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目的:著蓣皂苷元的皂苷为许多抗心血管中药中的主要活性成分,具有重要研究价值。本研究以经人工合成获得的著蓣皂苷元皂苷同系物甾体皂苷Trilliuo(署蓣皂苷元葡萄糖苷、Lc253[著蓣皂苷鼠李糖(1-2)葡萄糖苷]、Ic239(薯蓣皂苷元[鼠李糖(1-2),葡萄糖(1-3)]葡萄糖苷)为研究对象,通过考察它们对培养心肌细胞钙离子释放的影响,分析其构效关系。方法:利用激光共聚焦显微镜测定加入fluo3-AM培养的心肌细胞中的钙离子变化情况。结果:Ic253能明显增强心肌细胞节律性和呈浓度依赖性增加心肌细胞静息钙离子水平,加入CaCl210 mmoL/L or KCl 60 mmol/L后钙离子荧光峰强度仍维持在较高水平;而Trilliuo and Ic239在10-5mmol/L浓度时,对心肌细胞静息钙离子水平作用不明显,在高浓度胞外Ca2+或K+情况下,抑制心肌细胞内钙离子升高;其作用特点与verapamil相似,具有钙离子通道阻断作用。结论:研究结果显示三种甾体皂苷对细胞内钙离子浓度有所差异,结构中连接糖的数目与调孔钙内流的活性有重要的相关性。这些皂苷类化合物对钙离子通道的活性有潜在的开发价值。
Objective: To study the saponins of saponins is an important active ingredient in many anti-cardiovascular drugs and has important research value. In this study, the synthetically obtained saponins saponins homologues steroidal saponin Trilliuo (the Department of Saponin glucoside, Lc253 [saponins rhamnose (1-2) glucoside], Ic239 (diosgenin [ Rhamnose (1-2) and glucose (1-3) glucoside were studied for their effects on the release of calcium ions from cultured cardiomyocytes, and their structure-activity relationships were analyzed.Methods: Determination by laser confocal microscopy Calcium ion changes in cardiomyocytes cultured with fluo3-AM.Results: Ic253 can significantly increase the rhythm of cardiomyocytes and increase the resting calcium ion concentration of cardiomyocytes in a concentration-dependent manner, adding CaCl210 mmoL/L or KCl 60 mmol/L. The post-calcium fluorescence peak intensity remained at a relatively high level; while Trilliuo and Ic239 did not have a significant effect on the resting calcium ion level of cardiomyocytes at a concentration of 10-5 mmol/L, but inhibited in the presence of high concentrations of extracellular Ca2+ or K+. The increase of intracellular Ca2+ in cardiomyocytes is similar to that of verapamil and has the effect of blockade of Ca2+ channels.Conclusion: The results of the study show that three steroidal saponins have different intracellular calcium ion concentrations, and the number of linked sugars in the structure Adjustment hole Stream activity has important relevance. These saponins have potential value for the development of calcium channel activity.