Antiprostate Cancer Activity of Ineupatolide Isolated from Carpesium cernuum L.

Abstract

Objective. The aim of the study was to investigate the antiprostate cancer effects and mechanism of ineupatolide (T-21), a natural product isolated from the Compositae plant Carpesium cernuum L., on PC-3 human prostate cancer cells. Methods. The effect of T-21 on the proliferation of PC-3 cells was detected by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, cell migration, and invasion experiments; the morphology of cell apoptosis was observed by Hoechst-propidium iodide staining; the effects of T-21 on PC-3 cell apoptosis and the cell cycle were evaluated by flow cytometry; and the effect of T-21 on the expression levels of phosphorylated protein kinase B (p-AKT), AKT, X-linked inhibitor of apoptosis protein (xlAP), procaspase-3, and poly (ADP-ribose) polymerase (PARP) in PC-3 cells was measured by western blotting. Results. T-21 significantly inhibited the proliferation of cells, and its half-maximal inhibitory concentrations at 12, 24, and 48 h were 38.46 ± 1.01 , 24.63 ± 0.70 , and 7.36 ± 0.58 μ M , respectively. T-21 may promote cell apoptosis in a concentration-dependent manner and block the cell cycle in the G2 and S phases. In addition, T-21 significantly reduced the protein expression levels of p-AKT, AKT, xlAP, procaspase-3, and PARP. Conclusion. T-21 exhibits antiproliferation effects on PC-3 cells by promoting apoptosis and arresting the cell cycle in the G2 and S phases. The possible mechanism underlying its potential therapeutic effects against prostate cancer is related to the AKT/xlAP pathway.

Chemical Composition and Cytotoxic Activity of Extracts from Carpesium divaricatum: In Vitro- versus Field-Grown Plants

“…are rich in sesquiterpene lactones and monoterpenoid thymol derivatives of well documented anti-inflammatory and cytotoxic activity [ 3 , 4 ]. Germacranolides isolated from the plants were frequently studied in respect of their cytotoxic activity against human cancer cells in vitro [ 5 , 6 , 7 , 8 ], but only a few studies dealt with the molecular mechanism of action of the compounds [ 9 , 10 , 11 ]. Recently, a paper reporting on poor selectivity of the cytotoxic effect exerted by Carpesium germacranolides has been published [ 12 ].…”