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Antibiotics
Special Issues
Antimicrobial Agents for Drug-Resistant Infections: From Identification to Preclinical and...
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Antimicrobial Agents for Drug-Resistant Infections: From Identification to Preclinical and Clinical Trials

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Novel Antimicrobial Agents".

Deadline for manuscript submissions: 31 August 2026 | Viewed by 4948

Editors

Prof. Dr. Javier Eduardo García Castañeda

E-Mail Website
Guest Editor
Departamento de Farmacia, Facultad de Ciencias, Universidad Nacional de Colombia, Bogotá Carrera 45 No 26-85, Building 450, Bogotá 11321, Colombia
Interests: peptide synthesis; antimicrobial and anticancerigenic peptides; glycopeptides; organometallic peptides
Special Issues, Collections and Topics in MDPI journals
Dr. Zuly Jenny Rivera-Monroy

E-Mail Website
Guest Editor
Departamento de Química, Facultad de Ciencias, Universidad Nacional de Colombia, Bogotá Carrera 45 No 26-85, Building 451, Bogotá 11321, Colombia
Interests: peptide synthesis; peptide therapeutic application; peptide analysis by HPLC and MS
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Drug resistance, in both antimicrobial and anticancer therapies, arises when pathogens or cancer cells become less susceptible to drugs, reducing treatment efficacy. This growing health threat requires urgent multisectoral action to achieve the Sustainable Development Goals (SDGs) and imposes a significant economic burden due to prolonged hospital stays, higher healthcare costs, and premature mortality.

Multidrug-resistant and pan-resistant bacterial strains, causing infections untreatable with current antibiotics, are a critical concern. According to the World Health Organization (WHO), the clinical development pipeline for new antimicrobials is severely depleted. A 2019 report found that of 32 antibiotics in development, only 6 were considered innovative, underscoring the need for novel therapeutic approaches.

Peptides, both antimicrobial and anticancer, have emerged as promising alternatives due to their synthetic flexibility, favorable safety profiles, and lower propensity to induce resistance compared to small-molecule drugs.

This Special Issue seeks to compile research on identifying new antimicrobial and anticancer agents, including proteins, peptides, and amino acids, with or without non-protein components such as organic moieties, sugars, lipids, and organometallic compounds. Multidisciplinary strategies to discover bioactive molecules are essential for expanding therapeutic options capable of overcoming drug resistance and restoring treatment efficacy.

Prof. Dr. Javier Eduardo García Castañeda
Dr. Zuly Jenny Rivera-Monroy
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 250 words) can be sent to the Editorial Office for assessment.

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-anonymized peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Antibiotics 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 2900 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

  • antimicrobials agents
  • drug resistant
  • anti-cancerogenic agents
  • drug development
  • preclinical trials
  • clinical trials
  • pharmaceutical optimization

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Published Papers (2 papers)

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Research

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26 pages, 1978 KB  
Article
Fluorescent Peptides Internalize HeLa Cells and Kill Multidrug-Resistant Clinical Bacterial Isolates
by Daniel Castellar-Almonacid, Kelin Johana Cuero-Amu, Jose David Mendoza-Mendoza, Natalia Ardila-Chantré, Fernando José Chavez-Salazar, Andrea Carolina Barragán-Cárdenas, Jhon Erick Rivera-Monroy, Claudia Parra-Giraldo, Zuly Jenny Rivera-Monroy, Javier García-Castañeda and Ricardo Fierro-Medina
Antibiotics 2025, 14(8), 793; https://doi.org/10.3390/antibiotics14080793 - 4 Aug 2025
Viewed by 1958
Abstract
Palindromic antimicrobial peptides (PAMs) constitute versatile scaffolds for the design and optimization of anticancer agents with applications in therapy, diagnosis, and/or monitoring. In the present study, fluorolabeled peptides derived from the palindromic sequence RWQWRWQWR containing fluorescent probes, such as 2-Aminobenzoyl, 5(6)-Carboxyfluorescein, and Rhodamine [...] Read more.
Palindromic antimicrobial peptides (PAMs) constitute versatile scaffolds for the design and optimization of anticancer agents with applications in therapy, diagnosis, and/or monitoring. In the present study, fluorolabeled peptides derived from the palindromic sequence RWQWRWQWR containing fluorescent probes, such as 2-Aminobenzoyl, 5(6)-Carboxyfluorescein, and Rhodamine B, were obtained. RP-HPLC analysis revealed that the palindromic peptide conjugated to Rhodamine B (RhB-RWQWRWQWR) exhibited the presence of isomers, likely corresponding to the open-ring and spiro-lactam forms of the fluorescent probe. This equilibrium is dependent on the peptide sequence, as the RP-HPLC analysis of dimeric peptide (RhB-RRWQWR-hF-KKLG)2K-Ahx did not reveal the presence of isomers. The antibacterial activity of the fluorescent peptides depends on the probe attached to the sequence and the bacterial strain tested. Notably, some fluorescent peptides showed activity against reference strains as well as sensitive, resistant, and multidrug-resistant clinical isolates of E. coli, S. aureus, and E. faecalis. Fluorolabeled peptides 1-Abz (MIC = 62 µM), RhB-1 (MIC = 62 µM), and Abz-1 (MIC = 31 µM) exhibited significant activity against clinical isolates of E. coli, S. aureus, and E. faecalis, respectively. The RhB-1 (IC50 = 61 µM), Abz-1 (IC50 = 87 µM), and RhB-2 (IC50 = 35 µM) peptides exhibited a rapid, significant, and concentration-dependent cytotoxic effect on HeLa cells, accompanied by morphological changes characteristic of apoptosis. RhB-1 (IC50 = 18 µM) peptide also exhibited significant cytotoxic activity against breast cancer cells MCF-7. These conjugates remain valuable for elucidating the possible mechanisms of action of these novel anticancer peptides. Rhodamine-labeled peptides displayed cytotoxicity comparable to that of their unlabeled analogues, suggesting that cellular internalization constitutes a critical early step in their mechanism of action. These findings suggest that cell death induced by both unlabeled and fluorolabeled peptides proceeds predominantly via apoptosis and is likely contingent upon peptide internalization. Functionalization at the N-terminal end of the palindromic sequence can be evaluated to develop systems for transporting non-protein molecules into cancer cells. Full article
(This article belongs to the Special Issue Antimicrobial Agents for Drug-Resistant Infections: From Identification to Preclinical and Clinical Trials)
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Review

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26 pages, 883 KB  
Review
Clinical Potential of Essential Oils: Cytotoxicity, Selectivity Index and Antimicrobial Activity Against Gram-Negative ESKAPEE Pathogens
by Biruk Bayleyegn Belete, Jerome Ozkan, Parthasarathi Kalaiselvan, Muhammad Yasir and Mark Willcox
Antibiotics 2026, 15(3), 274; https://doi.org/10.3390/antibiotics15030274 - 6 Mar 2026
Cited by 5 | Viewed by 2509
Abstract
Background: Novel therapeutic compounds with strong efficacy and low resistance potential are urgently needed to combat life-threatening infections caused by antibiotic-resistant ESKAPEE pathogens. These pathogens contribute globally to a large share of bloodstream, respiratory, urinary, and wound infections, and often have levels of [...] Read more.
Background: Novel therapeutic compounds with strong efficacy and low resistance potential are urgently needed to combat life-threatening infections caused by antibiotic-resistant ESKAPEE pathogens. These pathogens contribute globally to a large share of bloodstream, respiratory, urinary, and wound infections, and often have levels of high antimicrobial resistance. This review examined the antimicrobial efficacy of different plant essential oils (EOs) against Gram-negative ESKAPEE pathogens and their cytotoxic effects and calculated selectivity indices in cancer and normal cell lines. Methods: This review was developed using studies retrieved from PubMed, Scopus, and Web of Science, covering publications between 2013 and 2024 using the search terms: “essential oils”, “plant extracts”, “safety”, “cytotoxicity”, “cell lines”, “human”, “in-vitro”, antimicrobial”, “antibacterial” and “antibiotic” with Boolean operators (“AND”, “OR”, “NOT”). Only studies that reported both antimicrobial inhibitory concentrations and concentrations causing toxicity to mammalian cells were included in the final review. These data were then used to calculate the selectivity indices of the EOs (toxic concentration/antimicrobial inhibitory concentration) to give an initial assessment of safety. Results: Ocimum basilicum EOs had strong antibacterial effects against the Gram-negative ESKAPEE pathogens Escherichia coli, Pseudomonas aeruginosa, and Klebsiella pneumoniae, with minimum inhibitory concentrations (MICs) as low as 1 μg/mL and high selectivity indices of >80.4. Likewise, Satureja nabateorum EOs had potent antibacterial activity, with a low MIC of 0.1 μg/mL against K. pneumoniae, 2.3 μg/mL against E. coli, and 12.5 μg/mL against P. aeruginosa, along with a very high selectivity index (>100). Other EOs such as those from Eucalyptus spp., Thymus spp., Mentha spp., Cinnamomum spp., Artemisia spp., and Aquilaria crassna also had broad-spectrum antibacterial potential and minimal toxicity toward mammalian cells, making them promising candidates for safe and effective antimicrobial agents in clinical and industrial applications. However, several EOs had selectivity indices of <10, indicating that at their MIC they would also be potentially highly cytotoxic. EOs tended to show increased toxicity to cells derived from cancers. Conclusions and recommendations: Certain EOs are highly active against Gram-negative ESKAPEE pathogens. They are also toxic to cancer-derived mammalian cells. Additional studies using normal cell lines and clinical trials are warranted to further validate their safety and therapeutic potential. Full article
(This article belongs to the Special Issue Antimicrobial Agents for Drug-Resistant Infections: From Identification to Preclinical and Clinical Trials)
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