Abstract
Antimicrobial lipids such as fatty acids and monoglycerides are promising antibacterial agents that destabilize bacterial cell membranes, causing a wide range of direct and indirect inhibitory effects. The goal of this review is to introduce the latest experimental approaches for characterizing how antimicrobial lipids destabilize phospholipid membranes within the broader scope of introducing current knowledge about the biological activities of antimicrobial lipids, testing strategies, and applications for treating bacterial infections. To this end, a general background on antimicrobial lipids, including structural classification, is provided along with a detailed description of their targeting spectrum and currently understood antibacterial mechanisms. Building on this knowledge, different experimental approaches to characterize antimicrobial lipids are presented, including cell-based biological and model membrane-based biophysical measurement techniques. Particular emphasis is placed on drawing out how biological and biophysical approaches complement one another and can yield mechanistic insights into how the physicochemical properties of antimicrobial lipids influence molecular self-assembly and concentration-dependent interactions with model phospholipid and bacterial cell membranes. Examples of possible therapeutic applications are briefly introduced to highlight the potential significance of antimicrobial lipids for human health and medicine, and to motivate the importance of employing orthogonal measurement strategies to characterize the activity profile of antimicrobial lipids.
Highlights
Molecular design principles underpin the structure and function of biological assemblies such as cells, and amphiphilic molecules drive the spontaneous self-assembly of key architectural elements like phospholipid membranes [1,2,3]
Linolenic acid and 18-carbon long analogues were prepared in liposomal formulations, and, out of the tested species, it was confirmed that LipoLLA had the most potent antibacterial activity against H. pylori and showed complete killing of the bacterium at 200 μg/mL based on causing an increase in bacterial membrane permeability
Over the past few decades, significant progress has been made towards understanding the relative potency and spectrum of antibacterial activity for different classes of antimicrobial lipids, in turn identifying promising drug candidates through biological investigations
Summary
Molecular design principles underpin the structure and function of biological assemblies such as cells, and amphiphilic molecules drive the spontaneous self-assembly of key architectural elements like phospholipid membranes [1,2,3]. The major findings obtained by each experimental approach are critically summarized, and supplemented by discussion about how biological and biophysical approaches can be integrated to better understand how the physicochemical properties of antimicrobial lipids influence molecular self-assembly and concentration-dependent interactions with model phospholipid and bacterial cell membranes. It is described how antimicrobial lipids in free form and nanostructured assemblies can be employed for therapeutic applications, including when administered via systemic and topical administration routes. The insights presented in this review underscore the utility of employing orthogonal measurement strategies to characterize the activity profile of antimicrobial lipids
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