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Application of benzene derivatives to prepare pain-easing anti-inflammation medicines

An anti-inflammatory drug and drug technology, applied in the field of medicine, can solve problems such as no report on analgesic effect, no report on anti-inflammatory effect in vivo, etc.

Active Publication Date: 2014-10-29
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Among the above compounds, the analgesic effects of 3,5-dimethoxytoluene, 2,3,5-trimethoxytoluene and 3,4,5-trimethoxytoluene have not been reported; In vivo anti-inflammatory effects of methoxytoluene, 2,3,5-trimethoxytoluene, 3,4,5-trimethoxytoluene, methyl eugenol have not been reported

Method used

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  • Application of benzene derivatives to prepare pain-easing anti-inflammation medicines
  • Application of benzene derivatives to prepare pain-easing anti-inflammation medicines
  • Application of benzene derivatives to prepare pain-easing anti-inflammation medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1: The effect of test monomer compound on mouse writhing response caused by acetic acid

[0015] 1 material

[0016] 1.1 Animals

[0017] ICR mice, weighing 18-22 g, half male and half male, were provided by the Experimental Animal Department of Peking University (permit number: SCXK11-00-0008). The animals were kept in a standard environment: temperature (23±1)°C, relative humidity (55±5)%, light and dark cycle 12h / 12h, and standard pellet feed.

[0018] 1.2 Reagents

[0019] Methyleugenol (methyleugenol, Lot: PH3YH-MG) was purchased from TCI Company, 3,5-dimethoxytoluene (3,5-dimethoxytoluene, Lot: 10099004) was purchased from Alfa Aesar Company, 3,4,5- Trimethoxytoluene (3,4,5-trimethoxytoluene, Lot: 19923) was purchased from Aladdin Company. 2,3,5-Trimethoxytoluene was synthesized by the author. The structure was identified by MS and NMR, and the purity was higher than 98% by GC-MS (area normalization method). Aspirin enteric-coated tablets (Beijing ...

Embodiment 2

[0028] Embodiment 2: The impact of test monomer compound on mouse ear swelling caused by xylene

[0029] 1 material

[0030] 1.1 Animals

[0031] Experimental animals are the same as in Example 1.

[0032] 1.2 Reagents

[0033] Methyleugenol (methyleugenol, Lot: PH3YH-MG) was purchased from TCI Company, 3,5-dimethoxytoluene (3,5-dimethoxytoluene, Lot: 10099004) was purchased from Alfa Aesar Company, 3,4,5- Trimethoxytoluene (3,4,5-trimethoxytoluene, Lot: 19923) was purchased from Aladdin Company. 2,3,5-Trimethoxytoluene was synthesized by the author. Dexamethasone sodium phosphate injection (Tianjin Pharmaceutical Jiaozuo Co., Ltd., batch number 11111311), xylene (Beijing Chemical Plant, batch number 20100513), Tween 80 (GFCO Chemical Supplies, batch number 0160Fc0099A28).

[0034] 1.3 Instruments

[0035] YLS2Q4 ear swelling puncher (Shandong Academy of Medical Sciences Equipment Station), BS / BT electronic balance (sartorius AG).

[0036] 2 methods

[0037] ICR mice, ...

Embodiment 3

[0043] Embodiment 3: The effect of the combination of test compounds on the writhing response of mice induced by acetic acid

[0044] 1 material

[0045] 1.1 Animals

[0046] Experimental animals are the same as in Example 1.

[0047] 1.2 Reagents

[0048]Methyleugenol (methyleugenol, Lot: PH3YH-MG) was purchased from TCI Company, 3,5-dimethoxytoluene (3,5-dimethoxytoluene, Lot: 10099004) was purchased from Alfa Aesar Company, 3,4,5- Trimethoxytoluene (3,4,5-trimethoxytoluene, Lot: 19923) was purchased from Aladdin Company. 2,3,5-Trimethoxytoluene was synthesized by the author. Aspirin enteric-coated tablets (Beijing Shuguang Pharmaceutical Co., Ltd., batch number 120505), acetic acid (Beijing Chemical Plant, batch number 20100916), Tween 80 (GFCO Chemical Supplies, batch number 0160Fc0099A28).

[0049] 1.3 Instruments

[0050] BS / BT electronic balance (sartorius AG).

[0051] 2 methods

[0052] ICR mice, half male and half male, were divided into random groups, 6 mice...

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Abstract

The invention relates to four main chemical compositions (3,5-dimethoxytoluene, 2,3,5-trimethoxytoluene, 3,4,5-Trimethoxytoluene and methyl eugenol) absorbable by human body after herba asari is applied and application of the four main chemical compositions to prepare pain-easing anti-inflammation medicines. Experiment research firstly discovers that 3,5-dimethoxytoluene, 2,3,5-trimethoxytoluene and 3,4,5-Trimethoxytoluene have effects of easing pain and diminishing inflammation in vivo, and methyl eugenol and combination of the four compounds have pain-easing effect. The chemical compositions and the combination thereof have good pain-easing anti-inflammation effects, and are beneficial for research and development of novel pain-easing anti-inflammation medicines.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of various effective monomer components of traditional Chinese medicine Asarum in the preparation of analgesic and anti-inflammatory drugs. Background technique [0002] Asarum is a commonly used traditional Chinese medicine, which is used to treat diseases such as wind-cold headache, phlegm retention, dyspnea and cough, joint pain and toothache. The 2010 edition of "Chinese Pharmacopoeia" stipulates that Asarum is Asarum heterotropoides Fr. Schmidt var. mandshuricum (Maxim.) Kitag., Asarum sieboldii Miq. Dried roots and rhizomes of Asarum sieboldii Miq. Modern pharmacological studies have shown that Asarum has good analgesic and anti-inflammatory effects. [0003] At present, the research on Asarum mainly focuses on its chemical constituents and pharmacological effects, and the research on its absorbable constituents after administration is still blank. After the inven...

Claims

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Application Information

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IPC IPC(8): A61K31/09A61P29/00
Inventor 蔡少青叶加徐风李晨杨华万丹高小力
Owner PEKING UNIV
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