Faculty of Sciences 3, Department of Biology, Lebanese University, Campus Michel Slayman Ras Maska, Tripoli 1352, Lebanon.
Biology Department, Faculty of Arts and Sciences, American University of Beirut, Beirut 1107 2020, Lebanon.
Mar Drugs. 2021 Oct 5;19(10):562. doi: 10.3390/md19100562.
Voltage-gated sodium channels (VGSCs) are considered to be one of the most important ion channels given their remarkable physiological role. VGSCs constitute a family of large transmembrane proteins that allow transmission, generation, and propagation of action potentials. This occurs by conducting Na ions through the membrane, supporting cell excitability and communication signals in various systems. As a result, a wide range of coordination and physiological functions, from locomotion to cognition, can be accomplished. Drugs that target and alter the molecular mechanism of VGSCs' function have highly contributed to the discovery and perception of the function and the structure of this channel. Among those drugs are various marine toxins produced by harmful microorganisms or venomous animals. These toxins have played a key role in understanding the mode of action of VGSCs and in mapping their various allosteric binding sites. Furthermore, marine toxins appear to be an emerging source of therapeutic tools that can relieve pain or treat VGSC-related human channelopathies. Several studies documented the effect of marine toxins on VGSCs as well as their pharmaceutical applications, but none of them underlined the principal marine toxins and their effect on VGSCs. Therefore, this review aims to highlight the neurotoxins produced by marine animals such as pufferfish, shellfish, sea anemone, and cone snail that are active on VGSCs and discuss their pharmaceutical values.
电压门控钠离子通道（VGSCs）被认为是最重要的离子通道之一，因为它们具有显著的生理作用。VGSCs 构成了一大类跨膜蛋白家族，允许动作电位的传递、产生和传播。这是通过在膜中传导 Na 离子来实现的，支持各种系统中的细胞兴奋性和通信信号。因此，可以完成从运动到认知等广泛的协调和生理功能。靶向和改变 VGSCs 功能的分子机制的药物对该通道的功能和结构的发现和认识做出了重要贡献。这些药物包括由有害微生物或有毒动物产生的各种海洋毒素。这些毒素在理解 VGSCs 的作用模式以及绘制其各种变构结合位点方面发挥了关键作用。此外，海洋毒素似乎是一种新兴的治疗工具来源，可以缓解疼痛或治疗与 VGSC 相关的人类通道病。有几项研究记录了海洋毒素对 VGSCs 的影响及其药物应用，但没有一项研究强调主要的海洋毒素及其对 VGSCs 的影响。因此，本综述旨在强调河豚鱼、贝类、海葵和芋螺等海洋动物产生的神经毒素对 VGSCs 的作用，并讨论它们的药用价值。
