One of the major therapeutic approaches to preventing relapse and accelerating the healing of duodenal and gastric ulcers is the eradication of Helicobacter pylori. Due to the emergence of antibiotic resistance among clinical strains of H. pylori, alternative approaches using newly discovered antimicrobial agents in combination with the standard regimens for the treatment of H. pylori are increasingly needed. The purpose of the present study was to investigate the effect of newly synthesized 8-nitroflouroqunolone derivatives when used either alone or when combined with metronidazole against metronidazole-resistant H. pylori. Based on the standard antimicrobial susceptibility testing methods and checkerboard titration assay, all of the tested compounds showed interesting antimicrobial activity against 12 clinical strains of H. pylori, with the best in vitro effect for compound 3c. In addition, synergistic and additive activities of some of the tested compounds were observed when combined with metronidazole. Furthermore, among the tested nitroflouroquinolone derivatives, compound 3b showed significant urease inhibition activity with IC50 of 62.5 µg/mL. These results suggest that 8-nitroflouroquinolone derivatives may have a useful role in combination with anti-H. pylori drugs in the management of H. pylori-associated diseases.
Background and Aim: Interest in plants with antimicrobial properties has been revived due to emerging problems associated with using antibiotics to eradicate Helicobacter pylori. Accordingly, this study aims to assess the antibacterial effects of Punica granatum and the possible synergistic effect of its extract along with metronidazole against H. pylori. Materials and Methods: Pomegranate peel ethanol extracts (PPEE) was tested against a control strain of H. pylori (NCTC 11916) in vitro and in vivo in female Wistar rats. Moreover, the synergistic effect of PPEE in combination with metronidazole was tested in vitro. Results: The PPEE exhibited a remarkable activity against H. pylori with a minimum inhibitory concentration (MIC) of 0.156 mg/mL. Furthermore, the extract exhibited a pronounced urease inhibitory activity (IC50 ∼6 mg/mL) against the tested strain. A synergistic effect between PPEE and metronidazole was also observed (fractional inhibitory concentrations <0.5). Oral treatment of rats with PPEE for 8 days produced a significant reduction in H. pylori gastritis and a significant decrease in both lymphocytic and positive chronicity. Conclusion: Pomegranate extract is probably safe and represents a potential alternative and complementary therapy for reducing H. pylori associated with gastric ulcers.
Helicobacter pylori infection can lead to gastritis, peptic ulcer, and the development of mucosa associated lymphoid tissue (MALT) lymphoma. Treatment and eradication of H. pylori infection can prevent relapse and accelerate the healing of gastric and duodenal ulcers as well as regression of malignancy. Due to the increasing emergence of antibiotic resistance among clinical isolates of H. pylori, alternative approaches using newly discovered antimicrobial agents in combination with the standard antibiotic regimens for the treatment of H. pylori are of major importance. The purpose of the present study was to investigate the effect of newly synthesized 8-amino 7-substituted fluoroquinolone and their correspondent cyclized triazolo derivatives when either alone or combined with metronidazole against metronidazole-resistant H. pylori. Based on standard antimicrobial susceptibility testing methods and checkerboard titration assay, all of the tested compounds showed interesting antimicrobial activity against 12 clinical strains of H. pylori, with best in vitro effect for compounds 4b and 4c. Fractional inhibitory concentration (FIC) mean values showed synergistic pattern in all compounds of Group 5. In addition, additive activities of some of the tested compounds of Group 4 were observed when combined with metronidazole. In contrast, the tested compounds showed no significant urease inhibition activity. These results support the potential of new fluoroquinolone derivatives to be useful in combination with anti-H. pylori drugs in the management of H. pylori-associated diseases.
Staphylococcus aureus is one of the most common pathogens in biofilm-associated chronic infections. S. aureus that live within biofilms avoid the host's immune response and are more resistant to antibiotics than planktonic bacteria. The current study was conducted to evaluate the antibacterial, antibiofilm and antivirulence of seven antibiotics (Ciprofloxacin (CP), Gentamicin (GEN), Tetracycline (TET), Amikacin (AMK), Clindamycin (CLI), Erythromycin (Ery) and Vancomycin (VAN) against S. aureus. The effects of seven antibiotics (CP, AMK, VAN, TET GEN, Ery and CLI) on S. aureus planktonic and biofilm were determined via Antibiotic susceptibility test, Minimum Inhibitory Concentration (MIC), Minimum Bactericidal Concentration (MBC), disruption of microcolony, biofilm inhibition and degradation (crystal violet staining) and RT-qPCR. Antibiotic susceptibility test showed that CP, AMK, VAN, TET GEN, Ery and CLI has antibacterial activity against S. aureus with an inhibition zone of 28 mm, 21 mm, 27 mm, 20 mm, 25 mm, 27 mm and 19 mm respectively. The results showed that CP and AMK possessed the lowest MIC value against S. aureus with 0.125 µg/mL and 0.25 µg/mL for VAN, TET and GEN and 1.0 for Ery and CLI. The recorded values for MBCs were 0.25 μg for CP and AMK for S. aureus, 0.5 μg for vancomycin, tetracycline and gentamicin for S. aureus and 1.0 μg for Ery and CLI for S. aureus. Notably, CP and AMK demonstrated considerable efficacy, as shown by the low values for MIC; 0.125 μg and MBC; 0.25 μg for S. aureus. All antibiotics were found to disrupt microcolony formation in S. aureus at MIC of each antibiotics. At 0.25 μg concentration to 8 μg concentration of each antibiotic were significantly found to degrade and inhibit biofilm formation of S. aureus. The RT-qPCR showed that four genes including argF, purC, adh, and fabG were downregulated, whilst, three genes including scdA, pykA and menB were upregulated after exposure to CP, AMK, VAN, TET GEN, Ery and CLI. This study showed the efficacy of seven antibiotics against planktonic, biofilm, gene expression and that different concentrations of antibiotics have different degrees of potential effect on established biofilm. In addition, a decreased expression of virulence genes in S. aureus will impact their pathogenicity. These results provide the theoretical parameters for the selection of effective antimicrobial in clinical therapy and demonstrate how to correctly use antibiotics at MIC and sub-MIC as preventive drugs.
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