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Published on: May 12, 2023
Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation
Bruno Pagano1, Marco Caterino2, Rosanna Filosa3
1Department of Pharmacy, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, Italy. bruno.pagano@unina.it.
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.
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