细叶远志皂苷治疗痴呆的研究进展

Tenuifolin in Treatment of Dementia:A Review

细叶远志皂苷是远志的主要成分之一,常作为远志及其炮制品质量控制的重要指标。痴呆是一种较严重的、持续性的认知障碍,患病人数在全球不断攀升,给家庭和社会带来了巨大的经济痛苦和精神压力。目前上市的胆碱酯酶抑制剂等药物仅能缓解痴呆的症状,且存在一定的不良反应。研究发现,细叶远志皂苷有显著地改善认知障碍和学习记忆的功效,有望成为治疗痴呆的潜在药物。细叶远志皂苷可以通过多种机制有效对抗神经退行性病变产生的淀粉样β蛋白沉积、乙酰胆碱减少、神经炎症、细胞氧化损伤、神经细胞凋亡,对多种类型痴呆均有作用。另外,细叶远志皂苷可以迅速吸收入血,主要分布于肝脏和肾脏,且可以透过血脑屏障吸收入脑。同时也会在体内迅速消除,由于其较大的相对分子质量和较差的脂溶性,存在口服吸收利用度和血脑屏障透过率低等问题。因此,笔者总结了细叶远志皂苷化学质量控制、药效机制、药代动力学、毒理4个方面的内容,以期为细叶远志皂苷的深入研究和应用提供参考和思路。

Tenuifolin,a main component in Polygalae Radix,is frequently used as an important indicator for quality control of Polygalae Radix and its processed products.Dementia is a serious and persistent cognitive disorder,and the number of dementia patients is increasing worldwide,which brings great economic burden and mental pressure to families and society.At present,cholinesterase inhibitor and other drugs can only alleviate the symptoms of dementia,and there are some toxic and side effects.It has been found that tenuifolin can significantly improve cognitive disorder,learning and memory and is expected to be a potential drug for treating dementia.Tenuifolin exerts protective effects on amyloid-β(Aβ)deposition,acetylcholine reduction,neuroinflammation,cellular oxidative damage and nerve cell apoptosis caused by neurodegenerative diseases via multiple mechanisms,and can be applied to various types of dementia.In addition,it can be quickly absorbed into the blood,mainly distributed in liver and kidney,and can enter into the brain through the blood-brain barrier.However,because of its large molecular mass and poor fat solubility,tenuifolin can be rapidly eliminated,generating some problems such as low oral absoBrbability and permeability of blood-brain barrier.Therefore,the information of chemistry,pharmacology,pharmacokinetics and toxicology of tenuifolin was summarized in this paper to provide reference and ideas for further research and application.