Related Experiment Video
Updated: Jun 8, 2025
Production and Visualization of Bacterial Spheroplasts and Protoplasts to Characterize Antimicrobial Peptide Localization
Published on: August 11, 2018
Amphiphilic small molecule antimicrobials: From cationic antimicrobial peptides (CAMPs) to mechanism-related,
Jiani Yuan1, Jiaxing Wang2, Xiaoxue Li3
1Department of Neurology, Joint Research Institution of Altitude Health and National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China; Department of Pulmonary and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Precision Medicine Key Laboratory of Sichuan Province & Precision Medicine Research Center, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China.
Abstract:
Bacterial infections are characterized by their rapid and widespread proliferation, leading to significant morbidity. Despite the availability of a variety of antimicrobial drugs, the resistance exhibited by pathogenic microorganisms towards these drugs demonstrates a consistent upward trajectory year after year. This trend can be attributed to the abuse or misuse of antibiotics. Although antimicrobial peptides can avoid the emergence of drug resistance to a certain extent, their clinical application has been hindered by factors such as their high production cost, poor in vivo stability, and potential cytotoxicity. Consequently, there arises an urgent need for the development of novel antimicrobial drugs. Small-molecule amphiphatic antimicrobials have a good prospect for research and development. These peptides hold the potential to address several issues, including the high cost of antimicrobial peptide production, poor in vivo stability, and cytotoxicity. Moreover, they exhibit the capability to overcome bacterial resistance, thereby considerably satisfying market demands and clinical needs. This paper reviews recent research pertaining to small molecule host-defending amphiphatic antimicrobials with cationic amphiphilic structures. It focuses on the design concepts, inherent relationships, drug-like properties, antimicrobial activities, application prospects, and emerging screening methods for novel antimicrobial. This review assumes paramount importance in mitigating the current shortcomings of antimicrobial agents. It also provides potential new ideas and methodologies for the research and development of antimicrobial agents.
Insights
Novel small-molecule antimicrobials offer a promising solution to combat rising antibiotic resistance. These compounds are cost-effective, stable, and less toxic, addressing key limitations of current treatments.
Area of Science:
- Medicinal Chemistry
- Microbiology
- Drug Discovery
Background:
- Bacterial infections cause significant morbidity and mortality.
- Increasing antibiotic resistance, driven by misuse, necessitates new therapeutic strategies.
- Antimicrobial peptides show promise but face challenges like high cost, poor stability, and cytotoxicity.
Purpose of the Study:
- To review recent advancements in small-molecule host-defending amphipathic antimicrobials.
- To explore the design, properties, and applications of these novel agents.
- To highlight emerging screening methods for new antimicrobial drug development.
Main Methods:
- Literature review of recent research on small-molecule amphipathic antimicrobials.
- Analysis of design concepts, structure-activity relationships, and drug-like properties.
- Evaluation of antimicrobial activities, in vivo stability, and cytotoxicity.
Main Results:
- Small-molecule amphipathic antimicrobials demonstrate potential to overcome bacterial resistance.
- These agents offer advantages over traditional antimicrobial peptides in terms of cost, stability, and safety.
- Emerging screening methods are improving the identification of novel antimicrobial candidates.
Conclusions:
- Small-molecule amphipathic antimicrobials represent a viable alternative to address the urgent need for new antibacterial drugs.
- Further research and development in this area can mitigate current shortcomings of antimicrobial agents.
- This review provides insights for future drug discovery and development in antimicrobial therapy.
Related Concept Videos
01:23Antimicrobial Proteins
Interferons
Interferons (IFNs) are proteins produced by lymphocytes, macrophages, and fibroblasts infected with viruses. While IFNs cannot prevent viruses from entering and...
01:27Chemical Agents for Microbial Control
01:28Biological Methods for Microbial Control
01:28Gene Regulation in Microbial Communities: Quorum Sensing
01:27Combined Effects of Drugs: Synergism
Such synergistic combinations...
01:26Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...