天然产物研究与开发 ›› 2020, Vol. 32 ›› Issue (9): 1576-1581.doi: 10.16333/j.1001-6880.2020.9.016

• 开发研究 • 上一篇    下一篇

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

刘衍季1,涂丽华1,虞佳2*,李瑾1,余卫强1,张莉萍1,王晓英1   

  1. 1南昌市卫生学校,南昌 330006;2南昌大学第三附属医院,南昌330008
  • 出版日期:2020-09-28 发布日期:2020-09-25
  • 基金资助:
    江西省中医药科研课题(2017A327)

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

LIU Yan-ji1,TU Li-hua1,YU Jia2*,LI Jin1,YU Wei-qiang1,ZHANG Li-ping1,WANG Xiao-ying1   

  1. 1Nanchang Health School,Nanchang 330006,China;2Third Affiliated Hospital of Nanchang University,Nanchang 330008,China

  • Online:2020-09-28 Published:2020-09-25

摘要:

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。

关键词: 水飞蓟宾, 微量元素, 配合物, 抗菌, 抗肿瘤

Abstract:

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.

Key words: silybin, trace elements, complex, antibiosis, antitumor

中图分类号:  R284.3 R285