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.
Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation / Pagano, Bruno; Caterino, Marco; Filosa, Rosanna; Giancola, Concetta. - In: MOLECULES. - ISSN 1420-3049. - 22:11(2017), p. 1831. [10.3390/molecules22111831]
Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation
Pagano, BrunoPrimo
;Caterino, Marco;Giancola, Concetta
2017
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
