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Sponge-derived meroterpenoid compound Dysiarenone as well as preparation method and application thereof

A compound and source technology, applied in the field of medicine, can solve the problems of no heteroterpene compounds, etc., and achieve the effect of significant release inhibitory activity, simple preparation method, and strong inhibitory activity

Active Publication Date: 2019-05-17
RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, so far there has been no inhibitory PEG that inhibits the expression of COX-2 enzymes 2 Reports of heteroterpenoids produced

Method used

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  • Sponge-derived meroterpenoid compound Dysiarenone as well as preparation method and application thereof
  • Sponge-derived meroterpenoid compound Dysiarenone as well as preparation method and application thereof
  • Sponge-derived meroterpenoid compound Dysiarenone as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The preparation of embodiment 1 compound dysiarenone

[0036] Get pre-frozen and chopped sponge (wet weight 520g), extract 8 times with 95% ethanol (1L) cold soaking respectively, each time for a week, combine the extracts, and concentrate the extracts under reduced pressure to obtain the total extract. The extract was suspended in water, and extracted 5 times with an equal volume of dichloromethane. The extracts were combined and concentrated under reduced pressure to obtain a dichloromethane extract (2.7 g).

[0037] The above-mentioned dichloromethane extract (2.7g) was separated by silica gel column chromatography under reduced pressure, and was eluted with petroleum ether-ethyl acetate gradient. According to the results of thin-layer chromatography TLC analysis, a fraction containing sesquiterpene quinone compounds was obtained, and then This cut is further enriched with SephadexLH-20 gel column, adopts sherwood oil-methylene chloride-methanol (4:1:5) system, obtai...

Embodiment 2

[0044] Example 2 Inhibition of lipopolysaccharide (LPS)-induced release of PGE from RAW 264.7 mouse macrophages in vitro 2 experiment

[0045] The compounds of the present invention, dysiarenone, avarol and dexamethasone (Dexamethasone, a synthetic anti-inflammatory drug) were used as samples to inhibit the release of PGE from RAW 264.7 mouse macrophages induced by lipopolysaccharide in vitro 2 In the experiment, a parallel experiment of a blank group (control) without adding samples was carried out at the same time. The sample was dissolved in DMSO and stored at low temperature, and the concentration of DMSO in the final system was controlled within the range that did not affect the detection activity. Three replicate wells were set up for each sample concentration in the test.

[0046] Specific experimental steps:

[0047] Raw 264.7 mouse macrophages purchased from Shanghai Institute of Biological Sciences were cultured in RPMI 1640 (including 10% (v / v) FBS, 100 U / mL peni...

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Abstract

The invention relates to the technical field of drugs, and discloses a sponge-derived triterpene compound dysiarenone. The chemical structural formula of the compound is as follows in the description.The invention further discloses a preparation method of dysiarenone. The compound dysiarenone shows strong inhibitory activity on expression of COX-2 enzymes and release of inflammatory mediator PGE2 and can be used for preparing anti-inflammatory and anti-tumor drugs.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a sponge-derived heteroterpene compound dysiarenone and a preparation method and application thereof. Background technique [0002] The sponge is a low-level multicellular animal with a history of more than 500 million years of evolution. It has formed a unique chemical defense mechanism in the harsh competitive environment of the ocean, which can efficiently produce active substances, and discover novel structures from sponges every year. Active substances account for more than one-third of marine natural products. At present, 3 of the 7 marine drugs approved by the FDA in the United States are derived from sponges. Therefore, sponges have become an important source of marine drugs and have always been an important source of marine natural product chemistry. research hotspots. [0003] Stubborn sponge (Dysidea arenaria) is a sponge belonging to Demospongiae, Dictyoceratida, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/96A61P29/00A61P35/00
CPCY02A50/30
Inventor 焦伟华林厚文李静石国华
Owner RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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