Anti-obesity-induced inflammation treatment study using adipose tissue homing glycyrrhizin derivative

Abstract

Obesity-induced inflammation is a major cause of complications of obesity and is mainly induced by obese white adipose tissue (WAT) caused by hypertrophy of adipocyte due to overnutrition. Treatment of such obesity-induced inflammation is difficult because it requires both targeted delivery to obese WAT and anti-inflammatory treatment at the same time. In this paper, glycyrrhizin (GL), which shows an anti-hypertrophic effect on adipocyte, and adipose tissue homing peptide (AHP), which has a target on adipocytes are conjugated through an amine poly-ethylene-glycol thiol (PEG) linkage to treat obesity-induced inflammation occurred from obese WAT through anti-hypertrophic effect on adipocyte. Glycyrrhizin- amine poly-ethylene-glycol thiol-homing peptide (GL-PEG-AHP) conjugates appear anti-hypertrophic effects on adipocytes and anti-inflammatory effects in obesity WAT mimicking environment. Mechanistically, these effects are presumed to occur through the expression of the ATP Binding Cassette subfamily A 1 transporter (ABCA1) in the adipocyte plasma membrane. Finally, GL-PEG-AHP is expected to be a next-generation anti-obesity and obesity-induced inflammatory drug that can expect not only anti-inflammatory effects on obese adipose tissue but also anti-obesity effects in animal models.