A chalcone derivative, 1m‐6, exhibits atheroprotective effects by increasing cholesterol efflux and reducing inflammation‐induced endothelial dysfunction

Abstract

Background and Purpose: Atherosclerosis, resulting from lipid dysregulation and vascular inflammation, causes atherosclerotic cardiovascular disease (ASCVD), which contributes to morbidity and mortality worldwide. Chalcone and its derivatives possess beneficial properties, including anti-inflammatory, antioxidant and antitumour activity with unknown cardioprotective effects. We aimed to develop an effective chalcone derivative with antiatherogenic potential. Experimental Approach: Human THP-1 cells and HUVECs were used as in vitro models. Western blots and real-time PCRs were performed to quantify protein, mRNA and miRNA expressions. The cholesterol efflux capacity was assayed by 3 H labelling of cholesterol. LDL receptor knockout (Ldlr −/−) mice fed a high-fat diet were used as an in vivo atherogenesis model. Haematoxylin and eosin and oil red O staining were used to analyse plaque formation.

The modulatory role of sulfated and non-sulfated small molecule heparan sulfate-glycomimetics in endothelial dysfunction: absolute structural clarification, molecular docking and simulated dynamics, SAR analyses and ADMET studies

“…1, including the polysaccharide-based glycomimetic Equitend, 6 an analogue of prostacyclin Iloprost 7 and chalcone derivative 1m-6. 8 Our approach uses glycomimetics-small molecules that are designed to mimic the function of polysaccharide based biomolecules-and serve as an attractive therapeutic technology in a wide range of diseases. 9,10 Recent advances of the glycomimetic approach have included the development of selective carbonic anhydrase inhibitors; 11 and the use of highly sulfated glycomimetics as inhibitors of viral binding.…”

Risk factors, co‐morbidities, and co‐medications in cardioprotection: Importance for translation

“…They give recommendations to evaluate common molecular targets of inflammatory and cardiovascular disease to design therapies to alleviate inflammatory disease‐related cardiovascular diseases. In line with this, Chen et al (2020) showed that a novel chalcone derivative exhibits atheroprotective effects by reducing inflammation‐induced endothelial dysfunction.…”

Knockdown of lnc-KCNC3-3:1 Alleviates the Development of Atherosclerosis via Downregulation of JAK1/STAT3 Signaling Pathway

“…Atherosclerosis is a major cause of CAD, and CAD is one of the main causes leading to death in most countries (18).…”

“…It has been reported that the JAK/STAT signaling pathway play a important role in cell growth, activation, differentiation, apoptosis, inflammation, and pathogen resistance (18). In addition, it is well known that endothelial cell injury is the early event during the occurrence of atherosclerosis (1).…”