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Application of chlorinated tetrahydrophenethylchromone derivatives in agarwood and their pharmaceutical compositions

A composition and drug technology, applied in the field of medicine, can solve problems such as metabolic dysfunction and high nephrotoxicity

Active Publication Date: 2019-06-07
BEIJING UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Long-term use of glucocorticoids can lead to metabolic dysfunction, while adaptive immunosuppressants such as cyclosporine and tacrolimus have high nephrotoxicity

Method used

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  • Application of chlorinated tetrahydrophenethylchromone derivatives in agarwood and their pharmaceutical compositions
  • Application of chlorinated tetrahydrophenethylchromone derivatives in agarwood and their pharmaceutical compositions
  • Application of chlorinated tetrahydrophenethylchromone derivatives in agarwood and their pharmaceutical compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: the preparation of compound G2

[0032] (1) Experimental materials

[0033] Medicinal material: agarwood. It was identified by Professor Tu Pengfei of the Modern Research Center of Traditional Chinese Medicine, Beijing University of Traditional Chinese Medicine as the resinous wood of Aquilaria sinensis (Lour.) Gilg. The specimen (CX2012029) is deposited in the Specimen Bank of the Modern Research Center of Traditional Chinese Medicine, Beijing University of Traditional Chinese Medicine.

[0034] Reagents: ethanol, petroleum ether, ethyl acetate, chloroform, methanol, dichloromethane, acetonitrile and other chemical reagents were of analytical grade and purchased from Beijing Chemical Plant.

[0035] Instruments and materials: American Rudolph Autopol IV automatic polarimeter; Japanese Shimadzu UV-2450 spectrophotometer; American Thermo Nicolet Nexus 470 FT-IR Fourier transform infrared spectrometer; American Varian Inova-500 nuclear magnetic resonance i...

Embodiment 2

[0042] Example 2: Determination of Compounds G1-G4 Inhibiting the Secretion of Nitric Oxide (NO) from Mouse Macrophages and Neuroglial Cells in Vitro

[0043] (1) Experimental materials

[0044] Cell lines: RAW264.7 cells were purchased from the Cell Center of the Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences; BV-2 cells were donated by Chen Naihong, a researcher at the Chinese Academy of Medical Sciences.

[0045] Reagents: Compounds G1-G4 were extracted and separated from Agarwood by the Modern Research Center of Chinese Medicine, Beijing University of Traditional Chinese Medicine; DMEM high-glucose medium and DMEM / F12 medium were purchased from Corning Company; bacterial lipopolysaccharide was purchased from Beijing Baierdi Biotechnology Co., Ltd. Responsible company (Product No.: L2880); Nitric Oxide Assay Kit (Griess Reagent) was purchased from Pulilai Gene Technology Co., Ltd. (Product No.: E1030); Thiazole Blue was purchased from Amresco Compa...

Embodiment 3

[0053] Example 3: Determination of Compound G4 Inhibiting the Secretion of Inflammatory Factors in Mouse Macrophages in Vitro

[0054] (1) Experimental materials

[0055] Cell line: RAW264.7 cells were purchased from the Cell Center of the Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences.

[0056] Reagents: Compound G4 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 and DMEM / F12 medium were purchased from Corning; bacterial lipopolysaccharide was purchased from Beijing Baierdi Biotechnology Co., Ltd. (Cat. No.: L2880); ELISA kits for the determination of TNF-α and IL-6 were purchased from Wuhan Boster Biotechnology Co., Ltd. (Cat. No.: EK0527 and EK0411).

[0057] Instrument: Enspire Multimode Plate Reader was purchased from Platinum Elmer Company in Germany.

[0058] (2) Experimental method

[0059] RAW264.7 cells in t...

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Abstract

The invention discloses application of chloro-substituted tetrahydrophenethyl chromone derivatives and a pharmaceutical composition thereof which are extracted and separated from agilawood in prevention or treatment of inflammation-related diseases, autoimmune diseases and organ transplantation rejection, especially prevention or treatment of systemic inflammatory response, pneumonia, bronchitis, hepatitis, enteritis, rheumatoid arthritis, systemic lupus erythematosus, kidney transplantation rejection, liver transplantation rejection and hematopoietic stem cell transplantation rejection.

Description

technical field [0001] The invention relates to the application of three chlorinated tetrahydrophenylethylchromone derivatives in the preparation of medicines for preventing or treating inflammation-related diseases, autoimmune diseases and 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 the body against various internal and external factors. But overactivation of the immune system can also lead to severe tissue damage. Diseases associated with overactivation of immune function mainly include inflammation-related diseases, autoimmune 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 diseases and organ transp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P29/00A61P37/02A61P37/06A61P11/00A61P1/16A61P1/00A61P13/12A61P25/00A61P17/00A61P19/02A61P7/00A61P7/06C07D311/74
Inventor 屠鹏飞李军朱枝祥顾宇凡赵云芳宋月林霍会霞
Owner BEIJING UNIV OF CHINESE MEDICINE
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