摘要
脑缺血再灌注损伤(CIRI)是缺血性脑卒中血流供应恢复后出现的脑组织结构和功能进一步损伤的现象,严重影响患者生存质量。CIRI的病理机制复杂,主要涉及兴奋性氨基酸毒性、细胞凋亡、炎症及氧化应激损伤等。研究发现,中药材及其活性成分在CIRI的防治方面显现出独特优势和良好应用前景。槲皮素为植物性黄酮类化合物,广泛存在于多种中药,已有研究证实其可通过抗炎、抗氧化、抑制细胞凋亡、保护血脑屏障、激活线粒体自噬等多种途径改善CIRI,减轻脑损伤,但对于其具体作用机制及分子靶点的研究略有不足。此外,研究人员针对槲皮素生物利用度低和溶解性差的问题,研制出多种改善槲皮素生物活性成分分散状态,提高化学稳定性,增加临床应用率的递送系统;并针对槲皮素长期使用的安全性进行了实验评价,证实低剂量使用槲皮素具有较好的耐受性及安全性。综上,笔者通过对近年来国内外相关文献进行分析,对槲皮素治疗CIRI的作用靶点及机制研究、药物递送及安全性评价等予以综述,以期为槲皮素的进一步开发和推广应用提供理论依据。
Cerebral ischemia-reperfusion injury(CIRI)is a further injury of brain tissue after the recovery of blood supply in ischemic stroke,which seriously affects the quality of life of patients.The pathological mechanism of CIRI is complex,mainly involving excitatory amino acid toxicity,apoptosis,inflammation,and oxidative stress.Studies have proved that Chinese herbal medicines and their active components have unique advantages and good application prospects in the prevention and treatment of CIRI.Quercetin is a flavonoid ubiquitous in a variety of Chinese medicinal herbs.It can alleviate CIRI and reduce brain injury through inhibiting inflammation,oxidation,and apoptosis,protecting blood-brain barrier,and activating mitophagy.However,little is known about the specific mechanism and molecular targets.In view of the low bioavailability and poor solubility of quercetin,researchers have developed a variety of delivery systems to facilitate the dispersion of quercetin,improve chemical stability,and increase clinical application.Furthermore,researchers have tested the long-term safety of quercetin and confirmed that low-dose quercetin has good safety.By reviewing the relevant studies in recent years,we summarized the targets,mechanism,delivery,and safety of quercetin in the treatment of CIRI,aiming to provide a theoretical basis for the further development and application of quercetin.
作者
娄原
姜雅楠
徐浩群
王媛
LOU Yuan;JIANG Yanan;XU Haoqun;WANG Yuan(College of Traditional Chinese Medicine(TCM),Shandong University of TCM,Jinan 250355,China;Shandong Co-Innovation Center of Classic TCM Formula,Jinan 250355,China)
出处
《中国实验方剂学杂志》
CAS
CSCD
北大核心
2022年第17期248-257,共10页
Chinese Journal of Experimental Traditional Medical Formulae
基金
山东省自然科学基金面上项目(ZR2021MH327)
山东省高等学校青创科技支持计划项目(2019KJK013)
济南市高校院所创新团队项目(2020GXRC012)
山东中医药大学青年科研创新团队项目(2020-54-17)
山东省高校青创人才引育计划项目(鲁教人字[2019]9号-202/201)。
关键词
槲皮素
脑缺血再灌注损伤
作用机制
药物递送
安全性评价
quercetin
cerebral ischemia-reperfusion injury
mechanisms of action
drug delivery
safety evaluation
作者简介
第一作者:娄原,在读硕士,从事中西医结合心脑血管疾病的防治研究.E-mail:Louyuan1995@163.com;通信作者:王媛,博士,副教授,从事中西医结合心脑血管疾病的防治研究.E-mail:demi0531@163.com。
