Estrada-Gómez Sebastián, Salinas-Restrepo Cristian, Vargas-Muñoz Leidy Johana, Guzmán Fanny, Segura Cesar, Pla Davinia, Sanz Libia, Calvete Juan J
Grupo de Toxinología y Alternativas Terapeuticas y Alimentarias - Serpentario, Facultad de Ciencias Farmacéuticas y Alimentarias, Universidad de Antioquia UdeA, Colombia, Medellin, 050010, Antioquia, Colombia.
Centro de Investigación en Recursos Naturales y Sustentabilidad, Universidad Bernardo O'Higgins, Avenida Viel 1497, Santiago, Chile.
Toxicon X. 2025 May 1;26:100224. doi: 10.1016/j.toxcx.2025.100224. eCollection 2025 Jun.
The attention to the increased resistance of to traditional insecticides has been directed to the development of bioinsecticides, such as those produced by insect predators, e.g. spiders. Here we present the solid-phase synthesis of native U-theraphotoxin-Pv1a_1 (n-Pv1a_1) from , an active (by contact) insecticidal peptide against . U-theraphotoxin-Pv1a_1 sequence was gathered from venom proteomics and venom gland transcriptomics of , and synthesized by solid phase using the Fmoc strategy followed by dimethyl sulfoxide promoted native disulfide bond formation. The synthetic peptide (s-Pv1a_1) was assayed for larvicidal activity in II and III instar larvae, as well as for cytotoxicity in human red blood and HaCat cells. s-Pv1a_1 showed potent activity towards . larvae in the micro molar range, while showing no hemolytic activity and mild cytotoxicity to HaCat cells. Its potent contact activity makes n-Pv1a_1 and its synthetic version, s-Pv1a, promising biopesticides for the control of mosquito populations.
对[某种昆虫]对传统杀虫剂抗性增加的关注促使人们开发生物杀虫剂，例如由昆虫捕食者（如蜘蛛）产生的杀虫剂。在此，我们展示了从[某种蜘蛛]中固相合成天然的U-theraphotoxin-Pv1a_1（n-Pv1a_1），这是一种对[某种昆虫]具有活性（通过接触）的杀虫肽。U-theraphotoxin-Pv1a_1序列从[某种蜘蛛]的毒液蛋白质组学和毒腺转录组学中获取，并采用Fmoc策略通过固相合成，随后通过二甲基亚砜促进天然二硫键形成。对合成肽（s-Pv1a_1）进行了针对[某种昆虫]二龄和三龄幼虫的杀幼虫活性以及对人红细胞和HaCat细胞的细胞毒性测定。s-Pv1a_1在微摩尔范围内对[某种昆虫]幼虫显示出强效活性，同时对HaCat细胞无溶血活性且细胞毒性轻微。其强效的接触活性使得n-Pv1a_1及其合成版本s-Pv1a有望成为控制蚊虫种群的生物杀虫剂。
