5P,a small GPX mimic,provides a new therapeutic method to tr eat liver cancer

【Author】

Ping Yu;Yanhong Sun;Juxin Yin;Shaowu Lv;

【Abstract】

Glutathione peroxidase(GPx)is a kind of protein containing selenium has potent antioxidant ability and it is important for treating and preventing cancer.Due to the limitations associated with native GPx,such as instability,limited availability,big molecular weight and immunogenicity,many scientists have made a great deal of efforts to study the GPx mimics.We design and compound a new pentapeptide containing selenium(Se-5P).The kinetic analysis showed that the mechanism of Se-5P catalyzed reduction of H_2O_2 by GSH is Ping-Pong mechanism and the values of k-(cat)/K_(mH2O2)and k_(cat)/K_(mGSH)are higher,indicating that Se-5P has higher affinity with both substrates.In vitro,Se-5P efficiently inhibited the growth of the H22 cells and promoted apoptosis by the method of MTT and flow cytometry.It can obviously influence the amount of mRNA expression of apoptosis related gene Bax/Bcl-2 and activate the caspase in the treated H22 cells.

【Keywords】

cytometry;Glutathione;selenium;mimic;affinity;caspase;inhibited;instability;peroxidase;activate;

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