荷叶碱药理作用的研究进展

Advance of Pharmacological Studies on Nuciferine

荷叶碱是来源于睡莲科植物莲干燥叶中的一种阿朴啡类生物碱,也是《中国药典》收载荷叶这味中药的质控成分。现代研究表明,荷叶碱具有降脂、降糖、抗肿瘤、抗脑缺血等多种药理作用,具有广阔的开发前景。但荷叶碱自身存在水溶性差、药物安全性数据缺失、生物利用度争议较大等成药性缺陷,极大地影响了荷叶碱的深入研究与开发。因此,如何从众多药理活性中获得启发,进而选择最适合荷叶碱产品开发的临床适应症,依据制剂或化学手段改善其溶解性和生物利用度,同时降低毒副作用的发生,是当前迫切需要解决的问题。该文在回顾荷叶碱的理化性质及药动学研究报道的基础上,系统总结了其药理活性及作用机制,以期为荷叶碱药理作用的深入研究及创新品种的开发提供参考。

Nuciferine is a key aporphine alkaloid in the dried leaves of Nelumbo nucifera Gaertn(LNNG),which is also the quality control component of LNNG in Chinese Pharmacopoeia.It is reported that nuciferine has many pharmacological effects,such as lipid-lowering,anti-hyperglycemia,anti-tumor,anti-cerebral ischemia,and has a broad development prospect.However,there are some medicinal defects,such as poor water solubility,lack of safety data,and controversy of bioavailability,which greatly affect the in-depth research and development of nuciferine.Therefore,how to choose the most suitable clinical indications from massive pharmacological activities,improve its solubility and bioavailability through preparation or chemical method,and reduce the occurrence of toxic and side effects,are urgent to be solved.In this paper,the physicochemical property,pharmacokinetic characteristics,pharmacological activity and underling mechanism of nuciferine were systematically summarized,which can be helpful for the further study of its pharmacological action and the development of innovative products.