Sun Yat-Sen University, Guangzhou, P R China.
Chem Biodivers. 2010 Dec;7(12):2908-16. doi: 10.1002/cbdv.200900386.
Three novel berberine derivatives bearing two, three, and four primary amino groups at C(9), respectively, were synthesized and characterized on the basis of ¹H- and ¹³C-NMR, MS, and HR-MS data. Their non-covalent binding with calf thymus (CT) DNA was investigated by means of spectrophotometric titration and ethidium bromide (EB) displacement experiments. The results indicated that these multivalent berberine derivatives exhibited up to 130-fold enhanced binding affinities relative to berberine, and thus, may be exploitable as potent DNA-binding agents.
基于 1H-NMR、13C-NMR、MS 和 HR-MS 数据，合成并表征了三个新型分别在 C(9)位带有两个、三个和四个伯氨基的小檗碱衍生物。通过分光光度滴定和溴化乙锭（EB）置换实验研究了它们与小牛胸腺（CT）DNA 的非共价结合。结果表明，与小檗碱相比，这些多价小檗碱衍生物表现出高达 130 倍的增强结合亲和力，因此可能可被开发为有效的 DNA 结合剂。
