Synthesis and in vitro anti-proliferative activity of β-elemene monosubstituted derivatives in HeLa cells mediated through arrest of cell cycle at the G1 phase

β-Elemene monosubstituted amine, ether and rhenium coordinated complex were synthesized. Their structures were characterized by IR, 1H NMR, 13C NMR, HRMS or EA. Their IC50 on HeLa cell lines, cell cycle and protein expression of G1 phase (Cyclin D1, Rb, P-Rb) were detected respectively by the method of WST-1, Flow Cytometry and Western Blot. The Results showed that the in vitro anti-proliferative activity of β-elemene monosubstituted amine and Re(CO)3-β-elemene derivatives in human cervix epitheloid carcinoma HeLa cells were improved significantly compared with both of ether derivatives and parent β-elemene. These derivatives could reduce Rb phosphorylation and cyclin D1 protein expression to arrest the cell cycle at G1 phase.

β-Elemene monosubstituted derivatives were synthesized. The in vitro anti-proliferative activity of β-elemene monosubstituted amine and Re(CO)3-β-elemene derivatives in human cervix epitheloid carcinoma HeLa cells were improved significantly compared with both of ether derivatives and parent β-elemene. These derivatives could reduce Rb phosphorylation and cyclin D1 protein expression to arrest the cell cycle at G1 phase.Figure optionsDownload as PowerPoint slide