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Depsidone acid cyclic ether compound as well as preparation method and application thereof

A technology of depsipphenolic acid cyclic ether and composition, which is applied in the field of microbial engineering and can solve the problems of limited effect and high toxicity

Inactive Publication Date: 2020-07-07
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Current chemically synthesized anti-inflammatory disease drugs have high toxicity and limited efficacy

Method used

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  • Depsidone acid cyclic ether compound as well as preparation method and application thereof
  • Depsidone acid cyclic ether compound as well as preparation method and application thereof
  • Depsidone acid cyclic ether compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0069] In a specific embodiment, the preparation method comprises the steps of:

[0070] 1) Transfer the strain activated on the PDA solid plate medium to a new PDA solid plate medium, and after culturing at 28°C for 6 days, dig out a 5mm×5mm bacterial block with an inoculation shovel and inoculate it in a 200mL PDB In a 500mL shake flask with baffles for the culture medium, the culture temperature is 28°C, the shaker speed is 180rpm, and it is used as the seed solution after 96 hours of culture;

[0071] 2) Inoculate the seed solution to a concentration containing 5mM Ca 2+ In the rice culture medium, ferment for 14 days under the condition of 28-30 ℃;

[0072] 3) extract the fermentation product obtained in step 2 with ethyl acetate for 3 times, and concentrate under reduced pressure to obtain oily crude extract A;

[0073] 4) The crude extract A is mixed with equal mass of silica gel and subjected to silica gel column chromatography. Carry out elution with petroleum ethe...

Embodiment 1

[0090] The solid fermentation of embodiment 1 marine source Curvularia IFB-Z10 (Curvularia sp.)

[0091] After thawing the frozen-preserved Curvularia sp.IFB-Z10 strain, spot the sample on the center of the PDA medium on the solid plate, activate and cultivate it at 28°C for 1 week, and transfer once every two weeks; The strain activated on the PDA solid plate medium was transferred to a new PDA solid plate medium. After culturing at 28°C for 6 days, a piece of 5mm×5mm bacterial block was excavated with an inoculation shovel and inoculated into a medium containing 200mL PDB medium. In a 500mL shaker flask with baffles, the culture temperature was 28°C, the shaker speed was 180rpm, and cultured for 96h; the seed liquid was transferred to the rice solid fermentation medium with an inoculation amount of 5mL, and calcium chloride solution was added to make the calcium ions The concentration is 5mM, and the fermentation culture is carried out in the culture medium. Each culture med...

Embodiment 2

[0092] Extraction and separation of embodiment 2 depsipphenolic acid cyclic ether compounds

[0093] The fermented liquid obtained in Example 1 was filtered through gauze, the filtrate was extracted with ethyl acetate, concentrated and dried under reduced pressure to obtain an oily crude extract A; the crude extract A was subjected to equal mass silica gel mixing, and silica gel column chromatography. Use 5 times of column volumes of petroleum ether, dichloromethane, ethyl acetate and methanol to elute sequentially, and concentrate the ethyl acetate fraction under reduced pressure to obtain extract A1; perform macroporous resin column chromatography on extract A1, and use 6 times of 30%, 50%, 75% and 95% of the column volume ethanol-water gradient elution, the 50% ethanol-water part is concentrated under reduced pressure to obtain extract A2; extract A2 with high pressure liquid chromatography (Chromatographic column: SHIMADZU Shim-pack GIS-C18 column (4.6mm×250mm, 5μm); mobil...

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Abstract

The invention provides a depsidone acid cyclic ether compound as well as a preparation method and application thereof, and particularly provides depsidone acid cyclic ether with a structure shown in aformula I or pharmaceutically acceptable salt thereof, and the depsidone acid cyclic ether or the pharmaceutically acceptable salt thereof has very good anti-inflammatory activity and can be used fortreating inflammatory diseases.

Description

technical field [0001] The invention belongs to the technical field of microbial engineering, and in particular relates to a depsipphenolic acid cyclic ether compound and its preparation method and application. Background technique [0002] The ocean is a treasure house of human resources, because of its complex environment, it contains extremely rich biomedical resources. The deep sea is rich in extremophiles. Due to its unique habitat, marine symbiotic microorganisms create unique metabolic pathways and produce biological macromolecules and small molecules that are different in structure and function from terrestrial compounds, with novel structures and / or diverse activities. , has important application prospects in the fields of agriculture and medicine. Exploring the blue ocean and discovering new marine lead compounds have become international research hotspots. [0003] The current chemically synthesized anti-inflammatory disease drugs have the problems of high toxici...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D321/10A61K31/365A61K31/203A61K31/198A61P29/00A61P17/10C12P17/08C12R1/645
CPCC07D321/10A61K31/365A61K31/203A61K31/198A61P29/00A61P17/10C12P17/08A61K2300/00
Inventor 卢艳花安法梁丁奕郑高帆朱筱婧
Owner EAST CHINA UNIV OF SCI & TECH