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JZTX-V, a Sodium Channel Inhibitor, Exhibits Excellent Analgesic Effects in Mouse Models

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Abstract

JZTX-V, an inhibitor of voltage-gated sodium and potassium channels, is derived from the venom of the spider Chilobrachys jingzhao in China. JZTX-V was synthesized using a solid-phase chemical approach with Fmoc-protected amino acids to explore its function further. The synthetic peptides were purified using reverse-phase high-performance liquid chromatography (RP-HPLC) and then subjected to oxidative refolding under optimal conditions. A unique peak was observed in the RP-HPLC chromatogram for refolded JZTX-V, and the ratio to native JZTX-V was 1:1 for the mixed samples. Subsequently, the analgesic potential of the synthetic peptide was evaluated in mouse models of pain. In the Formarin model, JZTX-V significantly reduced pain scores in 60 min and its efficacy was comparable to that of morphine. JZTX-V also exhibited excellent analgesic effects in models of postoperative pain and mechanical allodynia. However, JZTX-V had no effect on thermal stimulation injury in the hot plate experiment and did not affect motor coordination. These results indicate that JZTX-V effectively alleviates inflammatory pain in animals and provides a promising template for the design of future clinical analgesic drugs.

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Funding

National Innovation and Entrepreneurship Training Program (S202010548007).

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Author notes

  1. Chen Bo and Sun Zhenghua contributed equally to this work.

Authors and Affiliations

  1. College of Biology and Food Engineering, Huaihua University, Huaihua, 418000, China

    Chen Bo

  2. The National and Local Joint Engineering Laboratory of Animal Peptide Drug Development, College of Life Sciences, Hunan Normal University, Changsha, Hunan, 410000, China

    Chen Bo, Sun Zhenghua & Zeng Xiongzhi

  3. Key Laboratory of Research and Utilization of Ethnomedicinal Plant Resources of Hunan Province, College of Biological and Food Engineering, Huaihua University, Huaihua, 418000, China

    Chen Bo

  4. College of Life Science and Technology, Jinan University, Guangzhou, China

    Sun Zhenghua

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  1. Chen Bo
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  2. Sun Zhenghua
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Contributions

C.B. S.Z and Z.X wrote the main manuscript text, CB, S.Z, Z. Xprepared all figures. All authors reviewed the manuscript.

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Correspondence to Zeng Xiongzhi.

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Bo, C., Zhenghua, S. & Xiongzhi, Z. JZTX-V, a Sodium Channel Inhibitor, Exhibits Excellent Analgesic Effects in Mouse Models. Int J Pept Res Ther 30, 25 (2024). https://doi.org/10.1007/s10989-024-10603-z

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