Chen Minzhi, Yang Li, Zeng Guo, Xiao Xin, Liu Zhonghua, Zhang Gaihua, Zhou Xi
The National and Local Joint Engineering Laboratory of Animal Peptide Drug Development, College of Life Sciences, Hunan Normal University, Changsha 410081, China; Peptide and small molecule drug R&D platform, Furong Laboratory, Hunan Normal University, Changsha 410081, Hunan, China; Institute of Interdisciplinary Studies, Hunan Normal University, Changsha 410081, China.
Hunan Provincial Key Laboratory of Regional Hereditary Birth Defects Prevention and Control, Changsha Hospital for Maternal and Child Health Care Affiliated to Hunan Normal University, Changsha 410007, China.
Toxicol Appl Pharmacol. 2025 Jul;500:117374. doi: 10.1016/j.taap.2025.117374. Epub 2025 May 7.
The spider, Ornithoctonus hainana, is a large and formidable predatory arthropod that possesses strong lethality towards rodents through its venoms. Its venom and constituent bioactive peptide toxins have previously been shown to modulate the activity of voltage-gated ion channels. Therefore, venom toxins are an important weapon for rapidly subduing prey or escaping predators. Here, we discovered three new peptide toxins, termed HNTXs, from the venom of O. hainana. These toxins potently inhibit the peak currents of rKv4.2, a member of the Shal channel family. We demonstrated that HNTXs are gating modifiers that shift the voltage dependence of activation and inactivation to more positive potentials. Additionally, chimeric channel and site-directed mutagenesis analyses show that these toxins inhibit rKv4.2 by interacting with the S3-S4 linker in the channel. Furthermore, we found that HNTXs exhibited different responses to Shal channels of vertebrates and invertebrates, suggesting that venomous animals employ diversified toxins to efficiently and accurately defend against predation and interspecific competition. This research may expand our understanding of venom peptides in evolutionary adaptation.
海南捕鸟蛛是一种大型且令人畏惧的捕食性节肢动物,其毒液对啮齿动物具有很强的致死性。此前研究表明,其毒液及组成成分生物活性肽毒素可调节电压门控离子通道的活性。因此,毒液毒素是迅速制服猎物或躲避捕食者的重要武器。在此,我们从海南捕鸟蛛的毒液中发现了三种新的肽毒素,命名为HNTXs。这些毒素能有效抑制Shal通道家族成员rKv4.2的峰值电流。我们证明HNTXs是门控修饰剂,可将激活和失活的电压依赖性向更正的电位移动。此外,嵌合通道和定点诱变分析表明,这些毒素通过与通道中的S3 - S4连接子相互作用来抑制rKv4.2。此外,我们发现HNTXs对脊椎动物和无脊椎动物的Shal通道表现出不同反应,这表明有毒动物利用多样化的毒素来有效且准确地抵御捕食和种间竞争。这项研究可能会拓宽我们对毒液肽在进化适应方面的理解。