Transient receptor potential channels as targets for phytochemicals.
Transient receptor potential channels as targets for phytochemicals.
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DOI：
10.1021/cn500094a
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发表时间：
2014-11-19
影响因子：
5
通讯作者：
Premkumar, Louis S.
中科院分区：
文献类型：
--
作者：
Premkumar, Louis S.
迄今为止，已克隆和表征了28个哺乳动物瞬时受体电位（TRP）通道。根据其氨基酸序列同源性将其分为六个亚家族：TRP锚蛋白（TRPA）、TRP经典（TRPC）、TRP Melastatin（TRPM）、TRP粘脂（TRPML）、TRP多囊蛋白（TRPP）和TRP香草素（TRPV）。大多数TRP通道是在细胞膜上表达的非选择性阳离子通道，并且对Ca 2+与Na+表现出可变的渗透率比。它们介导感觉功能（如视觉、伤害感受、味觉传导、温度感觉和信息素信号传导）和稳态功能（如二价阳离子通量、激素释放和激素调节）。在我们对这些TRP通道的具体作用及其激活机制的理解方面取得了重大进展。在这篇综述中，重点将放在TRP通道的激活，声称发挥健康效益的植物化学物质。最近的研究结果补充了轶事证据，其中一些植物化学物质具有特定的受体，其激活是生理效应的原因。现在，这些植物化学物质的目标正在公布;可以提出一个特定的假设，并通过实验进行测试，以推断健康益处的科学有效性。必须解决的更广泛和紧迫的问题涉及给定制剂中活性成分的量、其生物利用度、代谢、不良反应、排泄以及全身与局部效应。
To date, 28 mammalian transient receptor potential (TRP) channels have been cloned and characterized. They are grouped into six subfamilies on the basis of their amino acid sequence homology: TRP Ankyrin (TRPA), TRP Canonical (TRPC), TRP Melastatin (TRPM), TRP Mucolipin (TRPML), TRP Polycystin (TRPP), and TRP Vanilloid (TRPV). Most of the TRP channels are nonselective cation channels expressed on the cell membrane and exhibit variable permeability ratios for Ca2+ versus Na+. They mediate sensory functions (such as vision, nociception, taste transduction, temperature sensation, and pheromone signaling) and homeostatic functions (such as divalent cation flux, hormone release, and osmoregulation). Significant progress has been made in our understanding of the specific roles of these TRP channels and their activation mechanisms. In this Review, the emphasis will be on the activation of TRP channels by phytochemicals that are claimed to exert health benefits. Recent findings complement the anecdotal evidence that some of these phytochemicals have specific receptors and the activation of which is responsible for the physiological effects. Now, the targets for these phytochemicals are being unveiled; a specific hypothesis can be proposed and tested experimentally to infer a scientific validity of the claims of the health benefits. The broader and pressing issues that have to be addressed are related to the quantities of the active ingredients in a given preparation, their bioavailability, metabolism, adverse effects, excretion, and systemic versus local effects.
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期刊：
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