葛根素的非内皮依赖性血管舒张作用机制Endothelium-independent vasorelaxant effect of puerarin on rat thoracic aorta
董侃,陶谦民,夏强,单绮娴,潘国标
DONG Kan 1, TAO Qian-min 1, XIA Qiang 2, SHAN Qi-xian 2, PA N Guo-biao 1 (1. Department of Cardiovascular, The First Affiliated Hospital, Z hejiang University School of Medicine, Hangzhou 310003, China; 2. Department of Physiology, Zhejiang University School of Medicine,Hangzhou 310003, China) [
摘要(Abstract):
目的 :研究葛根素对血管的舒张作用并探讨其机制。方法 :记录离体大鼠胸主动脉环张力反应。结果 :葛根素能明显舒张由苯肾上腺素诱导收缩的大鼠主动脉环 ,其血管舒张作用为非血管内皮依赖性 ;KCl预收缩下 ,葛根素对主动脉环无舒张作用。对去内皮的血管环 ,在无Ca2 + 溶液中 ,葛根素不能够抑制咖啡因或苯肾上腺素诱导的短暂收缩。钾通道阻断剂 4 氨基吡啶和四乙胺孵育后能够明显抑制葛根素的舒张血管作用 ,但格列苯脲不能抑制其舒张血管作用。结论 :葛根素的血管舒张作用是非内皮依赖性的 ,其机制可能是通过抑制α肾上腺素受体介导的血管平滑肌细胞外Ca2 + 内流而起作用的。同时 ,KV 通道和ATP敏感性K+ 通道参与了葛根素的舒血管作用。
Objective: To investigate the vasorelaxan t effect of puerarin in rat aortic rings and the mechanism. Method: The isolated thoracic aortic rings of male Sprague-Dawley rats were mounted on the organ bath and the contractile responses of the vessel were recorded. Result: Puerarin completely relaxed the contractions induced by phenylephrine in a concentration-dependent manner in en dothelium-intact and endothelium-denuded rat aorta,but it had no effect on th ose preconstricted by a high concentration of potassium chloride (KCl, 60 mmol ·L -1 ). The relaxant effect of puerarin was significantly inhibited by pr etreatment of endothelium-denuded aorta with potassium channel antagonists tetr aethylammonium,4-aminopyridine but not glibenclamide. Conclusion: Puerarin induces an endothelium-independent relaxation in rat aorti c rings. The mechanisms may involve the reduction in Ca 2+ influx through the calcium channels operated by α-adrenergic receptor and the activation of t he potassium channels (K V and BKca, but not K ATP ). [
关键词(KeyWords):
葛根素;主动脉环;α肾上腺素受体;钾通道
puerarin; aortic ring; α-adrenergic rec eptor; potassium channel
基金项目(Foundation):
作者(Author):
董侃,陶谦民,夏强,单绮娴,潘国标
DONG Kan 1, TAO Qian-min 1, XIA Qiang 2, SHAN Qi-xian 2, PA N Guo-biao 1 (1. Department of Cardiovascular, The First Affiliated Hospital, Z hejiang University School of Medicine, Hangzhou 310003, China; 2. Department of Physiology, Zhejiang University School of Medicine,Hangzhou 310003, China) [
Email:
DOI:
参考文献(References):
- [1] 柴象枢葛根素的抗心律失常作用中国药理学报,1985,(3):166
- [2] 黄漫翔,斐 红,林万莲葛根素对心血管系统作用的研究进展广东药学,2000,10(2):9
- [3] 陈连壁,柴 强葛根素对犬脑血流的影响中国中药杂志,1995,20(9):560
- [4] 金昔陆葛根素的药理及临床应用中国临床药学杂志,1996,5(3):130
- [5] 韩启德血管生物学北京:北京医科大学和北京协和医科大学联合出版社,199750
- [6] Rembold,CM RegulationofcontractionandrelaxationinarteriasmoothmuscleHypertension,1992,20(2):129
- [7] Bean,BP ClassesofcalciumchannelsAnnuRevPhysiol,1989,51:367
- [8] NelsonMT ,QJ Physiologicalrolesandpropertiesofpotassiumchan nelsinarterialsmoothmuscleAmJPhysiol,1995,268:C799
- [9] William,FJ IonchannelsandvasculartoneHypertension,2000,35(2):173
- [10] 苗维纳,沈映君,曾晓荣,等葛根素对豚鼠心室肌细胞钾离子通道的影响中国应用生理学杂志,2002,18(2):155
- [11] 张广钦,郝雪梅,周培爱,等葛根素抑制小鼠海马CA1区神经元瞬间外向钾电流和延迟整流钾电流中国药理学报,2001,22(3):253
- 董侃
- 陶谦民
- 夏强
- 单绮娴
- 潘国标
DONG Kan 1 - TAO Qian-min 1
- XIA Qiang 2
- SHAN Qi-xian 2
- PA N Guo-biao 1 (1. Department of Cardiovascular
- The First Affiliated Hospital
- Z hejiang University School of Medicine
- Hangzhou 310003
- China
- 2. Department of Physiology
- Zhejiang University School of Medicine
- Hangzhou 310003
- China) [
- 董侃
- 陶谦民
- 夏强
- 单绮娴
- 潘国标
DONG Kan 1 - TAO Qian-min 1
- XIA Qiang 2
- SHAN Qi-xian 2
- PA N Guo-biao 1 (1. Department of Cardiovascular
- The First Affiliated Hospital
- Z hejiang University School of Medicine
- Hangzhou 310003
- China
- 2. Department of Physiology
- Zhejiang University School of Medicine
- Hangzhou 310003
- China) [