Application of Propacin and derivatives of Propacin to preparation of anti-inflammatory drugs

Abstract

The invention provides application of a compound Propacin and pharmacologically acceptable derivatives of the compound Propacin to preparation of anti-inflammatory drugs. The inventor first finds thatthe Propacin can inhibit release of inflammatory factors NO and PGE2 in macrophages, expression of genes iNOS and COX-2 is inhibited, expression of inflammatory factors TNF-alpha and IL-1beta and a gene IL-6 is inhibited, release of ROS is inhibited, activation of an MAPK pathway is inhibited, nuclear transferring of a nuclear transcription factor p65 is inhibited, and thus the development of inflammation is inhibited. According to the application, for the first time, the Propacin and the pharmacologically acceptable derivatives of the Propacin are applied to the preparation of the anti-inflammatory drugs, the inflammation can be effectively eliminated, and the side effect is small.

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to new applications of existing compounds, in particular to the application of Propacin and its derivatives in the preparation of anti-inflammatory drugs. Background technique [0002] Inflammation refers to a complex physiological and pathological reaction mainly based on defense response caused by physical damage, bacterial infection or other harmful stimuli. It is a defense mechanism of the body, mainly manifested as redness, heat, swelling, pain and even Clinical symptoms such as dysfunction. The generation and development of inflammation involve the participation of various cells and the release of cytokines, among which macrophages play an important role. Lipopolysaccharide (LPS) is a powerful natural immune factor, which can activate macrophages, activate NF-κB, MAPKs, JAK and other signal transduction pathways, thereby inducing the expression of iNOS, COX-2 and other inflammator...

AI Technical Summary

Problems solved by technology

[0003] Existing anti-inflammatory drugs are mainly divided into non-steroidal anti-inflammatory drugs and steroidal anti-inflammatory drugs. Among them, non-steroidal anti-inflammatory drugs mainly treat the symptoms but not the root cause, and the anti-inflammatory effect is not obvious. Although steroidal anti-inflammatory drugs The curative effect is exact but often accompanied by obvious adverse reactions, so it is necessary to find a new anti-inflammatory drug with good curative effect and low side effects

[0004] Propacin, namely (E-1'-guaiacol-2'-methyl-ethylenedioxy)-1',2':7,8-6-methoxycoumarin, is a The coumarin compounds extracted from durian have not yet reported the pharmacological effects and applications of this compound

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