期刊
FOOD AND CHEMICAL TOXICOLOGY
卷 143, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.fct.2020.111550
关键词
Cirsilineol; Lung cancer; Apoptosis; ROS; Ornithine decarboxylase; Cycloxygenase-2
资金
- SERB-DST, New Delhi, India [EEQ/2016/000121]
- CST-UP, Lucknow, India [GAP-394]
- CSIR-Phytopharma Mission Project [HCP-010]
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 mu M. 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 subdiploid cell population, which then leads to an increase in apoptosis by 2.64 and 5.12 fold at 10 mu M and 100 mu M 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 mu M and 100 mu M 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.
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