Anti-Helicobacter pylori activities of selected N-substituted cinnamamide derivatives evaluated on reference and clinical bacterial strains
| Autor: | Paweł Nowak, Alicja Budak, Anna M. Waszkielewicz, Elżbieta Karczewska, Paulina Koczurkiewicz, Iwona Skiba-Kurek, Katarzyna Pańczyk, Karolina Klesiewicz, Henryk Marona, Edward Sito, Elżbieta Pękala, Dorota Żelaszczyk, Agnieszka Gunia-Krzyżak |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
food.ingredient Cell Survival Microbial Sensitivity Tests Cinnamic acid Ames test Helicobacter Infections 03 medical and health sciences Minimum inhibitory concentration chemistry.chemical_compound 0302 clinical medicine food Amide Drug Discovery Drug Resistance Bacterial Agar Humans Cytotoxicity Pharmacology Chromatography biology Strain (chemistry) Helicobacter pylori Mutagenicity Tests biology.organism_classification Anti-Bacterial Agents 030104 developmental biology chemistry Cinnamates 030211 gastroenterology & hepatology |
| Zdroj: | The Journal of antibiotics. 71(5) |
| ISSN: | 1881-1469 |
| Popis: | In this study, thirty-five N-substituted derivatives of cinnamic acid amide (cinnamamide) were evaluated for anti-Helicobacter pylori activity using an agar disc-diffusion method. Qualitative screening was performed on a reference H. pylori strain (ATCC 43504), resulting in the identification of the three most active compounds, 8 (R,S-(2E)-3-(4-chlorophenyl)-N-(2-hydroxypropyl)prop-2-enamide, minimal inhibitory concentration, MIC = 7.5 µg/mL), 23 ((2E)-3-(4-chlorophenyl)-N-(2-hydroxycyclohexyl)prop-2-enamide, MIC = 10 µg/mL), and 28 ((2E)-3-(4-chlorophenyl)-N-(4-oxocyclohexyl)prop-2-enamide, MIC = 10 µg/mL). These compounds were further tested on twelve well-characterized clinical strains, yielding MIC values that ranged from 10 to 1000 µg/mL. Preliminary safety assessments of the compounds were made using the MTT viability test for cytotoxicity and Ames test for mutagenicity, which showed them to be generally safe, although compounds 8 and 28 showed mutagenic activity at some of the tested concentrations. The results of this study showed the anti-H. pylori potential of cinnamamide derivatives. |
| Databáze: | OpenAIRE |
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