RT Journal Article SR Electronic T1 Antitumor Activity of Acriflavine in Lung Adenocarcinoma Cell Line A549 JF Anticancer Research JO Anticancer Res FD International Institute of Anticancer Research SP 6467 OP 6472 VO 34 IS 11 A1 CHIA-JEN LEE A1 CHIA-HERNG YUE A1 YU-JIE LIN A1 YU-YU LIN A1 SHAO-HSUAN KAO A1 JER-YUH LIU A1 YIENG-HOW CHEN YR 2014 UL http://ar.iiarjournals.org/content/34/11/6467.abstract AB Aim/Materials and Methods: In order to develop better drugs against non-small cell lung cancer (NSCLC), we screened a variety of compounds and treated the human lung adenocarcinoma cell line A549 with different drug concentrations. We then examined the cell viability using the MTT assay. Results: Data show that a new candidate drug, acriflavine (ACF), suppresses the viability of A549 cells in a concentration- and time-dependent manner. Flow cytometry analysis revealed that ACF significantly caused cell growth arrest in the G2/M phase on A549 cells. Moreover, ACF decreased Bcl-2 expression and increased Bax expression. The content of cleaved poly(ADP-ribose)polymerase-1 (PARP-1) and caspase-3 are significantly increased. These findings suggest that ACF is cytotoxic against A549 cells and suppresses A549 cells growth through the caspase-3 activation pathway. In the in vivo test, nude mice bearing A549 cells xenografts by intravenous injection were randomly assigned into two groups: control and experimental group. Treatment was initiated 10 days after implantation and intraperitoneal injection of 0.9% normal saline or 2 mg/kg of ACF was continued daily for five weeks. ACF treatment significantly decreased tumor size and tumor spots on lung surface of tumor-bearing mice. Conclusion: ACF can inhibit cell growth in A549 cells. Our results may assist on the delineation of the mechanism(s) leading to NSCLC cell growth inhibition and provide a new antitumor strategy against NSCLC.