Study Of Polyoxometalates Functionalized By Biological Active Molecules

Objective:Through modifying polyoxometalates by the drug molecules with different biological activity, we can screen the binding biological active molecules and synthesize the polyoxometalates based compound with the dual active sites; And the structures and the antitumor activity of new compounds are characterized and studied, respectively.Methods:All new polyoxometalates based compounds have been synthesized by the hydrothermal synthesis method and structurally characterized by element analysis, Infrared spectrum,TG-DTA and single crystal X-ray diffraction technology. The antitumor activities in vitro were studied by MTT experiments(The cancer cell line are :SG7901 gastric cancer cell lines, SMMC7721 hepatocellular carcinoma celllines).Results : Two series of five new polyoxometalates based compounds have been synthesized.The results of the antitumor activity in vitro showed that the different structures of the compounds exhibited different antitumor activity and selectivity on tumor cells. Finally, the corresponding IC50 values are reported.Conclusion : In this paper, compounds based on polyoxometalates have been synthesized by using the clinical drug molecules as organic ligands. Through the characterization of the structure, five new drugs molecules modifying polyoxometalates compounds are reported:(HPPA)4 [Mo8O26]·2H2O(1)[Ni2(PPA)2(H2O)4]·[Mo8O26]·3H2O(2)[Zn(PPA)2(H2O)]2·[Mo8O26]·3.5H2O(3)[Ni(H3fcz)6][H2PMo12O40]2(4)[Cu7(H3fcz)6] [PMo12O40]2?2H2O(5)The anti-tumor activities of compounds in vitro were studied by MTT experiments, and the results show that compounds 1-3 exhibit high anti-tumor activity to SGC7901 and SMMC7721 than their parent compound, which may be explained that the introduction of M-PPA/PPA into the polyoxoanion surface can change the surface properties, such as, the electronic distribution, redox, polar, and so on. As a result, the compounds penetrate into the cells easily and increase their antitumor activity. The antitumor activity of compounds 4-5 on SGC7901 cells was also tested by the MTT experiment, respectively. The result shows that the antitumor activity change weaken due to the grafting of M-FCZ, which may be associated with the POM matrix, further experiments need to be done.