Corina M Ionescu, Melissa A Jones, Susbin R Wagle, Bozica Kovacevic, Thomas Foster, Momir Mikov, Armin Mooranian, Hani Al-Salami
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引用次数: 0
Abstract
Bile acids play important roles in the human body, and changes in their pool can be used as markers for various liver pathologies. In addition to their functional effects in modulating inflammatory responses and cellular survivability, the unconjugated or conjugated, secondary, or primary nature of bile acids accounts for their various ligand effects. The common hydrophilic bile acids have been used successfully as local treatment to resolve drug-induced cell damage or to ameliorate hearing loss. From various literature references, bile acids show concentration and tissue-dependent effects. Some hydrophobic bile acids act as ligands modulating vitamin D receptors, muscarinic receptors, and calcium-activated potassium channels, important proteins in the inner ear system. Currently, there are limited resources investigating the therapeutic effects of bile acid on hearing loss and little to no information on detecting bile acids in the remote ear system, let alone baseline bile acid levels and their prevalence in healthy and disease conditions. This review presents both hydrophilic and hydrophobic human bile acids and their tissue-specific effects in modulating cellular integrity, thus considering the possible effects and extended therapeutic applicability of bile acids to the inner ear tissue.
胆汁酸在人体内发挥着重要作用,胆汁酸池的变化可作为各种肝脏病变的标志物。胆汁酸除了具有调节炎症反应和细胞存活率的功能性作用外,其非结合或结合、次生或原生的性质也是它们产生各种配体效应的原因。常见的亲水性胆汁酸已被成功用于局部治疗,以解决药物引起的细胞损伤或改善听力损失。从各种文献参考来看,胆汁酸显示出浓度和组织依赖性效应。一些疏水性胆汁酸可作为配体调节维生素 D 受体、毒蕈碱受体和钙激活钾通道等内耳系统中的重要蛋白质。目前,研究胆汁酸对听力损失的治疗效果的资源有限,而在远耳系统中检测胆汁酸的信息几乎为零,更不用说胆汁酸的基线水平及其在健康和疾病情况下的流行率了。本综述介绍了亲水性和疏水性人类胆汁酸及其在调节细胞完整性方面的组织特异性效应,从而考虑胆汁酸对内耳组织的可能影响和扩展治疗适用性。
期刊介绍:
Current Drug Targets aims to cover the latest and most outstanding developments on the medicinal chemistry and pharmacology of molecular drug targets e.g. disease specific proteins, receptors, enzymes, genes.
Current Drug Targets publishes guest edited thematic issues written by leaders in the field covering a range of current topics of drug targets. The journal also accepts for publication mini- & full-length review articles and drug clinical trial studies.
As the discovery, identification, characterization and validation of novel human drug targets for drug discovery continues to grow; this journal is essential reading for all pharmaceutical scientists involved in drug discovery and development.