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Membranes
Special Issues
Recent Advances in Biomembrane Models for Studying Interactions with Bio-/Molecules
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Recent Advances in Biomembrane Models for Studying Interactions with Bio-/Molecules

A special issue of Membranes (ISSN 2077-0375). This special issue belongs to the section "Biological Membranes".

Deadline for manuscript submissions: 31 October 2025 | Viewed by 9785

Special Issue Editors

Dr. Jadwiga Maniewska

E-Mail Website
Guest Editor
Department of Medicinal Chemistry, Faculty of Pharmacy, Wroclaw Medical University, Borowska 211, 50-556 Wroclaw, Poland
Interests: medicinal chemistry; lipid bilayers; model membranes; cancer chemoprevention; new drug-like compounds—their design and physicochemical properties; together with their interactions with model lipid membranes
Special Issues, Collections and Topics in MDPI journals
Dr. Katarzyna Gębczak

E-Mail Website
Guest Editor
Division of Basic Medical Sciences, Faculty of Pharmacy, Wroclaw Medical University, Borowska 211, 50-556 Wroclaw, Poland
Interests: COX-1/COX-2 inhibition; anticancer compounds; apoptosis; cancer chemoprevention; antioxidant compounds

Special Issue Information

Dear Colleagues,

Biological membrane models such as liposomes, phospholipid bilayers, Langmuir monolayers, etc. are used to model and study the interactions of biological membranes with various biomolecules.

The interaction of bioactive compounds with biological membranes is a very important process. The pharmacological effects of medicines (especially when taken orally), as well as their distribution and metabolism are often dependent on their penetration through the biological membranes. Moreover, many enzymes, which may be membrane-bound proteins, are drug targets, therefore the pharmacological actions of different drugs may be a consequence of their direct interactions with proteins. Furthermore, there are also reports that some alternative mechanisms of action, such as the chemoprevention of bioactive compounds, e.g., non-steroidal anti-inflammatory drugs (NSAIDs) or polyphenols, may also be related to their interactions with the biological membranes and specific membrane proteins. Changes induced in the lipid phase, such as an alteration of membrane curvature and phase behavior, may consequently also indirectly modify a conformation of membrane proteins. An interesting type of molecular interaction is also the interaction of surfactants with proteins, as well as with the membranes themselves; this is because some types of surfactants can also be used in the design of new types of drugs. For these reasons, the investigation of biomolecule–membrane interactions is essential for better understanding the molecular mechanisms of their action.

This Special Issue aims to investigate all types of bioactive compound–membrane interactions. We are pleased to invite you to submit your original research articles and reviews. Research areas may include (but are not limited to) the following topics relating to interactions of bioactive compounds:

  • cellular membranes, and their influence on membrane structure, function, biomolecular organization and dynamics, fluidity, and composition,
  • model membranes (eg. liposomes, phospholipid bilayers, Langmuir monolayers),
  • membrane proteins (eg. COX, P-gp),
  • membrane traffic, receptors, and channels.

Both molecular modeling and simulation as well as various biophysical (e.g., differential scanning calorimetry, fluorescence spectroscopy, infrared spectroscopy, circular dichroism, patch clamp) and biological techniques can be used as research methods.

We look forward to receiving your contributions.

Dr. Jadwiga Maniewska
Dr. Katarzyna Gębczak
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Membranes is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2200 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • drug–membrane interaction
  • polyphenols–membrane interaction
  • bioactive compounds
  • model lipid membranes
  • membrane proteins
  • membrane phospholipid composition
  • membrane channels
  • surfactants
  • new drug targets
  • cancer multidrug resistance
  • cancer chemoprevention
  • anticancer compounds

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Published Papers (5 papers)

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Research

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26 pages, 10330 KiB  
Article
Anti-Inflammatory Properties of Novel 1,2-Benzothiazine Derivatives and Their Interaction with Phospholipid Model Membranes
by Berenika M. Szczęśniak-Sięga, Jadwiga Maniewska, Benita Wiatrak, Tomasz Janek, Paulina Nowotarska and Żaneta Czyżnikowska
Membranes 2024, 14(12), 274; https://doi.org/10.3390/membranes14120274 - 18 Dec 2024
Viewed by 1029
Abstract
The design of novel anti-inflammatory drugs remains a critical area of research in the development of effective treatments for inflammatory diseases. In this study, a series of 1,2-benzothiazine was evaluated through a multifaceted approach. In particular, we investigated the potential interactions of the [...] Read more.
The design of novel anti-inflammatory drugs remains a critical area of research in the development of effective treatments for inflammatory diseases. In this study, a series of 1,2-benzothiazine was evaluated through a multifaceted approach. In particular, we investigated the potential interactions of the potential drugs with lipid bilayers, an important consideration for membrane permeability and overall pharmacokinetics. In addition, we evaluated their ability to inhibit cyclooxygenase 1 and cyclooxygenase 2 activity and selectivity using both a cyclooxygenase inhibition assay and molecular docking simulations. To evaluate their therapeutic potential, we performed in vitro assays to measure cytokine mRNA expression in inflamed cells. The antioxidant activity was evaluated using both in vitro assays, such as 2,2-diphenyl-1-picrylhydrazyl and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid scavenging, to determine the compounds’ capacity to neutralize free radicals and reduce oxidative stress. Theoretical calculations, including density functional theory, were used to predict the reactivity profiles of the compounds. Full article
(This article belongs to the Special Issue Recent Advances in Biomembrane Models for Studying Interactions with Bio-/Molecules)
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15 pages, 1241 KiB  
Article
“Head-to-Toe” Lipid Properties Govern the Binding and Cargo Transfer of High-Density Lipoprotein
by Florian Weber, Markus Axmann, Erdinc Sezgin, Mariana Amaro, Taras Sych, Armin Hochreiner, Martin Hof, Gerhard J. Schütz, Herbert Stangl and Birgit Plochberger
Membranes 2024, 14(12), 261; https://doi.org/10.3390/membranes14120261 - 6 Dec 2024
Viewed by 1333
Abstract
The viscoelastic properties of biological membranes are crucial in controlling cellular functions and are determined primarily by the lipids’ composition and structure. This work studies these properties by varying the structure of the constituting lipids in order to influence their interaction with high-density [...] Read more.
The viscoelastic properties of biological membranes are crucial in controlling cellular functions and are determined primarily by the lipids’ composition and structure. This work studies these properties by varying the structure of the constituting lipids in order to influence their interaction with high-density lipoprotein (HDL) particles. Various fluorescence-based techniques were applied to study lipid domains, membrane order, and the overall lateral as well as the molecule–internal glycerol region mobility in HDL–membrane interactions (i.e., binding and/or cargo transfer). The analysis of interactions with HDL particles and various lipid phases revealed that both fully fluid and some gel-phase lipids preferentially interact with HDL particles, although differences were observed in protein binding and cargo exchange. Both interactions were reduced with ordered lipid mixtures containing cholesterol. To investigate the mechanism, membranes were prepared from single-lipid components, enabling step-by-step modification of the lipid building blocks. On a biophysical level, the different mixtures displayed varying stiffness, fluidity, and hydrogen bond network changes. Increased glycerol mobility and a strengthened hydrogen bond network enhanced anchoring interactions, while fluid membranes with a reduced water network facilitated cargo transfer. In summary, the data indicate that different lipid classes are involved depending on the type of interaction, whether anchoring or cargo transfer. Full article
(This article belongs to the Special Issue Recent Advances in Biomembrane Models for Studying Interactions with Bio-/Molecules)
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Review

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20 pages, 945 KiB  
Review
Modulation of Biological Membranes Using Small-Molecule Compounds to Counter Toxicity Caused by Amyloidogenic Proteins
by Raina Marie Seychell, Adam El Saghir and Neville Vassallo
Membranes 2024, 14(11), 231; https://doi.org/10.3390/membranes14110231 - 6 Nov 2024
Viewed by 1629
Abstract
The transition of peptides or proteins along a misfolding continuum from soluble functional states to pathological aggregates, to ultimately deposit as amyloid fibrils, is a process that underlies an expanding group of human diseases—collectively known as protein-misfolding disorders (PMDs). These include common and [...] Read more.
The transition of peptides or proteins along a misfolding continuum from soluble functional states to pathological aggregates, to ultimately deposit as amyloid fibrils, is a process that underlies an expanding group of human diseases—collectively known as protein-misfolding disorders (PMDs). These include common and debilitating conditions, such as Alzheimer’s disease, Parkinson’s disease, and type-2 diabetes. Compelling evidence has emerged that the complex interplay between the misfolded proteins and biological membranes is a key determinant of the pathogenic mechanisms by which harmful amyloid entities are formed and exert their cytotoxicity. Most efforts thus far to develop disease-modifying treatments for PMDs have largely focused on anti-aggregation strategies: to neutralise, or prevent the formation of, toxic amyloid species. Herein, we review the critical role of the phospholipid membrane in mediating and enabling amyloid pathogenicity. We consequently propose that the development of small molecules, which have the potential to uniquely modify the physicochemical properties of the membrane and make it more resilient against damage by misfolded proteins, could provide a novel therapeutic approach in PMDs. By way of an example, natural compounds shown to intercalate into lipid bilayers and inhibit amyloid–lipid interactions, such as the aminosterols, squalamine and trodusquamine, cholesterol, ubiquinone, and select polyphenols, are discussed. Such a strategy would provide a novel approach to counter a wide range of toxic biomolecules implicit in numerous human amyloid pathologies. Full article
(This article belongs to the Special Issue Recent Advances in Biomembrane Models for Studying Interactions with Bio-/Molecules)
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19 pages, 2013 KiB  
Review
The Role of ABCB1, ABCG2, and SLC Transporters in Pharmacokinetic Parameters of Selected Drugs and Their Involvement in Drug–Drug Interactions
by Kajetan Kiełbowski, Małgorzata Król, Estera Bakinowska and Andrzej Pawlik
Membranes 2024, 14(11), 223; https://doi.org/10.3390/membranes14110223 - 24 Oct 2024
Cited by 1 | Viewed by 2193
Abstract
Membrane transporters are expressed in a wide range of tissues in the human organism. These proteins regulate the penetration of various substances such as simple ions, xenobiotics, and an extensive number of therapeutics. ABC and SLC drug transporters play a crucial role in [...] Read more.
Membrane transporters are expressed in a wide range of tissues in the human organism. These proteins regulate the penetration of various substances such as simple ions, xenobiotics, and an extensive number of therapeutics. ABC and SLC drug transporters play a crucial role in drug absorption, distribution, and elimination. Recent decades have shown their contribution to the systemic exposure and tissue penetration of numerous drugs, thereby having an impact on pharmacokinetic and pharmacodynamic parameters. Importantly, the activity and expression of these transporters depend on numerous conditions, including intestinal microbiome profiles or health conditions. Moreover, the combined intake of other drugs or natural agents further affects the functionality of these proteins. In this review, we will discuss the involvement of ABC and SLC transporters in drug disposition. Moreover, we will present current evidence of the potential role of drug transporters as therapeutic targets. Full article
(This article belongs to the Special Issue Recent Advances in Biomembrane Models for Studying Interactions with Bio-/Molecules)
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21 pages, 3811 KiB  
Review
The Influence of Cholesterol on Membrane Targeted Bioactive Peptides: Modulating Peptide Activity Through Changes in Bilayer Biophysical Properties
by Juan M. Giraldo-Lorza, Chad Leidy and Marcela Manrique-Moreno
Membranes 2024, 14(10), 220; https://doi.org/10.3390/membranes14100220 - 17 Oct 2024
Cited by 4 | Viewed by 2735
Abstract
Cholesterol is a biological molecule that is essential for cellular life. It has unique features in terms of molecular structure and function, and plays an important role in determining the structure and properties of cell membranes. One of the most recognized functions of [...] Read more.
Cholesterol is a biological molecule that is essential for cellular life. It has unique features in terms of molecular structure and function, and plays an important role in determining the structure and properties of cell membranes. One of the most recognized functions of cholesterol is its ability to increase the level of lipid packing and rigidity of biological membranes while maintaining high levels of lateral mobility of the bulk lipids, which is necessary to sustain biochemical signaling events. There is increased interest in designing bioactive peptides that can act as effective antimicrobial agents without causing harm to human cells. For this reason, it becomes relevant to understand how cholesterol can affect the interaction between bioactive peptides and lipid membranes, in particular by modulating the peptides’ ability to penetrate and disrupt the membranes through these changes in membrane rigidity. Here we discuss cholesterol and its role in modulating lipid bilayer properties and discuss recent evidence showing how cholesterol modulates bioactive peptides to different degrees. Full article
(This article belongs to the Special Issue Recent Advances in Biomembrane Models for Studying Interactions with Bio-/Molecules)
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