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Preparation method of phenylpropanoid compound

A compound, phenylpropanoid technology, applied in the field of medicine, can solve problems such as complex biological effects

Active Publication Date: 2016-08-24
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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  • Preparation method of phenylpropanoid compound
  • Preparation method of phenylpropanoid compound
  • Preparation method of phenylpropanoid compound

Examples

Experimental program
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Embodiment 1

[0063] The preparation of embodiment 1 phenylpropanoid compound

[0064] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0065] 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;

[0066] 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;

[0067] 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

[0070] The preparation of embodiment 2 phenylpropanoid compounds

[0071] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0072] 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;

[0073] 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;

[0074] 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

[0077] The preparation of embodiment 3 phenylpropanoid compounds

[0078] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0079] 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;

[0080] 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;

[0081] S3. The fraction MM-1 collected in step S2 is eluted with reverse phase ODS column chromatography, the eluent is a methanol-water system, and its volume ratio is 30:...

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Abstract

The invention relates to the technical field of medicines, discloses a preparation method of a phenylpropanoid compound, and particularly relates to a phenylpropanoid compound which is obtained by being separated from dried roots of moghania macrophylla (Willd.) O Ktze.. The phenylpropanoid compound is prepared through the steps of solvent extraction, column chromatographic separation and liquid phase preparation, separation and purification. The phenylpropanoid compound obtained through the method is reported for the first time and is high in purity. It is proved through experiments that the obtained novel phenylpropanoid compound can inhibit expression effects of cell inflammatory factors of TNF-alpha, IL-1 beta and IL-6, has an inhibiting effect on hydroxyl free radicals (-OH), has anti-inflammatory and antioxidant activities, is beneficial for treatment of various inflammatory diseases such as cervicitis, endometritis, pelvic inflammation, mastitis, faucitis and / or arthritis and can be developed into a novel drug. The compound is the phenylpropanoid compound with the structural formula as shown in a formula (I) and pharmaceutically acceptable salts thereof. Please see the formula (I) in the description.

Description

technical field [0001] The invention relates to the technical field of medicine, and more specifically, to a preparation method of a new phenylpropanoid compound. 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 antibodies, and perform immune regulation. Endocrine effects when produced in large quantities: ...

Claims

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Application Information

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IPC IPC(8): C07H15/203C07H1/08A61K31/704A61P29/00A61P19/02A61P15/00A61P11/04A61P39/06
CPCC07H1/08C07H15/203
Inventor 刘逆夫龚云夏博候李亚梅林丽美伍实花
Owner ZHUZHOU QIANJIN PHARMA
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