槲皮素多核铜配合物的制备及活性表征

Preparation and Activity Study of Quercetin Multicopper Complexes

槲皮素金属配合物具有多种生理活性,其中肿瘤细胞抑制活性是重要研究课题之一。选用槲皮素和苯甲酸铜合成槲皮素铜配合物,通过元素分析、红外、紫外对配合物进行分析;通过体外细胞实验检测配合物对肝癌细胞Hep3B细胞形态与细胞毒性的影响;应用凝胶电泳法,研究配合物对超螺旋p BR322 DNA的裂解作用,初步探索抗肿瘤作用机制。结果分析表明槲皮素和苯甲酸铜形成两种配合物,槲皮素和铜比分别为2:1和1:4配位形式,其中1:4配位为新型配合物。MTT实验表明两种配合物对肿瘤细胞具有抑制作用,且呈剂量依赖和时间依赖,配合物对Hep3B肝癌细胞的IC_(50)值分别为122.36μg·mL^(-1)和102.89μg·mL^(-1)。DNA裂解实验显示,两种槲皮素铜配合物具有核酸酶活性,能高效裂解DNA,1:4配位的新型配合物表现出较强的裂解能力。

Quercetin metal complexes had variety bioactivities.The antitumor ability became an important research topic.Quercetin and copper benzoate were used to synthesize new type of complexes which were analyzed by elemental analysis,infrared and UV spectroscopy. The morphology and cytotoxicity effects of the quercetin copper complexes on Hep3B cells were detected by in vitro cell experiments. The DNA cleavage activities were examined using gel electrophoresis experiments on pBR322 DNA to illustrate the basic antitumor mechanism.The results showed that two copper complexes were formed with quercetin and copper ratio 2:1 and 1:4,respectively. The 1:4 coordination complex was a new form of complex.MTT experiments showed that the complexes had inhibitory effects on tumor cells and the inhibition was dose and time dependent.IC50 of complexes on Hep3B were 122.36 μg·mL^-1 and 102.89 μg·mL^-1,respectively. The DNA cleavage results showed that the complexes could interact and cleave DNA effectively,and the 1:4 coordination complex had stronger cleavage ability.