Antibacterial activity of isopropoxy benzene guanidine against Riemerella anatipestifer
Introduction:Riemerella anatipestifer (R. anatipestifer) is an important pathogen in waterfowl, leading to substantial economic losses. In recent years, there has been a notable escalation in the drug resistance rate of R. anatipestifer. Consequently, there is an imperative need to expedite the deve...
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2024-02-01
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| Series: | Frontiers in Pharmacology |
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| Online Access: | https://www.frontiersin.org/articles/10.3389/fphar.2024.1347250/full |
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| author | Yixing Lu Yixing Lu Weimei Qiao Weimei Qiao Yaqian Xue Yaqian Xue Xiaoxin Hong Xiaoxin Hong Yuhang Jin Yuhang Jin Jie Li Jie Li Xianfeng Peng Dongping Zeng Dongping Zeng Zhenling Zeng Zhenling Zeng |
| author_facet | Yixing Lu Yixing Lu Weimei Qiao Weimei Qiao Yaqian Xue Yaqian Xue Xiaoxin Hong Xiaoxin Hong Yuhang Jin Yuhang Jin Jie Li Jie Li Xianfeng Peng Dongping Zeng Dongping Zeng Zhenling Zeng Zhenling Zeng |
| author_sort | Yixing Lu |
| collection | DOAJ |
| description | Introduction:Riemerella anatipestifer (R. anatipestifer) is an important pathogen in waterfowl, leading to substantial economic losses. In recent years, there has been a notable escalation in the drug resistance rate of R. anatipestifer. Consequently, there is an imperative need to expedite the development of novel antibacterial medications to effectively manage the infection caused by R. anatipestifer.Methods: This study investigated the in vitro and in vivo antibacterial activities of a novel substituted benzene guanidine analog, namely, isopropoxy benzene guanidine (IBG), against R. anatipestifer by using the microdilution method, time-killing curve, and a pericarditis model. The possible mechanisms of these activities were explored.Results and Discussion: The minimal inhibitory concentration (MIC) range of IBG for R. anatipestifer was 0.5–2 μg/mL. Time-killing curves showed a concentration-dependent antibacterial effect. IBG alone or in combination with gentamicin significantly reduced the bacterial load of R. anatipestifer in the pericarditis model. Serial-passage mutagenicity assays showed a low probability for developing IBG resistance. Mechanistic studies suggested that IBG induced membrane damage by binding to phosphatidylglycerol and cardiolipin, leading to an imbalance in membrane potential and the transmembrane proton gradient, as well as the decreased of intracellular adenosine triphosphate. In summary, IBG is a potential antibacterial for controlling R. anatipestifer infections. |
| first_indexed | 2024-03-08T08:07:08Z |
| format | Article |
| id | doaj.art-069305981c264f54bab9e8a7a2946a36 |
| institution | Directory Open Access Journal |
| issn | 1663-9812 |
| language | English |
| last_indexed | 2024-03-08T08:07:08Z |
| publishDate | 2024-02-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Pharmacology |
| spelling | doaj.art-069305981c264f54bab9e8a7a2946a362024-02-02T10:05:18ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122024-02-011510.3389/fphar.2024.13472501347250Antibacterial activity of isopropoxy benzene guanidine against Riemerella anatipestiferYixing Lu0Yixing Lu1Weimei Qiao2Weimei Qiao3Yaqian Xue4Yaqian Xue5Xiaoxin Hong6Xiaoxin Hong7Yuhang Jin8Yuhang Jin9Jie Li10Jie Li11Xianfeng Peng12Dongping Zeng13Dongping Zeng14Zhenling Zeng15Zhenling Zeng16Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangzhou, ChinaGuangzhou Insighter Biotechnology Co, Ltd., Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangzhou, ChinaIntroduction:Riemerella anatipestifer (R. anatipestifer) is an important pathogen in waterfowl, leading to substantial economic losses. In recent years, there has been a notable escalation in the drug resistance rate of R. anatipestifer. Consequently, there is an imperative need to expedite the development of novel antibacterial medications to effectively manage the infection caused by R. anatipestifer.Methods: This study investigated the in vitro and in vivo antibacterial activities of a novel substituted benzene guanidine analog, namely, isopropoxy benzene guanidine (IBG), against R. anatipestifer by using the microdilution method, time-killing curve, and a pericarditis model. The possible mechanisms of these activities were explored.Results and Discussion: The minimal inhibitory concentration (MIC) range of IBG for R. anatipestifer was 0.5–2 μg/mL. Time-killing curves showed a concentration-dependent antibacterial effect. IBG alone or in combination with gentamicin significantly reduced the bacterial load of R. anatipestifer in the pericarditis model. Serial-passage mutagenicity assays showed a low probability for developing IBG resistance. Mechanistic studies suggested that IBG induced membrane damage by binding to phosphatidylglycerol and cardiolipin, leading to an imbalance in membrane potential and the transmembrane proton gradient, as well as the decreased of intracellular adenosine triphosphate. In summary, IBG is a potential antibacterial for controlling R. anatipestifer infections.https://www.frontiersin.org/articles/10.3389/fphar.2024.1347250/fullisopropoxy benzene guanidineRiemerilla anatipestiferantibacterial activitymembrane damageresistance |
| spellingShingle | Yixing Lu Yixing Lu Weimei Qiao Weimei Qiao Yaqian Xue Yaqian Xue Xiaoxin Hong Xiaoxin Hong Yuhang Jin Yuhang Jin Jie Li Jie Li Xianfeng Peng Dongping Zeng Dongping Zeng Zhenling Zeng Zhenling Zeng Antibacterial activity of isopropoxy benzene guanidine against Riemerella anatipestifer Frontiers in Pharmacology isopropoxy benzene guanidine Riemerilla anatipestifer antibacterial activity membrane damage resistance |
| title | Antibacterial activity of isopropoxy benzene guanidine against Riemerella anatipestifer |
| title_full | Antibacterial activity of isopropoxy benzene guanidine against Riemerella anatipestifer |
| title_fullStr | Antibacterial activity of isopropoxy benzene guanidine against Riemerella anatipestifer |
| title_full_unstemmed | Antibacterial activity of isopropoxy benzene guanidine against Riemerella anatipestifer |
| title_short | Antibacterial activity of isopropoxy benzene guanidine against Riemerella anatipestifer |
| title_sort | antibacterial activity of isopropoxy benzene guanidine against riemerella anatipestifer |
| topic | isopropoxy benzene guanidine Riemerilla anatipestifer antibacterial activity membrane damage resistance |
| url | https://www.frontiersin.org/articles/10.3389/fphar.2024.1347250/full |
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