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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

Inactive Publication Date: 2020-06-19
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

[0038] The preparation of embodiment 1 compound of the present invention

[0039] (1) Take the dried medicinal material of Flos Japonica, extract twice with 70% 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, 25% ethanol, 45% ethanol, and 90% ethanol in sequence, and each eluate was collected separately, concentrated under reduced pressure to no alcohol Taste, get water elution site, 25% ethanol elution site, 45% ethanol elution site, 90% ethanol elution site;

[0040](2) Take the 45% ethanol elution part of step (1), separate it by silica gel column chromatography, and use chloroform-methanol-water gradient elution (100:0:0; 95:5:0; 90:10:0; 85:15:4; 75:25:6to 60:40:8, v / v / v), and 16 fractions (A-P) were collected, and fraction F was subjected to SiO2 co...

Embodiment 2

[0042] The preparation of embodiment 2 compounds of the present invention

[0043] (1) Take the dried medicinal material of Flos Japonica, extract twice with 70% 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, eluted with water, 30% ethanol, 50% ethanol, and 95% ethanol in turn, and the eluents are collected respectively, concentrated under reduced pressure to no alcohol Taste, get water elution site, 30% ethanol elution site, 50% ethanol elution site, 95% ethanol elution site;

[0044] (2) Take the 50% ethanol elution part of step (1), separate through silica gel column chromatography, and use chloroform-methanol-water gradient elution (95:5:0; 90:10:0; 85:15:0; 80:20:4; 70:30:6to 60:40:8, v / v / v), and 16 fractions (A-P) were collected, and Fraction F was subjected to SiO2 c...

Embodiment 3

[0046] The preparation of embodiment 3 compounds of the present invention

[0047] (1) Take the dried medicinal material of Flos Japonica, extract twice with 70% 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, eluted with water, 35% ethanol, 55% ethanol, and 100% ethanol in turn, and the eluents are collected respectively, concentrated under reduced pressure to no alcohol Taste, get water elution site, 35% ethanol elution site, 55% ethanol elution site, 100% ethanol elution site;

[0048] (2) Take the 50% ethanol eluted part of step (1), separate it by silica gel column chromatography, and use chloroform-methanol-water gradient elution (90:10:0; 80:20:0; 75:25:0; 70:30:4to 60:40:8, v / v / v), collected 16 fractions (A-P), and fraction F was subjected to SiO2 column chromatograp...

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Abstract

The invention discloses an iridoid glycoside compound. The iridoid glycoside compound is a new chemical component discovered in lonicerae flos. A compound separated by virtue of a method is further structurally identified by virtue of physicochemical properties and modern spectroscopic measures. Activity evaluation is carried out by virtue of activity screening systems such as an LPS-induced RAW 264.7 cell inflammation model, and a result shows that the compound has a certain protecting effect on a mouse macrophage system RAW 264.7, is capable of remarkably inhibiting IL-6 and presents a relatively 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] The traditional Chinese medicine Lonicerae Flos is Lonicera macranthoides Hand.-Mazz., Lonicera hypoglauca Miq., Lonicera confusa D C., Lonicera fulvotomentosa, Lonicera fulvotomentosa, Caprifoliaceae Lonicera The dried buds or flowers with first blooms of Hsu etS.C.Cheng are important medicinal resources. Have heat-clearing and toxic substances removing, evacuate wind-heat effect, be clinically used for carbuncle furuncle, sore throat, erysipelas, pyretic toxin bloody dysentery, wind-heat cold, febrile disease heating. [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 stro...

Claims

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Application Information

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IPC IPC(8): C07H17/04C07H1/08A61K31/7048A61P29/00
CPCC07H17/04C07H1/08A61P29/00
Inventor 肖伟李海波姚新生于洋梅玉丹王振中邓奕杨彪
Owner JIANGSU KANION PHARMA CO LTD
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