Harnessing advanced computational approaches to design novel antimicrobial peptides against intracellular bacterial infections

Intracellular bacterial infections pose a significant challenge to current therapeutic strategies due to the limited penetration of antibiotics through host cell membranes. This study presents a novel computational framework for efficiently screening candidate peptides against these infections. The...

Full description

Saved in:
Bibliographic Details
Main Authors: Yanpeng Fang, Duoyang Fan, Bin Feng, Yingli Zhu, Ruyan Xie, Xiaorong Tan, Qianhui Liu, Jie Dong, Wenbin Zeng
Format: Article
Language:English
Published: KeAi Communications Co., Ltd. 2025-08-01
Series:Bioactive Materials
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S2452199X25001550
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1849693909775548416
author Yanpeng Fang
Duoyang Fan
Bin Feng
Yingli Zhu
Ruyan Xie
Xiaorong Tan
Qianhui Liu
Jie Dong
Wenbin Zeng
author_facet Yanpeng Fang
Duoyang Fan
Bin Feng
Yingli Zhu
Ruyan Xie
Xiaorong Tan
Qianhui Liu
Jie Dong
Wenbin Zeng
author_sort Yanpeng Fang
collection DOAJ
description Intracellular bacterial infections pose a significant challenge to current therapeutic strategies due to the limited penetration of antibiotics through host cell membranes. This study presents a novel computational framework for efficiently screening candidate peptides against these infections. The proposed strategy comprehensively evaluates the essential properties for the clinical application of candidate peptides, including antimicrobial activity, permeation efficiency, and biocompatibility, while also taking into account the speed and reliability of the screening process. A combination of multiple AI-based activity prediction models allows for a thorough assessment of sequences in the cell-penetrating peptides (CPPs) database and quickly identifies candidate peptides with target properties. On this basis, the CPP microscopic dynamics research system was constructed. Exploration of the mechanism of action at the atomic level provides strong support for the discovery of promising candidate peptides. Promising candidates are subsequently validated through in vitro and in vivo experiments. Finally, Crot-1 was rapidly identified from the CPPsite 2.0 database. Crot-1 effectively eradicated intracellular MRSA, demonstrating significantly greater efficacy than vancomycin. Moreover, it exhibited no apparent cytotoxicity to host cells, highlighting its potential for clinical application. This work offers a promising new avenue for developing novel antimicrobial materials to combat intracellular bacterial infections.
format Article
id doaj-art-0a2128eda8294b72b026654ca3cc935a
institution DOAJ
issn 2452-199X
language English
publishDate 2025-08-01
publisher KeAi Communications Co., Ltd.
record_format Article
series Bioactive Materials
spelling doaj-art-0a2128eda8294b72b026654ca3cc935a2025-08-20T03:20:15ZengKeAi Communications Co., Ltd.Bioactive Materials2452-199X2025-08-015051052410.1016/j.bioactmat.2025.04.016Harnessing advanced computational approaches to design novel antimicrobial peptides against intracellular bacterial infectionsYanpeng Fang0Duoyang Fan1Bin Feng2Yingli Zhu3Ruyan Xie4Xiaorong Tan5Qianhui Liu6Jie Dong7Wenbin Zeng8Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410083, PR China; Hunan Key Laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases, Changsha 410078, PR ChinaXiangya School of Pharmaceutical Sciences, Central South University, Changsha 410083, PR China; Hunan Key Laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases, Changsha 410078, PR ChinaXiangya School of Pharmaceutical Sciences, Central South University, Changsha 410083, PR China; Hunan Key Laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases, Changsha 410078, PR ChinaXiangya School of Pharmaceutical Sciences, Central South University, Changsha 410083, PR China; Hunan Key Laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases, Changsha 410078, PR ChinaXiangya School of Pharmaceutical Sciences, Central South University, Changsha 410083, PR China; Hunan Key Laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases, Changsha 410078, PR ChinaXiangya School of Pharmaceutical Sciences, Central South University, Changsha 410083, PR China; Hunan Key Laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases, Changsha 410078, PR ChinaXiangya School of Pharmaceutical Sciences, Central South University, Changsha 410083, PR China; Hunan Key Laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases, Changsha 410078, PR ChinaXiangya School of Pharmaceutical Sciences, Central South University, Changsha 410083, PR China; Hunan Key Laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases, Changsha 410078, PR China; Corresponding author. Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410083, PR China.Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410083, PR China; Hunan Key Laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases, Changsha 410078, PR China; Corresponding author. Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410083, PR China.Intracellular bacterial infections pose a significant challenge to current therapeutic strategies due to the limited penetration of antibiotics through host cell membranes. This study presents a novel computational framework for efficiently screening candidate peptides against these infections. The proposed strategy comprehensively evaluates the essential properties for the clinical application of candidate peptides, including antimicrobial activity, permeation efficiency, and biocompatibility, while also taking into account the speed and reliability of the screening process. A combination of multiple AI-based activity prediction models allows for a thorough assessment of sequences in the cell-penetrating peptides (CPPs) database and quickly identifies candidate peptides with target properties. On this basis, the CPP microscopic dynamics research system was constructed. Exploration of the mechanism of action at the atomic level provides strong support for the discovery of promising candidate peptides. Promising candidates are subsequently validated through in vitro and in vivo experiments. Finally, Crot-1 was rapidly identified from the CPPsite 2.0 database. Crot-1 effectively eradicated intracellular MRSA, demonstrating significantly greater efficacy than vancomycin. Moreover, it exhibited no apparent cytotoxicity to host cells, highlighting its potential for clinical application. This work offers a promising new avenue for developing novel antimicrobial materials to combat intracellular bacterial infections.http://www.sciencedirect.com/science/article/pii/S2452199X25001550Intracellular bacterial infectionArtificial intelligenceCell-penetrating peptideMolecular dynamics simulationAntimicrobial peptide
spellingShingle Yanpeng Fang
Duoyang Fan
Bin Feng
Yingli Zhu
Ruyan Xie
Xiaorong Tan
Qianhui Liu
Jie Dong
Wenbin Zeng
Harnessing advanced computational approaches to design novel antimicrobial peptides against intracellular bacterial infections
Bioactive Materials
Intracellular bacterial infection
Artificial intelligence
Cell-penetrating peptide
Molecular dynamics simulation
Antimicrobial peptide
title Harnessing advanced computational approaches to design novel antimicrobial peptides against intracellular bacterial infections
title_full Harnessing advanced computational approaches to design novel antimicrobial peptides against intracellular bacterial infections
title_fullStr Harnessing advanced computational approaches to design novel antimicrobial peptides against intracellular bacterial infections
title_full_unstemmed Harnessing advanced computational approaches to design novel antimicrobial peptides against intracellular bacterial infections
title_short Harnessing advanced computational approaches to design novel antimicrobial peptides against intracellular bacterial infections
title_sort harnessing advanced computational approaches to design novel antimicrobial peptides against intracellular bacterial infections
topic Intracellular bacterial infection
Artificial intelligence
Cell-penetrating peptide
Molecular dynamics simulation
Antimicrobial peptide
url http://www.sciencedirect.com/science/article/pii/S2452199X25001550
work_keys_str_mv AT yanpengfang harnessingadvancedcomputationalapproachestodesignnovelantimicrobialpeptidesagainstintracellularbacterialinfections
AT duoyangfan harnessingadvancedcomputationalapproachestodesignnovelantimicrobialpeptidesagainstintracellularbacterialinfections
AT binfeng harnessingadvancedcomputationalapproachestodesignnovelantimicrobialpeptidesagainstintracellularbacterialinfections
AT yinglizhu harnessingadvancedcomputationalapproachestodesignnovelantimicrobialpeptidesagainstintracellularbacterialinfections
AT ruyanxie harnessingadvancedcomputationalapproachestodesignnovelantimicrobialpeptidesagainstintracellularbacterialinfections
AT xiaorongtan harnessingadvancedcomputationalapproachestodesignnovelantimicrobialpeptidesagainstintracellularbacterialinfections
AT qianhuiliu harnessingadvancedcomputationalapproachestodesignnovelantimicrobialpeptidesagainstintracellularbacterialinfections
AT jiedong harnessingadvancedcomputationalapproachestodesignnovelantimicrobialpeptidesagainstintracellularbacterialinfections
AT wenbinzeng harnessingadvancedcomputationalapproachestodesignnovelantimicrobialpeptidesagainstintracellularbacterialinfections