羟基酪醇的药理作用和药代动力学研究进展

Research Progress on Pharmacological Action and Pharmacokinetics of Hydroxytyrosol

羟基酪醇(HT)是以酯类形式广泛存在于木犀科植物油橄榄的枝叶和果实中的多酚类化合物,是天然的抗氧化剂之一。近年来,大量研究发现,HT在代谢综合征、心血管疾病、神经退行性疾病等方面均有较好的活性,能够有效抗癌、抗炎、抗抑郁等;此外,HT属于亲水亲油性物质,具有较高的生物利用度和细胞毒性小的特点,能够快速分布于各组织器官且易透过血脑屏障。因此,研究人员将其视为新药开发的重点研究对象;但该药物在体内半衰期短,靶向性差,临床应用往往受到限制,仍需更深入的研究。笔者查阅了近年来国内外有关HT的报道,并对其基本性质、药理作用及作用机制、药代动力学进行归纳总结,着重介绍了HT的抗氧化应激损伤、缓解心血管疾病、抑制神经退行性疾病等的药理活性及作用机制,并对其抗炎、抗肿瘤、抗抑郁等生物活性以及体内药代动力学的现有研究进行简要综述,同时对其未来研究方向提出建议,以期为HT的进一步开发、研究和临床应用提供参考。

Hydroxytyrosol as one of natural anti-oxidants,extracted from the fruits and leaves of Olea europaea,is a natural polyphenol compound in the form of esters. Recently,considerable studies showed that hydroxytyrosol demonstrated intrinsic biological activity for metabolic syndromes, cardiovascular-and neurodegenerative-related diseases,and it was revealed to play the roles in the anti-activities of cancerous,inflammatory as well as depressing issues. In addition,hydroxytyrosol is an oleophilic and hydrophilic compound with high bioavailability and low cellular cytotoxicity. It could be absorbed by various tissues and could easily passe through blood brain barrier. Therefore,hydroxytyrosol was introduced as one of the key subjects targeted by innovative drug development. However,it has a short half-life in vivo and non-tissue specific,which lead to its limitation in clinical application,so further in-depth studies are still needed. The authors had a literature review of hydroxytyrosol,and summarized the basic properties of its pharmacokinetic,pharmacological effects and molecular mechanisms. This article mainly focused on it’s pharmacological activity and the mechanism involved in treating damages induced by the oxidative stress,in alleviating cardiovascular diseases and in inhibition of neurodegenerative diseases. In this article, its anti-inflammatory,anti-tumor,anti-depressant effects,other biological activities,and pharmacokinetics were also briefly reviewed. The authors put forward some personal thoughts on its future research direction,hoping to provide ideas and inspirations for the vast number of researchers,and provide references for its further development,research and application.