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Novel medicine application of elvitegravir for enhancing anti-inflammatory action of glucocorticoid

A technology of glucocorticoid, anti-inflammatory effect, applied in the field of chemical medicine

Inactive Publication Date: 2017-06-13
BINZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The pharmacological effects of anti-HIV integrase inhibitor evitagravir combined with glucocorticoids to prevent or treat tolerance caused by long-term use of glucocorticoids have not been reported

Method used

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Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0013] Experimental example 1 Effects of anti-HIV integrase inhibitor evitagravir on GRα and phosphorylated NF-κB in pulmonary microvascular endothelial cells stimulated by LPS

[0014] 1.1 Drugs and reagents

[0015] The DMEM medium is the product of Gibco Company, and the newborn bovine serum is the product of Hangzhou Sijiqing Company

[0016] LPS (product of Sigma, purchased from Dalian Meilun Biotechnology Co., Ltd.)

[0017] Evitagravir (purity 99.5%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0018] GRα antibody (Glucocorticoid Receptor (D8H2) Rabbit mAb, cellsignal company, catalog number: 3660s) Human pulmonary microvascular endothelial cells (Cell Bank of Chinese Academy of Sciences)

[0019] Methylprednisolone (methylprednisolone sodium succinate for injection, produced by Pfizer, 500mg / bottle)

[0020] 1.2 Experimental methods and results

[0021] When the pulmonary microvascular endothelial cells grew and merged to 70%-80%, fresh culture med...

experiment example 2

[0025] Experimental example 2 Effect of anti-HIV integrase inhibitor evitavir on LPS-induced acute respiratory distress syndrome (ALI / ARDS) model rats

[0026] 2.1 Drugs and reagents

[0027] LPS (product of Sigma, purchased from Dalian Meilun Biotechnology Co., Ltd.)

[0028] Evitagravir (purity 99.5%, purchased from Shanghai Hanxiang Biotechnology Co., Ltd.)

[0029] Methylprednisolone (methylprednisolone sodium succinate for injection, produced by Pfizer, 500mg / bottle)

[0030] GRα antibody (Glucocorticoid Receptor (D8H2) Rabbit mAb, cellsignal company, product number: 3660s) Experimental animals: SPF grade Sprague Dawley rats, male, weighing 150g-200g, provided by the Experimental Animal Center of Shandong Luye Pharmaceutical Co., Ltd., the animal qualification certificate number is: SYXK (Lu) 20030020.

[0031] 2.2 Experimental methods and results

[0032] 2.2.1 Preparation, grouping and administration of endotoxin double-hit ARDS rat model

[0033]70 male rats, wei...

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PUM

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Abstract

The invention provides novel medicine application of elvitegravir, and particularly relates to application for preparing medicine adopting combination of elvitegravir and glucocorticoid for enhancing the anti-inflammatory action of glucocorticoid. According to the application, the dosage range is 50 mg-1,600 mg.

Description

technical field [0001] The invention belongs to the field of chemical medicine, and in particular relates to the combined use of anti-HIV integrase inhibitor Evitagravir and glucocorticoids to enhance the anti-inflammatory effect of glucocorticoids and to treat the resistance caused by long-term use of glucocorticoids in the treatment of acute respiratory distress syndrome. by. Background technique [0002] Glucocorticoid (GC) is a class of steroid hormones secreted by the adrenal cortex. Glucocorticoids have rapid, potent and nonspecific anti-inflammatory effects. Effective for all kinds of inflammation. In the early stage of inflammation, GC inhibits telangiectasia, relieves exudation and edema, and inhibits infiltration and phagocytosis of white blood cells, thereby reducing inflammatory symptoms. In the late stage of inflammation, it inhibits the proliferation of capillaries and fibroblasts, and delays the formation of granulation tissue. And reduce the sequelae of i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/573A61K31/47A61P29/00A61P11/00
CPCA61K31/573A61K31/47
Inventor 蒋王林张广华纪云霞叶亮朱海波李德芳
Owner BINZHOU MEDICAL COLLEGE