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Coumaronochromones compound and preparation and application thereof

A technology of chromone compounds and coumarones, which is applied in the direction of active ingredients of heterocyclic compounds, organic chemistry, and drug combination, and can solve the problems of less research on chemical ingredients and no reported application of Dahongpao

Active Publication Date: 2010-02-17
BASILEA PHARM CHINA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Dahongpao contains derivatives of isoflavones, but there are relatively few studies on its chemical components, especially the application of chemical components in Dahongpao in the preparation of immunosuppressants or treatment of immune diseases has not been reported.

Method used

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  • Coumaronochromones compound and preparation and application thereof
  • Coumaronochromones compound and preparation and application thereof
  • Coumaronochromones compound and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: Compound 1 preparation

[0029] First, 2 kg of Dahongpao medicinal material was added, and 16 L (2 L was added for the first time) of 80% ethanol was heated and extracted at 80° C. for 3 times, each time for 1 hour. Then the extract was concentrated under reduced pressure (pressure 98Kpa) at a temperature of 50° C., and the concentrate was dispersed in 2 L of water to prepare a suspension. Add chloroform for extraction three times, 2 L each time, to obtain chloroform extract, which is concentrated under reduced pressure at 40° C. (pressure 98 Kpa), to obtain 91.3 g of chloroform extract.

[0030] Take 50 g of the chloroform extract and mix the sample with an equal amount of silica gel, separate by silica gel column chromatography (300-400 mesh), elute with petroleum ether: ethyl acetate (2:1-1:1), check with TLC, combine and wash The liquid was removed, concentrated, and the eluate was applied to a reversed-phase C18 column, methanol: water (50:50-70:30),...

Embodiment 2

[0040] Embodiment 2: immunosuppressive activity test:

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Abstract

The invention discloses a coumaronochromones compound as shown by a formula 1. Pharmacological experiments show that the coumaronochromones compound has significant inhibitory action on the proliferation of B lymphocytes and T lymphocytes, and can be used for preparing immunosuppressive agents or medicaments for treating various immunologic diseases such as rheumatoid arthritis, lupus erythematosus and the like, and the medicaments for treating B cell type chronic lymphocytic leukemia. The invention also provides a preparation method.

Description

Technical field: [0001] The present invention relates to natural medicinal chemistry, in particular to isoflavone derivatives extracted and separated from the stem of Dahongpao [Myrsine Africana L.]—coumaronochromones (Coumaronochromones) compounds and its preparation method and preparation method for immunotherapy Inhibitor or treatment of various immune diseases, such as rheumatoid arthritis, lupus erythematosus and preparation of drugs for treating B-cell chronic lymphocytic leukemia. Background technique: [0002] Coumaronochromones (Coumaronochromones) are isoflavone derivatives. It is known that naturally occurring plant isoflavones exhibit a wide range of biological activities, including anti-oxidation, regulation of signal transduction and enzyme activity; Inhibition of mitosis and cytotoxicity; increase capillary permeability; increase cell adhesion; increase the response of vascular smooth muscle to vascular relaxants; stimulate estrogen receptors, etc. These biol...

Claims

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Application Information

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IPC IPC(8): C07D493/14A61K31/352A61K31/35A61P19/04A61P37/00A61P19/02A61P35/00
Inventor 沈征武寿清耀
Owner BASILEA PHARM CHINA LTD
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