2. Academic Validation
  3. Lubeluzole: from anti-ischemic drug to preclinical antidiarrheal studies

Lubeluzole: from anti-ischemic drug to preclinical antidiarrheal studies

  • Pharmacol Rep. 2021 Feb;73(1):172-184. doi: 10.1007/s43440-020-00167-2.
Maria Maddalena Cavalluzzi 1,  Roberta Budriesi 2,  Maria Antonietta De Salvia 3,  Laura Quintieri 4,  Monica Piarulli 1,  Gualtiero Milani 1,  Roberta Gualdani 5,  Matteo Micucci 6,  Ivan Corazza 7,  Antonio Rosato 1,  Maurizio Viale 8,  Leonardo Caputo 4,  Carlo Franchini 1,  Giovanni Lentini 1
Affiliations

Affiliations

  • 1 Department of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Bari, Italy.
  • 2 Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Bologna, Italy.
  • 3 Department of Biomedical Sciences and Human Oncology, University of Bari "Aldo Moro", Bari, Italy.
  • 4 Institute of Sciences of Food Production, CNR-ISPA) National Council of Research, Bari, Italy.
  • 5 Laboratory of Cell Physiology, Institute of Neuroscience, Université Catholique de Louvain, 1200, Brussels, Belgium.
  • 6 Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Bologna, Italy. [email protected].
  • 7 Department of Specialistic, Experimental and Diagnostic Medicine, Alma Mater Studiorum-University of Bologna, Bologna, Italy.
  • 8 IRCCS Azienda Ospedaliera Universitaria San Martino , U.O. Bioterapie, L.go R. Benzi, 10, 16132 , Genoa, Italy.
PMID: 33074530 DOI: 10.1007/s43440-020-00167-2
Abstract

Background: Lubeluzole, a neuroprotective anti-ischemic drug, was tested for its ability to act as both Antibiotic chemosensitizing and antipropulsive agent for the treatment of infectious diarrhea.

Methods: In the present report, the effect of lubeluzole against antidiarrheal target was tested. The antimicrobial activity towards Gram-positive and Gram-negative bacteria was investigated together with its ability to affect ileum and colon contractility.

Results: Concerning the antimicrobial activity, lubeluzole showed synergistic effects when used in combination with minocycline against four common Gram-positive and Gram-negative bacteria (Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 29213, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 25922), although relatively high doses of lubeluzole were required. In ex vivo experiments on sections of gut smooth muscles, lubeluzole reduced the intestinal contractility in a dose-dependent manner, with greater effects observed on colon than on ileum, and being more potent than reference compounds otilonium bromide and loperamide.

Conclusion: All above results identify lubeluzole as a possible starting compound for the development of a novel class of Antibacterial adjuvants endowed with spasmolytic activity.

Keywords

Antibiotics; Diarrhoea; Gut contractility; Ion channels; Lubeluzole; Synergism.

Figures
Products