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Prenylated flavonoid, and applications thereof in preparing drugs used for treating inflammatory diseases

A technology for isopentenyl flavonoids and inflammatory diseases, which is applied to the application field of isopentenyl flavonoids in the preparation of medicines for treating inflammatory diseases, and can solve damage to vascular endothelial cells and extravascular tissue cells, tissue damage, Problems such as blocking microcirculation

Active Publication Date: 2017-07-04
深圳市贝美药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, while ROS kills invading bacteria, it can also cause damage to surrounding normal tissues, causing obstruction of microcirculation, damage to vascular endothelial cells and extravascular tissue cells, release and promote the release of inflammatory mediators, and become a "destroyer".

Method used

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  • Prenylated flavonoid, and applications thereof in preparing drugs used for treating inflammatory diseases
  • Prenylated flavonoid, and applications thereof in preparing drugs used for treating inflammatory diseases
  • Prenylated flavonoid, and applications thereof in preparing drugs used for treating inflammatory diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Preparation of prenyl flavone artoheteroid C in jackfruit

[0019] The jackfruit root medicinal material (17 Kg) was extracted by leakage with 95% ethanol, and the extract was concentrated under reduced pressure to obtain 1.5 Kg of extract. The extract was suspended in water, extracted successively with petroleum ether, chloroform, ethyl acetate and n-butanol, and concentrated to dryness respectively. Take 532 g of the extract from the chloroform extraction part, perform macroporous resin column chromatography (column size: 15*55cm, 5.3 Kg), and elute with ethanol-water gradient to obtain 10 fractions frs. H1-H10. Fraction H5 (10.0 g) was applied to a Sephadex LH-20 column and eluted with methanol to obtain 10 fractions: frs.H5L1-H5L10. Fraction H5L5 (1.5 g) was applied to a reverse ODS column and eluted with methanol-water (2:8→10:0, v / v) to obtain 4 fractions H5L5O1-H5L5O4. Fraction H5L5O4 (483.0 mg) was further applied to Sephadex LH-20 gel column, eluted...

Embodiment 2

[0020] Example 2 Structural Identification of the Prenyl Flavone Artoheteroid C in Jackfruit

[0021] Artoheteroid C, a yellow amorphous powder with quasi-molecular ion peaks by HR-ESI-MS m / z 381.0979 ([M-H] - , C 21 h 17 o 7 , Calculated value: 381.0980), confirm its molecular formula as C 21 h 18 o 7 . IR ( ν max 3430, 2974, 1651, 1612, 1504, 1467, 1356 cm -1 ) and UV spectra ( lambda max 263, 316, 378 nm) showed that the compound had typical absorption characteristics of prenylflavonoids. Artoheteroid C's 1 H NMR spectrum (600 MHz, dimethyl sulfoxide- d 6 ) shows the following proton signal: a hydrogen-bonded hydroxyl δ H 12.33(1H, s, OH-5); a pair of meta-coupled aromatic protons δ H 6.33 (1H, d, J = 1.8 Hz, H-8) and 6.13(1H, d, J = 1.8 Hz, H-6); a lone aromatic proton δ H 6.38 (H-3'); a methoxy group δ H 3.77(3H, s, MeO-4′); two methyl groups δ H 1.57 (3H, s, H 3 -14) and 1.23 (3H, s, H 3 -15) and an ABX-type spin-coupled system δ ...

Embodiment 3

[0025] Example 3 Cytotoxicity evaluation experiment of artoheteroid C on rat PMNs

[0026] The cytotoxicity of artoheteroid C on PMNs was determined by referring to the relevant literature of the standard trypan blue exclusion method. At 37°C, 1 mL of PMNs cell suspension (1×10 6 ) (2% FCS-HBSS) were incubated with 10 μL DMSO or artoheteroid C (final concentration ranging from 1 to 1000 μM) for 30 min. 112 μL of 0.4% trypan blue staining solution was added to each sample, and under a high-power microscope, the cytotoxic effect of the sample on PMNs was calculated by counting the absorption of trypan blue by 100 cells. The results showed that artoheteroid C at 180 M above began to show toxicity to PMNs.

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Abstract

The invention relates to a prenylated flavonoid, and applications thereof in preparing drugs used for treating inflammatory diseases. The prenylated flavonoid is a novel compound separated from artocarpus heterophyllus of Artocarpus, Moraceae, and is named as artoheteroid C. The structure of artoheteroid C is disclosed in the invention, possesses high inhibition activity on mouse neutrophil respiratory burst, can be used for preparing drugs used for treating inflammatory diseases, and can be used for clinical treatment of oxidative damages, such as rheumatoid arthritis, compensatory anti-inflammatory response syndrome, and systemic inflammatory response syndrome, caused by neutrophil excessive activation; and the IC50 value is 7.5<mu>M.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of a prenyl flavonoid compound in jackfruit in the preparation of medicines for treating inflammatory diseases. Background technique [0002] Neutrophils (PMNs) are the body's first line of defense against the invasion of foreign pathogens. When PMNs recognize the small peptide secreted by the receptor or the complex formed by the bacteria and the antibody in the serum, the cell is activated through the mediation of the receptor on the membrane, and a large amount of superoxide anion (O 2 •- ). o 2 •- Under the catalysis of superoxide dismutase and myeloperoxidase, a series of free radical chain reactions occurred, producing various reactive oxygen species (ROS), including hydroxyl radical (HO ), hydrogen peroxide (H 2 o 2 ) and hypochlorous acid (HOCl). These ROS can efficiently eliminate invading pathogenic microorganisms, a phenomenon called respirato...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/06A61P29/00
CPCC07D493/06
Inventor 任刚李文艳彭加兵肖川云元文君袁金斌曾金祥
Owner 深圳市贝美药业有限公司
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