Cirsimaritin, a lung squamous carcinoma cells (NCIH-520) proliferation inhibitor

Cirsimaritin is a dimethoxy flavone, which is present in Ocimum sanctum, Microtea debilis, Artemisia judaica, Cirsium japonicum, and Lithocarpus dealbatus. Its antiproliferative potential has been explored in breast and gall bladder cancer cell lines. However, no reports are available on skin and squamous lung carcinoma. Also, the complete mode of action is unknown. Therefore, in the present study, the anticancer potential of cirsimaritin is explored in organ-specific cell lines by using MTT assay. Further, the inhibitory potential and binding interaction with the selected targets were analyzed through in vitro and in-silico analysis. Cirsimaritin showed selective anticancer activity against NCIH-520 cell-line (IC50 23.29 mu M), also inhibited the proliferation of other cell-lines up to 48% at 100 mu M. In NCIH-520 cell-line, cirsimaritin significantly increased the apoptosis of the cells at both the tested concentrations (10 and 100 mu M), which was confirmed by Annexin-V signifying the induction of late apoptosis. Besides, an increase in the ROS levels of 1.6 fold (10 mu M) and 1.8 fold (100 mu M), circimaritin also inhibits the activity of ODC and CATD with the IC50 57.30 and 68.22 mu M respectively. It exhibited a good binding score with the selected targets, follow Lipinski's rule of five and non-mutagenic. Hence, cirsimaritin is a potent molecule, which inhibits the proliferation of lung squamous cell lines by inducing apoptosis. It also inhibited the activity of ODC and CATD responsible for the progression phase in the cancer cells. Communicated by Ramaswamy H. Sarma

Automated summary

Cirsimaritin, a dimethoxy flavone found in various plants, exhibits potent anticancer activity in multiple cancer cell lines, particularly showing selective inhibition against NCIH-520 cell-line. It induces apoptosis and increases ROS levels in cells, while also inhibiting the activity of key enzymes related to cancer progression.