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...

Descripción completa

Detalles Bibliográficos
Autores principales: Pagano, Bruno, Caterino, Marco, Filosa, Rosanna, Giancola, Concetta
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6150274/
https://www.ncbi.nlm.nih.gov/pubmed/29077046
http://dx.doi.org/10.3390/molecules22111831
_version_ 1783356956117827584
author Pagano, Bruno
Caterino, Marco
Filosa, Rosanna
Giancola, Concetta
author_facet Pagano, Bruno
Caterino, Marco
Filosa, Rosanna
Giancola, Concetta
author_sort Pagano, Bruno
collection PubMed
description 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.
format Online
Article
Text
id pubmed-6150274
institution National Center for Biotechnology Information
language English
publishDate 2017
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-61502742018-11-13 Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation Pagano, Bruno Caterino, Marco Filosa, Rosanna Giancola, Concetta Molecules Article 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. MDPI 2017-10-27 /pmc/articles/PMC6150274/ /pubmed/29077046 http://dx.doi.org/10.3390/molecules22111831 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Pagano, Bruno
Caterino, Marco
Filosa, Rosanna
Giancola, Concetta
Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation
title Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation
title_full Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation
title_fullStr Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation
title_full_unstemmed Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation
title_short Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation
title_sort binding of harmine derivatives to dna: a spectroscopic investigation
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6150274/
https://www.ncbi.nlm.nih.gov/pubmed/29077046
http://dx.doi.org/10.3390/molecules22111831
work_keys_str_mv AT paganobruno bindingofharminederivativestodnaaspectroscopicinvestigation
AT caterinomarco bindingofharminederivativestodnaaspectroscopicinvestigation
AT filosarosanna bindingofharminederivativestodnaaspectroscopicinvestigation
AT giancolaconcetta bindingofharminederivativestodnaaspectroscopicinvestigation

Ejemplares similares