Discovery of Melittin as Triple-Action Agent: Broad-Spectrum Antibacterial, Anti-Biofilm, and Potential Anti-Quorum Sensing Activities
The development of antibiotic-resistant microorganisms is a major global health concern. Recently, there has been an increasing interest in antimicrobial peptides as a therapeutic option. This study aimed to evaluate the triple-action (broad-spectrum antibacterial, anti-biofilm, and anti-quorum sens...
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| Format: | Article |
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MDPI AG
2024-01-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/29/3/558 |
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| author | Hongyan Yang Rong Ma Jiarou Chen Qian Xie Wenhui Luo Pinghua Sun Zheng Liu Jialiang Guo |
| author_facet | Hongyan Yang Rong Ma Jiarou Chen Qian Xie Wenhui Luo Pinghua Sun Zheng Liu Jialiang Guo |
| author_sort | Hongyan Yang |
| collection | DOAJ |
| description | The development of antibiotic-resistant microorganisms is a major global health concern. Recently, there has been an increasing interest in antimicrobial peptides as a therapeutic option. This study aimed to evaluate the triple-action (broad-spectrum antibacterial, anti-biofilm, and anti-quorum sensing activities) of melittin, a membrane-active peptide present in bee venom. The minimum inhibitory concentration and minimum bactericidal concentration of the melittin were determined using the microdilution method and agar plate counting. Growth curve analysis revealed that melittin showed a concentration-dependent antibacterial activity. Scanning electron microscope analysis revealed that melittin treatment altered the morphology. Confocal laser scanning microscope revealed that melittin increased the membrane permeability and intracellular ROS generation in bacteria, all of which contribute to bacterial cell death. In addition, the crystal violet (CV) assay was used to test the anti-biofilm activity. The CV assay demonstrated that melittin inhibited biofilm formation and eradicated mature biofilms. Biofilm formation mediated by quorum sensing (QS) plays a major role in this regard, so molecular docking and molecular dynamics analysis confirmed that melittin interacts with LasR receptors through hydrogen bonds, and further evaluates the anti-QS activity of melittin through the production of virulence factors (pyocyanin, elastase, and rhamnolipid), exopolysaccharides secretion, and bacterial motility, that may be the key to inhibiting the biofilm formation mechanism. The present findings highlight the promising role of melittin as a broad-spectrum antibacterial, anti-biofilm agent, and potential QS inhibitor, providing a new perspective and theoretical basis for the development of alternative antibiotics. |
| first_indexed | 2024-03-08T03:52:56Z |
| format | Article |
| id | doaj.art-a261bead1f5640eaa4d100ff4cd1113d |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-08T03:52:56Z |
| publishDate | 2024-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-a261bead1f5640eaa4d100ff4cd1113d2024-02-09T15:18:36ZengMDPI AGMolecules1420-30492024-01-0129355810.3390/molecules29030558Discovery of Melittin as Triple-Action Agent: Broad-Spectrum Antibacterial, Anti-Biofilm, and Potential Anti-Quorum Sensing ActivitiesHongyan Yang0Rong Ma1Jiarou Chen2Qian Xie3Wenhui Luo4Pinghua Sun5Zheng Liu6Jialiang Guo7School of Medicine, Foshan University, Foshan 528000, ChinaSchool of Medicine, Foshan University, Foshan 528000, ChinaSchool of Medicine, Foshan University, Foshan 528000, ChinaSchool of Medicine, Foshan University, Foshan 528000, ChinaGuangdong Yifang Pharmaceutical Co., Ltd., Foshan 528244, ChinaCollege of Pharmacy, Jinan University, Guangzhou 510632, ChinaSchool of Medicine, Foshan University, Foshan 528000, ChinaSchool of Medicine, Foshan University, Foshan 528000, ChinaThe development of antibiotic-resistant microorganisms is a major global health concern. Recently, there has been an increasing interest in antimicrobial peptides as a therapeutic option. This study aimed to evaluate the triple-action (broad-spectrum antibacterial, anti-biofilm, and anti-quorum sensing activities) of melittin, a membrane-active peptide present in bee venom. The minimum inhibitory concentration and minimum bactericidal concentration of the melittin were determined using the microdilution method and agar plate counting. Growth curve analysis revealed that melittin showed a concentration-dependent antibacterial activity. Scanning electron microscope analysis revealed that melittin treatment altered the morphology. Confocal laser scanning microscope revealed that melittin increased the membrane permeability and intracellular ROS generation in bacteria, all of which contribute to bacterial cell death. In addition, the crystal violet (CV) assay was used to test the anti-biofilm activity. The CV assay demonstrated that melittin inhibited biofilm formation and eradicated mature biofilms. Biofilm formation mediated by quorum sensing (QS) plays a major role in this regard, so molecular docking and molecular dynamics analysis confirmed that melittin interacts with LasR receptors through hydrogen bonds, and further evaluates the anti-QS activity of melittin through the production of virulence factors (pyocyanin, elastase, and rhamnolipid), exopolysaccharides secretion, and bacterial motility, that may be the key to inhibiting the biofilm formation mechanism. The present findings highlight the promising role of melittin as a broad-spectrum antibacterial, anti-biofilm agent, and potential QS inhibitor, providing a new perspective and theoretical basis for the development of alternative antibiotics.https://www.mdpi.com/1420-3049/29/3/558antimicrobial peptidesmelittinantibacterialanti-biofilmanti-quorum sensing |
| spellingShingle | Hongyan Yang Rong Ma Jiarou Chen Qian Xie Wenhui Luo Pinghua Sun Zheng Liu Jialiang Guo Discovery of Melittin as Triple-Action Agent: Broad-Spectrum Antibacterial, Anti-Biofilm, and Potential Anti-Quorum Sensing Activities Molecules antimicrobial peptides melittin antibacterial anti-biofilm anti-quorum sensing |
| title | Discovery of Melittin as Triple-Action Agent: Broad-Spectrum Antibacterial, Anti-Biofilm, and Potential Anti-Quorum Sensing Activities |
| title_full | Discovery of Melittin as Triple-Action Agent: Broad-Spectrum Antibacterial, Anti-Biofilm, and Potential Anti-Quorum Sensing Activities |
| title_fullStr | Discovery of Melittin as Triple-Action Agent: Broad-Spectrum Antibacterial, Anti-Biofilm, and Potential Anti-Quorum Sensing Activities |
| title_full_unstemmed | Discovery of Melittin as Triple-Action Agent: Broad-Spectrum Antibacterial, Anti-Biofilm, and Potential Anti-Quorum Sensing Activities |
| title_short | Discovery of Melittin as Triple-Action Agent: Broad-Spectrum Antibacterial, Anti-Biofilm, and Potential Anti-Quorum Sensing Activities |
| title_sort | discovery of melittin as triple action agent broad spectrum antibacterial anti biofilm and potential anti quorum sensing activities |
| topic | antimicrobial peptides melittin antibacterial anti-biofilm anti-quorum sensing |
| url | https://www.mdpi.com/1420-3049/29/3/558 |
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