1,2,5-硒二唑嘧啶衍生物ASPO的合成及其抗氧化与抗肿瘤活性研究

selenadiazole pyrimidine heterocyclic compound 5-amino-[1,2,5]selenadiazolo[3,4-d] -pyrimidin-7-ol (ASPO) has been synthesized, characterized and evaluated for its antioxidant and anticancer activities. The results showed that ASPO could effectively scavenge the ABTS and DPPH free radicals in a time-dependent manner, suggesting that it has strong antioxidant activity. The in vitro anticancer activities of ASPO were screened by MTT assay against various cancer cell lines and it was found that ASPO could effectively inhibit cancer cell growth, especially for A-375 human skin melanoma cells. Further investigation on the action mode showed that ASPO could induce Sub-G1 peak accumulation, chromatin condensation and the formation of apoptotic body in a dose-dependent manner in cancer cells, indicating that induction of apoptosis the main mechanism accounting for the action of ASPO. Moreover, The DNA-binding properties of ASPO have also been investigated by spectroscopic and viscometric methods. The results show that ASPO can bind to CT-DNA by minor groove. Taken together, our results support that ASPO induces cancer cell apoptosis through its interaction with DNA.