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Phenolic acid compound, as well as preparation method and pharmaceutical applications thereof

A kind of compound and phenolic acid technology, which is applied in the field of preparation of phenolic acid compound-ethyl rosmarinate

Inactive Publication Date: 2015-01-07
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no evidence that ethyl rosmarinate can improve the apoptosis of vascular endothelial cells induced by high glucose, reduce the apoptosis of vascular endothelial cells induced by free fatty acids, improve the glucose consumption of hepatocytes under insulin resistance, and inhibit the hepatocytes induced by oleic acid. Fat accumulation and regulation of postprandial blood glucose activity report

Method used

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  • Phenolic acid compound, as well as preparation method and pharmaceutical applications thereof
  • Phenolic acid compound, as well as preparation method and pharmaceutical applications thereof
  • Phenolic acid compound, as well as preparation method and pharmaceutical applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Embodiment 1: the preparation of ethyl rosmarinate :

[0059] Take 5kg of dried Pinnaea chinensis whole herb, pulverize it, and extract 3 times with 10 times the amount of 80% ethanol under reflux, combine the extracts, concentrate under reduced pressure, and extract the concentrated solution 4 times with 4 times the amount of petroleum ether and ethyl acetate successively , after concentrating the ethyl acetate extract under reduced pressure, it was subjected to macroporous resin D101 column chromatography, and eluted with distilled water, 60%, and 95% ethanol successively. Collect 60% ethanol water eluate, concentrate under reduced pressure, MCI column chromatography (50% methanol water elution), collect eluate, concentrate under reduced pressure, obtain ethyl rosmarinate crude product, ethyl rosmarinate The crude product was subjected to silica gel column chromatography and eluted with dichloromethane:methanol (20:1). The eluate was collected, concentrated under re...

Embodiment 2

[0060] Embodiment 2: the preparation of ethyl rosmarinate :

[0061] Take 5kg of dried Pinnaea chinensis whole herb, pulverize it, and extract 3 times with 12 times the amount of 85% ethanol under reflux, combine the extracts, concentrate under reduced pressure, and extract the concentrated solution 4 times with 5 times the amount of petroleum ether and ethyl acetate successively , after the ethyl acetate extract is concentrated under reduced pressure, carry out macroporous resin CAD-40 column chromatography, use methanol aqueous solution to elute successively, collect 50% methanol water eluate, concentrate under reduced pressure, carry out MCI column chromatography again ( 50% methanol for water elution), collect the eluate, concentrate under reduced pressure to obtain the crude product of ethyl rosmarinate, the crude product of ethyl rosmarinate is subjected to silica gel column chromatography, dichloromethane: acetone (4: 1) washing The eluate was collected, concentrated ...

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Abstract

The invention belongs to the field of pharmaceutical technology. The invention discloses a preparation method and pharmaceutical applications of a phenolic acid compound, namely ethyl rosmarinate. The ethyl rosmarinate is prepared by comprising the following steps: by taking Clinopodium. chinense (Benth.)O. Kuntze whole herb as a raw material, performing grinding, alcohol extraction and reduced pressure recovery to obtain a concentrate, extracting through petroleum ether and ethyl acetate to obtain ethyl acetate extract, and performing repeated column chromatography through macroporous resin, silica gel and MCI. The ethyl rosmarinate has effects of remarkably inhibiting vascular endothelial cell apoptosis induced by high glucose and freefatty acid, improving liver cytolipin consumption under insulin resistance, improving lipid metabolism and inhibiting the activity of alpha-glucosidase. The phenolic acid compound can be used for preparing a medicament for preventing and treating diabetes mellitus, diabetic peripheral vasculopathy, diabetic cardiovascular complications, glucose and lipid metabolism disorders, atherosclerosis, coronary heart diseases and other cardiovascular and cerebrovascular diseases, obesity and fatty liver diseases.

Description

1. Technical field [0001] The invention belongs to the technical field of pharmacy, relates to a preparation method of phenolic acid compound-ethyl rosmarinate, and relates to the concurrent use of ethyl rosmarinate in the preparation of prevention and treatment of diabetes, diabetic peripheral vascular disease, and diabetic cardiovascular and cerebrovascular diseases. disease, glucose and lipid metabolism disorders, atherosclerosis, coronary heart disease and other cardiovascular and cerebrovascular diseases, obesity and fatty liver disease. 2. Background technology [0002] Diabetes mellitus is a group of metabolic abnormal syndromes caused by the interaction of genetic and environmental factors, characterized by hyperglycemia, metabolic disorders, and closely related to insulin secretion. Diabetes can be divided into insulin-dependent diabetes mellitus (Insulin Dependent Diabetes Mellitus, IDDM is also called type 1) and non-insulin-dependent diabetes mellitus (Noinsulin ...

Claims

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Application Information

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IPC IPC(8): C07C69/732A61K31/216A61P3/10A61P9/00A61P3/06A61P9/10A61P3/04A61P1/16
CPCC07C69/732C07C67/48
Inventor 吴斐华梁敬钰王立英何柏球王珊珊陈凯曾彪
Owner CHINA PHARM UNIV
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