Branch of Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Pushchino, Moscow Region, Russia.
PushchGENI - Branch of BIOTECH University, Pushchino, Moscow Region, Russia.
Bull Exp Biol Med. 2024 Jun;177(2):217-220. doi: 10.1007/s10517-024-06159-z. Epub 2024 Aug 2.
PT1 peptide isolated from the venom of spider Geolycosa sp. is a modulator of P2X3 receptors that play a role in the development of inflammation and the transmission of pain impulses. The anti-inflammatory and analgesic efficacy of the PT1 peptide was studied in a model of complete Freund's adjuvant-induced paw inflammation in CD-1 mice. The analgesic activity of PT1 peptide was maximum after intramuscular injection at a dose of 0.01 mg/kg, which surpassed the analgesic effect of diclofenac at a dose of 1 mg/kg. The anti-inflammatory activity was maximum after intramuscular injection at a dose of 0.0001 mg/kg; a decrease in paw thickness was observed as soon as 2 h after the administration of the PT1 peptide against the background of inflammation development. All tested doses of PT1 peptide showed high anti-inflammatory activity 4 and 24 h after administration. PT1 peptide at a dose of 0.01 mg/kg when injected intramuscularly simultaneously produced high anti-inflammatory and analgesic effects compared to other doses of the peptide. Increasing the dose of PT1 peptide led to a gradual decrease in its analgesic and anti-inflammatory activity; increasing the dose of intramuscular injection to 0.1 and 1 mg/kg is inappropriate.
PT1 肽是从蜘蛛 Geolycosa sp. 的毒液中分离出来的，是 P2X3 受体的调节剂，在炎症的发展和疼痛冲动的传递中起作用。在 CD-1 小鼠完全弗氏佐剂诱导的爪炎症模型中研究了 PT1 肽的抗炎和镇痛功效。PT1 肽的镇痛活性在 0.01mg/kg 的肌内注射剂量下最大，超过了 1mg/kg 剂量的双氯芬酸钠的镇痛效果。抗炎活性在 0.0001mg/kg 的肌内注射剂量下最大；在炎症发展的背景下，注射 PT1 肽后仅 2 小时即可观察到爪厚度的减少。在给药后 4 小时和 24 小时，所有测试剂量的 PT1 肽均显示出很高的抗炎活性。与肽的其他剂量相比，当以 0.01mg/kg 的剂量肌内注射时，PT1 肽同时产生了高抗炎和镇痛作用。增加 PT1 肽的剂量会导致其镇痛和抗炎活性逐渐降低；将肌内注射剂量增加到 0.1 和 1mg/kg 是不适当的。
