摘要
槲皮素具有多种控制各种细胞功能的潜能,能保持身体健康。在本文中,我们从细胞溶质Cl-环境的角度来描述槲皮素如何发挥其对血压、神经突伸长和上皮离子转运的作用的分子机制,这是近年来公认的各种细胞中的一个重要信号因子。近年来的研究表明,细胞溶质Cl-在调节血压和神经突伸长以及预防细菌和病毒感染方面具有不同的作用。我们发现槲皮素对Cl-转运体,Na+-K+-2Cl-共转运体1(NKCC1; NKCC的一种亚型)的刺激作用,被认为是槲皮素最有趣的基本作用之一。本文根据槲皮素对NKCC1的刺激作用,介绍了槲皮素的分子机制:1)血压,2)神经节伸长,3)上皮组织中形成紧密连接的内皮细胞分泌。1)槲皮素通过激活NKCC1诱导细胞溶质cl-浓度升高,通过降低肾钠离子再吸收的关键离子通道上皮钠离子通道(ENAC)的表达而产生抗高血压作用,而槲皮素对正常盐摄入的血压无影响。2)槲皮素还通过激活NKCC1来提高细胞溶质Cl-浓度,通过Cl-诱导的GTPase抑制促进小管蛋白聚合,从而对轴突伸长具有刺激作用。3)此外,在肺气道上皮中,槲皮素通过提高细胞溶质Cl-浓度来增加Cl-分泌的驱动力来刺激Cl-分泌:这会导致水分分泌,参与预防我们身体受到细菌和病毒感染。除了跨细胞离子转运,槲皮素通过调节表达和组装紧密连接形成蛋白来增强紧密连接的完整性来调节紧密连接的功能。根据这些观察结果,槲皮素是一种有效的保持人体健康的药物化合物。
关键词: 类黄酮,Na-K-2Cl-转运体,ENaC,神经突起,Cl-,微管蛋白,GTPase.
Current Medicinal Chemistry
Title:Quercetin is a Useful Medicinal Compound Showing Various Actions Including Control of Blood Pressure, Neurite Elongation and Epithelial Ion Transport
Volume: 25 Issue: 37
关键词: 类黄酮,Na-K-2Cl-转运体,ENaC,神经突起,Cl-,微管蛋白,GTPase.
摘要: Quercetin has multiple potential to control various cell function keeping our body condition healthy. In this review article, we describe the molecular mechanism on how quercetin exerts its action on blood pressure, neurite elongation and epithelial ion transport based from a viewpoint of cytosolic Cl- environments, which is recently recognized as an important signaling factor in various types of cells. Recent studies show various roles of cytosolic Cl- in regulation of blood pressure and neurite elongation, and prevention from bacterial and viral infection. We have found the stimulatory action of quercetin on Cl- transporter, Na+-K+-2Cl- cotransporter 1 (NKCC1; an isoform of NKCC), which has been recognized as one of the most interesting, fundamental actions of quercetin. In this review article, based on this stimulatory action of quercetin on NKCC1, we introduce the molecular mechanism of quercetin on: 1) blood pressure, 2) neurite elongation, and 3) epithelial Cl- secretion including tight junction forming in epithelial tissues. 1) Quercetin induces elevation of the cytosolic Cl- concentration via activation of NKCC1, leading to anti-hypertensive action by diminishing expression of epithelial Na+ channel (ENaC), a key ion channel involved in renal Na+ reabsorption, while quercetin has no effects on the blood pressure with normal salt intake. 2) Quercetin also has stimulatory effects on neurite elongation by elevating the cytosolic Cl- concentration via activation of NKCC1 due to tubulin polymerization facilitated through Cl--induced inhibition of GTPase. 3) Further, in lung airway epithelia quercetin stimulates Cl- secretion by increasing the driving force for Cl- secretion via elevation of the cytosolic Cl- concentration: this leads to water secretion, participating in prevention of our body from bacterial and viral infection. In addition to transcellular ion transport, quercetin regulates tight junction function via enhancement of tight junction integrity by modulating expression and assembling tight junction-forming proteins. Based on these observations, it is concluded that quercetin is a useful medicinal compound keeping our body to be in healthy condition.
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Cite this article as:
Quercetin is a Useful Medicinal Compound Showing Various Actions Including Control of Blood Pressure, Neurite Elongation and Epithelial Ion Transport, Current Medicinal Chemistry 2018; 25 (37) . https://dx.doi.org/10.2174/0929867323666160919095043
DOI https://dx.doi.org/10.2174/0929867323666160919095043 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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