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Polypeptide having pain stopping effect, and applications thereof

A technology of action and product, applied to polypeptides with analgesic effect and their application fields, can solve the problems of addiction, neuropathic pain without curative effect, severe needle-like withdrawal, etc., achieve broad development prospects, avoid gastrointestinal tract Toxicity, high safety effect

Inactive Publication Date: 2018-10-16
SHANGHAI XINSHENGYUAN BIOLOGICAL MEDICAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The action site of narcotic analgesics is in the thalamus and cerebral cortex, which can relieve sharp pain, dull pain and visceral colic, but it has no effect on neuropathic pain, and it is easy to cause addiction when used repeatedly, and the withdrawal needle is severe. The analgesic effect must be continuously increased; moreover, narcotic analgesics are listed as controlled drugs and listed as "narcotic drugs" in drug administration. Strictly manage and restrict
Antipyretic and analgesic drugs are a class of drugs with antipyretic and analgesic effects. By inhibiting endocycloxygenase, the production of prostaglandins is reduced, the sensitivity of nerve endings to pain-causing substances is reduced, and anti-inflammatory and analgesic effects are achieved. The site of action is mainly in the periphery, mainly used for contact with inflammatory pain or other dull pain, and it is ineffective for the treatment of neuropathic inflammation and neuralgia

Method used

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  • Polypeptide having pain stopping effect, and applications thereof
  • Polypeptide having pain stopping effect, and applications thereof
  • Polypeptide having pain stopping effect, and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The cyclic polypeptide TLN-7 of the present invention is synthesized by chemical solid phase synthesis. Follow these steps:

[0026] 1. Resin swelling: Soak Rink Amide AM Resin in dichloromethane, and remove the dichloromethane after the resin expands.

[0027] 2. Removal of amino group protection: add hexahydropyridine / DMF solution, use nitrogen gas to agitate the reaction, and wash the resin with DMF after the reaction is completed. Take a small amount of resin and add 2-3 drops each of color test reagents A, B, and C (A: ninhydrin / dehydrated ethanol solution; B: pyridine; C: phenol / dehydrated ethanol solution), and then co-heat at 100°C After 3 minutes, the color of the solution and the resin should be blue, which means the reaction is complete.

[0028] 3. Condensation reaction: Add Fmoc-Thr(tBu)-OH and HBTU (O-benzotriazole-tetramethyluronium hexafluorophosphate), dissolve with an appropriate amount of DMF, add DIEA, blow with nitrogen, and use DMF washes the re...

Embodiment 2

[0035] Embodiment 2 hot plate method analgesic test

[0036] Place the mice on a hot plate at 55±0.5°C, and thermally stimulate the feet of the mice to produce pain responses, that is, foot licking responses. The time when the mice appeared to lick their feet was used as the index of pain response to judge whether the drug has analgesic effect.

[0037]In the hot plate analgesic test, female KM mice were given TLN-7 (doses were 0.04mg / kg, 0.08mg / kg, 0.16mg / kg) and diclofenac sodium (doses were 15mg / kg ) Afterwards, compared with female KM mice injected with saline in the tail vein, the latency of the mice to the hot plate heat stimulation to induce pain sensation was affected to varying degrees. All female KM mice firstly measured the normal pain threshold once, and then measured the pain threshold once respectively at 30 min, 60 min, and 90 min after injection, recorded the pain threshold, and calculated the increase rate of pain threshold. The test results are shown in Tab...

Embodiment 3

[0042] Embodiment 3 twisting body test

[0043] Chemical stimulants are injected into the abdominal cavity of mice, causing large-scale and long-lasting pain stimulation in the deep part, causing mice to produce writhing reactions (abdomen concave, hind limbs stretched, buttocks raised, etc.). The number of writhing in mice was used as the index of pain response to judge whether the drug has analgesic effect.

[0044] In the writhing test, after KM mice were given TLN-7 (doses were 0.04mg / kg, 0.08mg / kg, 0.16mg / kg) and diclofenac sodium (doses were 15mg / kg), compared In female KM mice injected with saline in the tail vein, the times of writhing were affected to varying degrees. 30 minutes after the administration, all mice were intraperitoneally injected with 0.3ml of 1% glacial acetic acid, and then observed the writhing reaction of the mice within 15 minutes, recorded the times of writhing, and calculated the analgesic rate. The test results are shown in Table 2.

[0045] ...

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Abstract

The invention discloses a polypeptide having pain stopping effect, wherein the amino acid sequence is Phe-Cys-Ser-Trp-Lys-Cys-Thr, and the two Cys are linked by a disulfide bond. According to the present invention, the polypeptide can be used for preparing products for the prevention and / or treatment of pains, has strong pain stopping effect, can inhibit neurogenic inflammations and block neuralgia, and further has characteristics of high safety and broad development prospects.

Description

technical field [0001] The invention relates to a polypeptide, in particular to a polypeptide with analgesic effect and application thereof. Background technique [0002] Pain is an unpleasant sensory and emotional experience caused by tissue damage or disease. According to statistics, about 30% of adults suffer from pain, and 2 of every 3 outpatients are patients with various pain symptoms or symptoms. There are at least 100 million pain patients in my country. Pain not only brings pain to patients, but also brings serious psychological and physical damage to them, increases the incidence of complications, prolongs recovery time, and increases medical expenses. Based on different pathogenesis, pain has different manifestations in various diseases, which brings certain difficulties to clinical pain treatment. [0003] Analgesics mainly act on the central or peripheral nervous system, selectively inhibit and relieve various pains, and relieve pain caused by fear, tension an...

Claims

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Application Information

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IPC IPC(8): C07K7/08A61K38/08A61P29/00
CPCA61K38/00C07K7/08
Inventor 游磊祁园鑫唐泽紫袁胜峰曲站红吴海玲
Owner SHANGHAI XINSHENGYUAN BIOLOGICAL MEDICAL
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