An α1-adrenergic receptor ligand repurposed as a potent antiproliferative agent for head and neck squamous cell carcinoma

Chiara Zagni; Douglas Magno Guimarães; Loredana Salerno; Francesco Punzo; Cristiane H. Squarize; Placido Giuseppe Mineo; Giuseppe Romeo; Antonio Rescifina

doi:10.1039/C4RA11856A

You do not have JavaScript enabled. Please enable JavaScript to access the full features of the site or access our non-JavaScript page.

An α₁-adrenergic receptor ligand repurposed as a potent antiproliferative agent for head and neck squamous cell carcinoma†

Chiara Zagni,^ab Douglas Magno Guimarães,^b Loredana Salerno,^a Francesco Punzo,^a Cristiane H. Squarize,^b Placido Giuseppe Mineo,^cd Giuseppe Romeo*^a and Antonio Rescifina

*^a

Author affiliations

* Corresponding authors

^a Dipartimento di Scienze del Farmaco, Università di Catania, V.le A. Doria 6, 95125 Catania, Italy
E-mail: arescifina@unict.it, gromeo@unict.it
Fax: +39-06233208980
Tel: +39-0957385017

^b Laboratory of Epithelial Biology, Department of Periodontics and Oral Medicine, University of Michigan, Ann Arbor, MI 48109-1078, USA

^c CNR-IPCF Istituto per i Processi Chimico Fisici, Viale Ferdinando Stagno D'Alcontres, 37, 98158 Messina, Italy

^d Dipartimento di Scienze Chimiche and I.N.S.T.M. UdR of Catania, Università di Catania, Viale A. Doria, 6, 95125 Catania, Italy

Abstract

In this study we report the anticancer properties of RN5-Me, an α₁-adrenergic receptor ligand. Biological screening and circular dichroism data indicate that it acts as a DNA intercalator. Docking studies, confirming this behaviour, suggest that RN5-Me possesses great selectivity for alternating AT nucleobases upon GC ones. In the cytotoxicity assay, it shows IC₅₀ values in the range of 4.2–25.0 nM towards the cancer cell lines HN6, HN13, HeLa, SK-Me1-103, PC3, and MCF7. It is noteworthy that RN5-Me shows a higher selectivity than Cisplatin for HN6 and HN13 over NOK-SI non-cancerous cells.

Download options Please wait...

Supplementary files

Supplementary information PDF (694K)

Article information

DOI: https://doi.org/10.1039/C4RA11856A
Article type: Paper
Submitted: 06 Oct 2014
Accepted: 17 Dec 2014
First published: 17 Dec 2014

Download Citation

RSC Adv., 2015,5, 6536-6542

Permissions

Request permissions

An α₁-adrenergic receptor ligand repurposed as a potent antiproliferative agent for head and neck squamous cell carcinoma

C. Zagni, D. M. Guimarães, L. Salerno, F. Punzo, C. H. Squarize, P. G. Mineo, G. Romeo and A. Rescifina, RSC Adv., 2015, 5, 6536 DOI: 10.1039/C4RA11856A

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Social activity

Fetching data from CrossRef.
This may take some time to load.

RSC Advances