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Alkaloid compound as well as preparation method and application thereof

A technology of alkaloids and compounds, applied in the field of medicine, can solve problems such as toxic and side effects

Active Publication Date: 2021-02-26
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because many synthetic drugs have strong toxic and side effects, people pay more and more attention to the development of anti-inflammatory drugs from natural drugs

Method used

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  • Alkaloid compound as well as preparation method and application thereof
  • Alkaloid compound as well as preparation method and application thereof
  • Alkaloid compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The preparation of embodiment 1 compound of the present invention

[0037] (1) Take the dry aerial part of Artemisia annua L. (the same below), extract twice with 3 times hydrothermal reflux, each time for 2 hours, combine the extracts, and recover the solvent under reduced pressure to 1 / 10 of the original volume , add 95% ethanol until the alcohol concentration reaches 80%, let it stand overnight, collect the supernatant and concentrate under reduced pressure to obtain the total extract. The total extract is dissolved in water, separated by HP-20 macroporous adsorption resin column chromatography, eluted with water, 45% ethanol, and 90% ethanol in sequence, and the eluents are collected respectively, concentrated under reduced pressure until there is no alcohol smell, and water Elution site, 45% ethanol elution site, 90% ethanol elution site;

[0038] (2) Take the 45% ethanol elution part of step (1), separate it by silica gel column chromatography, and use dichlorome...

Embodiment 2

[0040] The preparation of embodiment 2 compounds of the present invention

[0041] (1) Take the dry aerial part of Artemisia annua, extract twice with 4 times of hydrothermal reflux, each time for 2 hours, combine the extracts, recover the solvent under reduced pressure to 1 / 10 of the original volume, add 95% ethanol until the alcohol concentration reaches 80 %, let stand overnight, collect the supernatant and concentrate under reduced pressure to obtain the total extract. The total extract is dissolved in water, separated by HP-20 macroporous adsorption resin column chromatography, eluted with water, 50% ethanol, and 95% ethanol in sequence, and the eluents are collected respectively, concentrated under reduced pressure until there is no alcohol smell, and water Elution site, 50% ethanol elution site, 95% ethanol elution site;

[0042] (2) Separation by silica gel column chromatography, elution with dichloromethane-methanol gradient (100:0 to 0:100, v / v), 4 column volumes fo...

Embodiment 3

[0044] The preparation of embodiment 3 compounds of the present invention

[0045] (1) Take the dry aerial part of Artemisia annua, extract it with 4 times of hydrothermal reflux for 3 times, each time for 2 hours, combine the extracts, recover the solvent under reduced pressure to 1 / 10 of the original volume, add 95% ethanol until the alcohol concentration reaches 80 %, let stand overnight, collect the supernatant and concentrate under reduced pressure to obtain the total extract. The total extract is dissolved in water, separated by HP-20 macroporous adsorption resin column chromatography, eluted with water, 55% ethanol, and 100% ethanol in sequence, and the eluents are collected respectively, concentrated under reduced pressure until there is no alcohol smell, and water Elution site, 55% ethanol elution site, 100% ethanol elution site;

[0046] (2) Take the 55% ethanol elution part of step (1), separate it by silica gel column chromatography, and use dichloromethane-methan...

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PUM

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Abstract

The invention discloses an alkaloid compound. The separated compound undergoes structural identification through physicochemical properties and modern spectroscopy means. In addition, an activity screening system of an LPS-induced RAW 264.7 cell inflammation model is used for evaluating the activity of the compound, and it is found that the compound has a certain protection effect on a mouse macrophage line RAW 264.7, can remarkably inhibit PGE2 and shows a high anti-inflammatory effect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a novel compound and its preparation method and application. Background technique [0002] Artemisia annua is the dry aboveground part of Artemisia annua L. of Compositae. It is harvested when the flowers are in full bloom in autumn, and the old stems are removed and dried in the shade. Bitter in taste, pungent and cold in nature, it returns to the liver and gallbladder meridian, and has the effects of clearing deficiency heat, removing bone steam, relieving summer heat, intercepting rejection, and reducing jaundice. It is used for warming evils and hurting yin, night heat and morning coolness, yin deficiency fever, bone steaming labor heat, heat evil fever, malaria cold and heat, and damp heat jaundice. [0003] Anti-inflammatory drugs are the second largest class of drugs after anti-infective drugs in clinical treatment, including steroidal anti-inflammatory drugs (SAIDs) and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D221/04A61P29/00A61K31/435
CPCC07D221/04A61P29/00
Inventor 曹亮肖伟李海波杨一帆顾莎莎王团结杨彪胡晗绯王振中
Owner JIANGSU KANION PHARMA CO LTD
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