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Updated: Jun 30, 2025
A Platform of Anti-biofilm Assays Suited to the Exploration of Natural Compound Libraries
Published on: December 27, 2016
Evaluation of novel compounds as anti-bacterial or anti-virulence agents
Brankica Filipić1, Dušan Ušjak2, Martina Hrast Rambaher3
1Department of Microbiology and Immunology, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.
Abstract:
Antimicrobial resistance is a global threat, leading to an alarming increase in the prevalence of bacterial infections that can no longer be treated with available antibiotics. The World Health Organization estimates that by 2050 up to 10 million deaths per year could be associated with antimicrobial resistance, which would equal the annual number of cancer deaths worldwide. To overcome this emerging crisis, novel anti-bacterial compounds are urgently needed. There are two possible approaches in the fight against bacterial infections: a) targeting structures within bacterial cells, similar to existing antibiotics; and/or b) targeting virulence factors rather than bacterial growth. Here, for the first time, we provide a comprehensive overview of the key steps in the evaluation of potential new anti-bacterial and/or anti-virulence compounds. The methods described in this review include: a) in silico methods for the evaluation of novel compounds; b) anti-bacterial assays (MIC, MBC, Time-kill); b) anti-virulence assays (anti-biofilm, anti-quorum sensing, anti-adhesion); and c) evaluation of safety aspects (cytotoxicity assay and Ames test). Overall, we provide a detailed description of the methods that are an essential tool for chemists, computational chemists, microbiologists, and toxicologists in the evaluation of potential novel antimicrobial compounds. These methods are cost-effective and have high predictive value. They are widely used in preclinical studies to identify new molecular candidates, for further investigation in animal and human trials.
Insights
Antimicrobial resistance (AMR) is a growing global crisis. This review outlines essential methods for evaluating novel antibacterial and anti-virulence compounds to combat resistant bacterial infections.
Area of Science:
- Microbiology
- Pharmacology
- Computational Chemistry
Background:
- Antimicrobial resistance (AMR) poses a significant global health threat, with projections of 10 million annual deaths by 2050.
- The increasing prevalence of untreatable bacterial infections necessitates the urgent development of novel antimicrobial and anti-virulence compounds.
- Current strategies include targeting bacterial structures or virulence factors, requiring robust evaluation methods.
Purpose of the Study:
- To provide a comprehensive overview of key methods for evaluating novel antibacterial and anti-virulence compounds.
- To detail cost-effective, high-predictive-value preclinical evaluation techniques.
- To guide chemists, computational chemists, microbiologists, and toxicologists in identifying new antimicrobial candidates.
Main Methods:
- In silico computational methods for initial compound screening.
- Standard antimicrobial assays: Minimum Inhibitory Concentration (MIC), Minimum Bactericidal Concentration (MBC), and Time-kill assays.
- Anti-virulence assays including anti-biofilm, anti-quorum sensing, and anti-adhesion tests, alongside safety evaluations (cytotoxicity and Ames test).
Main Results:
- The review consolidates a range of essential preclinical evaluation methods for potential antimicrobial agents.
- The described methods offer a cost-effective approach with high predictive value for identifying promising drug candidates.
- These techniques are crucial for advancing compounds from discovery to clinical trials.
Conclusions:
- A standardized, comprehensive evaluation framework is critical for developing new antimicrobial and anti-virulence therapies.
- The integration of in silico, antimicrobial, anti-virulence, and safety assays accelerates the identification of effective treatments.
- These methods are indispensable tools in the global fight against antimicrobial resistance.
