Synthesis and in vitro anti-proliferative activity of beta-elemene monosubstituted derivatives in HeLa cells mediated through arrest of cell cycle at the G1 phase.
Beta-elemene monosubstituted amine, ether and rhenium coordinated complex were synthesized. Their structures were characterized by IR, (1)H NMR, (13)C NMR, HRMS or EA. Their IC(50) on HeLa cell lines, cell cycle and protein expression of G(1) phase (Cyclin D(1), 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 beta-elemene monosubstituted amine and Re(CO)(3)-beta-elemene derivatives in human cervix epitheloid carcinoma HeLa cells were improved significantly compared with both of ether derivatives and parent beta-elemene. These derivatives could reduce Rb phosphorylation and cyclin D(1) protein expression to arrest the cell cycle at G(1) phase.
Sun
Yanhong
Y
Research Center of Radiopharmaceuticals, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, 2019 BaoJia Road, Shanghai 201800, PR China.
Liu
Guifeng
G
Zhang
Yuangqing
Y
Zhu
Hua
H
Ren
Yunfeng
Y
Shen
Yu-Mei
YM
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D019938:Cyclin D1 / Q000378:metabolism; D005260:Female; D005434:Flow Cytometry; D016193:G1 Phase / Q000187:drug effects*; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D012717:Sesquiterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D012717:Sesquiterpenes; C445979:beta-elemene; D019938:Cyclin D1