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Analgesic applications of snake toxin polypeptide

A technology of toxins and venoms, applied in medical preparations containing active ingredients, peptide/protein ingredients, non-central pain relievers, etc., can solve the problem of lack of inhibitors

Inactive Publication Date: 2016-12-07
HUNAN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The research on screening specific inhibitors for Nav1.8 pain target has become a hot spot in the field of pain, but inhibitors with strong activity and good specificity have not been obtained so far.

Method used

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  • Analgesic applications of snake toxin polypeptide
  • Analgesic applications of snake toxin polypeptide
  • Analgesic applications of snake toxin polypeptide

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Experimental program
Comparison scheme
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Embodiment Construction

[0018] μ-EPTX-Na1a (Na1a for short) can be extracted by separating and purifying from crude venom of Cobra sinensis, and can also be obtained by expressing Saccharomyces cerevisiae. The polypeptide has a relative molecular weight of 7053.63Da, consists of 62 amino acid residues, and consists of 8 cysteines and 4 pairs of disulfide bonds (see Figure 1).

[0019] In order to reveal the analgesic application of this polypeptide toxin, we measured the inhibitory effect of Na1a on Nav1.8 channel by patch clamp technique, verified the analgesic activity of Na1a by using pain model experiments, and analyzed the side effects of Na1a.

[0020] 1. Main materials and instruments

[0021] Constant temperature shaker, ultra-clean bench, Olympus IX70 inverted microscope, constant temperature cell incubator. The mice and rats used in the experiments were all from Shanghai Shrek Experimental Animal Company, Chinese Academy of Sciences.

[0022] 2. Experimental methods and results

[0023] ...

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Abstract

The present invention relates to analgesic applications of a polypeptide toxin mu-EPTX-Na1a (short for Na1a) from Naja atra. According to the present invention, the Na1a provides a strong inhibition effect for the voltage-gated sodium channel subtype Nav1.8, wherein the half-maximal inhibition concentration is 167 nM; the subtype selectivity shows that the Na1a is highly specific; the pharmacodynamics activity experiment results show that the Na1a provides stronger analgesic activities in acetic acid writhing pain models, formalin pain models and complete Freund's adjuvant pain models compared to morphine, and provides similar or slightly excellent analgesic activities in hot plate pain models and sciatic nerve ligation models compared to morphine; the evaluation results of the side effects of the Na1a show that the weak side effects are provided in the movement function, the cardiotoxicity, the hemolytic activity and the cytotoxic activity; and the Na1a is the analgesic polypeptide having the application value.

Description

technical field [0001] The invention relates to an analgesic application of a polypeptide, in particular to an analgesic application of a polypeptide toxin specifically inhibiting Nav1.8 channel obtained from the venom of the Chinese cobra (Naja atra). Background technique [0002] Tetrodotoxin-insensitive (TTX-R) sodium channel Nav1.8 on rat dorsal root ganglion (DRG) cells is mainly expressed in small-diameter nociceptive neurons, and participates in the action potential and rhythmic discharge of sensory neurons. Nav1.8 is regulated by inflammatory mediators, and its expression is upregulated in the sciatic nerve injury model. Knockout and silencing studies of Nav1.8 suggest its involvement in the regulation of neuropathic and inflammatory pain. Related experiments of Nav1.8 inhibitors also prove that it is involved in pain regulation. The research on the screening of specific inhibitors targeting Nav1.8 pain target has become a hot spot in the field of pain, but so far ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/17A61P25/00A61P29/00
Inventor 刘中华梁宋平张凡
Owner HUNAN NORMAL UNIVERSITY
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