PDF(Sci-hub)
Abstract：
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.
摘要：
Cirsilineol属于黄酮类尚未详细探索抗增殖潜力，因此被选中进行调查。因此，已经在NCIH-520细胞中建立了cirsilineol的抗增殖潜力。Cirsilineol表现出良好的结合能并抑制ODC的活性，CATD,DHFR,HYAL,LOX-5和COX-2在100μM时高达45.14%。显著抑制NCIH-520细胞增殖(81.96%),其他细胞系的增殖率高达48.50%。它还诱导了亚二倍体细胞群的增加，然后在10μM和100μM时分别导致细胞凋亡增加2.64和5.12倍。Further,Annexin-V-FITC测定证实了cirsilineol诱导的NCIH-520细胞系的晚期凋亡和坏死。在10μM和100μM时，ROS的产生分别增加了1.16和2.22倍。此外,Cirsilineol显示出可接受的ADME特性，无毒和非诱变化合物。总之,这些发现提供了证据表明cirsilineol通过诱导ROS介导的细胞凋亡来抑制NCIH-520细胞的增殖，并为cirsilineol的抗增殖潜力提供了新的见解。可以进一步利用它来合成新的衍生物，或者将其作为草药治疗癌症的线索。
