title: Rosbin, a synthetic small molecule, induces A549 cells apoptosis through a ROS-mediated pathway.
abstract: 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.
authors.affiliation: Faculty of Environmental Science and Engineering, Kunming University of Science and Technology, Kunming, Yunnan, 6505001, P.R. China.|Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, Yunnan, 650500, P.R. China.
authors.forename: Ting
authors.initials: T
authors.lastname: Zhao
authors.affiliation: Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, Yunnan, 650500, P.R. China.
authors.forename: Wenling
authors.initials: W
authors.lastname: Jin
authors.affiliation: Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, Yunnan, 650500, P.R. China.
authors.forename: Hui
authors.initials: H
authors.lastname: Pan
authors.affiliation: Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, Yunnan, 650500, P.R. China.
authors.forename: Haizhou
authors.initials: H
authors.lastname: Li
authors.affiliation: Institute of Plant Physiology and Ecology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai, 20000, P.R. China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Zhao
authors.affiliation: Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, Yunnan, 650500, P.R. China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Feng
mesh_terms: D000072283:A549 Cells; D000111:Acetylcysteine / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D053148:Caspase 3 / Q000378:metabolism; D053179:Caspase 7 / Q000378:metabolism; D053453:Caspase 9 / Q000378:metabolism; D005434:Flow Cytometry; D006801:Humans; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D008928:Mitochondria / Q000378:metabolism; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity*; D017382:Reactive Oxygen Species / Q000378:metabolism*; D013876:Thiophenes / Q000737:chemistry / Q000633:toxicity*
chemical_list: D000970:Antineoplastic Agents; D010880:Piperidines; D017382:Reactive Oxygen Species; D013876:Thiophenes; C000613751:rosbin; C032727:piperidine; D053148:Caspase 3; D053179:Caspase 7; D053453:Caspase 9; D000111:Acetylcysteine
keywords: ROS; apoptosis; caspase; non-small cell lung cancer; rosbin