Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation

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 t...

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Bibliographic Details
Main Authors: Bruno Pagano, Marco Caterino, Rosanna Filosa, Concetta Giancola
Format: Article
Language:English
Published: MDPI AG 2017-10-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/22/11/1831
Description
Summary: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.
ISSN:1420-3049