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In Silico and In Vitro Investigation of Anti Helicobacter Activity of Selected Phytochemicals

INTRODUCTION: Helicobacter pylori is Gram-negative helical bacteria that inhibit stomach mucosal lining and establish infection. Urease enzyme was confirmed to be pivotal target in which its suppression will prompt bacteria treatment and eradication. METHODS: Series of naturally bioactive compounds...

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Autores principales: Al Tawalbeh, Deniz, Aburjai, Talal, Al Balas, Qosay, Al Samydai, Ali
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Wolters Kluwer - Medknow 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9728063/
https://www.ncbi.nlm.nih.gov/pubmed/36506725
http://dx.doi.org/10.4103/jpbs.jpbs_850_21
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author Al Tawalbeh, Deniz
Aburjai, Talal
Al Balas, Qosay
Al Samydai, Ali
author_facet Al Tawalbeh, Deniz
Aburjai, Talal
Al Balas, Qosay
Al Samydai, Ali
author_sort Al Tawalbeh, Deniz
collection PubMed
description INTRODUCTION: Helicobacter pylori is Gram-negative helical bacteria that inhibit stomach mucosal lining and establish infection. Urease enzyme was confirmed to be pivotal target in which its suppression will prompt bacteria treatment and eradication. METHODS: Series of naturally bioactive compounds were selected based on ethnobotanical and molecular modeling techniques with potential urease inhibitory effect. The selected phytochemical compounds were in-silico and in-vitro assayed against urease enzyme, minimal inhibitory concentrations (MIC) and a synergistic effect was studied and cultured specifically for H. pylori. RESULTS: Terpineol was considered as the most active compound with an IC(50) of 1.443 μg/ml (R(2) = 0.9374). The synergistic effect of terpineol and metronidazole indicated a possible additive effect (fractional inhibitory concentration result is 0.78) with improvement of MIC results for both terpineol and metronidazole. CONCLUSION: This study suggests that terpineol is best to be considered as a lead compound for H. pylori infection treatment and could be a potent inhibitor when combined with metronidazole targeting urease enzyme.
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spelling pubmed-97280632022-12-08 In Silico and In Vitro Investigation of Anti Helicobacter Activity of Selected Phytochemicals Al Tawalbeh, Deniz Aburjai, Talal Al Balas, Qosay Al Samydai, Ali J Pharm Bioallied Sci Original Article INTRODUCTION: Helicobacter pylori is Gram-negative helical bacteria that inhibit stomach mucosal lining and establish infection. Urease enzyme was confirmed to be pivotal target in which its suppression will prompt bacteria treatment and eradication. METHODS: Series of naturally bioactive compounds were selected based on ethnobotanical and molecular modeling techniques with potential urease inhibitory effect. The selected phytochemical compounds were in-silico and in-vitro assayed against urease enzyme, minimal inhibitory concentrations (MIC) and a synergistic effect was studied and cultured specifically for H. pylori. RESULTS: Terpineol was considered as the most active compound with an IC(50) of 1.443 μg/ml (R(2) = 0.9374). The synergistic effect of terpineol and metronidazole indicated a possible additive effect (fractional inhibitory concentration result is 0.78) with improvement of MIC results for both terpineol and metronidazole. CONCLUSION: This study suggests that terpineol is best to be considered as a lead compound for H. pylori infection treatment and could be a potent inhibitor when combined with metronidazole targeting urease enzyme. Wolters Kluwer - Medknow 2022 2022-09-19 /pmc/articles/PMC9728063/ /pubmed/36506725 http://dx.doi.org/10.4103/jpbs.jpbs_850_21 Text en Copyright: © 2022 Journal of Pharmacy and Bioallied Sciences https://creativecommons.org/licenses/by-nc-sa/4.0/This is an open access journal, and articles are distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as appropriate credit is given and the new creations are licensed under the identical terms.
spellingShingle Original Article
Al Tawalbeh, Deniz
Aburjai, Talal
Al Balas, Qosay
Al Samydai, Ali
In Silico and In Vitro Investigation of Anti Helicobacter Activity of Selected Phytochemicals
title In Silico and In Vitro Investigation of Anti Helicobacter Activity of Selected Phytochemicals
title_full In Silico and In Vitro Investigation of Anti Helicobacter Activity of Selected Phytochemicals
title_fullStr In Silico and In Vitro Investigation of Anti Helicobacter Activity of Selected Phytochemicals
title_full_unstemmed In Silico and In Vitro Investigation of Anti Helicobacter Activity of Selected Phytochemicals
title_short In Silico and In Vitro Investigation of Anti Helicobacter Activity of Selected Phytochemicals
title_sort in silico and in vitro investigation of anti helicobacter activity of selected phytochemicals
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9728063/
https://www.ncbi.nlm.nih.gov/pubmed/36506725
http://dx.doi.org/10.4103/jpbs.jpbs_850_21
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