[Anti-insect scorpion toxins: historical account, activities and prospects].

M Pelhate, M Stankiewicz, R Ben Khalifa
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Abstract

Some toxins from scorpion venoms, much more toxic to insects than to other animal classes, possess high affinity to Na+ channels. These anti-insect scorpion toxins have been divided into: 1) alpha toxins which lack strict selectivity for insects, do not compete with following groups of anti-insect toxins, resemble other alpha scorpion toxins by their structure and their ability, as alpha anemone toxins, to prolong insect axonal action potential durations through a drastic slowing down of the Na+ current inactivation, 2) excitatory insect selective scorpion toxins which induce in blowfly larvae an immediate fast paralysis; in isolated cockroach axons, they depolarize and induce a sustained repetitive activity of short (normal) action potentials through a shift of Na+ activation mechanism towards more negative potentials and some decrease of inactivation at these potential values, 3) depressant insect selective neurotoxins which cause a slow progressive flaccid paralysis of larvae, depolarize insect axons and reduce or even suppress evoked action potentials; resting depolarizations which are antagonized by a post-application of TTX, are due to the opening of sodium channels at very negative potential values and to the suppression of their inactivation mechanism. The decrease of the maximal Na+ conductance following flaccid toxin action may be understood if toxin-modified channels opened at very negative potentials values remain open (or re-open) for much longer times than in control conditions and pass by substate less conductant states. Anti-insect scorpion toxins become of major interest into insect neurophysiology and also into insect pest control, due to their specific target sites and to the recent constructions of insecticidal baculovirus expressions of several of these toxins.

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[抗虫蝎子毒素:历史记载、活动与展望]。
蝎子毒液中的一些毒素对昆虫的毒性比其他动物的毒性大得多,它们对Na+通道具有很高的亲和力。这些抗虫蝎子毒素分为:1)α毒素对昆虫缺乏严格的选择性,不与以下几种抗虫毒素竞争,其结构和能力与其他α蝎子毒素相似,与α海葵毒素一样,通过急剧减缓Na+电流的失活来延长昆虫轴突动作电位的持续时间;2)兴奋性昆虫选择性蝎子毒素诱导苍蝇幼虫立即快速瘫痪;在离体蟑螂轴突中,它们通过Na+激活机制向负电位的转变和在这些电位值处失活的减少,使短(正常)动作电位去极化并持续重复活动;3)抑制昆虫选择性神经毒素,导致幼虫缓慢进行性弛缓性麻痹,使昆虫轴突去极化并降低甚至抑制诱发动作电位;静息去极化是由于钠通道在非常负的电位值下打开和抑制了它们的失活机制。如果毒素修饰的通道在非常负的电位值下打开,保持打开(或重新打开)的时间比在控制条件下长得多,并且通过亚态低电导状态,则可以理解弛缓毒素作用后最大Na+电导的降低。抗虫蝎子毒素由于其特定的靶点和最近构建的几种这些毒素的杀虫杆状病毒表达,成为昆虫神经生理学和害虫防治的主要兴趣。
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