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Agarwood containing ternary oxycyclophenethyl chromone derivatives and application of pharmaceutical compositions thereof

A technology of phenylethyl chromone and derivatives, which is applied in the field of medicine and can solve problems such as metabolic dysfunction, ulcers, and limited applications

Active Publication Date: 2020-12-25
BEIJING UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although glucocorticoids and NSAIDs have good anti-inflammatory effects, adverse drug reactions severely limit their application
Long-term use of glucocorticoids can lead to metabolic dysfunction, and long-term use of NSAIDs can lead to gastric ulcers

Method used

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  • Agarwood containing ternary oxycyclophenethyl chromone derivatives and application of pharmaceutical compositions thereof
  • Agarwood containing ternary oxycyclophenethyl chromone derivatives and application of pharmaceutical compositions thereof
  • Agarwood containing ternary oxycyclophenethyl chromone derivatives and application of pharmaceutical compositions thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Compound G21 inhibits the secretion of nitric oxide (NO) in mouse macrophages and microglia in vitro

[0030] (1) Experimental materials

[0031] Cell line: RAW264.7 cells were purchased from the Cell Center of the Institute of Basic Medicine, Chinese Academy of Medical Sciences; BV-2 cells were gifted by researcher Chen Naihong, Chinese Academy of Medical Sciences.

[0032] Reagents: Compound G21 was extracted and isolated from Agarwood by the Modern Research Center of Traditional Chinese Medicine, Beijing University of Traditional Chinese Medicine; DMEM high glucose medium, DMEM / F12 medium and fetal bovine serum were purchased from Corning Company; bacterial lipopolysaccharide (LPS) was purchased from Sigma, Germany -Aldrich Company (Item No.: L2880); Nitric Oxide Determination Kit (Griess Reagent) was purchased from Prily Gene Technology Co., Ltd. (Item No.: E1030); Thiazolan was purchased from American Amresco Company (Item No.: 0793); Methyl sulfoxide w...

Embodiment 2

[0040] Example 2: Compound G21 inhibits the secretion of inflammatory factors in mouse macrophages in vitro

[0041] (1) Experimental materials

[0042] Cell line: RAW264.7 cells were purchased from the Cell Center of the Institute of Basic Medicine, Chinese Academy of Medical Sciences.

[0043] Reagents: Compound G21 was extracted and isolated from Agarwood by the Modern Research Center of Traditional Chinese Medicine, Beijing University of Traditional Chinese Medicine; DMEM high glucose medium, DMEM / F12 medium and fetal bovine serum were purchased from Corning Company; bacterial lipopolysaccharide was purchased from Sigma-Aldrich Company in Germany (Cat. No. L2880); ELISA kits for the determination of TNF-α, IL-6 and IL-1β were purchased from Wuhan Boster Biotechnology Co., Ltd. (Cat. Nos.: EK0527, EK0411 and EK0394).

[0044] Instrument: Enspire Multimode Plate Reader was purchased from Platinum Elmer, Germany.

[0045] (2) Experimental method

[0046] RAW264.7 cells in ...

Embodiment 3

[0052] Example 3: In vitro inhibition of mouse macrophage chemokine secretion by compound G21

[0053] (1) Experimental materials

[0054] Cell line: RAW264.7 cells were purchased from the Cell Center of the Institute of Basic Medicine, Chinese Academy of Medical Sciences.

[0055] Reagents: Compound G21 was extracted and isolated from Agarwood by the Modern Research Center of Traditional Chinese Medicine, Beijing University of Traditional Chinese Medicine; DMEM high glucose medium, DMEM / F12 medium and fetal bovine serum were purchased from Corning Company; bacterial lipopolysaccharide was purchased from Sigma-Aldrich Company in Germany (Item No.: L2880); ELISA kits for the determination of MCP-1 and MIP-1α were purchased from Wuhan Boster Biotechnology Co., Ltd. (Item No.: EK0568 and EK0449).

[0056] Instrument: Enspire Multimode Plate Reader was purchased from Platinum Elmer, Germany.

[0057] (2) Experimental method

[0058] RAW264.7 cells in logarithmic growth phase we...

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Abstract

The invention discloses a phenethyl chromone derivative extracted from agilawood and containing ternary oxygen rings and an application of pharmaceutical composition of the phenethyl chromone derivative in preventing or treating inflammation-associated diseases, autoimmune diseases, allergic diseases and organ transplantation rejection, particularly in preventing or treating systemic inflammatoryresponse, pneumonia, bronchitis, hepatitis, enteritis, rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, ulcerative colitis, allergic shock, allergic asthma, renal transplantation rejection, liver transplantation rejection and hematopoietic stem cell transplantation rejection.

Description

technical field [0001] The invention relates to the application of a ternary oxygen-containing phenethylchromone derivative in preparing a medicine for preventing or treating inflammation-related diseases, autoimmune diseases, allergic diseases or organ transplant rejection, and belongs to the technical field of medicine. Background technique [0002] The human immune system, including innate immunity and adaptive immunity, plays an important role in defending against damage caused by various internal and external factors. But overactive immune function can also lead to severe tissue damage. Diseases related to excessive activation of immune function mainly include inflammation-related diseases, autoimmune diseases, allergic diseases and organ transplant rejection. Excessive activation of innate immunity mainly leads to inflammation-related diseases or aggravates the body damage of inflammation-related diseases. Excessive activation of adaptive immunity leads to autoimmune...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P29/00A61P37/06A61P37/08
CPCA61K31/352
Inventor 屠鹏飞李军朱枝祥赵云芳郭冉顾宇凡李珊珊霍会霞宋月林高小力
Owner BEIJING UNIV OF CHINESE MEDICINE
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