Dipartimento di Chimica, Università di Roma "La Sapienza", Piazzale Aldo Moro 5, 00185 Rome, Italy.
Dipartimento di Biologia e Biotecnologie, Università di Roma "La Sapienza", Piazzale Aldo Moro 5, 00185 Rome, Italy.
Molecules. 2018 Jun 12;23(6):1423. doi: 10.3390/molecules23061423.
In this paper, the selective interactions of synthetic derivatives of two natural compounds, berberine and palmatine, with DNA G-quadruplex structures were reported. In particular, the previous works on this subject concerning berberine were further presented and discussed, whereas the results concerning palmatine are presented here for the first time. In detail, these palmatine derivatives were developed by inserting seven different small peptide basic chains, giving several new compounds that have never been reported before. The preliminary studies of the interactions of these compounds with various G-quadruplex-forming sequences were carried out by means of various structural and biochemical techniques, which showed that the presence of suitable side chains is very useful for improving the interaction of the ligands with G-quadruplex structures. Thus, these new palmatine derivatives might act as potential anticancer drugs.
本文报道了两种天然化合物（小檗碱和巴马汀）的合成衍生物与 DNA G-四链体结构的选择性相互作用。特别是，本文进一步介绍和讨论了之前关于小檗碱的相关工作，而关于巴马汀的结果则是首次呈现。具体而言，这些巴马汀衍生物是通过插入七个不同的小肽碱性链开发的，得到了几种以前从未报道过的新化合物。通过各种结构和生化技术对这些化合物与各种 G-四链体形成序列的相互作用进行了初步研究，结果表明适当的侧链的存在对于改善配体与 G-四链体结构的相互作用非常有用。因此，这些新的巴马汀衍生物可能作为潜在的抗癌药物。
