水飞蓟宾微量元素配合物的合成及其抗菌抗肿瘤活性研究

Synthesis of silybin complexes with trace elements and their anti-bacterial and anti-tumor activities

合成水飞蓟宾钙、铁、锌、硒、铬、钴配合物6个中药新药,采用IR、UV、Lc-MS、EDTA络合滴定和元素分析仪表征配合物化学结构,结果显示合成的配合物配位比为2∶1(水飞蓟宾∶微量元素),且小鼠急性毒性实验显示6个配合物均无明显毒性。采用倍比稀释法测定配合物对枯草杆菌等9种致病菌的抑制活性,发现其最小抑菌浓度MIC均低于水飞蓟宾,抗菌活性提升至2~4倍;采用MTT法测定配合物对5株肿瘤细胞增殖的影响,发现其半数抑制浓度IC50均小于水飞蓟宾,抗肿瘤活性提升至1.11~1.53倍。综上,水飞蓟宾与微量元素形成配合物后,其抗菌及抗肿瘤活性均增强。

Six new Chinese medicine complexes of silybin calcium,iron,zinc,selenium,cobalt and chromium were synthesized and characterized by IR,UV,LC-MS,EDTA complexometric titration and elemental analysis.The results showed that coordination ratios of these six silybin complexes were 2∶1(silybin ratio to trace elements).The safety of complexes was evaluated by acute toxicity test on mice,and found that no obvious toxicity of these complexes in vivo.Furthermore,the anti-bacterial and anti-tumor activities were determined respectively by double dilution method and MTT assay.For the anti-bacterial assay,nine types of bacteria were used in this experiment and the minimum inhibitory concentration(MIC)were determined.The results showed that the anti-bacterial effect of silybin was increased to 2 to 4 times after reaction with the six trace elements.For the anti-tumor assay,experiments were carried out in 5 types of cancer cells and the half inhibitory concentration(IC50)of the six complexes was determined.The results showed that the anti-tumor effect of these complexes was increased to 1.11-1.53 times compared with that of Silybin.In conclusion,the anti-bacterial and anti-tumor activities of silybin are elevated after the formation of complexes with the trace elements.