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Phenylpropanoid compounds, pharmaceutically acceptable salts and pharmaceutical compositions thereof

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

Active Publication Date: 2019-01-08
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, pharmaceutically acceptable salts and pharmaceutical compositions thereof
  • Phenylpropanoid compounds, pharmaceutically acceptable salts and pharmaceutical compositions thereof
  • Phenylpropanoid compounds, pharmaceutically acceptable salts and pharmaceutical compositions thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] The preparation of embodiment 1 phenylpropanoid compound

[0056] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0057] 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;

[0058] 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;

[0059] 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

[0062] The preparation of embodiment 2 phenylpropanoid compounds

[0063] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0064] 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;

[0065] 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;

[0066] 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

[0069] The preparation of embodiment 3 phenylpropanoid compounds

[0070] This embodiment provides a preparation method of phenylpropanoid compounds shown in formula (I), comprising the following steps:

[0071] 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;

[0072] 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;

[0073] 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 discloses a phenylpropanoid compound and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition, belonging to the field of medical technology. The structure of the phenylpropanoid compound is as shown in a formula (I) which is described in the specification; and the structure of the pharmaceutically acceptable salt is as shown in a formula (II) or formula (III) which is described in the specification. The phenylpropanoid compound and the pharmaceutically acceptable salt thereof are capable of inhibiting the content of the inflammation cytokine NO and expression of the inflammation cytokines TNF-alpha, IL-1beta and IL-6 and exerts inhibitory effect on hydroxyl radicals (-OH), so the phenylpropanoid compound and the pharmaceutically acceptable salt thereof have anti-inflammatory and anti-oxidation activity and have good application prospect in preparation of drugs used for treating inflammatory diseases related to the inflammation cytokines, e.g., cervicitis, endometritis, pelvic inflammation, mastitis, pharyngolaryngitis and / or arthritis.

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): C07H15/203C07H1/08C07H1/06A61K31/704A61P29/00A61P15/00A61P11/04A61K36/758A61K36/738A61K36/486A61K36/29A61K36/19A61K36/232A61K36/344A61P19/02
CPCA61K31/704A61K36/19A61K36/232A61K36/29A61K36/344A61K36/486A61K36/738A61K36/758C07H1/06C07H1/08C07H15/203A61K2300/00
Inventor 龚云张鹏夏博候彭开锋李亚梅佘娜
Owner ZHUZHOU QIANJIN PHARMA
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