Selective in vitro Synergistic Evaluation of Probiotic Tolerant morpholinyl- and 4-ethylpiperazinyl-Imidazole-chalcone Derivatives on Gastrointestinal System Pathogens

• Published in: Current microbiology Vol. 81; no. 8; p. 258
• Main Authors: Söylemez, Tuncay, Kaplancıklı, Zafer Asım, Osmaniye, Derya, Özkay, Yusuf, Demirci, Fatih
• Format: Journal Article
• Language: English
• Published: New York Springer US 01-08-2024; Springer Nature B.V
• Subjects: Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; Antifungal activity; Antifungal Agents - chemistry; Antifungal Agents - pharmacology; Antiinfectives and antibacterials; Antimicrobial activity; Antimicrobial agents; Bacteria - drug effects; Biomedical and Life Sciences; Biotechnology; Chalcone - analogs & derivatives; Chalcone - chemistry; Chalcone - pharmacology; Chalcones - chemistry; Chalcones - pharmacology; Drug Synergism; E coli; Evaluation; Fungicides; Gastrointestinal system; Gastrointestinal Tract - microbiology; Humans; Imidazole; Imidazoles - chemistry; Imidazoles - pharmacology; Lactobacilli; Life Sciences; Microbial Sensitivity Tests; Microbiology; Microorganisms; Original Paper; Pathogens; Probiotics; Probiotics - pharmacology; Synergistic effect
• ISSN: 0343-8651; 1432-0991; 1432-0991
• DOI: 10.1007/s00284-024-03788-5

Imidazole-chalcone compounds are recognised for their broad-spectrum antimicrobial properties. Probiotic-friendly, selective new-generation antimicrobials prove to be more efficient in combating gastrointestinal system pathogens. The aim of this study is to identify imidazole-chalcone derivatives that probiotics tolerate and evaluate their in vitro synergistic antimicrobial effects on pathogens. In this study, fifteen previously identified imidazole-chalcone derivatives were analyzed for their in vitro antimicrobial properties against gastrointestinal microorganisms. Initially, the antimicrobial activity of pathogens was measured using the agar well diffusion method, while the susceptibility of probiotics was determined by microdilution. The chosen imidazole-chalcone derivatives were assessed for synergistic effects using the checkerboard method. Four imidazole-chalcone derivatives to which probiotic bacteria were tolerant exhibited antibacterial and antifungal activity against the human pathogens tested. To our knowledge, this study is the first to reveal the fractional inhibitory concentration (FIC) of combinations of imidazole-chalcone derivatives. Indeed, the minimum inhibitory concentrations (MIC) for morpholinyl- (ZDO-3f) and 4-ethylpiperazinyl- (ZDO-3 m) imidazole-chalcones were notably low when tested against
E. coli
and
B. subtilis
, with values of 31.25 μg/mL and 125 μg/mL, respectively. The combination of morpholinyl- and 4-ethylpiperazinyl derivatives demonstrated an indifferent effect against
E. coli
, but an additive effect was observed for
B. subtilis
. Additionally, it was observed that imidazole-chalcone derivatives did not exhibit any inhibitory effects on probiotic organisms like
Lactobacillus fermentum
(CECT-5716),
Lactobacillus rhamnosus
(GG), and
Lactobacillus casei
(RSSK-591). This study demonstrates that imidazole-chalcone derivatives that are well tolerated by probiotics can potentially exert a synergistic effect against gastrointestinal system pathogens.