Abstract: Griffipavixanthone (GPX) is a dimeric xanthone which was isolated in a systematic investigation of Garcinia oblongifolia Champ. In this study, we investigate the effect of GPX on cell proliferation and apoptosis on human Non-small-cell lung cancer (NSCLC) cells in vitro and determine the mechanisms of its action. GPX inhibited the growth of H520 cells in dose- and time-dependent manners, with IC50 values of 3.03 ± 0.21 μM at 48 h. The morphologic characteristics of apoptosis and apoptotic bodies were observed by fluorescence microscope and transmission electron microscope. In addition, Annexin V/PI double staining assay revealed that cells in early stage of apoptosis were significantly increased upon GPX treatment dose-dependently. Rh123 staining assay indicated that GPX reduced the mitochondrial membrane potential. DCFH-DA staining revealed that intracellular ROS increased with GPX treatment. Moreover, GPX cleaved and activated caspase-3. In summary, this study showed that GPX inhibited H520 cell proliferation in dose- and time-dependent manner. Further mechanistic study indicated that GPX induced cell apoptosis through mitochondrial apoptotic pathway accompanying with ROS production. Our results demonstrate the potential application of GPX as an anti-non-small cell lung cancer agent.
Keywords: griffipavixanthone; H520 cells; apoptosis; caspase; mitochondrial transmembrane potential; ROS generation
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Shi, J.-M.; Huang, H.-J.; Qiu, S.-X.; Feng, S.-X.; Li, X.-E. Griffipavixanthone from Garcinia oblongifolia Champ Induces Cell Apoptosis in Human Non-Small-Cell Lung Cancer H520 Cells in Vitro. Molecules 2014, 19, 1422-1431.
Shi J-M, Huang H-J, Qiu S-X, Feng S-X, Li X-E. Griffipavixanthone from Garcinia oblongifolia Champ Induces Cell Apoptosis in Human Non-Small-Cell Lung Cancer H520 Cells in Vitro. Molecules. 2014; 19(2):1422-1431.
Shi, Jun-Min; Huang, Hui-Juan; Qiu, Sheng-Xiang; Feng, Shi-Xiu; Li, Xu-E. 2014. "Griffipavixanthone from Garcinia oblongifolia Champ Induces Cell Apoptosis in Human Non-Small-Cell Lung Cancer H520 Cells in Vitro." Molecules 19, no. 2: 1422-1431.