Lubeluzole: from anti-ischemic drug to preclinical antidiarrheal studies.
Pharmacol Rep
; 73(1): 172-184, 2021 Feb.
Article
in En
| MEDLINE
| ID: mdl-33074530
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.Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Piperidines
/
Thiazoles
/
Diarrhea
/
Antidiarrheals
Limits:
Animals
Language:
En
Journal:
Pharmacol Rep
Journal subject:
FARMACOLOGIA
Year:
2021
Document type:
Article
Affiliation country:
Italy