Isopropoxy Benzene Guanidine Kills Staphylococcus aureus Without Detectable Resistance
Serious infections caused by multidrug-resistant Staphylococcus aureus clearly urge the development of new antimicrobial agents. Drug repositioning has emerged as an alternative approach that enables us to rapidly identify effective drugs. We first reported a guanidine compound, isopropoxy benzene g...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2021-02-01
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| Series: | Frontiers in Microbiology |
| Subjects: | |
| Online Access: | https://www.frontiersin.org/articles/10.3389/fmicb.2021.633467/full |
| _version_ | 1818664251203518464 |
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| author | Xiufeng Zhang Xiufeng Zhang Wenguang Xiong Wenguang Xiong Xianfeng Peng Yixing Lu Yixing Lu Jie Hao Jie Hao Zonghua Qin Zhenling Zeng Zhenling Zeng |
| author_facet | Xiufeng Zhang Xiufeng Zhang Wenguang Xiong Wenguang Xiong Xianfeng Peng Yixing Lu Yixing Lu Jie Hao Jie Hao Zonghua Qin Zhenling Zeng Zhenling Zeng |
| author_sort | Xiufeng Zhang |
| collection | DOAJ |
| description | Serious infections caused by multidrug-resistant Staphylococcus aureus clearly urge the development of new antimicrobial agents. Drug repositioning has emerged as an alternative approach that enables us to rapidly identify effective drugs. We first reported a guanidine compound, isopropoxy benzene guanidine, had potent antibacterial activity against S. aureus. Unlike conventional antibiotics, repeated use of isopropoxy benzene guanidine had a lower probability of resistance section. We found that isopropoxy benzene guanidine triggered membrane damage by disrupting the cell membrane potential and cytoplasmic membrane integrity. Furthermore, we demonstrated that isopropoxy benzene guanidine is capable of treating invasive MRSA infections in vivo studies. These findings provided strong evidence that isopropoxy benzene guanidine represents a new chemical lead for novel antibacterial agent against multidrug-resistant S. aureus infections. |
| first_indexed | 2024-12-17T05:29:46Z |
| format | Article |
| id | doaj.art-faf1828fa9144726a25fbc03a0dd65c3 |
| institution | Directory Open Access Journal |
| issn | 1664-302X |
| language | English |
| last_indexed | 2024-12-17T05:29:46Z |
| publishDate | 2021-02-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Microbiology |
| spelling | doaj.art-faf1828fa9144726a25fbc03a0dd65c32022-12-21T22:01:45ZengFrontiers Media S.A.Frontiers in Microbiology1664-302X2021-02-011210.3389/fmicb.2021.633467633467Isopropoxy Benzene Guanidine Kills Staphylococcus aureus Without Detectable ResistanceXiufeng Zhang0Xiufeng Zhang1Wenguang Xiong2Wenguang Xiong3Xianfeng Peng4Yixing Lu5Yixing Lu6Jie Hao7Jie Hao8Zonghua Qin9Zhenling Zeng10Zhenling Zeng11National Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaGuangdong Laboratory for Lingnan Modern Agriculture, Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaGuangdong Laboratory for Lingnan Modern Agriculture, Guangzhou, ChinaGuangzhou Insighter Biotechnology Co., Ltd., Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaGuangdong Laboratory for Lingnan Modern Agriculture, Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaGuangdong Laboratory for Lingnan Modern Agriculture, Guangzhou, ChinaGuangzhou Insighter Biotechnology Co., Ltd., Guangzhou, ChinaNational Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaGuangdong Laboratory for Lingnan Modern Agriculture, Guangzhou, ChinaSerious infections caused by multidrug-resistant Staphylococcus aureus clearly urge the development of new antimicrobial agents. Drug repositioning has emerged as an alternative approach that enables us to rapidly identify effective drugs. We first reported a guanidine compound, isopropoxy benzene guanidine, had potent antibacterial activity against S. aureus. Unlike conventional antibiotics, repeated use of isopropoxy benzene guanidine had a lower probability of resistance section. We found that isopropoxy benzene guanidine triggered membrane damage by disrupting the cell membrane potential and cytoplasmic membrane integrity. Furthermore, we demonstrated that isopropoxy benzene guanidine is capable of treating invasive MRSA infections in vivo studies. These findings provided strong evidence that isopropoxy benzene guanidine represents a new chemical lead for novel antibacterial agent against multidrug-resistant S. aureus infections.https://www.frontiersin.org/articles/10.3389/fmicb.2021.633467/fullisopropoxy benzene guanidinemultidrug-resistant Staphylococcus aureusmembrane damageresistance sectiontranscriptome |
| spellingShingle | Xiufeng Zhang Xiufeng Zhang Wenguang Xiong Wenguang Xiong Xianfeng Peng Yixing Lu Yixing Lu Jie Hao Jie Hao Zonghua Qin Zhenling Zeng Zhenling Zeng Isopropoxy Benzene Guanidine Kills Staphylococcus aureus Without Detectable Resistance Frontiers in Microbiology isopropoxy benzene guanidine multidrug-resistant Staphylococcus aureus membrane damage resistance section transcriptome |
| title | Isopropoxy Benzene Guanidine Kills Staphylococcus aureus Without Detectable Resistance |
| title_full | Isopropoxy Benzene Guanidine Kills Staphylococcus aureus Without Detectable Resistance |
| title_fullStr | Isopropoxy Benzene Guanidine Kills Staphylococcus aureus Without Detectable Resistance |
| title_full_unstemmed | Isopropoxy Benzene Guanidine Kills Staphylococcus aureus Without Detectable Resistance |
| title_short | Isopropoxy Benzene Guanidine Kills Staphylococcus aureus Without Detectable Resistance |
| title_sort | isopropoxy benzene guanidine kills staphylococcus aureus without detectable resistance |
| topic | isopropoxy benzene guanidine multidrug-resistant Staphylococcus aureus membrane damage resistance section transcriptome |
| url | https://www.frontiersin.org/articles/10.3389/fmicb.2021.633467/full |
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