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Molecules 2017, 22(11), 1831; doi:10.3390/molecules22111831

Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation

1
Department of Pharmacy, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, Italy
2
Department of Experimental Medicine, Campania University “Luigi Vanvitelli”, Via L. De Crecchio 7, 80138 Naples, Italy
*
Author to whom correspondence should be addressed.
Received: 28 September 2017 / Revised: 20 October 2017 / Accepted: 24 October 2017 / Published: 27 October 2017
(This article belongs to the Collection New Frontiers in Nucleic Acid Chemistry)
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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. View Full-Text
Keywords: alkaloids; DNA duplex; spectroscopy alkaloids; DNA duplex; spectroscopy
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Pagano, B.; Caterino, M.; Filosa, R.; Giancola, C. Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation. Molecules 2017, 22, 1831.

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