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A kind of iridoid glycoside compound and its preparation method and application

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

Active Publication Date: 2022-03-18
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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  • A kind of iridoid glycoside compound and its preparation method and application
  • A kind of iridoid glycoside compound and its preparation method and application
  • A kind of iridoid glycoside compound and its preparation method and application

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), col...

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; 70:30:4to60:40:8, v / v / v), and 8 frac...

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Abstract

The invention discloses an iridoid glycoside compound, which is a new chemical component found in gardenia. In the present invention, the structure identification of the compound separated by the above method is also carried out through physical and chemical properties and modern spectroscopy means. The present invention also uses LPS-induced RAW 264.7 cell inflammation model and other activity screening systems for activity evaluation, and finds that the compound has a certain protective effect on the mouse macrophage cell line RAW 264.7, and can significantly inhibit PGE 2 , showing a strong 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] 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 Patents(China)
IPC IPC(8): C07H17/04C07H1/08A61P29/00A61K31/7048
CPCC07H17/04C07H1/08A61P29/00
Inventor 肖伟李海波邓奕葛雯胡晗绯杨彪曹亮王振中
Owner JIANGSU KANION PHARMA CO LTD
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