胃肠安丸对大鼠离体回肠平滑肌收缩的影响  

Effects of Weichang′an Pill on contraction of isolated ileum smooth muscles in rats

作　　者：王娜 陆兴玥 高盼微 贾思童 王怡[1] 苗琳[1] 张晗[1] 柴丽娟[1] WANG Na;LU Xing-yue;GAO Pan-wei;JIA Si-tong;WANG Yi;MIAO Lin;ZAHNG Han;CHAI Li-juan(Institute of Traditional Chinese Medicine,Tianjin University of Traditional Chinese Medicine,Tianjin Key Laboratory of Traditional Chinese Medicine Pharmacology,Tianjin 301617,China)

机构地区：[1]天津中医药大学中医药研究院,天津市中药药理重点实验室,天津301617

出　　处：《中国药理学通报》2023年第9期1774-1781,共8页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No 81102860);天津中新药业集团股份有限公司开发项目(No.HX2018-30)。

摘　　要：目的研究胃肠安丸(Weichang′an pill,WCA)、胃肠安丸醇提物(Ethanol extract of Weichang′an pill,EE)、胃肠安丸水提物(Water extract of Weichang′an pill,WE)及其活性成分对乙酰胆碱(Acetylcholine,ACh)诱导的大鼠离体回肠平滑肌收缩的影响及机制。方法采用离体组织浴实验,在ACh的作用下,加入WCA、EE、WE或其活性成分,记录离体大鼠回肠平滑肌的收缩张力;通过分子对接的方法探究活性成分与毒蕈碱型乙酰胆碱M3受体的结合亲和力。结果WCA、EE、WE均可明显抑制ACh诱导的回肠平滑肌兴奋性收缩。活性成分木香烃内酯、去氢木香内酯、檀香醇、麝香酮、大黄素、大黄酚、大黄素甲醚、巴豆苷、厚朴酚及和厚朴酚也对ACh诱导的回肠平滑肌收缩有明显的抑制作用。结论WCA、EE、WE及其活性成分可能通过阻断回肠平滑肌细胞膜上的M3受体与ACh的结合,发挥促进肠平滑肌松弛的作用。Aim To investigate the impact and mechanism of Weichang′an Pill(WCA),its ethanol extract(EE),water extract(WE),and active ingredients on the contraction of isolated rat ileum smooth muscles induced by acetylcholine(ACh).Methods In vitro tissue bath experiment,WCA,EE,WE,or their active ingredients were added under the action of ACh,and then the contraction tension of isolated ileum smooth muscle from rats was recorded.The binding affinity of the active ingredients to the muscarinic acetylcholine M3 receptor was explored by molecular docking.Results WCA,EE,and WE were able to considerably inhibit the excitatory contraction of the ileal smooth muscles induced by ACh.Costunolide,dehydrocostus lactone,santalol,muscone,emodin,chrysophanol,physcion,crotonoside,magnolol,and honokiol were also significantly effective against ACh-induced ileal smooth muscle contraction.Conclusions WCA,EE,WE,and their active ingredients may help to promote intestinal smooth muscle relaxation by blocking the binding of the M3 receptor on the membrane of ileal smooth muscle with ACh.

关 键 词：胃肠安丸 醇提物 水提物 活性成分 回肠平滑肌 ACH 

分 类 号：R-332[医药卫生] R284.1R285.5R322.45R322.74