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Iridoid glycoside compound as well as preparation method and application thereof

A technology of iridoid glycosides and compounds, which is applied in the field of medicine and can solve problems such as toxic and side effects

Active Publication Date: 2020-10-02
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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  • Iridoid glycoside compound as well as preparation method and application thereof
  • Iridoid glycoside compound as well as preparation method and application thereof
  • Iridoid glycoside compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The preparation of embodiment 1 compound of the present invention

[0035] (1) Take the dried medicinal material of Gardenia jasmine, extract twice with 60% ethanol under reflux for 2 hours each time, combine the extracts, and remove the solvent under reduced pressure to obtain the total extract. The total extract is dissolved in water, separated by HP-20 macroporous adsorption resin column chromatography, and eluted with water, 25% ethanol, 45% ethanol, 65% ethanol, 90% ethanol in sequence, each gradient elution has 4 column volumes (The same below), each eluate was collected separately, concentrated under reduced pressure until no alcohol smell, and obtained water elution site, 25% ethanol elution site, 45% ethanol elution site, 65% ethanol elution site, 90% ethanol elution site Elution site;

[0036] (2) Take the 25% ethanol elution part of step (1), separate through silica gel column chromatography, and use ethyl acetate-methanol-water gradient elution (100:0:0; 95...

Embodiment 2

[0038] The preparation of embodiment 2 compounds of the present invention

[0039] (1) Take the dried medicinal material of Gardenia jasmine, extract twice with 70% ethanol under reflux, each time for 2 hours, combine the extracts, remove the solvent under reduced pressure, and obtain the total extract. The total extract was dissolved in water, separated by HP-20 macroporous adsorption resin column chromatography, eluted with water, 30% ethanol, 50% ethanol, 70% ethanol, and 95% ethanol in turn, and each eluate was collected respectively, and depressurized Concentrate until there is no alcohol smell, and obtain water elution sites, 30% ethanol elution sites, 50% ethanol elution sites, 70% ethanol elution sites, and 95% ethanol elution sites;

[0040] (2) Take the 30% ethanol elution part of step (1), separate through silica gel column chromatography, and use ethyl acetate-methanol-water gradient elution (95:5:0; 90:10:0; 85:15: 0; 80:20:4; 70:30:6to60:40:8,0:100:0, v / v / v), co...

Embodiment 3

[0042] The preparation of embodiment 3 compounds of the present invention

[0043] (1) Take the dried medicinal material of Gardenia jasmine, extract twice with 50% ethanol under reflux for 2 hours each time, combine the extracts, and remove the solvent under reduced pressure to obtain the total extract. The total extract was dissolved in water, separated by HP-20 macroporous adsorption resin column chromatography, eluted with water, 35% ethanol, 55% ethanol, 75% ethanol, and 100% ethanol successively, and each eluate was collected respectively, and depressurized Concentrate until there is no alcohol smell, and obtain water elution sites, 35% ethanol elution sites, 55% ethanol elution sites, 75% ethanol elution sites, and 100% ethanol elution sites;

[0044] (2) Take the 35% ethanol elution part of step (1), separate through silica gel column chromatography, and use ethyl acetate-methanol-water gradient elution (90:10:0; 80:20:0; 75:25: 0; 70:30:4 to 60:40:8, v / v / v), collecte...

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PUM

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Abstract

The invention discloses an iridoid glycoside compound, which is a novel chemical component discovered from cape jasmines. The compound separated by virtue of the method is further structurally identified by virtue of measures of physicochemical properties and modern spectroscopy. Activity evaluation is further carried out by virtue of activity screening systems such as an LPS-induced RAW 264.7 cell inflammation model so as to discover that the compound has a certain protecting effect on a mouse macrophage system RAW 264.7, is capable of remarkably inhibiting PGE2 and presents a relatively strong anti-inflammatory action.

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] Gardenia jasminoides Ellis, derived from the dried and mature fruit of Gardenia (Gardenia) in the Rubiaceae family (Rubiaceae), belongs to the first batch of medicinal and edible resources promulgated by the Ministry of Health. , sedation, hemostasis, swelling and other effects. In traditional Chinese medicine, it is often used to treat jaundice hepatitis, sprains, high blood pressure, diabetes and other diseases. [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 non-steroidal anti-inflammatory drugs (NSAIDs). However, because many synthetic drugs have strong toxic and side effects, people pay more and more attention to the development of anti-inflammatory drugs ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/04C07H1/08A61K31/7048A61P29/00
CPCC07H17/04C07H1/08A61P29/00
Inventor 肖伟杨一帆李莲莲葛雯邓奕杨彪曹亮
Owner JIANGSU KANION PHARMA CO LTD
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