Binding of Harmine Derivatives to DNA: A Spectroscopic Investigation

• Main Authors: Bruno Pagano, Marco Caterino, Rosanna Filosa, Concetta Giancola
• Format: Article
• Language: English
• Published: MDPI AG 2017-10-01
• Series: Molecules
• Subjects: alkaloids; DNA duplex; spectroscopy
• Online Access: https://www.mdpi.com/1420-3049/22/11/1831

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.