile activity of isolated rat intestine strips

which may be related to inhibition of the function of smooth muscle myosin.

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