De novo design of a pH-triggered self-assembled β-hairpin nanopeptide with the dual biological functions for antibacterial and entrapment
Abstract Background Acid-tolerant enteric pathogens can evade small intestinal acid barriers, colonize and infect the intestinal tract. However, broad-spectrum antibiotics are not the best therapeutic strategy because of the disruption of intestinal flora caused by its indiscriminate antimicrobial a...
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| Format: | Article |
| Language: | English |
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BMC
2021-06-01
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| Series: | Journal of Nanobiotechnology |
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| Online Access: | https://doi.org/10.1186/s12951-021-00927-z |
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| author | Qiuke Li Jinze Li Weikang Yu Zhihua Wang Jiawei Li Xingjun Feng Jiajun Wang Anshan Shan |
| author_facet | Qiuke Li Jinze Li Weikang Yu Zhihua Wang Jiawei Li Xingjun Feng Jiajun Wang Anshan Shan |
| author_sort | Qiuke Li |
| collection | DOAJ |
| description | Abstract Background Acid-tolerant enteric pathogens can evade small intestinal acid barriers, colonize and infect the intestinal tract. However, broad-spectrum antibiotics are not the best therapeutic strategy because of the disruption of intestinal flora caused by its indiscriminate antimicrobial activity against beneficial and harmful bacteria. So that is what inspired us to combine pH regulation with nanotechnology to develop a pH-triggered site-targeted antimicrobial peptide with entrapping function. Results A pH-triggered dual biological functional self-assembled peptide (SAP) was designed according to the features of amino-acid building blocks and the diagonal cation–π interaction principle. The results of characterization experiments showed that changes in pH conditions could trigger microstructural transformation of the nanopeptide from nanospheres to nanofibers. The subsequent antibacterial and toxicity experiments determined that SAP had great antimicrobial activity against Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, and Bacillus cereus above 15.6 μg/mL under acidic conditions by disrupting bacterial membrane integrity, excellent biocompatibility in vitro even at 250 μg/mL and high tolerance in physical environment. Moreover, at peptide concentrations greater than 62.5 μg/mL, SAP showed the entrapment property, which played an important role in phagocytic clearance in infection forces. Meanwhile, the in vivo results revealed that SAP possessed excellent therapeutic effect and good biosafety. Conclusions Our study revealed the antibacterial activity of a short β-hairpin forming self-assembled peptide, and established an innovative design strategy for peptide-based nanomaterials and a new treatment strategy for gastrointestinal bacterial infections. Graphic Abstract |
| first_indexed | 2024-04-14T04:33:53Z |
| format | Article |
| id | doaj.art-58a918c14ab44dfd92a0e6ed54c70767 |
| institution | Directory Open Access Journal |
| issn | 1477-3155 |
| language | English |
| last_indexed | 2024-04-14T04:33:53Z |
| publishDate | 2021-06-01 |
| publisher | BMC |
| record_format | Article |
| series | Journal of Nanobiotechnology |
| spelling | doaj.art-58a918c14ab44dfd92a0e6ed54c707672022-12-22T02:11:57ZengBMCJournal of Nanobiotechnology1477-31552021-06-0119111910.1186/s12951-021-00927-zDe novo design of a pH-triggered self-assembled β-hairpin nanopeptide with the dual biological functions for antibacterial and entrapmentQiuke Li0Jinze Li1Weikang Yu2Zhihua Wang3Jiawei Li4Xingjun Feng5Jiajun Wang6Anshan Shan7Laboratory of Molecular Nutrition and Immunity, The Institute of Animal Nutrition, Northeast Agricultural UniversityLaboratory of Molecular Nutrition and Immunity, The Institute of Animal Nutrition, Northeast Agricultural UniversityLaboratory of Molecular Nutrition and Immunity, The Institute of Animal Nutrition, Northeast Agricultural UniversityLaboratory of Molecular Nutrition and Immunity, The Institute of Animal Nutrition, Northeast Agricultural UniversityLaboratory of Molecular Nutrition and Immunity, The Institute of Animal Nutrition, Northeast Agricultural UniversityLaboratory of Molecular Nutrition and Immunity, The Institute of Animal Nutrition, Northeast Agricultural UniversityLaboratory of Molecular Nutrition and Immunity, The Institute of Animal Nutrition, Northeast Agricultural UniversityLaboratory of Molecular Nutrition and Immunity, The Institute of Animal Nutrition, Northeast Agricultural UniversityAbstract Background Acid-tolerant enteric pathogens can evade small intestinal acid barriers, colonize and infect the intestinal tract. However, broad-spectrum antibiotics are not the best therapeutic strategy because of the disruption of intestinal flora caused by its indiscriminate antimicrobial activity against beneficial and harmful bacteria. So that is what inspired us to combine pH regulation with nanotechnology to develop a pH-triggered site-targeted antimicrobial peptide with entrapping function. Results A pH-triggered dual biological functional self-assembled peptide (SAP) was designed according to the features of amino-acid building blocks and the diagonal cation–π interaction principle. The results of characterization experiments showed that changes in pH conditions could trigger microstructural transformation of the nanopeptide from nanospheres to nanofibers. The subsequent antibacterial and toxicity experiments determined that SAP had great antimicrobial activity against Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, and Bacillus cereus above 15.6 μg/mL under acidic conditions by disrupting bacterial membrane integrity, excellent biocompatibility in vitro even at 250 μg/mL and high tolerance in physical environment. Moreover, at peptide concentrations greater than 62.5 μg/mL, SAP showed the entrapment property, which played an important role in phagocytic clearance in infection forces. Meanwhile, the in vivo results revealed that SAP possessed excellent therapeutic effect and good biosafety. Conclusions Our study revealed the antibacterial activity of a short β-hairpin forming self-assembled peptide, and established an innovative design strategy for peptide-based nanomaterials and a new treatment strategy for gastrointestinal bacterial infections. Graphic Abstracthttps://doi.org/10.1186/s12951-021-00927-zHistidine functionedpH-triggered self-assembled peptideAntimicrobial activityEntrapment propertyβ-hairpin structure |
| spellingShingle | Qiuke Li Jinze Li Weikang Yu Zhihua Wang Jiawei Li Xingjun Feng Jiajun Wang Anshan Shan De novo design of a pH-triggered self-assembled β-hairpin nanopeptide with the dual biological functions for antibacterial and entrapment Journal of Nanobiotechnology Histidine functioned pH-triggered self-assembled peptide Antimicrobial activity Entrapment property β-hairpin structure |
| title | De novo design of a pH-triggered self-assembled β-hairpin nanopeptide with the dual biological functions for antibacterial and entrapment |
| title_full | De novo design of a pH-triggered self-assembled β-hairpin nanopeptide with the dual biological functions for antibacterial and entrapment |
| title_fullStr | De novo design of a pH-triggered self-assembled β-hairpin nanopeptide with the dual biological functions for antibacterial and entrapment |
| title_full_unstemmed | De novo design of a pH-triggered self-assembled β-hairpin nanopeptide with the dual biological functions for antibacterial and entrapment |
| title_short | De novo design of a pH-triggered self-assembled β-hairpin nanopeptide with the dual biological functions for antibacterial and entrapment |
| title_sort | de novo design of a ph triggered self assembled β hairpin nanopeptide with the dual biological functions for antibacterial and entrapment |
| topic | Histidine functioned pH-triggered self-assembled peptide Antimicrobial activity Entrapment property β-hairpin structure |
| url | https://doi.org/10.1186/s12951-021-00927-z |
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