A new generation of MDR modulating agents with dual activity: P-gp inhibitor and iNOS inducer agents

Nicola Antonio Colabufo, Marialessandra Contino, Francesco Berardi, Roberto Perrone, Maria Antonietta Panaro, Antonia Cianciulli, Vincenzo Mitolo, Amalia Azzariti, Annelisa Quatrale, Angelo Paradiso

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

Multidrug Resistance (MDR) is due to the ability of some ATPase transporters to efflux chemotherapeutic agents out from tumor cells decreasing the endocellular concentration for the pharmacological effect, causing cancer cells chemoresistance. In the present work, a set of MDR modulating agents (MC89, MC70, PB28, IG9) able to modulate transmembrane ATP-dependent transporter, P-glycoprotein (P-gp), and also to induce inducible nitric oxide synthase (iNOS) expression in a panel of tumor cell lines are presented. All selected compounds, known as potent P-gp modulating agents, stimulated nitric oxide (NO) via iNOS in U937, Caco-2 and MCF7-Adr cell lines. The results displayed a new pharmacological strategy to revert MDR and lead to develop a new class of MDR reverting agents devoid of the limits of P-gp inhibitors third generation.

Original languageEnglish
Pages (from-to)222-230
Number of pages9
JournalToxicology in Vitro
Volume25
Issue number1
DOIs
Publication statusPublished - Feb 2011

Fingerprint

Multiple Drug Resistance
P-Glycoprotein
Nitric Oxide Synthase Type II
Cells
Tumors
Pharmacology
MCF-7 Cells
Tumor Cell Line
Adenosine Triphosphatases
Neoplasms
Nitric Oxide
Adenosine Triphosphate
Cell Line

Keywords

  • Inducible nitric oxide synthase
  • Multidrug Resistance
  • Nitric oxide
  • P-glycoprotein

ASJC Scopus subject areas

  • Toxicology

Cite this

A new generation of MDR modulating agents with dual activity : P-gp inhibitor and iNOS inducer agents. / Colabufo, Nicola Antonio; Contino, Marialessandra; Berardi, Francesco; Perrone, Roberto; Panaro, Maria Antonietta; Cianciulli, Antonia; Mitolo, Vincenzo; Azzariti, Amalia; Quatrale, Annelisa; Paradiso, Angelo.

In: Toxicology in Vitro, Vol. 25, No. 1, 02.2011, p. 222-230.

Research output: Contribution to journalArticle

Colabufo, NA, Contino, M, Berardi, F, Perrone, R, Panaro, MA, Cianciulli, A, Mitolo, V, Azzariti, A, Quatrale, A & Paradiso, A 2011, 'A new generation of MDR modulating agents with dual activity: P-gp inhibitor and iNOS inducer agents', Toxicology in Vitro, vol. 25, no. 1, pp. 222-230. https://doi.org/10.1016/j.tiv.2010.11.004
Colabufo, Nicola Antonio ; Contino, Marialessandra ; Berardi, Francesco ; Perrone, Roberto ; Panaro, Maria Antonietta ; Cianciulli, Antonia ; Mitolo, Vincenzo ; Azzariti, Amalia ; Quatrale, Annelisa ; Paradiso, Angelo. / A new generation of MDR modulating agents with dual activity : P-gp inhibitor and iNOS inducer agents. In: Toxicology in Vitro. 2011 ; Vol. 25, No. 1. pp. 222-230.
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