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Application of amurensin H derivative EAPP in the treatment and prevention of aplastic anemia

A technology of aplastic and derivatives, applied in the field of biomedicine, to achieve good pharmacodynamic characteristics, prevent and treat aplastic anemia, and simple preparation process

Active Publication Date: 2022-05-20
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

And the application of this compound in the treatment and / or prevention of aplastic anemia has not yet been reported.

Method used

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  • Application of amurensin H derivative EAPP in the treatment and prevention of aplastic anemia
  • Application of amurensin H derivative EAPP in the treatment and prevention of aplastic anemia
  • Application of amurensin H derivative EAPP in the treatment and prevention of aplastic anemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1: Preparation of compound (I) [3-(3,5-dimethoxyphenyl)-6-methoxy-4-benzofurancarboxylic acid-4-acetylphenyl ester].

[0051] The synthetic steps of compound EAPP (I) are as follows:

[0052] Step 1: Synthesis of α-phenoxyketocarboxylic acid through etherification reaction between methyl 3-methoxy-5-hydroxybenzoate and 1-(3,5-dimethoxyphenyl)-2-bromoacetophenone methyl ester.

[0053] Methyl 3-methoxy-5-hydroxybenzoate (4.5g, 26.8mmol) was dissolved in 1-(3,5-dimethoxyphenyl)-2-bromoacetophenone (6.94g, 26.8mmol) In 150ml of dry acetone, slowly add K under vigorous stirring 2 CO 3 The solid was 7.39g (53.5mmol), and the reaction solution was stirred at room temperature for 3h, and then heated to reflux for 3h. TLC monitoring showed that the reaction of raw materials was complete. The reaction solution was cooled to room temperature, filtered with diatomaceous earth, washed with acetone, and the organic phase was concentrated under reduced pressure. The obta...

experiment example 1

[0065] Experimental example 1: The effect of EAPP on aplastic anemia mouse model

[0066] experimental method:

[0067] Get male BALB / c mouse of 18-20g, divide into normal control group, model control group, positive control group (cyclosporine 10mg / kg, intragastric administration) at random, EAPP group (5mg / kg, 10mg / kg, 20mg / kg, intragastric administration). In addition to the blank control group, the animals in each group were inoculated intravenously with cobalt-60γ rays (5.80Gy cobalt-60γ rays for one whole body irradiation) + DBA / 2 mouse thymus:spleen immune cells (2:1) to prepare aplastic anemia models ; From the day of modeling, intragastric administration, once a day, for 14 consecutive days. One hour after the last administration, blood was collected from the orbital vein of the mice, and EDTA-K 2 Anticoagulation, five-differential blood cell analyzer to detect blood routine and flow cytometry to detect reticulocyte count; remove the thymus and spleen of the mouse,...

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Abstract

The invention discloses the application of EAPP, an amurensin H derivative represented by formula (I), in the preparation of products for treating and / or preventing aplastic anemia. The preparation method of the Amurensin H derivative EAPP described in the present invention is simple, has obvious anti-inflammatory activity, and has a significant therapeutic effect on aplastic anemia, and can be used in the clinical practice of aplastic anemia in the form of a monomer or a pharmaceutical composition In the treatment, it has potential application value in the treatment of aplastic anemia and immune-related diseases.

Description

technical field [0001] The present invention relates to the field of biomedicine, in particular to an Amurensin H derivative EAPP or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the derivative or a pharmaceutically acceptable salt thereof. Application in aplastic anemia. Background technique [0002] Aplastic anemia (referred to as aplastic anemia, AA) is a relatively serious blood system disease caused by chemical, physical, biological factors or other unknown reasons, characterized by pancytopenia caused by bone marrow hematopoietic failure, The main clinical manifestations are anemia, bleeding and infection, which can be life-threatening. Its etiology and pathogenesis are very complex, and it is currently believed to be related to hematopoietic stem / progenitor cell defects, abnormal bone marrow hematopoietic microenvironment, and bone marrow hematopoietic suppression mediated by immune disorders. Among them, the key role of imm...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/343A61P7/06
CPCA61K31/343A61P7/06Y02A50/30
Inventor 林明宝姚春所侯琦张梓倩李姝仪朱其彬滕彬豪
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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