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Application of cerebrosides in preparation of analgesic drugs

A compound and cerebroside technology, applied in the field of natural medicinal chemistry, can solve the problems of lack of significant and reliable curative effect, less side effects, etc., and achieve the effect of improving pain threshold and relieving visceral pain

Inactive Publication Date: 2013-12-04
NANJING MEDICAL UNIV +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is still a lack of analgesics with significant and reliable efficacy, few side effects, and no dependence (addiction) for long-term use.

Method used

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  • Application of cerebrosides in preparation of analgesic drugs
  • Application of cerebrosides in preparation of analgesic drugs
  • Application of cerebrosides in preparation of analgesic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Cerebroside A and Cerebroside B can dose-dependently inhibit the activity of TRPV1

[0041] Main materials for the experiment: ICR mice (10 males and 10 females each), weighing 25 g to 30 g, were purchased from the Experimental Animal Center of Jiangsu Province.

[0042] Experimental operation: take adult ICR mice, kill them by cervical dislocation, decapitate and remove the brain tissue, take a pair of rice grain-sized trigeminal ganglia at the base of the skull, wash them in ice-cold Hank's balanced salt solution, and then put them into I Type collagenase (1.5mg / ml) and trypsin (0.5mg / ml), digested in a 37°C water bath for 15 minutes, washed the tissue 3 times with standard extracellular fluid, and gently blown with a polished Pasteur tube tissue until the ganglia are dispersed. After filtering through a 200-mesh filter, place it in a 35mm petri dish, and after 1-6 hours of attachment at room temperature, use the technique of electrophysiological patch clam...

Embodiment 2

[0044] Example 2 Intraperitoneal injection (i.p.) of cerebroside A can increase the threshold of thermal pain and mechanical pain in mice

[0045] Main materials for the experiment: ICR mice (20 males and 20 females each), weighing 25 g to 30 g, were purchased from the Experimental Animal Center of Jiangsu Province.

[0046] Experimental operation: Cerebroside A is relatively insoluble in water. Therefore, the extracted cerebroside A was first dissolved in 99.5% ethanol, and then the mother solution was diluted to the concentration required for treatment with physiological saline (to keep the final concentration of ethanol below 1%) to obtain a pharmaceutical preparation according to 5.0mg / kg dose was injected intraperitoneally.

[0047] Determination of pain threshold: (1) Determination of mechanical pain threshold (paw withdrawal threshold, PWT): 50% PWT was calculated by using von Frey filaments. The determination of 50% PWT refers to the mechanical force that can cause 50...

Embodiment 3

[0050] Example 3 Cerebroside A gavage (o.p.) can increase the threshold of thermal pain and mechanical pain in mice

[0051] Experimental main materials: with embodiment 2.

[0052] Experimental operation: Therefore, first dissolve the extracted cerebroside A in 99.5% ethanol, and then dilute the mother solution with physiological saline to the concentration required for treatment (to keep the final concentration of ethanol below 1%) to obtain a pharmaceutical preparation. Gavage. After 20 minutes of mechanical paw withdrawal threshold detection or thermal pain threshold detection, determine the basic threshold level, then intragastrically administer cerebroside A at a dose of 5.0 mg per kg body weight, and then detect the mechanical paw withdrawal threshold and thermal pain threshold of mice for 8 hours .

[0053] Experimental results: (1) After 60 minutes of intragastric administration of cerebroside A, the mechanical pain threshold of mice began to increase, and reached t...

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Abstract

The invention provides application of cerebrosides in preparation of analgesic drugs. An animal experiment on pharmacology verifies that the cerebrosides are administrated through the ways such as intraperitoneal injection, gavage and skin smearing; all the three ways can improve the threshold values of a mouse to pains caused by heat and mechanical stimulation in a dose-dependent manner; the cerebrosides can remarkably relieve a neuropathic pain, an inflammatory pain and an acetic-acid-induced visceral pain. A cerebroside A or a cerebroside B can inhibit the activity of a vanilloid receptor TRPV1, so that the cerebrosides can increase an algesia threshold value and achieve the purpose of abirritation by lowering the activity of the vanilloid receptor TRPV1. According to the invention, the application of the cerebrosides serving as internal and external analgesic drugs is developed.

Description

technical field [0001] The invention belongs to the field of natural medicinal chemistry and relates to the application of cerebroside compounds in preparing analgesic drugs. Background technique [0002] Pain is a complex physiological and psychological activity, and it is one of the most common clinical symptoms. Pain often plagues people's health and quality of life, and long-term severe pain (such as cancer pain, intractable pain, etc.) is an unbearable torture. In 1970, endogenous enkephalins and exogenous morphine were found to have powerful analgesic effects. Since then, neurotransmitters such as serotonin and their corresponding receptors have also been reported to participate in the control of the endogenous pain system. Unless narcotic analgesics (such as aspirin) and narcotic analgesics (such as morphine) are used for pain relief, some non-steroidal anti-inflammatory drugs have also been used. However, there is still a lack of analgesic drugs with significant an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7032A61P25/04A61P29/00
Inventor 陈玲戚建华缪冶炼周丽彬叶英陈蕾沙莎
Owner NANJING MEDICAL UNIV
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