Iminostilbene, a novel small-molecule modulator of PKM2, suppresses macrophage inflammation in myocardial ischemia-reperfusion injury.

ABSTRACT:

Introduction

Inflammation is a key factor in myocardial ischemia/reperfusion (MI/R) injury. Targeting leucocyte-mediated inflammation is an important strategy for MI/R therapy. Iminostilbene (ISB), a simple dibenzoazepine small molecule compound, has a strong anti-neurodegenerative effect. However, no study has shown the cardioprotective effect of ISB.

Objectives

This study aimed to investigate the role of ISB against MI/R injury and identify its molecular target.

Methods

To verify the cardiac protection of ISB in vivo and in vitro, we performed rat MI/R surgery and subjected inflammatory modeling of macrophages. In terms of molecular mechanisms, we designed and synthesized a small molecular probe of ISB and employed it on the click chemistry-activity-ba

SUBMITTER: Lu S 

PROVIDER: S-EPMC8020153 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature