Protić Dragana, Radunović Nebojša, Spremović-Rađenović Svetlana, Živanović Vladimir, Heinle Helmut, Petrović Aleksandar, Gojković-Bukarica Ljiljana
Department of Pharmacology, Clinical Pharmacology and Toxicology, Faculty of Medicine, University of Belgrade, 11000, Belgrade, Serbia.
Drug Dev Res. 2015 Feb;76(1):17-23. doi: 10.1002/ddr.21236. Epub 2015 Jan 25.
Preclinical Research Potassium (K ) channels have a key role in the maintenance of smooth muscle tone; a variety of agonists can modify the tone by altering K -channel activity. The aim of this study was assess the effects of the phenols, resveratrol, and naringenin on K -channels of the vascular smooth muscle. Segments of human umbilical vein (HUV) without endothelium were precontracted using serotonin (100 μM) or 100 mM K to derive cumulative concentration-response curves using increasing concentrations of resveratrol or naringenin. K -channel inhibitors were added in the bath before resveratrol (1-100 μM) or naringenin (0.01-1 mM) in assess the role of K -channels in their effects on HUV precontracted by serotonin. 4-Aminopiridine (4-AP; 1 mM), a nonselective blocker of voltage-dependent, tetraethylammonium (TEA; 1 mM) and barium chloride (1 mM), a nonselective blocker of Ca -dependent and inward rectifier K -channels (respectively) induced significant shifts to the right (P < 0.05) of resveratrol. concentration-response curves. The effect of naringenin was antagonized by 4-AP (1 mM). 4-AP-, TEA-, and barium chloride-sensitive K -channels are probably involved in the resveratrol vasodilatatory effect, while naringenin seems to affect 4-AP-sensitive K -channels. However, other mechanisms of vasodilation induced by polyphenols could not be excluded. Drug Dev Res, 2015. © 2015 Wiley Periodicals, Inc.
临床前研究 钾（K⁺）通道在维持平滑肌张力方面起关键作用；多种激动剂可通过改变K⁺通道活性来调节张力。本研究旨在评估酚类、白藜芦醇和柚皮素对血管平滑肌K⁺通道的影响。使用血清素（100 μM）或100 mM K⁺对无内皮的人脐静脉（HUV）节段进行预收缩，然后使用浓度递增的白藜芦醇或柚皮素得出累积浓度-反应曲线。在加入白藜芦醇（1 - 100 μM）或柚皮素（0.01 - 1 mM）之前，先在浴槽中加入K⁺通道抑制剂，以评估K⁺通道在它们对血清素预收缩的HUV的作用中的角色。4-氨基吡啶（4-AP；1 mM），一种电压依赖性的非选择性阻滞剂，四乙铵（TEA；1 mM）和氯化钡（1 mM），分别是Ca²⁺依赖性和内向整流K⁺通道的非选择性阻滞剂，可使白藜芦醇的浓度-反应曲线显著右移（P < 0.05）。柚皮素的作用可被4-AP（1 mM）拮抗。4-AP、TEA和氯化钡敏感的K⁺通道可能参与了白藜芦醇的血管舒张作用，而柚皮素似乎影响4-AP敏感的K⁺通道。然而，不能排除多酚诱导血管舒张的其他机制。药物研发研究，2015年。© 2015威利期刊公司。
