A Novel Toxin from Haplopelma lividum Selectively Inhibits the Na_V1.8 Channel and Possesses Potent Analgesic Efficacy.

ABSTRACT: Spider venoms are a complex mixture of peptides with a large number of neurotoxins targeting ion channels. Although thousands of peptide toxins have been identified from venoms of numerous species of spiders, many unknown species urgently need to be investigated. In this study, a novel sodium channel inhibitor, µ-TRTX-Hl1a, was identified from the venom of Haplopelma lividum. It contained eight cysteines and formed a conserved cysteine pattern of ICK motif. µ-TRTX-Hl1a inhibited the TTX-resistant (TTX-r) sodium channel current rather than the TTX-sensitive (TTX-s) sodium channel current. Meanwhile, µ-TRTX-Hl1a selectively inhibited Na_V1.8 with an IC₅₀ value of 2.19 μM. Intraperitoneal injection of µ-TRTX-Hl1a dose-dependently reduced inflammatory and neuropathi

SUBMITTER: Meng P 

PROVIDER: S-EPMC5308240 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature