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Phenylpropanoid compound and application of pharmaceutically acceptable salt thereof to preparing drugs for treating inflammatory diseases

A technology for inflammatory diseases and compounds, applied in the field of medicine, can solve problems such as complex biological effects, and achieve the effects of high purity, simple structure, and simple extraction and separation methods.

Active Publication Date: 2016-06-15
ZHUZHOU QIANJIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many target cells for IL-6, including macrophages, liver cells, resting T cells, activated B cells, and plasma cells; its biological effects are also very complex

Method used

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  • Phenylpropanoid compound and application of pharmaceutically acceptable salt thereof to preparing drugs for treating inflammatory diseases
  • Phenylpropanoid compound and application of pharmaceutically acceptable salt thereof to preparing drugs for treating inflammatory diseases
  • Phenylpropanoid compound and application of pharmaceutically acceptable salt thereof to preparing drugs for treating inflammatory diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] The preparation of embodiment 1 phenylpropanoid compound

[0058] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0059] S1. Take 50 kg of big-leaved jackfruit, use the root as raw material, dry it, and cut it into small pieces. Reflux extraction with 8 times the amount of 60% ethanol for 3 times, each time for 2 hours, combine the extracts, concentrate until there is no alcohol smell, and obtain the extract for later use;

[0060] S2. Dissolve the extract concentrated in step S1 in 10L of water, and use D101 macroporous adsorption resin column to elute it. The eluent is water, and the eluent is eluted for 3 column volumes. The eluate is collected and named as MM -1, standby;

[0061] S3. The fraction MM-1 collected in step S2 is eluted with reverse-phase ODS column chromatography, the eluent is methanol-water system, and its volume ratio is 25:75, and 18 column volumes are eluted, acco...

Embodiment 2

[0064] The preparation of embodiment 2 phenylpropanoid compounds

[0065] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0066] S1. Take 40 kg of big-leaved jackfruit, use the root as raw material, dry it, and cut it into small pieces. Reflux extraction with 6 times the amount of 50% ethanol for 2 times, each time for 1 hour, combine the extracts, concentrate until there is no alcohol smell, and obtain the extract for later use;

[0067] S2. Dissolve the concentrated extract in step S1 in 5L of water, and use D101 macroporous adsorption resin column to elute it. The eluent is ethanol and water with a volume ratio of 15:85, and eluted for 3 column volumes , collect the eluate, name it MM-1, and set aside;

[0068] S3. The fraction MM-1 collected in step S2 is eluted with reverse-phase ODS column chromatography, the eluent is methanol-water system, and its volume ratio is 20:80, and 18 column v...

Embodiment 3

[0071] The preparation of embodiment 3 phenylpropanoid compounds

[0072] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0073] S1. Take 60 kg of big-leaved jackfruit, use the root as raw material, dry it, and cut it into small pieces. 7 times the amount of 70% ethanol was refluxed and extracted 4 times, each time for 3 hours, the extracts were combined, concentrated until there was no alcohol smell, and the extract was obtained for later use;

[0074] S2. Dissolve the concentrated extract in step S1 in 8L of water, and use a D101 macroporous adsorption resin column to elute it. The eluent is ethanol and water with a volume ratio of 10:90, and eluted for 3 column volumes , collect the eluate, name it MM-1, and set aside;

[0075] S3. The fraction MM-1 collected in step S2 is eluted with reversed-phase ODS column chromatography, the eluent is methanol-water system, its volume ratio is 30:70, a...

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Abstract

The invention relates to the technical field of medicine and discloses a phenylpropanoid compound and application of pharmaceutically acceptable salt thereof to preparing drugs for treating inflammatory diseases. The phenylpropanoid compound can suppress the expression effects of cell inflammatory factors TNF-alpha, IL-1beta and IL-6 and has a suppressing effect on (-OH) of hydroxyl radicals so that anti-inflammatory and anti-oxidant activity can be achieved, and direction is provided for development of drugs for treating inflammatory diseases such as cervicitis, endometritis, pelvic inflammation, mastitis, sphagitis and / or arthritis. Please see the structural formula in the description.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of a phenylpropanoid compound and a pharmaceutically acceptable salt thereof in the preparation of medicines for treating inflammatory diseases. Background technique [0002] The components extracted and separated from natural medicines have various structures and significant activities. Separation, purification, structural modification, transformation and total synthesis of the components have always been a main idea in the development of new drugs. [0003] TNF-α: It is a cytokine that can directly kill tumor cells without obvious toxicity to normal cells. It is one of the biologically active factors with the strongest direct tumor killing effect found so far, but its toxic and side effects are also very serious. [0004] IL-1β: At local low concentrations, it can co-stimulate the activation of APC and T cells, promote the proliferation of B cells and secrete...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7034A61P29/00A61K36/758
CPCA61K31/7034A61K36/19A61K36/232A61K36/29A61K36/344A61K36/486A61K36/738A61K36/758A61K2300/00
Inventor 刘逆夫龚云夏博候李亚梅林丽美伍实花赵威
Owner ZHUZHOU QIANJIN PHARMA
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