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雅保瑞托克斯,一种从刀豆脲酶衍生而来的天然杀虫剂,通过激活电压门控钠离子通道来调节昆虫行为。

Jaburetox, a natural insecticide derived from Jack Bean Urease, activates voltage-gated sodium channels to modulate insect behavior.

机构信息

Graduate Program in Biological Sciences: Biochemical Toxicology, Federal University of Santa Maria-UFSM, Santa Maria, RS, Brazil; University of Toronto Mississauga-UTM, Department of Biology. Mississauga, ON, Canada.

Graduate Program in Biological Sciences, Federal University of Pampa-UNIPAMPA, São Gabriel, RS, Brazil.

出版信息

Pestic Biochem Physiol. 2019 Jan;153:67-76. doi: 10.1016/j.pestbp.2018.11.003. Epub 2018 Nov 5.

Abstract

Jaburetox (Jbtx) is an insecticidal peptide derived from Canavalia ensiformis urease, whose mechanism of action is not completely elucidated. We employed behavioral, electromyographical and electrophysiological protocols to identify the cellular and molecular targets involved in the Jbtx entomotoxicity in cockroaches and locusts. In Nauphoeta cinerea, Jbtx (32 μg/g) altered the locomotory behaviour inducing a significative decrease in the distance travelled followed by a significant increase in stopped time (52 ± 85 cm and 2573 ± 89 s, p < .05, n = 40). Jbtx (8 to 32 μg/g body weight, respectively) also increased the leg and antennae grooming activities (p < .05, n = 40, respectively). Jbtx (8 to 16 μg/g) induced a maximum neuromuscular blockade of 80.72% (n = 6, p < .05) and was cardiotoxic, decreasing the cockroach heart rate. The electrophysiological profiles of both muscle and nerve of L. migratoria showed that Jbtx (2.5 × 10 and 2.5 × 10 μg/ body weight) induced a significant increase in the amplitude of nerve action potentials (n = 5, p < .05). Voltage clamp analysis of Jbtx (200 nM) applied in Xenopus laevis oocytes heterologously expressed with Nav 1.1 channels showed a significant increase in the sodium currents. In conclusion, this work revealed that the entomotoxic activity of Jbtx involves complex behavioral alterations that begins with an initial activation of voltage-gated sodium channels.

摘要

刺桐昆虫毒素(Jbtx)是一种从刀豆脲酶衍生而来的杀虫肽,其作用机制尚未完全阐明。我们采用行为学、肌电图和电生理学方案,鉴定了 Jbtx 在蟑螂和蝗虫中的杀虫毒性所涉及的细胞和分子靶标。在 Nauphoeta cinerea 中,Jbtx(32μg/g)改变了运动行为,导致行进距离显著减少,随后停止时间显著增加(52±85cm 和 2573±89s,p<.05,n=40)。Jbtx(分别为 8 至 32μg/g 体重)还增加了腿部和触角的梳理活动(p<.05,n=40,分别)。Jbtx(8 至 16μg/g)诱导最大的神经肌肉阻断率为 80.72%(n=6,p<.05),并具有心脏毒性,降低了蟑螂的心率。L. migratoria 的肌肉和神经的电生理谱表明,Jbtx(2.5×10 和 2.5×10μg/体重)诱导神经动作电位幅度显著增加(n=5,p<.05)。用 Xenopus laevis 卵母细胞中异源表达的 Nav 1.1 通道进行的 Jbtx(200nM)电压钳分析显示,钠离子电流显著增加。总之,这项工作表明 Jbtx 的杀虫活性涉及复杂的行为改变,这些改变始于电压门控钠离子通道的初始激活。

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