Chemotherapeutic potential of 9-phenyl acridine: biophysical studies on its binding to DNA.

European Biophysics Journal : EBJ
Rita GhoshSomnath Ghosh

Abstract

Acridines and their derivatives are well-known probes for nucleic acids as well as being relevant in the field of drug development to establish new chemotherapeutic agents. We have shown from molecular modelling studies that 9-phenyl acridine and some of its derivatives can act as inhibitors of topoisomerase I and thus have potential to act as anticancer agents. Rational design of new compounds for therapeutics requires knowledge about their structural stability and interactions with various cellular macromolecules. In this regard it is important to know how these molecules would interact with DNA. Here we report the interaction of 9-phenyl acridine (ACPH) with calf thymus DNA (CT-DNA) based on various biophysical and molecular modelling studies. Spectrophotometric studies indicated that ACPH binds to CT-DNA. DNA melting studies revealed that binding of ACPH to CT-DNA resulted in a small increase in melting temperature, which is unlikely in case of classical intercalator; rather, it indicates external binding. Viscosity measurements show that ACPH exhibits groove binding. Competitive binding of ACPH to CT-DNA pre-bound to ethidium bromide (EB) showed slow quenching. Measurement of the binding constant of ACPH by fluorescent int...Continue Reading

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Citations

May 4, 2013·Molecular Biology Reports·Robert SeligaJan Mojzis
Dec 11, 2013·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Elizabeth Almeida LafayetteMaria do Carmo Alves de Lima
Oct 4, 2011·Molecular and Cellular Biochemistry·Rita GhoshDipanjan Guha
Mar 27, 2020·Combinatorial Chemistry & High Throughput Screening·Bapu R ThoratSuraj N Mali
Feb 16, 2021·Nucleosides, Nucleotides & Nucleic Acids·Surajit HansdaRita Ghosh
Sep 19, 2020·Heliyon·Surajit HansdaRita Ghosh

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