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Application of cerebroside compounds in the preparation of analgesic drugs

A technology of compounds and cerebrosides, which is applied in the field of natural medicinal chemistry, can solve the problems of lack of significant and reliable curative effect and few side effects, and achieve the effect of increasing pain threshold and relieving visceral pain

Inactive Publication Date: 2015-10-21
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 cerebroside compounds in the preparation of analgesic drugs
  • Application of cerebroside compounds in the preparation of analgesic drugs
  • Application of cerebroside compounds in the 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] Experimental main materials : 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 : Adult ICR mice were killed by cervical dislocation. After decapitation to remove brain tissue, a pair of trigeminal ganglia the size of a grain of rice at the base of the skull were washed in ice-cold Hank's balanced salt solution, and then put into type Ⅰ collagen Enzyme (1.5mg / ml) and trypsin (0.5mg / ml), digested in a water bath at 37°C for 15 minutes, washed the tissue 3 times with standard extracellular solution, and gently blown the tissue with a polished Pasteur tube. until the ganglion disperses. 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 electrophysiolog...

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] Experimental main materials : 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 has the characteristics of being difficult to dissolve 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] Pain Threshold Determination: (1) Determination of mechanical pain threshold (paw withdrawal threshold, PWT): Calculate 50% PWT with von Frey fiber. The determination of 50% PWT refers to the mechanical ...

Embodiment 3

[0050] Example 3 Oral administration of cerebroside A (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 to the concentration required for treatment with physiological saline (to keep the final concentration of ethanol below 1%) to obtain a pharmaceutical preparation for intragastric administration . 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 pai...

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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 Patents(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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