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...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2017-10-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/22/11/1831 |
| _version_ | 1819078195616415744 |
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| author | Bruno Pagano Marco Caterino Rosanna Filosa Concetta Giancola |
| author_facet | Bruno Pagano Marco Caterino Rosanna Filosa Concetta Giancola |
| author_sort | Bruno Pagano |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-12-21T19:09:14Z |
| format | Article |
| id | doaj.art-8ffec1d3618e4be2afeb36d218f1392a |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-21T19:09:14Z |
| publishDate | 2017-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-8ffec1d3618e4be2afeb36d218f1392a2022-12-21T18:53:14ZengMDPI AGMolecules1420-30492017-10-012211183110.3390/molecules22111831molecules22111831Binding of Harmine Derivatives to DNA: A Spectroscopic InvestigationBruno Pagano0Marco Caterino1Rosanna Filosa2Concetta Giancola3Department of Pharmacy, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, ItalyDepartment of Pharmacy, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, ItalyDepartment of Experimental Medicine, Campania University “Luigi Vanvitelli”, Via L. De Crecchio 7, 80138 Naples, ItalyDepartment of Pharmacy, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, ItalyHarmine 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.https://www.mdpi.com/1420-3049/22/11/1831alkaloidsDNA duplexspectroscopy |
| spellingShingle | Bruno Pagano Marco Caterino Rosanna Filosa Concetta Giancola Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation Molecules alkaloids DNA duplex spectroscopy |
| 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 | alkaloids DNA duplex spectroscopy |
| url | https://www.mdpi.com/1420-3049/22/11/1831 |
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