石房蛤毒素结合靶点的研究进展

Research Progress of Binding Targets of Saxitoxin

石房蛤毒素（saxitoxin,STX）是已知毒性最强的海洋生物毒素之一,严重威胁人类安全和健康,但也具有潜在的药用价值。本文概述了STX及其类似物的结构与性质,总结了近年来报道的STX的结合靶点及其结合的结构基础。STX既能结合Na＋、K＋、Ca2＋通道抑制通道离子流,也能被牛蛙的Saxiphilin蛋白及河鲀STX/TTX结合蛋白结合从而使机体免于STX毒性作用。此外,除了作为STX代谢酶的底物,STX还影响机体一氧化氮合酶、抗氧化酶等的活性。本文基于这些靶标对STX发挥活性的机制进行全面探讨,对STX麻醉、镇痛等方面的药用价值和STX解毒剂的研发进行初步讨论,期望能够为后续STX的研究提供参考。

Saxitoxin （STX） is one of the most toxic marine toxins.Scientists have been focusing on STX research due to the potentially pharmaceutical values and serious threat to human safety and health.. This review summarizes the structure, properties, binding targets and combination of structural basis of STX and its analogues in recent years reported. STX can bind Na＋, K＋, Ca2＋channels to suppress the channel ion current, but also combine the bullfrog Saxiphilin protein and puffer fish STX/TTX binding protein （PSTBP） to protect the body from STX toxicity. STX also as a substrate for STX enzymes and affects the activity of nitric oxide synthase, antioxidant enzymes. Furthermore,this review has a comprehensive analysis of these targets of STX and a preliminary discussion of the medicinal value of anesthesia and analgesia and the development of antidotes to STX. It is expected to provide a reference for further study of the nature of STX and its application in various fields.