色满类化合物HEF-05对兔离体血管平滑肌舒张作用的研究  

Relaxing effect of chroman hydrochloride HEF-05 on vascular smooth muscle in vitro of rabbits

作　　者：李建婷 付守廷[2] 胡春[3] LI Jian-ting;FU Shou-ting;HU Chun(Psychiatric Hospital ofChangsha,Changsha 410004;School of Life Science and Bio-Pharmaceutics,Shenyang Pharmaceutical University,Shenyang 110016;School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016)

机构地区：[1]长沙市精神病医院,长沙410004 [2]沈阳药科大学生命科学与生物制药学院,沈阳110016 [3]沈阳药科大学制药工程学院,沈阳110016

出　　处：《中南药学》2019年第2期195-198,共4页Central South Pharmacy

摘　　要：目的研究色满类化合物HEF-05对兔离体血管平滑肌的舒张作用。方法以兔降主动脉为标本,加入高钾液、氯化钡诱导收缩后,累积加入HEF-05,观察HEF-05舒张作用。收缩的兔降主动脉标本,加入四乙胺(TEA)、吲哚美辛溶液分别阻断钾通道及PGs类物质合成后,累积加入HEF-05,分析HEF-05舒张作用机制与钾通道、前列腺素类物质(PGs)的关系。标本去内皮后,观察HEF-05舒张作用与内皮关系。给予不同浓度HEF-05,观察其对氯化钙量效曲线的影响。结果 HEF-05降低由高钾溶液(60 mmol·L^(-1))、氯化钡(2 mg·mL^(-1))收缩的兔降主动脉;经四乙胺(TEA,3×10-5 mol·L^(-1))阻断后,HEF-05舒张兔降主动脉作用有明显变化;经吲哚美辛(1×10^(-6) mol·L^(-1))孵育或血管去内皮后,HEF-05舒张作用无显著变化。HEF-05能非竞争性抑制氯化钙收缩量效曲线。结论 HEF-05对收缩的兔降主动脉有舒张作用,其机制可能与钾通道及钙通道有关,与PGs类物质及内皮无关。Objective To determine the relaxing effect of HEF-05 on the descending aorta smooth muscle of rabbit. Methods The descending aorta of rabbits was used as the specimens, the effect of HEF-05 on agonistinduced contraction by High-K+and BaCl2 respectively was investigated in vitro. The experimental and relaxing effect of HEF-05 on the endothelium-intact(EC +) and endothelium-denuded(EC-) thoracic aortic rings were compared. Potassium channel blockers, and COX-inhibitoers were used to explore the association between the relaxing effects of HEF-05 with potassium channels, and prostaglandin-like substances respectively. The inhibition effect of HEF-05 on the dose-effect curve of CaCl2 was also observed. Results HEF-05 relaxed the descending aorta smooth muscle contraction by High-K+(60 mmol·L-1) or BaCl2(2 mg·m L^-1) in a dose-dependently way. Indomethacin(1×10^6 mol·L^-1) had no obvious contribution to the vasorelaxant effect of HEF-05. There was no difference in the relaxing effect of HEF-05 between EC + and EC-on the thoracic aortic rings. In contrast, the vasorelaxant effect of HEF-05 was significantly inhibited by TEA(3×10^-5 mol·L^-1). HEF-05 affected the doseeffect curve of CaCl2 in a non-competitive way. Conclusion The relaxant effect of HEF-05 on the descending aorta smooth muscle might be attributed to the potassium channels and calcium channels.

关 键 词：色满类化合物 血管平滑肌 舒张作用 钾通道 钙通道 

分 类 号：R96[医药卫生—药理学] R285.5[医药卫生—药学]