摘要
目的:了解竹节参皂苷Ⅳa及其衍生物药理活性和作用机制的研究进展,为其进一步开发利用提供参考。方法:以"竹节参""竹节参皂苷""竹节参皂苷Ⅳa""衍生物""药理活性""Chikusetsusaponin""ChikusetsusaponinⅣa""Panacis Japonici""Derivative""Pharmacological activity"等为关键词,组合查询1989年1月-2017年12月发表并收录于中国知网、万方、维普、Pub Med、Web of Science等数据库的相关文献,就竹节参皂苷Ⅳa及其衍生物的种类、药理活性、作用机制及靶点进行归纳与总结。结果与结论:共检索得到相关文献489篇,其中有效文献43篇。具药理活性的相关化合物包括竹节参皂苷Ⅳa、竹节参皂苷Ⅳa甲酯、竹节参皂苷Ⅳa丁酯、去葡萄糖竹节参皂苷Ⅳa,主要药理活性为保护心/脑、调节代谢、抗炎、抗凝血、抗肿瘤、抗病毒等。其相关作用机制及靶点主要包括激活沉默信息调节因子2相关酶1/细胞外调节蛋白激酶1/2/突触后膜骨架蛋白Homer1a途径,增强机体清除氧自由基的能力、降低心肌细胞膜脂质过氧化的程度,上调同源丢失性磷酸酶张力蛋白、下调核因子κB的表达,调节Ca2+、K+、Na+等离子的跨膜转运,促进糖原合酶激酶3β的磷酸化,抑制蛋白激酶C的磷酸化,抑制细胞外因子/β-联蛋白信号通路,抑制炎症因子表达,抑制血小板聚集,诱导肿瘤细胞周期停滞及凋亡,导致病毒直接失活或抑制子代病毒释放等。目前尚缺乏竹节参皂苷Ⅳa及其衍生物单体药理活性及作用机制的系统性深入研究,同时上述化合物是否具有其他药理作用、其药动学特征及剂型研发等均有待进一步探索。
引文
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