In Vitro and in Vivo Antitumor Activity of Scutebarbatine A on Human Lung Carcinoma A549 Cell Lines

Molecules

Xiao-Kun Yang¹  Ming-Yuan Xu²  Gui-Sen Xu²  Yu-Lan Zhang² 

[1] Department of Emergency, Chengdu Military General Hospital, Chengdu 610083, China;

关键词: scutebarbatine A;    antitumor;    apoptosis;    A549 cells;    lung cancer;   

DOI  :  10.3390/molecules19078740

来源: mdpi

【 摘 要 】

During our systematic study on the anticancer activities of Scutellaria barbata, scutebarbatine A (SBT-A), one of the major alkaloids in S. barbata, was found to have antitumor effects on A549 cells. Thus, we designed the present study to investigate in detail the antitumor effects of SBT-A. The cytotoxic effect of SBT-A on A549 in vitro were determined by an MTT assay and evaluated by IC₅₀ values. Furthermore, results of Hoechst 33258 and Annexin V/PI staining assays demonstrated that SBT-A had significant antitumor effects on A549 cells via apoptosis, in a concentration-dependent manner. What’s more, the mechanism was explored by western blotting, and our study revealed that SBT-A can up-regulate the expressions of cytochrome c, caspase-3 and 9, and down-regulate the levels of Bcl-2 in A549 cells. Finally, the antitumor effects of SBT-A were evaluated in vivo by using transplanted tumor nude mice, and the results confirmed that SBT-A has a notable antitumor effect on A549 cancer via mitochondria-mediated apoptosis. Collectively, our results demonstrated that SBT-A showed significant antitumor effects on A549 cells in vivo and in vitro via mitochondria-mediated apoptosis by up-regulating expressions of caspase-3 and 9, and down-regulating Bcl-2.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.