CAJ | 학술논문

目的:探讨色满类化合物HEF-19对家兔离体小肠平滑肌的舒张作用及其机制.方法:采用家兔小肠离体实验法, 观察HEF-19对家兔离体小肠自发活动的影响, 研究BaCl2诱导收缩时格列苯脲(10-5 mol/L)、维拉帕米(10-7 mol/L )、酚妥拉明(10-7 mol/L)和普奈洛尔(10-7 mol/L)对HEF-19的舒张作用的影响.结果:HEF-19可以剂量依赖性地降低家兔离体小肠平滑肌自发性收缩的张力和振幅; 分别加入格列苯脲和维拉帕米孵育后,HEF-19(10-6 mol/L-10-3 mol/L)的舒张量效曲线均发生明显变化, EC50值分别由4.36±0.12mol/L和4.43±0.19 mol/L转变为4.16±0.22mol/L和3.96±0.24 mol/L, 差异具有统计学意义(P <0.05). 酚妥拉明和普奈洛尔对HEF-19的舒张作用没有影响.结论:HEF-19具有舒张小肠平滑肌的作用并且其作用机制与ATP-敏感性钾通道和L 型钙通道开放有关.而与α受体和β受体无关.
목적:탐토색만류화합물HEF-19대가토리체소장평활기적서장작용급기궤제.방법:채용가토소장리체실험법, 관찰HEF-19대가토리체소장자발활동적영향, 연구BaCl2유도수축시격렬분뇨(10-5 mol/L)、유랍파미(10-7 mol/L )、분타랍명(10-7 mol/L)화보내락이(10-7 mol/L)대HEF-19적서장작용적영향.결과:HEF-19가이제량의뢰성지강저가토리체소장평활기자발성수축적장력화진폭; 분별가입격렬분뇨화유랍파미부육후,HEF-19(10-6 mol/L-10-3 mol/L)적서장량효곡선균발생명현변화, EC50치분별유4.36±0.12mol/L화4.43±0.19 mol/L전변위4.16±0.22mol/L화3.96±0.24 mol/L, 차이구유통계학의의(P <0.05). 분타랍명화보내락이대HEF-19적서장작용몰유영향.결론:HEF-19구유서장소장평활기적작용병차기작용궤제여ATP-민감성갑통도화L 형개통도개방유관.이여α수체화β수체무관.
AIM: To study the relaxant effect of a chromane HEF-19 on isolated small intestinal smooth muscle of rabbits and its underlying mechanism. METHODS: Routine experimental methods using isolated small intestine smooth muscle of rabbits, the effect of HEF-19 on automatic contraction of small intestinal smooth muscle was investigated. The relaxant effects of glibenclamide (10-5 mol/L), Verapamil (10-7 mol/L) Phentolamine (10-7 mol/L) and Propranolol (10-7 mol/L) on HEF-19 with contraction induced by BaCl2 were studied. RESULTS: HEF-19 significantly attenuated the tension and amplitude of automatic contraction of isolated small intestinal smooth muscle in a dose-dependent manner. The relaxing concentration-response curves of HEF-19 (10-6-10-3 mol/L) were significantly different after incubation with glibenclamide (EC50: 4.16 ± 0.22 mol/L vs 4.36 ± 0.12 mol/L, P < 0.05 )and Verapamil (EC50: 3.96 ± 0.24 mol/L vs 4.43 ± 0.19 mol/L, P < 0.05). Phentolamine and Propranolol had no effect on relaxant effect of HEF-19. CONCLUSION: HEF-19 relaxes isolated small intestinal smooth muscle of rabbits and the mechanism may be related to K+-ATP opening and L-calcium channel but not related to α- receptor and β- receptor.