【摘要】 目的:研究羟基红花黄色素A(HSYA)对离体猪冠状动脉血管的舒张作用及其可能作用机制,为红花的生物学活性研究和应用提供参考。方法:以猪冠状动脉血管环为材料,以离体血管功能实验方法检测羟基红花黄色素A对猪冠状动脉血管活性作用。结果:羟基红花黄色素A对静息状态猪冠状动脉血管环无明显舒张作用;HSYA在10-4.5~10-2mol/L的浓度范围内对PGF2α(10-6mol/L)预收缩的冠状动脉血管环具有浓度依赖性舒张作用,最大舒张效应为124.22%±6.25%,相应的pD2值为2.91±0.23,HSYA的有效剂量为10-3mol/L,该剂量能使PGF2α(10-6mol/L)预收缩的冠状动脉血管环达到65.55%±4.15%的舒张效应;HSYA可使KCl的量效曲线下移,呈浓度依赖性。用一氧化氮合成酶抑制剂L-NNA、鸟苷酸环化酶抑制剂亚甲蓝、β受体阻断剂普萘洛尔、β1受体抑制剂atenolol和β2受体抑制剂ICI 118551预处理后,均可明显减弱HSYA诱导的舒张血管作用;前列腺素合成酶抑制剂吲哚美辛,K+通道抑制剂TEA预处理后,血管舒张作用不能被阻断。结论:羟基红花黄色素A的舒血管活性作用通过内皮-NO-cGMP途径和β-肾上腺素受体途径,并能够阻断血管平滑肌上的电压依赖性钙通道,但与血管平滑肌舒张因子前列腺素的释放及钾离子(KCa)通道无关。更多还原

【Abstract】 Objective: Through the study of hydroxysafflor yellow A on isolated porcine coronary artery vascular vasodilation function and its possible mechanism of action,as the study of biological activity and application of safflower reference. Methods: The materials was porcine coronary arterial rings,in vitro vascular function detection of hydroxysafflor yellow A vasoactive effects. Results: HSYA did not change the resting tension of porcine coronary arterial ring; but HSYA in 10-4. 5~ 10-2mol / L concentration range showed concentration-dependent relaxant effects with PGF 2α( 10-6mol / L)-pre-contracted coronary arteries,the two values were 124. 22% ± 6. 25%( Emax) and 2. 91 ± 0. 23( pD 2). The effective dose of HSYA is 10-3mol / L,The dose can make PGF 2α( 10-6mol / L)-pre-contracted coronary arteries get to 65. 55% ± 4. 15% relaxation effect. HSYA inhibited the KCl-induced contraction and downward shifted concentration-response curve of coronary artery rings. Incubation with L-NNA( an inhibitor of NOS),methylene blue( an inhibitor of cGMP synthesis),propranolol( β-adrenoceptor antagonist),β1-adrenoceptor antagonist atenolol,as well as β2-adrenoceptor antagonist ICI 118551 significantly attenuated the vaso-relaxation in porcine coronary rings induced by HSYA. However,incubation with indomethacin( an inhibitor of COX),tetraethylammonium( an inhibitor of K+channels) did not affect the vaso-relaxation. Conclusion: The effect of HSYA on vasodilator may relate to activation of β-adrenoceptors,dependent VDCC, and endothelium-NO-cGMP pathway,but not related to PGI2 pathway and potassium channels.更多还原