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A kind of polypeptide with analgesic activity and its application

A technology of activity and peptide sequence, which is applied in the field of biopharmaceuticals, can solve problems such as side effects, and achieve the effects of easy synthesis, weak adverse reactions and side effects of peptides, and simple peptide structure

Active Publication Date: 2020-09-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at problems such as side effects of existing conotoxin polypeptides, the present invention provides a polypeptide with analgesic activity and its application. The polypeptide of the present invention acts on ion channels and has analgesic efficacy. It has been verified by various experimental models, and Conotoxin has the same analgesic effect and less adverse reactions such as tolerance, and has great development prospects

Method used

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  • A kind of polypeptide with analgesic activity and its application
  • A kind of polypeptide with analgesic activity and its application
  • A kind of polypeptide with analgesic activity and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The present invention relates to a polypeptide with analgesic activity, which has the amino acid sequence Gly-Cys-Ser-Ser-Thr-Pro-Pro-Cys, or a pharmaceutically acceptable salt of the polypeptide, or one of the polypeptide sequences A polypeptide that still has analgesic effect after multiple amino acids are deleted, substituted or added, and a pair of disulfide bonds are formed between two cysteines in the sequence. Has a good inhibitory effect.

[0029] In the embodiment, the polypeptide Gly-Cys-Ser-Ser-Thr-Pro-Pro-Cys is mainly used as an object to study its pain-inhibiting activity. The peptide was synthesized by Nanjing GenScript Biotechnology Co., Ltd. with a purity of over 95%.

[0030] Inhibitory effect of analgesic polypeptide on pain in analgesic hot plate test

[0031] Kunming mice, female, weighing 20±2g. The indoor temperature was kept at 22-25°C. Put the mouse on a constant temperature metal plate with a temperature of 55°C, keep the temperature consta...

Embodiment 2

[0049] Inhibitory effect of analgesic polypeptide on pain in thermal radiation tail flick test

[0050] Kunming mice, half male and half male, body weight 20±2g. The indoor temperature is maintained at 22-25°C. A small spotlight is used to generate a beam of certain intensity, which is focused on the mouse's tail through a lens to induce pain. During the experiment, put the mouse tail on the tail groove of the tail flick pain measuring instrument, so that the light spot falls on the middle and lower 1 / 3 of the mouse tail (use a pen to mark the color before the experiment, so that the pain point is at the same position each time) Upper) The latency from radiant heat exposure to tail flick response (TFL, Tail Flick Latency) is an indicator of pain response.

[0051] Before administration, the basic pain threshold of all mice was firstly measured, and the mice whose response latency was less than 1s or greater than 3s were excluded, and 10s was set as the cut-off time in order ...

Embodiment 3

[0064] Effects of analgesic peptides on the spontaneous activity and exploratory behavior of mice in open field experiments

[0065] 1. Materials and methods

[0066] 1.1 Experimental animals

[0067] 60 Kunming female mice.

[0068] Breeding conditions: room temperature (23±1)°C; humidity (50±5)%; fluorescent lighting, light-dark cycle 12 / 12 (lighting time 7:00-19:00); animals had free access to water and food.

[0069] 1.2 Experimental Instruments

[0070] The computer real-time monitoring and analysis system SMART VIDEO-TRACKING (USA, SMARTv3.0.02) is adopted. The instrument is mainly composed of four 40cm×40cm×40cm experimental open boxes. A camera connected to the recording system is placed in the center of the top of the box, and the real-time images of the mice are analyzed by the system to obtain the behavior data of the mice in the open field.

[0071] 2. Experimental method:

[0072] Before the start of the experiment, the body mass of each mouse was statistical...

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Abstract

The present invention belongs to the field of biological medicine, and provides a polypeptide having an analgesic activity, a pharmaceutically acceptable salt thereof and uses thereof. Said polypeptide has a pair of disulfide bridges formed between the two cysteines of the amino acid sequence Gly-Cys-Ser-Ser-Thr-Pro-Pro-Cys. Said polypeptide inhibits physical and chemical stimuli, pathological and neurological pains, while prolongating the duration of heat tolerance in mice. Adverse reactions in mice, such as voluntary movement, excitability, and the like are lower than the normal values.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals, and more specifically relates to a polypeptide with analgesic activity and its application. Background technique [0002] The process of pain generation is relatively complex, involving pain receptors, conduction nerves, pain centers and other factors. The main causes of pain are as follows: (1) A series of mechanical stimuli in the outside world and local edema of the tissue during an inflammatory reaction will compress the nerve endings and cause pain; (2) Physical and chemical stimuli will cause pain through sensory stimulation. Neurons excite the pain-sensing center and cause pain; (3) pathological damage to peripheral nerves stimulates sympathetic nerve fibers, and finally stimulates the cerebral cortex to over-excite, causing neuropathic pain; Or the pain-causing substances released by nociceptors will stimulate the local receptors, excite the central nervous system and cause pain. [00...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06A61K38/08A61P29/00A61P25/04
CPCA61K38/00C07K7/06
Inventor 徐寒梅戚微岩刘晨吴鹏翔
Owner CHINA PHARM UNIV
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