Glycyrrhetinic acid inhibits non-small cell lung cancer via promotion of Prdx6- and caspase-3-mediated mitochondrial apoptosis.

Glycyrrhetinic acid (GA) shows great efficiency against non-small cell lung cancer (NSCLC), but the detailed mechanism is unclear, which has limited its clinical application. Herein, we investigated the potential targets of GA against NSCLC by activity-based protein profiling (ABPP) technology and the combination of histopathology and proteomics validation. In vitro and in vivo results indicated GA significantly inhibited NSCLC via promotion of peroxiredoxin-6 (Prdx6) and caspase-3 (Casp3)-mediated mitochondrial apoptosis. This original finding will provide theoretical and data support to improve the treatment of NSCLC with the application of GA. [Display omitted] • First-time integrated analysis profiling of non-small cell lung cancer (NSCLC) and Glycyrrhetinic acid (GA) treatment by integrating activity-based protein profiling (ABPP) technology, histopathology and proteomics validation both in vitro and in vivo. • Identification of GA promoted ROS accumulation and inhibited proliferation of NSCLC cells. • Identification of Casp3 and Prdx6 were direct target proteins of GA in the treatment of NSCLC cells. [ABSTRACT FROM AUTHOR]