Rosbin, a synthetic small molecule, induces A549 cells apoptosis through a ROS-mediated pathway

Rosbin (Thieno [2, 3-c] piperidine-3-carboxamide-2-[(3-methoxy-naphtha-lene-2-carbonyl)-amino]-6-(benzyl)-, hydrochloride), a synthetic piperidinothieno derivative compound obtained from chemical genetics screenings, significantly suppresses the viability of non-small cell lung cancer A549 cells with an IC50 of 2.05 ± 0.31 µM. It only decreases growth of non-tumour MRC-5 cells at the doses higher than 10 µM. Rosbin induces apoptosis in a dose-dependent manner by reducing the mitochondrial membrane potential (MMP) and increasing activities of caspases-3/7 and caspase-9 in A549 cells, without affecting the activity of caspase-8. Further studies showed that reactive oxygen species (ROS) induced apoptosis of A549 in the presence of rosbin as apoptosis was inhibited by N-acetyl cysteine (NAC). These results suggest that rosbin is a novel apoptosis inducer, and ROS played a significant role in the A549 apoptosis induced by rosbin.