Lung cancer is a common malignant disease with a high incidence rate worldwide, posing a great threat to human health. To date, only a small number of studies have assessed the potential anti-cancer effect of artesunate (Art) and the associated mechanisms in lung cancer. The present study aimed to investigate the inhibitory effects of Art in human lung cancer cells and investigated the underlying molecular mechanisms. The inhibitory effect of Art on the growth of A549 lung cancer cells was detected by the MTT assay, and flow cytometry was utilized to determine cell cycle progression, apoptosis, mitochondrial membrane potential, as well as the expression of Bcl-2 and Bax proteins in A549 cells after Art treatment for 24 h. Art inhibited the growth of A549 cells in a dose-dependent manner, induced cell apoptosis and cell cycle arrest, decreased the expression of Bcl-2 protein and mitochondrial membrane potential, and increased the expression of Bax protein. In conclusion, Art significantly inhibited the growth of lung cancer cells by preventing cell cycle progression. This phenomenon indicated its promising therapeutic potential in the treatment of lung cancer.