The Studies On The Anticancer Activity Of β-Elemene Derivates

This paper reported the structures-effect relationship ofβ-elemene derivates detected using a panel of cultured human tumor cell lines in vitro. The anticancer activity of Elemene Piperazine and the involved mechanisms were also investigated.The analysis of the elementary structure-effect relationships showed that the anticancer activity ofβ-elemene derivates had noting to do with the anticancer activity of substituent. And the active hydrogen was indispensable to the anticancer activity ofβ-elemene derivates containing fatty amine or aromatic heterocycles.In vitro, Elemene Piperazine had the inhibitory effects on the proliferation of Hela, HepG-2, SGC-7901 and Bel-7402 cells. Optic microscope, fluorescence microscope photomicroscopical observation and DNA agarose gel electrophoresis showed that Elemene Piperazine could induce apoptosis in Hela cells. Moreover, the results of flow cytometric methods showed that cell cycle was arrested at G₀/G₀ period, and then the cells were induced apoptosis can be induced. So, it can be said that Elemene Piperazine can induce cell apoptosis in Hela cells and has the arresting effects on cell cycle.In vivo, Elemene piperazine had the inhibitory effects on the growth of mice transplanted S₁₈₀ tumor or H₂₂ tumor. It did not affect the weight of immune organ, but the nature killer cells activity and lymphocyte proliferaion ratio were elevated significant （P＜0.05-0.001）. The anti-tumor effect of elemene piperazine may be due to activation of the immunocompetence of the body.