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Antibiotics
Special Issues
Antibiotic Conjugates: Applications from Tools to Drug Development
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Antibiotic Conjugates: Applications from Tools to Drug Development

A special issue of Antibiotics (ISSN 2079-6382).

Deadline for manuscript submissions: closed (31 December 2020) | Viewed by 7385

Special Issue Editor

Dr. Julien Tailhades

E-Mail Website
Guest Editor
Department of Biochemistry and Molecular Biology, The Monash Biomedicine Discovery Institute, Monash University, Monash, Australia
Interests: glycopeptides antibiotics; chemotaxis; P450 enzymes; non-ribosomal peptides; bioorthogonal chemistry, Microwave peptide and organic syntheses and protein expression and purification; mass spectrometry analyses

Special Issue Information

Dear Colleagues,

Natural products are the greatest source of antimicrobial agents; nevertheless, this research is an endless beginning due to the increasing bacterial resistance. Interestingly, modifying a defined antibiotic with any other molecule is often a great strategy to generate a bioconjugate for various applications. This Special Issue will publish original research articles as well as reviews on cross-/ interdisciplinary applications related to antibiotic conjugates.

In this context, all fields in biology, microbiology, chemistry, structural biology, biochemistry, and biophysics are relevant as long as the article or review proposes cross-/interdisciplinary applications. The common link between each material of this Special Issue is the formation of the antibiotic conjugates.

These are intended to be full-length articles that are accessible to the broad readership of the journal, and emphasize broadly relevant themes and speculate about what the future holds.

Thank you very much for your consideration and we look forward to hearing from you.

Dr. Julien Tailhades
Guest Editor

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. 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

  • antibiotic conjugates
  • synergetic effect
  • bioorthogonal chemistry
  • fluorescence imaging

Published Papers (2 papers)

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Research

16 pages, 7770 KiB  
Article
Membrane-Targeting Triphenylphosphonium Functionalized Ciprofloxacin for Methicillin-Resistant Staphylococcus aureus (MRSA)
by Sangrim Kang, Kyoung Sunwoo, Yuna Jung, Junho K. Hur, Ki-Ho Park, Jong Seung Kim and Dokyoung Kim
Antibiotics 2020, 9(11), 758; https://doi.org/10.3390/antibiotics9110758 - 30 Oct 2020
Cited by 17 | Viewed by 3568
Abstract
Multidrug-resistant (MDR) bacteria have become a severe problem for public health. Developing new antibiotics for MDR bacteria is difficult, from inception to the clinically approved stage. Here, we have used a new approach, modification of an antibiotic, ciprofloxacin (CFX), with triphenylphosphonium (TPP, PPh [...] Read more.
Multidrug-resistant (MDR) bacteria have become a severe problem for public health. Developing new antibiotics for MDR bacteria is difficult, from inception to the clinically approved stage. Here, we have used a new approach, modification of an antibiotic, ciprofloxacin (CFX), with triphenylphosphonium (TPP, PPh3) moiety via ester- (CFX-ester-PPh3) and amide-coupling (CFX-amide-PPh3) to target bacterial membranes. In this study, we have evaluated the antibacterial activities of CFX and its derivatives against 16 species of bacteria, including MDR bacteria, using minimum inhibitory concentration (MIC) assay, morphological monitoring, and expression of resistance-related genes. TPP-conjugated CFX, CFX-ester-PPh3, and CFX-amide-PPh3 showed significantly improved antibacterial activity against Gram-positive bacteria, Staphylococcus aureus, including MDR S. aureus (methicillin-resistant S. aureus (MRSA)) strains. The MRSA ST5 5016 strain showed high antibacterial activity, with MIC values of 11.12 µg/mL for CFX-ester-PPh3 and 2.78 µg/mL for CFX-amide-PPh3. The CFX derivatives inhibited biofilm formation in MRSA by more than 74.9% of CFX-amide-PPh3. In the sub-MIC, CFX derivatives induced significant morphological changes in MRSA, including irregular deformation and membrane disruption, accompanied by a decrease in the level of resistance-related gene expression. With these promising results, this method is very likely to combat MDR bacteria through a simple TPP moiety modification of known antibiotics, which can be readily prepared at clinical sites. Full article
(This article belongs to the Special Issue Antibiotic Conjugates: Applications from Tools to Drug Development)
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14 pages, 1711 KiB  
Article
Isoniazid Conjugated Magnetic Nanoparticles Loaded with Amphotericin B as a Potent Antiamoebic Agent against Acanthamoeba castellanii
by Kawish Iqbal, Sumayah Abdelnasir Osman Abdalla, Ayaz Anwar, Kanwal Muhammad Iqbal, Muhammad Raza Shah, Areeba Anwar, Ruqaiyyah Siddiqui and Naveed Ahmed Khan
Antibiotics 2020, 9(5), 276; https://doi.org/10.3390/antibiotics9050276 - 25 May 2020
Cited by 11 | Viewed by 3342
Abstract
The pathogenic free-living amoeba, Acanthamoeba castellanii, is responsible for a rare but deadly central nervous system infection, granulomatous amoebic encephalitis and a blinding eye disease called Acanthamoeba keratitis. Currently, a combination of biguanides, amidine, azoles and antibiotics are used to manage these [...] Read more.
The pathogenic free-living amoeba, Acanthamoeba castellanii, is responsible for a rare but deadly central nervous system infection, granulomatous amoebic encephalitis and a blinding eye disease called Acanthamoeba keratitis. Currently, a combination of biguanides, amidine, azoles and antibiotics are used to manage these infections; however, the host cell cytotoxicity of these drugs remains a challenge. Furthermore, Acanthamoeba species are capable of transforming to the cyst form to resist chemotherapy. Herein, we have developed a nano drug delivery system based on iron oxide nanoparticles conjugated with isoniazid, which were further loaded with amphotericin B (ISO-NPs-AMP) to cause potent antiamoebic effects against Acanthamoeba castellanii. The IC50 of isoniazid conjugated with magnetic nanoparticles and loaded with amphotericin B was found to be 45 μg/mL against Acanthamoeba castellanii trophozoites and 50 μg/mL against cysts. The results obtained in this study have promising implications in drug discovery as these nanomaterials exhibited high trophicidal and cysticidal effects, as well as limited cytotoxicity against rat and human cells. Full article
(This article belongs to the Special Issue Antibiotic Conjugates: Applications from Tools to Drug Development)
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