阿朴哈尔明衍生物与 DNA 的结合：光谱研究。

Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation.

机构信息

Department of Pharmacy, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, Italy.

Department of Experimental Medicine, Campania University "Luigi Vanvitelli", Via L. De Crecchio 7, 80138 Naples, Italy.

出版信息

Molecules. 2017 Oct 27;22(11):1831. doi: 10.3390/molecules22111831.

DOI:10.3390/molecules22111831

PMID:29077046

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6150274/

Abstract

Harmine belongs to a group of β-carboline alkaloids endowed with antitumor properties. Harmine and its derivatives are thought to bind to DNA and interfere with topoisomerase activities. We investigated the base-dependent binding of harmine, and three of its synthetic anticancer-active derivatives to the genomic DNA from calf thymus and two synthetic 20-mer double helices, the poly(dG-dC)·poly(dG-dC) and the poly(dA-dT)·poly(dA-dT), by means of UV-Vis and circular dichroism (CD) spectroscopies. The data show that the DNA binding and stabilising properties of the investigated derivatives are base pair-dependent. These results could be used as a guide to design and develop further bioactive analogues.

摘要

哈尔明属于具有抗肿瘤特性的β-咔啉生物碱群。哈尔明及其衍生物被认为能与 DNA 结合并干扰拓扑异构酶的活性。我们通过紫外可见分光光度法和圆二色性（CD）光谱法研究了哈尔明及其三种合成抗癌活性衍生物与小牛胸腺基因组 DNA 和两条合成 20 聚体双链，即聚（dG-dC）·聚（dG-dC）和聚（dA-dT）·聚（dA-dT）的碱基依赖性结合。数据表明，所研究的衍生物的 DNA 结合和稳定特性取决于碱基对。这些结果可作为设计和开发进一步的生物活性类似物的指导。