Glyceride compounds with anti-inflammatory activity, and preparation method and application thereof

A technology of ester compounds and compounds, applied in anti-inflammatory agents, organic chemistry, active ingredients of esters, etc., can solve problems that have not been reported

Inactive Publication Date: 2012-09-19
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] But do not see the report of the glyceride compound with anti-inflammatory activity isolated from propolis provided by the present invention so far

Method used

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  • Glyceride compounds with anti-inflammatory activity, and preparation method and application thereof
  • Glyceride compounds with anti-inflammatory activity, and preparation method and application thereof
  • Glyceride compounds with anti-inflammatory activity, and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0037] The preparation of embodiment 1 glyceride compound

[0038] 1. Preparation of propolis extract

[0039] The propolis is soaked in methanol overnight, ultrasonically extracted 2-3 times, 1-2 hours each time, the extracts are combined, the solvent is recovered under reduced pressure, and the extract extract is obtained.

[0040] 2. Separation and purification of glyceride compounds

[0041] The extract extract was routinely subjected to silica gel decompression column chromatography (the silica gel in the column is 100-200 mesh, 10 Pa), and petroleum ether (60-90°C)-acetone system was used at a volume ratio of 50:1, 20:1 , 10:1, 8:2, 7:3 each 2500ml, carry out gradient elution successively, collect a part every 500ml, spot each eluate, carry out thin-layer chromatography analysis, with petroleum ether (60-90 ℃ )-acetone system was used as a developing agent, and silica gel G254 thin-layer chromatography was carried out at room temperature. According to the thin-layer ch...

Embodiment 2

[0054] Embodiment 2 anti-inflammatory activity test

[0055] The anti-inflammatory activity of monomeric compounds 1-5 was demonstrated on the expression levels of IL-1β, IL-6 and COX-2 mRNA in lipopolysaccharide (LPS)-induced RAW 264.7 mouse macrophages.

[0056] 1. Preparation of drug solution

[0057] 1) Prepare monomer compounds 1~5 with DMSO to make 100mmol / mL solutions respectively, and store at -4°C;

[0058] 2) LPS: E.Coli O111:B4 (Merck Millipore, USA, product number: LPS25), made into a 100 μg / mL solution with redistilled water, and stored at -20°C.

[0059] 2. Cell line: RAW 264.7 mouse macrophages, provided by the Chinese Academy of Sciences in Shanghai.

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Abstract

The invention relates to glyceride compounds with anti-inflammatory activity, and a preparation method and application thereof. The preparation method comprises the following steps: acquiring an extractive from propolis, conventionally carrying out silica gel reduced pressure column chromatography, carrying out gradient elution with a petroleum ether (60-90 DEG C)-acetone system, merging the eluates according to the analytic result of thin-layer chromatography, and separating to obtain the glyceride compounds. The in-vitro anti-inflammatory activity test proves that the glyceride compounds can obviously inhibit the expression levels of IL-1beta, IL-6 and COX-2mRNA in the mouse macrophage RAW 264.7 caused by lipopolysaccharide (LPS), and have a dosage dependency relationship, which indicates that the glyceride compounds have obvious anti-inflammatory activity. The invention can be used for preparing new anti-inflammatory activity medicines.

Description

technical field [0001] The present invention relates to glyceride compositions. Specifically, the present invention relates to a glyceride compound with anti-inflammatory activity and a preparation method thereof. Background technique [0002] Propolis is a viscous substance formed by Italian bees (Apismellifera L.) from the secretions of new shoots and calluses collected from plants and mixed with the secretions of their mandibular glands and wax glands. Propolis has a medicinal history of more than 2,000 years. It has antibacterial, antiviral, antiulcer, anti-inflammatory and immune-enhancing effects. The 2005 edition of "Chinese Pharmacopoeia" has begun to include propolis. [0003] The chemical composition of propolis is very complex, and its pharmacological activities are diverse. Propolis from different production areas around the world has great differences in its chemical composition and pharmacological activity. At present, about a thousand compounds have been i...

Claims

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Application Information

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IPC IPC(8): C07C69/732C07C69/734C07C69/618C07C69/675C07C67/48A61K31/22A61P29/00
Inventor 史海明杨海莎张晓伟
Owner SHANGHAI JIAO TONG UNIV
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