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石房蛤毒素结合靶点的研究进展

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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.
Research Progress of Binding Targets of Saxitoxin
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.

saxitoxinion channelsinhibitorssaxiphilinantidotes

周蓉、欧阳生群、王梁华、焦炳华

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第二军医大学基础部生物化学与分子生物学教研室,上海 200433

第二军医大学海洋军事医学院海洋药物中心,上海 200433

石房蛤毒素 离子通道 抑制剂 麻痹性贝类毒素受体蛋白 解毒剂

2017

中国生化药物杂志
南京生物化学制药研究所,全国生化制药情报中心站,中国生化制药工业协会,中国药品生物制品检定所

中国生化药物杂志

ISSN:1005-1678
年,卷(期):2017.37(8)
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