吡唑啉酮配合物杀菌抗肿瘤活性及与DNA的作用

Studies on Antitumor Activities,Antibacterial Activities and Interactions with DNA of Pyrazolone Complexes

目的:合成5种吡唑啉酮金属配合物,测定其杀菌抗肿瘤活性及与DNA的作用。方法:牛津杯法和MTT法检测其杀菌抗肿瘤活性,紫外光谱法研究其与DNA的作用。结果:Cd-PMPP-SAL抗菌抗肿瘤活性较好,对金黄色葡萄球菌的最小抑制浓度为15μg/mL,对人食管癌细胞和人宫颈癌细胞作用72 h细胞存活率仅为9.67%和0.74%;该类配合物使DNA紫外吸收呈现减色效应。结论:Cd-PMPP-SAL有显著的杀菌抗肿瘤活性。

Objective： Five kinds of pyrazolone complexes were synthesized. Their antitumor activities, antibacterial activities and the inter- action relationship between the pyrazolone complexes and DNA were investigated. Method：These compounds were tested for antibacterial activities and the antitumor activities using cylinder - plate assay and MTT assay, the interaction relationship between pyrazolone and DNA by UV - vis spectra. Result： Among them tested, Cd - PMPP - SAL complex showed good to excellent antibacterial activity against Staphy- lococcus aureus with a MIC value of 15 μg/mL. It was also able to inhibit the proliferation of esophageal cancer cells （ Eca - 109） and cer- vical carcinoma cells （HeLa） with the cell viability of 9. 67 % and O. 74 % after treated for 72 h, respectively. The hypochromic effect of the DNA ultraviolet absorption was caused by pyrazolone complexes. Conclusion：The results indicate that Cd -PMPP -SAL complex has remarkable antibacterial and antitumor activities, and affect the ultraviolet absorption spectra of DNA, which can be useful as a potent anti- microbial and antitumor agent.