Anticancer Activity of Leonurus sibiricus L.: Possible Involvement of Intrinsic Apoptotic Pathway

Abstract

Liver cancer is the most common cause of mortality in men and women. The aim of this study was to evaluate the methanolic extract of aerial parts of Leonurus sibiricus L (LS) for its anticancer activity on HCC cell lines. Human HCC cell lines, Huh-7 and HSC-T6 were used for cytotoxicity assay, determination of ROS and gene expression analysis (p53, Bcl-2, Bax, caspase-3, caspase-8, and caspase-9). Western blotting was used to assess ERK, AKT, and Caspase-3 activation. HPLC-MS analysis was also performed to determine the phytochemicals present in LS-M extract. LS-M extract has increased the expression of proapoptotic genes, including p53, Bax, and caspase-9 and down-regulated the activation of ERK and Akt. The caspase-3 activity as well as the ROS generation were significantly increased in a dose-dependent manner compared to control. The carotenoids, lutein and beta carotene present in LS-M extract exhibited anticancer activity. In overall, the methanolic extract of LS induces apoptosis in Huh-7 as well as in HSC-T6 cells possibly involving a ROS-mediated mitochondrial signaling pathway.

Graphical abstract - The methanolic extract of LS induces apoptosis in Huh-7 as well as in HSC-T6 cells possibly involving a ROS-mediated mitochondrial signaling pathway

Authors’ contributions

Krishnan Vasanth and Subramaniam Selvakumar carried out the experiments and drafted the manuscript. Chia–Chuan Chang participated in experiments, interpretation, and revised the manuscript. Venkatachalam Balamurugan and Thomas Cheeran Amal analyzed the data. Chi-Ying F. Huang planned the study and critical review on the manuscript. All authors have read and approved the final manuscript.

Disclosure statement

The authors declare that they have no conflict of interest.

Ethical approval

This article does not contain any studies with human or animals performed by any of the authors.

Additional information

Funding

This work was supported by the NSC-National Science Council in the year January-2009 to July-2011.