Centipede polypeptide with analgesic activity and application thereof

A pathological and irritating technology, applied in the field of biopharmaceuticals, can solve the problems of side effects of analgesic drugs, and achieve the effects of easy synthesis, prolonged heat tolerance time, and fast onset of action

Active Publication Date: 2022-01-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Aiming at the problems of toxic and side effects of existing analgesic drugs, the present invention provides a class of centipede polypeptides with analgesic activity and applications thereof. The polypeptides of the present invention act on ion channels and have analgesic effects. After verification by various experimental models, It has good analgesic effect and low adverse reactions such as tolerance, and has great development prospects

Method used

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  • Centipede polypeptide with analgesic activity and application thereof
  • Centipede polypeptide with analgesic activity and application thereof
  • Centipede polypeptide with analgesic activity and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The present invention relates to a class of centipede polypeptides with analgesic activity

[0027] One is named WG-11, which has the amino acid sequence Pro-Ala-Pro-Val-Val-Thr-Tyr-Gly-Gly-Phe, or a pharmaceutically acceptable salt of the polypeptide, which has an analgesic effect. Peptides have a good inhibitory effect on physical and chemical irritation, pathological and neuropathic pain;

[0028]The second is named WG-12, which has the amino acid sequence Gly-Val-Val-Thr, or a pharmaceutically acceptable salt of the polypeptide, which has an analgesic effect. Has a good inhibitory effect;

[0029] The third name is WG-13, which has the amino acid sequence Val-Val-Thr-Tyr-Gly-Thr-Phe, or the pharmaceutically acceptable salt of the polypeptide, which has analgesic effect. Pathological and neuropathic pain has a good inhibitory effect;

[0030] The fourth is named WG-14, which has the amino acid sequence Thr-Phe-Pro-Val-Val-Thr, or a pharmaceutically acceptable salt...

Embodiment 2

[0034] Inhibitory effect of analgesic polypeptide on pain in analgesic hot plate test

[0035] Kunming mice, female, weighing 20±2g. The indoor temperature was kept at 20-24°C. Put the mouse on a constant temperature metal plate with a temperature of 55±0.5°C, start timing when the mouse touches the metal plate, and the time from when the mouse licks its hind feet or jumps is its pain threshold indicator.

[0036] 1. Experimental animals: Kunming female mice

[0037] The mice were kept in the ventilation system of the experimental mouse cage; the breeding temperature was about 22°C; the normal day and night cycle; all experimental animals had free access to water and food; the purchased experimental animals were raised in this laboratory for 3 to 5 days to adapt to the experimental environment; all animal experiments All were carried out between 8:00 and 18:00; the experimental animals were kept in single cages after administration.

[0038] 2. Experimental equipment: elect...

Embodiment 3

[0052] Effect of analgesic polypeptide on pain inhibition rate in formalin pain test

[0053] Simulates persistent pain resulting from acute tissue injury. Diluted formalin solution was injected subcutaneously on the dorsum of one limb of the animal, resulting in behavioral changes of the animal such as bending the leg when resting, limping when exercising, and licking the foot. The extent of these behaviors (eg, foot licking time) is directly proportional to the concentration of formalin, which is generally considered a symptom of pain. In addition, other behaviors such as grooming, exploration and locomotor activity were also affected by formalin injection.

[0054] Kunming mice, half male and half male, body weight 20±2g. The indoor temperature was kept at 23-24°C. The mice were divided into groups according to the random number table, and the negative control group, the positive control group, the centipede polypeptide WG-11 group, the centipede polypeptide WG-12 group,...

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Abstract

The invention discloses centipede polypeptide with analgesic activity and application thereof, and belongs to the technical field of biological medicine. The polypeptide has an amino acid sequence Xa-Xb-Xc-Val-Val-Thr-Xd-Xe-Xf-Xg or pharmaceutically acceptable salt thereof. The polypeptide has a good inhibiting effect on mechanical irritation, physicochemical irritation and neuropathic pain, the analgesic effect is good in all experimental models, the specific effects are that the pain threshold value of a mouse is remarkably increased, the heat tolerance time of the mouse is prolonged, and adverse reactions such as autonomous movement and excitability of the mouse are all lower than normal values.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals, and more specifically relates to a class of centipede polypeptides with analgesic activity and applications thereof. Background technique [0002] Centipede is a kind of traditional Chinese medicine in my country. It has the effects of detoxifying and anti-cancer, calming wind and relieving spasm. S.subspinipesmutilans L.Koch is a similar species of S. subspinipesmutilans L.Koch. Mainly distributed in China and Japan. Common in the middle and lower reaches of the Yangtze River. It hides under rocks or among rocks during the day, and hunts insects (such as crickets, grasshoppers, scarabs, and various moths) at night, and can also kill small vertebrates (such as sparrows, lizards, snakes, etc.) with its poisonous jaws. ). In humans, a centipede's bite can be excruciatingly painful, similar to a high-temperature burn. In recent years, people have extracted many active molecules from centipede ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K5/103A61K38/08A61K38/07A61P25/00A61P25/04A61P29/00
CPCC07K7/06C07K5/1008A61P25/00A61P25/04A61P29/00A61K38/00
Inventor 徐寒梅戚微岩于瑞河刘晨
Owner CHINA PHARM UNIV
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