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Application of dragon's blood and flavonoid chemical component thereof in serving as antagonist of capsaicin receptor TRPV1 (transient receptor potential vanilloid 1)

A capsaicin receptor and chemical composition technology, applied in the fields of pharmacology and biology, can solve the problems that the modulation effect has not been reported yet

Inactive Publication Date: 2012-04-11
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The modulating effect of Dracaena A on the TRPV1 receptor has not been reported yet.

Method used

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  • Application of dragon's blood and flavonoid chemical component thereof in serving as antagonist of capsaicin receptor TRPV1 (transient receptor potential vanilloid 1)
  • Application of dragon's blood and flavonoid chemical component thereof in serving as antagonist of capsaicin receptor TRPV1 (transient receptor potential vanilloid 1)
  • Application of dragon's blood and flavonoid chemical component thereof in serving as antagonist of capsaicin receptor TRPV1 (transient receptor potential vanilloid 1)

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1: dragon's blood preparation

[0046] Prepare extracellular fluid first: Take 8.4824g of NaCl, 2.3832g of HEPES, 1.9816g of D-Glucose, 0.3728g of KCl, 0.222g of CaCl, 20.2032g of MgCl, add 800ml of purified water to fully dissolve, adjust the pH value of the solution to 7.4 with NaOH, and then add Dilute purified water to 1L and use it after filtering through a microporous membrane with a diameter of 0.45 μm.

[0047] Dissolve 5 mg of dragon's blood powder in 1 mL of dimethyl sulfoxide solution to make 5‰ dragon's blood dry liquid, and take 1 μL of dragon's blood dry liquid to dissolve in 1 L of extracellular fluid to make 1 L with a concentration of 5×10 -9 g / L dragon's blood preparation.

Embodiment 2

[0048] Embodiment 2: Stenophyllin A preparation

[0049] According to the method of Example 1, the extracellular fluid was prepared, and 0.0286 g of phoenixin A powder was dissolved in 10 mL of dimethyl sulfoxide solution to make a 10 mmol / L dry solution of cyphophyllin A, and 3.8 μL of phophyllin A was taken. The dry solution of astragalusin A was dissolved in 0.1L of extracellular fluid to make 0.1L of cyphophyllin A preparation with a concentration of 0.38 μmol / L

Embodiment 3

[0050] Example 3: Mixed preparations of cypholongerin A and phopholyptin B

[0051]According to the method of Example 1, the extracellular fluid was prepared, and 0.0286 g of phoenixin A powder was dissolved in 10 mL of dimethyl sulfoxide solution to make a 10 mmol / L dry liquid of cyphophyllin A. Dissolve 0.0286g of glucoside powder in 10mL dimethyl sulfoxide solution to make 10mmol / L dry solution of photolongin B, and take 38μL dry solution of photolongin A and 19μL dry solution of phodolongin B Dissolved in 0.1L of extracellular fluid to make 0.1L of eolongin A and phophoramin B mixed preparation, which contains phopholongin A at a concentration of 3.8 μmol / L and phopholongin B at a concentration of 1.9 μmol / L.

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PUM

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Abstract

The invention relates to applications of dragon's blood and a flavonoid chemical component thereof in serving as an antagonist of a capsaicin receptor TRPV1 (transient receptor potential vanilloid 1) and in preparing a medicament for treating diseases related to TRPV1 receptors, wherein the flavonoid chemical component is cochinchinenin A or a mixture of at least two of cochinchinenin A, cochinchinenin B and loureirin B. The invention also relates to a medicinal composition comprising the dragon's blood and and the flavonoid chemical component thereof. Independent component of the dragon's blood or the cochinchinenin A, or a combination of every two of the cochinchinenin A, the cochinchinenin B and the loureirin B, or a combination comprising the cochinchinenin A, the cochinchinenin B and the loureirin B has strong capsaicin receptor TRPV1 activation inhibition effect and excellent pharmacological action based on the inhibition effect, so that the dragon's blood or the flavonoid chemical component thereof serving as an active component can be used for preparing medicaments for treating or preventing TRPV1 related diseases, such as nociceptive pains, neurogenic pains, cancer pains, headache, urinary bladder functional disorder, inflammation and the like.

Description

technical field [0001] The invention relates to the fields of pharmacology and biology, in particular to the application of Dracaena japonicus and its flavonoid chemical components as an antagonist of capsaicin receptor TRPV1. Background technique [0002] There are two main types of analgesics currently available: opioids and non-opioids. Typical opioid analgesics, such as morphine, codeine, methadone, etc., have been used for a long time, but their analgesic mechanism has not been fully elucidated so far, and long-term use may cause dependence, addiction and other shortcomings. Restricted use. Non-opioid analgesics are mainly non-steroidal anti-inflammatory drugs, anilines, and salicylic acids. Most of these drugs are inhibitors of prostaglandin synthase, which mainly act on the nerve endings at the pain site. However, due to their The analgesic effect is not good, and there are obvious toxic and side effects so that its use is limited. Therefore, it is a major problem ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/889A61P25/04A61P29/00
Inventor 刘向明陈素梅之南维力斯沈州
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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