Phenylpropanoid compounds and their pharmaceutically acceptable salts and pharmaceutical compositions

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

Active Publication Date: 2018-12-11
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 compounds and their pharmaceutically acceptable salts and pharmaceutical compositions
  • Phenylpropanoid compounds and their pharmaceutically acceptable salts and pharmaceutical compositions
  • Phenylpropanoid compounds and their pharmaceutically acceptable salts and pharmaceutical compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] The preparation of embodiment 1 phenylpropanoid compound

[0055] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0056] 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;

[0057] 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;

[0058] 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

[0061] The preparation of embodiment 2 phenylpropanoid compounds

[0062] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0063] 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;

[0064] 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;

[0065] 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

[0068] The preparation of embodiment 3 phenylpropanoid compounds

[0069] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0070] 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;

[0071] 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;

[0072] 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 phenylpropanoids, and pharmaceutically acceptable salts and a pharmaceutical composition thereof. The structure of the phenylpropanoids is disclosed as Formula (I), and the structure of the pharmaceutically acceptable salts is disclosed as Formula (II) or Formula (III). The phenylpropanoids and pharmaceutically acceptable salts thereof have the action of inhibiting expression of cell inflammatory factors TNF-alpha, IL-1beta and IL-6, have the inhibiting action on hydroxy free radicals (-OH), further have anti-inflammatory and antioxidation activities, and thus, have favorable application prospects in preparing drugs for treating diseases related to the factors above, such as cervicitis, endometritis, pelvic inflammation, mastitis, faucitis, arthritis and / or other inflammation diseases.

Description

technical field [0001] The present invention relates to the technical field of medicine, and more specifically, relates to a phenylpropanoid compound, a pharmaceutically acceptable salt thereof and a pharmaceutical composition. 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 r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H15/203A61K31/7034A61K36/758A61P29/00A61P19/02A61P11/04A61P15/14A61P15/00
CPCA61K9/0019A61K31/7034A61K36/758C07H15/203A61K2300/00
Inventor 张鹏彭开锋林丽美伍实花夏博候佘娜朱大安
Owner ZHUZHOU QIANJIN PHARMA
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