Cirsilineol belonging to the flavones category have not been explored in detail for anti-proliferative potential, therefore selected for the investigation. Hence, the antiproliferative potential of cirsilineol has been established in NCIH-520 cells. Cirsilineol exhibited good binding-energy and inhibited the activity of ODC, CATD, DHFR, HYAL, LOX-5, and COX-2 up to 45.14% at 100 μM. It significantly inhibited the proliferation of NCIH-520 cells (81.96%) and likewise, the proliferation of other cell lines up to 48.50%. It also induced an increase in the sub-diploid cell population, which then leads to an increase in apoptosis by 2.64 and 5.12 fold at 10 μM and 100 μM respectively. Further, the Annexin-V-FITC assay confirmed the late apoptosis and necrosis in the NCIH-520 cell line induced by cirsilineol. The ROS production was enhanced by 1.16 and 2.22 folds at 10 μM and 100 μM respectively. Besides, cirsilineol revealed acceptable ADME properties, non-toxic and non-mutagenic compound. Altogether, these findings provide evidence that cirsilineol inhibited the proliferation of NCIH-520 cells by inducing ROS-mediated apoptosis and offer new insight into the anti-proliferative potential of cirsilineol, which can further be exploited to either synthesise new derivatives or its candid usage as a herbal lead for cancer treatment.
Keywords: Apoptosis; Cirsilineol; Cycloxygenase-2; Lung cancer; Ornithine decarboxylase; ROS.
Copyright © 2020 Elsevier Ltd. All rights reserved.