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Volume 14
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Abstract

Resveratrol-Loaded Glycosylated Liposomes for Targeting Bacteria †

by
Cecilia Bombelli
1,*,
Livia Pagano
2,
Stefano Aiello
2,
Foteini Gkartziou
3,
Beatrice Simonis
1,2,
Francesca Ceccacci
1,
Simona Sennato
4,
Alessia Ciogli
5,
Francesca Bugli
6,7,*,
Cecilia Martini
7,
Maurizio Sanguinetti
6,7,
Riccardo Torelli
6,7,
Spyridon Mourtas
8,
Iris Spiliopoulou
9,
Sophia G. Antimisiaris
3,8 and
Giovanna Mancini
10
1
Institute for Biological Systems, Italian National Research Council (ISB-CNR) Secondary Office of Rome-Reaction Mechanisms c/o Department of Chemistry, Sapienza University, P.le A. Moro 5, 00185 Rome, Italy
2
Department of Chemistry, Sapienza University, P.le A. Moro 5, 00185 Rome, Italy
3
Institute of Chemical Engineering Sciences (ICE-HT), Foundation for Research and Technology, Hellas (FORTH), Platani, 26504 Patras, Greece
4
Institute of Complex Systems, Italian National Research Council (ISC-CNR), Sede Sapienza c/o Physics Department, Sapienza University, P.le A. Moro 5, 00185 Rome, Italy
5
Department of Chemistry and Technology of Drug, Sapienza University, P.le A. Moro 5, 00185 Rome, Italy
6
Dipartimento di Scienze di Laboratorio e Infettivologiche, Fondazione Policlinico Universitario “A. Gemelli” IRCCS, 00168 Rome, Italy
7
Dipartimento di Scienze Biotecnologiche di Base, Cliniche Intensivologiche e Perioperatorie, Università Cattolica del Sacro Cuore, 00168 Rome, Italy
8
Lab Pharm Technology, Department of Pharmacy, School of Health Sciences, University of Patras, 26504 Rio-Patras, Greece
9
Department of Microbiology, School of Medicine, University of Patras, Rio, 26504 Patras, Greece
10
Institute for Biological Systems, Italian National Research Council (ISB-CNR), Area della Ricerca di Roma 1, Via Salaria Km 29,300, 00015 Monterotondo, Italy
*
Authors to whom correspondence should be addressed.
†
Presented at the 8th International Electronic Conference on Medicinal Chemistry, 1–30 November 2022; Available online: https://ecmc2022.sciforum.net/.
Med. Sci. Forum 2022, 14(1), 61; https://doi.org/10.3390/ECMC2022-13158
Published: 1 November 2022
(This article belongs to the Proceedings of The 8th International Electronic Conference on Medicinal Chemistry)
Versions Notes

Biofilm-associated bacterial diseases are a major health problem due to the high antibiotic resistance of biofilm infections [1,2]. In recent years, several methods, some of which rely on nanotechnology [3], have been developed to tackle this problem. The search for non-antibiotic strategies has renewed interest in natural molecules that exploit alternative bacterial-fighting mechanisms and, above all, do not induce resistance. In this context, we have developed two sets of cationic glycosylated liposomes for the targeted delivery of trans-resveratrol (RSV), a secondary plant metabolite with antimicrobial properties, to bacteria that express carbohydrate-specific proteins able to recognize monosaccharides, namely Staphylococcus epidermidis [4] and Methicillin Resistant Staphylococcus Aureus (MRSA) [5]. Liposome physico-chemical properties (diameter, polidispersity index-PDI-, charge, and RSV entrapment efficiency) were measured by dynamic light scattering (DLS), electrophoretic mobility, and high-performance liquid chromatography (HPLC). Liposomes used in the experiments on MRSA were composed of 1,2-dioleoyl-sn-glycero-3-phosphocholine, cholesterol (Chol), and glycoamphiphiles featuring a galactosyl, mannosyl, or glucosyl moiety [5]. The objective was to identify the best sugar moiety to target MRSA biofilm. Microbiological tests carried out to monitor the demolition effect of RSV-loaded liposomes on MRSA mature biofilms showed that RSV-galactosylated liposomes are the most effective at an RSV concentration 60 times below the minimum inhibitory concentration (MIC). Liposomes used in the experiments on S. epidermidis were formulated with 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, Chol, and the glycoamphiphile featuring the glucose residue [4]. The ability of RSV-loaded liposomes to inhibit the growth of a slime-positive and a slime-negative strain of S. epidermidis was evaluated. Glucosylated liposomes, which are non-toxic, kill bacteria at concentrations tenfold under the MIC of RSV.

Supplementary Materials

The following are available online at https://www.mdpi.com/article/10.3390/ECMC2022-13158/s1.

Author Contributions

C.B.: Conceptualization, Methodology, Project administration, Writing—original draft, Visualization, Writing—review & editing; L.P.: Investigation, Visualization; S.A.: Investigation, Visualization; F.G.: Investigation, Visualization; B.S.: Investigation, Visualization; F.C.: Validation, Visualization, Writing—review & editing; S.S.: Investigation, Formal analysis; A.C.: Methodology, Investigation; F.B.: Methodology, Validation, Writing—review & editing, Supervision; C.M.: Investigation; M.S.: Supervision; R.T.: Investigation, Formal analysis, Visualization; S.M.: Methodology, Investigation; I.S.: Methodology, Supervision. S.G.A.: Supervision, Validation; G.M.: Conceptualization, Supervision. All authors have read and agreed to the published version of the manuscript.

Funding

This research received no external funding.

Data Availability Statement

Data supporting the presented data are published in [4,5].

Conflicts of Interest

The authors declare no conflict of interest.

References

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  3. Ferreira, M.; Ogren, M.; Dias, J.N.R.; Silva, M.; Gil, S.; Tavares, L.; Aires-da-Silva, F.; Gaspar, M.M.; Aguiar, S.I. Liposomes as Antibiotic Delivery Systems: A Promising Nanotechnological Strategy against Antimicrobial Resistance. Molecules 2021, 26, 2047. [Google Scholar] [CrossRef] [PubMed]
  4. Pagano, L.; Gkartziou, F.; Aiello, S.; Simonis, B.; Ceccacci, F.; Sennato, S.; Ciogli, A.; Mourtas, S.; Spiliopoulou, I.; Antimisiaris, S.G.; et al. Resveratrol loaded in cationic glucosylated liposomes to treat Staphylococcus epidermidis infections. Chem. Phys. Lipids 2022, 243, 105174. [Google Scholar] [CrossRef] [PubMed]
  5. Aiello, S.; Pagano, L.; Ceccacci, F.; Simonis, B.; Sennato, S.; Bugli, F.; Martini, C.; Torelli, R.; Sanguinetti, M.; Ciogli, A.; et al. Mannosyl, glucosyl or galactosyl liposomes to improve resveratrol efficacy against Methicillin Resistant Staphylococcus aureus biofilm. Colloids Surf. A: Physicochem. Eng. Asp. 2021, 617, 126321. [Google Scholar] [CrossRef]
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MDPI and ACS Style

Bombelli, C.; Pagano, L.; Aiello, S.; Gkartziou, F.; Simonis, B.; Ceccacci, F.; Sennato, S.; Ciogli, A.; Bugli, F.; Martini, C.; et al. Resveratrol-Loaded Glycosylated Liposomes for Targeting Bacteria. Med. Sci. Forum 2022, 14, 61. https://doi.org/10.3390/ECMC2022-13158

AMA Style

Bombelli C, Pagano L, Aiello S, Gkartziou F, Simonis B, Ceccacci F, Sennato S, Ciogli A, Bugli F, Martini C, et al. Resveratrol-Loaded Glycosylated Liposomes for Targeting Bacteria. Medical Sciences Forum. 2022; 14(1):61. https://doi.org/10.3390/ECMC2022-13158

Chicago/Turabian Style

Bombelli, Cecilia, Livia Pagano, Stefano Aiello, Foteini Gkartziou, Beatrice Simonis, Francesca Ceccacci, Simona Sennato, Alessia Ciogli, Francesca Bugli, Cecilia Martini, and et al. 2022. "Resveratrol-Loaded Glycosylated Liposomes for Targeting Bacteria" Medical Sciences Forum 14, no. 1: 61. https://doi.org/10.3390/ECMC2022-13158

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