Compound with anti-inflammatory effect and preparation method and application thereof

An anti-inflammatory effect and compound technology, applied in the field of medicine, can solve problems such as complex components, difficult to clarify the material basis and mechanism of action

Inactive Publication Date: 2020-05-08
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically, the antipyretic and anti-inflammatory drugs of traditional Chinese medicine are mostly compound prescriptions. Due to their complex components, it is difficult to clarify their material basis and mechanism of action. Finding effective ingredients is of great significance for the development of antipyretic and anti-inflammatory drugs with clear ingredients, quality controllable, safe and effective, and provides a wider choice for clinical medication

Method used

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  • Compound with anti-inflammatory effect and preparation method and application thereof
  • Compound with anti-inflammatory effect and preparation method and application thereof
  • Compound with anti-inflammatory effect and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The preparation of embodiment 1 compound of the present invention

[0041] 1) 5Kg of dried water wenghua, add 10 times the volume concentration of 70% ethanol aqueous solution, extract twice, each time for 2h, to obtain the extract;

[0042] 2) Add an appropriate amount of purified water to the extract of step 1) to adjust the volume concentration of ethanol to 60%, let it stand overnight, take the supernatant and absorb it with D101 macroporous resin, and then elute with 60% ethanol for 4 column volumes to remove impurities , and then 4 column volumes were eluted with 90% ethanol, and the 90% ethanol eluate was collected and concentrated under reduced pressure to recover the solvent to obtain an extract;

[0043] 3) Dissolve the extract in step 2) with ethyl acetate, add petroleum ether and stir, wherein the volume ratio of ethyl acetate to petroleum ether is 1:10; take the supernatant to recover the solvent to obtain the extract;

[0044] 4) The medicinal extract in st...

Embodiment 2

[0057] The preparation of embodiment 2 compounds of the present invention

[0058] 1) 5Kg of dried water wenghua, add 7 times the volume concentration of 80% ethanol aqueous solution, extract 3 times, each time for 1.5h, to obtain the extract;

[0059] 2) Add appropriate amount of purified water to the extract of step 1) to adjust the volume concentration of ethanol to 50%, let it stand overnight, take the supernatant and absorb it through HP-20 macroporous resin, and then elute with 70% ethanol for 4 column volumes Remove impurities, then elute 4 column volumes with 95% ethanol, collect the 95% ethanol eluate and concentrate under reduced pressure to recover the solvent to obtain an extract;

[0060] 3) Dissolve the extract in step 2) with ethyl acetate, add petroleum ether and stir, wherein the volume ratio of ethyl acetate to petroleum ether is 1:15; take the supernatant to recover the solvent to obtain the extract;

[0061] 4) The medicinal extract in step 3) is separated...

Embodiment 3

[0063] The preparation of embodiment 3 compounds of the present invention

[0064] 1) 5Kg of dried water wenghua, add 8 times the volume concentration of 90% ethanol aqueous solution, extract once, each time for 1h, to obtain the extract;

[0065] 2) Take the extract of step 1) and let it stand overnight, take the supernatant and absorb it through AB-8 macroporous resin, then use 50% ethanol to elute 4 column volumes to remove impurities, and then use 80% ethanol to elute 4 columns Volume, collect 80% ethanol eluate and concentrate under reduced pressure to recover the solvent to obtain extract;

[0066] 3) Dissolve the extract in step 2) with ethyl acetate, add petroleum ether and stir, wherein the volume ratio of ethyl acetate to petroleum ether is 1:5; take the supernatant to recover the solvent to obtain the extract;

[0067] 4) The medicinal extract in step 3) is separated by preparative HPLC, and the volume concentration is 60% acetonitrile-0.1% formic acid aqueous solu...

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Abstract

The invention provides a compound with an anti-inflammatory effect or a pharmaceutically acceptable salt, a solvate, an isomer, a prodrug molecule or a metabolite thereof, and the chemical formula ofthe compound is 6-hydroxy-4-methoxy-5, 7-dimethyl aurone. The compound provided by the invention has a relatively strong inhibition effect on generation of mouse RAW264.7 macrophage PGE2 induced by lipopolysaccharide (LPS), the activity of the compound is superior to that of ibuprofen, and the compound has certain anti-inflammatory activity; and mouse acetic acid twisting tests show that the compound has a certain analgesic effect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a compound with anti-inflammatory effect and its preparation method and application. Background technique [0002] At present, clinical antipyretic drugs mainly include non-steroidal anti-inflammatory drugs and steroid antipyretic drugs. The former includes salicylic acid, aniline, Ppiridone, and other anti-inflammatory organic acids. The common mechanism of action of these drugs is to reduce the synthesis of prostaglandin (PG) by inhibiting cyclooxygenase, so as to regulate body temperature. The central SP returns to normal and produces antipyretic effect, but these drugs simultaneously inhibit the synthesis of gastric mucosal PG, increase gastric acid secretion, weaken the barrier function, cause adverse reactions in the gastrointestinal tract, and even cause severe gastric mucosal damage. Duodenal bleeding and feed disease. Due to its many components, traditional Chinese me...

Claims

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Application Information

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IPC IPC(8): C07D307/83A61P29/00
CPCA61P29/00C07D307/83
Inventor 肖伟刘文君苏真真杨一帆杨彪曹亮王振中
Owner JIANGSU KANION PHARMA CO LTD
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