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δ-Ctenitoxin-Pn1a, a Peptide from Phoneutria nigriventer Spider Venom, Shows Antinociceptive Effect Involving Opioid and Cannabinoid Systems, in Rats. | LitMetric

AI Article Synopsis

  • - δ-Ctenitoxin-Pn1a (δ-CNTX-Pn1a) is a peptide from spider venom that interacts with sodium channels to modulate nerve activity, showing low toxicity in mice.
  • - The study found that δ-CNTX-Pn1a effectively reduced pain in different animal pain models: it restored sensitivity in inflammatory pain, reversed nerve damage pain, and provided dose-dependent relief in acute pain.
  • - The antinociceptive properties of δ-CNTX-Pn1a are linked to cannabinoid (CB₁ receptors) and opioid receptor systems (μ and δ receptors), demonstrating its potential as a pain relief agent.

Article Abstract

PnTx4(6-1), henceforth renamed δ-Ctenitoxin-Pn1a (δ-CNTX-Pn1a), a peptide from Phoneutria nigriventer spider venom, initially described as an insect toxin, binds to site 3 of sodium channels in nerve cord synaptosomes and slows down sodium current inactivation in isolated axons in cockroaches (Periplaneta americana). δ-CNTX-Pn1a does not cause any apparent toxicity to mice, when intracerebroventricularly injected (30 μg). In this study, we evaluated the antinociceptive effect of δ-CNTX-Pn1a in three animal pain models and investigated its mechanism of action in acute pain. In the inflammatory pain model, induced by carrageenan, δ-CNTX-Pn1a restored the nociceptive threshold of rats, when intraplantarly injected, 2 h and 30 min after carrageenan administration. Concerning the neuropathic pain model, δ-CNTX-Pn1a, when intrathecally administered, reversed the hyperalgesia evoked by sciatic nerve constriction. In the acute pain model, induced by prostaglandin E₂, intrathecal administration of δ-CNTX-Pn1a caused a dose-dependent antinociceptive effect. Using antagonists of the receptors, we showed that the antinociceptive effect of δ-CNTX-Pn1a involves both the cannabinoid system, through CB₁ receptors, and the opioid system, through μ and δ receptors. Our data show, for the first time, that δ-Ctenitoxin-Pn1a is able to induce antinociception in inflammatory, neuropathic and acute pain models.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4848632PMC
http://dx.doi.org/10.3390/toxins8040106DOI Listing

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