蝎毒素多肽致/抗痛的靶离子通道机制
刘 霞,袁琛皓,杨清湖,白占涛*
(延安大学生命科学学院/多肽资源药物研究中心,延安 716000)

摘 要:摘 要:疼痛调控是多通道、多受体和多系统介导的复杂生命医学热点问题。诸多靶通道特异性工具药的普遍缺乏,致使其机制解析和临床诊疗转化任重道远。蝎毒是多种毒素多肽的集合体,用于捕食和防御天敌,蛰伤诱致长时程炎症和疼痛。通常认为,类α 长链肽类蝎毒素作用于钠通道,延缓钠通道失活,产生致痛效应,而类β 长链多肽蝎毒素则相反。短链肽类蝎毒素作用于钾通道、氯通道和钙通道,呈现疼痛相关的功能多样化。因此,开发应用极具潜力的靶向蝎毒素,是解析疼痛调制新机制的重要工具分子。现对蝎毒素与疼痛相关离子通道互作的工作做一综述,并探讨蝎毒素多肽致/ 抗痛的分子功能多样性。

Pain induction and analgesia mechanisms of scorpion toxins targeting to ion channels
LIU Xia, YUAN Chen-Hao, YANG Qing-Hu, BAI Zhan-Tao*
(Research Center for Resource Polypeptide Drugs & College of Life Sciences, Yanan University, Yanan 716000, China)

Abstract: Abstract: Pain is still a popular biomedical problem involving plenty of ion channels, receptors and signal systems. So far, our understanding of pain induction and therapy is delayed by lack of specific drugs for pain-related ion channels. Scorpion venom is composed of diverse peptides for preying and defending. Generally, long-chain α-like toxins induce pain by activating peak currents and delaying inactivation of sodium channels. On the contrary, long-chain β-like toxins always show anti-pain effects. Furthermore, short-chain toxins binding to potassium, chloride and calcium channels demonstrate complex activities. Many reports indicated that target-specific scorpion toxins would be the available molecular tools for elucidating pain mechanism and for developing novel analgesic drugs. The paper reviews these molecular, cellular and behavioral evidence, and thus attempts to further our understanding to the scientific and medicinal potential of scorpion toxins.

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