摘要
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。
AIM:To study the effects of Trilliuo, Lc253 and Lc239, which belong to a group of structurally similar diosgenyl saponins, on Ca + release in cultured primary rat cardiomyocytes. METHOD: Cardiomyocytes were cultured and loaded with fluo3-AM. [Ca2 + ]; was measured by fluorescent intensity in each cell with laser confocal microscopy. RESULT: Lc253 enhanced the frequency from 10+2 to 20+3 beat/min, and simultaneously induced a very obvious increase in the peak fluorescent intensity (pFI) of [Ca2+ ]; in a concentration-dependent manner: the pFI was maintained at a high level followed by addition of CaCl2 10 mmol/L or KC1 60 mmol/L. However, Trilliuo and Lc239 10 mmol/L, which had little effect on spontaneous Ca2 + release activity, prevented the increase in frequency and pFI of Ca + oscillation caused by high extracellular Ca2+ or K+ . These actions were similar to those in verapamil-treated cells showing q calcium channel blocking affect. CONCLUSION: These results indicated that the different actions of three saponins on intracellular Ca2+ patterns are associated with their structure, and number of sugar residues in the sugar chain which seems to play an important role to regulate Ca 2+ influx. These saponins are potential for their effects on Ca2+ channels of cardiomyocytes.
出处
《中国天然药物》
SCIE
CAS
CSCD
2003年第1期41-43,共3页
基金
国家自然科学基金(No.29802008)
江苏省杰出青年学者基金资助项目~~
