Phenylpropanoid compounds, pharmaceutically acceptable salts and pharmaceutical compositions thereof

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

Active Publication Date: 2019-01-04
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

[0054] Example 1 Preparation of phenylpropanoids

[0055] This embodiment provides a method for preparing the phenylpropanoid compound represented by formula (I), which includes the following steps:

[0056] S1. Take 50 kg of big leaves, take the roots as raw materials, dry, and cut into small pieces. Reflux with 8 times the amount of 60% ethanol for 3 times, 2 hours each time, combine the extracts, concentrate until there is no alcohol taste, and obtain the extract for use;

[0057] S2. Dissolve the concentrated extract in step S1 in 10L of water, and use D101 macroporous adsorption resin column to elute it, the eluent is water, elute 3 column volumes, collect the eluent and name it MM -1, spare;

[0058] S3. The fraction MM-1 collected in step S2 is eluted by reverse-phase ODS column chromatography. The eluent is a methanol-water system with a volume ratio of 25:75. The elution is performed by 18 column volumes. Collect the eluent of one fraction for every 3 column volumes, and co...

Embodiment 2

[0061] Example 2 Preparation of phenylpropanoids

[0062] This embodiment provides a method for preparing the phenylpropanoid compound represented by formula (I), which includes the following steps:

[0063] S1. Take 40kg of big leaves, take root as raw material, dry, and cut into small pieces. Reflux with 6 times the amount of 50% ethanol for 2 times, 1 hour each time, combine the extracts, concentrate until there is no alcohol taste, 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 the volume ratio of water is 15:85, eluting 3 column volumes , Collect the eluate and name it MM-1 for use;

[0065] S3. The fraction MM-1 collected in step S2 is eluted by reverse-phase ODS column chromatography. The eluent is a methanol-water system with a volume ratio of 20:80, and 18 column volumes are eluted. Collect the eluent of one fraction for ev...

Embodiment 3

[0068] Example 3 Preparation of phenylpropanoids

[0069] This embodiment provides a method for preparing the phenylpropanoid compound represented by formula (I), which includes the following steps:

[0070] S1. Take 60 kg of big leaves, take root as raw material, dry, and cut into small pieces. Seven times the amount of 70% ethanol was refluxed and extracted 4 times for 3 hours each time, the extracts were combined and concentrated until there was no alcohol taste, and the extract was obtained for use;

[0071] S2. Dissolve the concentrated extract in step S1 in 8L of water, and use D101 macroporous adsorption resin column to elute it. The eluent is ethanol and water with a volume ratio of 10:90, eluting 3 column volumes , Collect the eluate and name it MM-1 for use;

[0072] S3. The fraction MM-1 collected in step S2 is eluted by reverse-phase ODS column chromatography. The eluent is a methanol-water system with a volume ratio of 30:70, and 18 column volumes are eluted. Collect th...

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Abstract

The invention relates to the technical field of medicine, and discloses a phenylpropanoid compound and pharmaceutically acceptable salt and a medicinal composition thereof. The structure of the phenylpropanoid compound is as shown in a formula (I). The phenylpropanoid compound and the pharmaceutically acceptable salt have an effect of inhibiting content of a macrophage inflammatory cytokine NO so as to achieve the anti-inflammatory activity by an NO inhibiting approach, and has very wide application prospect on the aspects of preparing medicaments for treating diseases related to the macrophage inflammatory cytokine NO, such as inflammatory diseases of cervicitis, endometritis, pelvic inflammation, mastitis, sphagitis and / or arthritis and the like. (referring to the specification) (I).

Description

Technical field [0001] The present invention relates to the technical field of medicine, and more specifically, to a phenylpropanoid compound and a pharmaceutically acceptable salt and pharmaceutical composition thereof. Background technique [0002] The components extracted and separated from natural medicines have diverse structures and significant activities. Their separation, purification, structural modification, transformation and total synthesis have always been a main idea for new drug development. [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 side effects are also very serious. [0004] IL-1β: Co-stimulates APC and T cell activation at local low concentrations, promotes B cell proliferation and secretion of antibodies, and performs immune regulation. When produced in large quantities, it has a...

Claims

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Application Information

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Patent Type & AuthorityPatents(China)
IPC IPC(8): C07H15/203A61K31/7034A61P29/00A61P15/00A61P19/02A61P1/02A61K9/20A61K9/14A61K9/48A61K9/16A61K9/08A61K47/04A61K36/758A61K36/48
CPCA61K9/0019A61K9/08A61K9/143A61K9/1611A61K9/2009A61K9/485A61K31/7034A61K36/19A61K36/232A61K36/29A61K36/344A61K36/48A61K36/486A61K36/738A61K36/758C07H15/203A61K2300/00
Inventor张鹏彭开锋林丽美伍实花夏博候佘娜廖爱玲
OwnerZHUZHOU QIANJIN PHARMA