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膳食槲皮素对脑缺血损伤的保护作用:药理学、药代动力学和生物利用度增强型纳米制剂。

Protective effects of dietary quercetin on cerebral ischemic injury: pharmacology, pharmacokinetics and bioavailability-enhancing nanoformulations.

机构信息

State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu 611137, China.

School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.

出版信息

Food Funct. 2023 May 22;14(10):4470-4489. doi: 10.1039/d2fo03122a.

Abstract

Cerebral ischemia, as an ischemic stroke-like disease, has become a health problem of global concern. Studies have found that oxidative stress, inflammation, apoptosis, and impaired blood-brain barrier (BBB) and ion channel regulation are the basis for the development of cerebral ischemia pathology. Quercetin, a flavonoid compound, commonly found in the daily diet and in some Chinese herbal medicines, including vegetables, fruits, and tea, is one of the most prominent dietary antioxidants. Modern pharmacological studies have shown that quercetin can effectively protect against cerebral ischemic injury, and its mechanisms may involve antioxidant, anti-inflammatory, anti-apoptotic, BBB protection, ion channel regulation, cell excitatory glutamate toxicity alleviation and cognitive impairment recovery activities. However, the low bioavailability of quercetin and the presence of the BBB structure limit the therapeutic efficacy. There have been studies targeting the delivery of quercetin to the injury site through nanotechnology to enhance the therapeutic effect of quercetin. This review discusses and reviews the pharmacological activity, pharmacokinetic characteristics, and targeted delivery nanosystems of quercetin in protecting against cerebral ischemic injury, and provides information on various downstream signaling pathways regulated by quercetin, such as PI3k/Akt, MAPK, and Sirt1. We hope to provide a scientific basis for the development and application of quercetin in the field of cerebral ischemia.

摘要

脑缺血,作为一种类似缺血性脑卒中的疾病,已成为全球关注的健康问题。研究发现,氧化应激、炎症、细胞凋亡以及血脑屏障(BBB)和离子通道调节受损是脑缺血病理发展的基础。槲皮素是一种黄酮类化合物,常见于日常饮食和一些中草药中,包括蔬菜、水果和茶,是最突出的膳食抗氧化剂之一。现代药理学研究表明,槲皮素能有效防治脑缺血损伤,其机制可能涉及抗氧化、抗炎、抗凋亡、保护 BBB、调节离子通道、减轻细胞兴奋性谷氨酸毒性和恢复认知障碍等活性。然而,槲皮素的生物利用度低和 BBB 结构的存在限制了其治疗效果。已有研究通过纳米技术将槲皮素靶向递送至损伤部位,以增强其治疗效果。本综述讨论并综述了槲皮素防治脑缺血损伤的药理学活性、药代动力学特征和靶向递药纳米系统,并提供了槲皮素调节的各种下游信号通路的信息,如 PI3k/Akt、MAPK 和 Sirt1。我们希望为槲皮素在脑缺血领域的开发和应用提供科学依据。

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