Antitumor activity of acriflavine in lung adenocarcinoma cell line A549

Area of Science:

• Oncology
• Pharmacology
• Molecular Biology

Background:

• Non-small cell lung cancer (NSCLC) remains a leading cause of cancer-related deaths worldwide.
• Development of novel therapeutic agents is crucial for improving patient outcomes.
• Targeting cancer cell proliferation and survival pathways is a key strategy in NSCLC drug discovery.

Purpose of the Study:

• To evaluate the efficacy of acriflavine (ACF) as a potential anti-cancer drug against NSCLC.
• To investigate the mechanism of action of ACF in human lung adenocarcinoma A549 cells.
• To assess the in vivo anti-tumor activity of ACF in a mouse xenograft model.

Main Methods:

• Human lung adenocarcinoma A549 cells were treated with varying concentrations of ACF.
• Cell viability was assessed using the MTT assay.
• Cell cycle analysis was performed using flow cytometry.
• Expression levels of Bcl-2, Bax, cleaved PARP-1, and caspase-3 were analyzed.
• In vivo efficacy was evaluated in nude mice bearing A549 xenografts.

Main Results:

• ACF demonstrated significant dose- and time-dependent suppression of A549 cell viability.
• ACF induced cell growth arrest in the G2/M phase of the cell cycle.
• ACF altered the expression of apoptosis-related proteins, increasing Bax and cleaved PARP-1/caspase-3, while decreasing Bcl-2.
• ACF treatment significantly reduced tumor size and the number of lung surface tumor spots in vivo.

Conclusions:

• ACF exhibits potent cytotoxic effects against A549 NSCLC cells.
• ACF mediates its anti-cancer effects through the induction of apoptosis via caspase-3 activation.
• ACF demonstrates promising anti-tumor activity in both in vitro and in vivo models, suggesting its potential as a novel therapeutic agent for NSCLC.