Special Issue "Synthesis and Pharmacokinetics of Antibiotics"

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

Deadline for manuscript submissions: closed (30 November 2020).

Special Issue Editor

Prof. Alessia Carocci
E-Mail Website
Guest Editor
Department of Pharmacy-Drug Science, University of Bari Aldo Moro, Bari, Italy
Interests: Biological active compounds: antimicrobials; antiarrhythmics; anticancers; melatonergic drugs; voltage-gated sodium channel blockers
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Special Issue Information

Dear Colleagues,

The development of antibiotics has contributed greatly to increases in life expectancy and improvements in the quality of life. However, many decades after the first patients were treated with antibiotics, bacterial infections have again become a threat. Unfortunately, the development of multidrug resistance by common pathogens has seriously limited the efficacy of antibiotic therapies. Therefore, there is an urgent medical need for the development of new effective antibiotics that are refractory to most common mechanisms of bacterial resistance or that may restrain or inhibit the mechanisms of resistance. Recently, some delivery systems have proved particularly effective as antimicrobial carriers due to their ability to carry out targeted drug delivery at active sites, reduced drug resistance and side effects, and increased therapeutic index.

This Special Issue of Antibiotics aims to present a collection of the latest research in this field including, but not limited to, the following topics:

  • The design and synthesis of antimicrobial agents with novel scaffolds;
  • Promising new classes of antibiotics acting on novel targets;
  • The development of new synthetic approaches starting both from natural and synthetic compounds;
  • Structural modifications of antimicrobial natural products for the identification and development of novel antibacterial agents;
  • The synthesis of antibiotic analogues with improved pharmacokinetic properties;
  • Delivery systems for targeted antimicrobial therapies.

Dr. Alessia Carocci
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 papers will be 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 1800 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

  • Synthesis of antimicrobial agents
  • Antibiotics targeted delivery systems
  • Pharmacokinetic of antibiotics
  • New molecular target for antimicrobial therapy

Published Papers (5 papers)

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Research

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Article
Antimicrobial and Antibiofilm Activities of Essential Oils against Escherichia coli O157:H7 and Methicillin-Resistant Staphylococcus aureus (MRSA)
Antibiotics 2020, 9(11), 730; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9110730 - 24 Oct 2020
Cited by 1 | Viewed by 955
Abstract
The emergence of multidrug resistant microorganisms represents a global challenge due to the lack of new effective antimicrobial agents. In this sense, essential oils (EOs) are an alternative to be considered because of their anti-inflammatory, antiviral, antibacterial, and antibiofilm biological activities. Therefore, multiple [...] Read more.
The emergence of multidrug resistant microorganisms represents a global challenge due to the lack of new effective antimicrobial agents. In this sense, essential oils (EOs) are an alternative to be considered because of their anti-inflammatory, antiviral, antibacterial, and antibiofilm biological activities. Therefore, multiple efforts have been made to consider the potential use of EOs in the treatment of infections which are caused by resistant microorganisms. In this study, 15 EOs of both Colombian and introduced aromatic plants were evaluated against pathogenic strains of E. coli O157:H7 and methicillin resistant Staphylococcus aureus (MRSA) in planktonic and sessile states in order to identify relevant and promising alternatives for the treatment of microbial infections. Forty different compounds were identified in the 15 EO with nine of them constituted mainly by oxygenated monoterpenes (OM). EOs from Lippia origanoides, chemotypes thymol, and carvacrol, displayed the highest antibacterial activity against E. coli O157:H7 (MIC50 = 0.9 and 0.3 mg/mL, respectively) and MRSA (MIC50 = 1.2 and 0.6 mg/mL, respectively). These compounds from EOs had also the highest antibiofilm activity (inhibition percentage > 70.3%). Using scanning electron microscopy (SEM), changes in the size and morphology of both bacteria were observed when they were exposed to sub-inhibitory concentrations of L. origanoides EO carvacrol chemotype. EOs from L. origanoides, thymol, and carvacrol chemotypes represented a viable alternative for the treatment of microbial infections; however, the Selectivity Index (SI ≤ 3) indicated that it was necessary to study alternatives to reduce its in vitro cytotoxicity. Full article
(This article belongs to the Special Issue Synthesis and Pharmacokinetics of Antibiotics)
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Article
Anti-Biofilm Inhibitory Synergistic Effects of Combinations of Essential Oils and Antibiotics
Antibiotics 2020, 9(10), 637; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9100637 - 24 Sep 2020
Cited by 6 | Viewed by 2082
Abstract
In recent years, the increase of bacteria antibiotic- resistance has been a severe problem for public health. A useful solution could be to join some phytochemicals naturally present in essential oils (EOs) to the existing antibiotics, with the aim to increase their efficacy [...] Read more.
In recent years, the increase of bacteria antibiotic- resistance has been a severe problem for public health. A useful solution could be to join some phytochemicals naturally present in essential oils (EOs) to the existing antibiotics, with the aim to increase their efficacy in therapies. According to in vitro studies, EOs and their components could show such effects. Among them, we studied the activity of Cinnammonum zeylanicum, Mentha piperita, Origanum vulgare, and Thymus vulgaris EOs on bacterial biofilm and their synergism when used in association with some common antibiotics such as norfloxacin, oxacillin, and gentamicin. The chemical composition of EOs was determined using gas chromatography (GC) coupled with mass spectrometry (MS) techniques. The EOs drug efficacy was evaluated on four different strains of Gram-positive bacteria forming biofilms. The synergistic effects were tested through the chequerboard microdilution method. The association EOs-antibiotics showed a strong destruction of the biofilm growth of the four bacterial species considered. The interaction of norfloxacin with EOs was the most effective in all the tested combinations against the strains object of this study. These preliminary results suggest the formulation of a new generation of antimicrobial agents based on a combination of antimicrobial compounds with different origin. Full article
(This article belongs to the Special Issue Synthesis and Pharmacokinetics of Antibiotics)
Article
Potent and Specific Antibacterial Activity against Escherichia coli O157:H7 and Methicillin Resistant Staphylococcus aureus (MRSA) of G17 and G19 Peptides Encapsulated into Poly-Lactic-Co-Glycolic Acid (PLGA) Nanoparticles
Antibiotics 2020, 9(7), 384; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9070384 - 07 Jul 2020
Cited by 7 | Viewed by 1228
Abstract
Antimicrobial peptides constitute an excellent alternative against conventional antibiotics because of their potent antimicrobial spectrum, unspecific action mechanism and low capacity to produce antibiotic resistance. However, a potential use of these biological molecules as therapeutic agents is threatened by their low stability and [...] Read more.
Antimicrobial peptides constitute an excellent alternative against conventional antibiotics because of their potent antimicrobial spectrum, unspecific action mechanism and low capacity to produce antibiotic resistance. However, a potential use of these biological molecules as therapeutic agents is threatened by their low stability and susceptibility to proteases. In order to overcome these limitations, encapsulation in biocompatible polymers as poly-lactic-glycolic-acid (PLGA) is a promising alternative for increasing their stability and bioavailability. In this work, the effect of new synthetic antimicrobial peptides GIBIM-P5S9K (G17) and GAM019 (G19) encapsulated on PLGA and acting against methicillin resistant Staphylococus aureus (MRSA) and Escherichia coli O157:H7 was studied. PLGA encapsulation allowed us to load around 7 µg AMPs/mg PLGA with an efficiency of 90.5%, capsule sizes around 290 nm and positive charges. Encapsulation improved antimicrobial activity, decreasing MIC50 from 1.5 to 0.2 (G17NP) and 0.7 (G19NP) µM against MRSA, and from 12.5 to 3.13 µM for E. coli O157:H7. Peptide loaded nanoparticles could be a bacteriostatic drug with potential application to treat these bacterial E. coli O157:H7 and MRSA infections, with a slow and gradual release. Full article
(This article belongs to the Special Issue Synthesis and Pharmacokinetics of Antibiotics)
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Article
Essential Oils of Aromatic Plants with Antibacterial, Anti-Biofilm and Anti-Quorum Sensing Activities against Pathogenic Bacteria
Antibiotics 2020, 9(4), 147; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9040147 - 30 Mar 2020
Cited by 18 | Viewed by 2438
Abstract
Both the ability of bacteria to form biofilms and communicate through quorum sensing allows them to develop different survival or virulence traits that lead to increased bacterial resistance against conventional antibiotic therapy. Here, seventeen essential oils (EOs) were investigated for the antimicrobial, antibiofilm, [...] Read more.
Both the ability of bacteria to form biofilms and communicate through quorum sensing allows them to develop different survival or virulence traits that lead to increased bacterial resistance against conventional antibiotic therapy. Here, seventeen essential oils (EOs) were investigated for the antimicrobial, antibiofilm, and anti-quorum sensing activities on Escherichia. coli O157:H7, Escherichia coli O33, and Staphylococcus epidermidis ATCC 12228. All essential oils were isolated from plant material by using hydrodistillation and analyzed by GC-MS. The antimicrobial activity was performed by using the microdilution technique. Subinhibitory concentrations of each EO were assayed for biofilm inhibition in both bacterial strains. Quantification of violacein in Chromobacterium violaceum CV026 was performed for the anti-quorum sensing activity. The cytotoxicity activity of the EOs was evaluated on Vero cell line by using MTT method. Thymol-carvacrol-chemotype (I and II) oils from Lippia origanoides and Thymus vulgaris oil exhibited the higher antimicrobial activity with MIC values of 0.37–0.75 mg/mL. In addition, these EOs strongly inhibited the biofilm formation and violacein (QS) production in a concentration-dependent manner, highlighting thymol-carvacrol-chemotype (II) oil as the best candidate for further studies in antibiotic design and development against bacterial resistance. Full article
(This article belongs to the Special Issue Synthesis and Pharmacokinetics of Antibiotics)
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Review

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Review
Influence of Single Nucleotide Polymorphisms on Rifampin Pharmacokinetics in Tuberculosis Patients
Antibiotics 2020, 9(6), 307; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9060307 - 08 Jun 2020
Cited by 2 | Viewed by 1159
Abstract
Rifampin (RF) is metabolized in the liver into an active metabolite 25-desacetylrifampin and excreted almost equally via biliary and renal routes. Various influx and efflux transporters influence RF disposition during hepatic uptake and biliary excretion. Evidence has also shown that Vitamin D deficiency [...] Read more.
Rifampin (RF) is metabolized in the liver into an active metabolite 25-desacetylrifampin and excreted almost equally via biliary and renal routes. Various influx and efflux transporters influence RF disposition during hepatic uptake and biliary excretion. Evidence has also shown that Vitamin D deficiency (VDD) and Vitamin D receptor (VDR) polymorphisms are associated with tuberculosis (TB). Hence, genetic polymorphisms of metabolizing enzymes, drug transporters and/or their transcriptional regulators and VDR and its pathway regulators may affect the pharmacokinetics of RF. In this narrative review, we aim to identify literature that has explored the influence of single nucleotide polymorphisms (SNPs) of genes encoding drug transporters and their transcriptional regulators (SLCO1B1, ABCB1, PXR and CAR), metabolizing enzymes (CES1, CES2 and AADAC) and VDR and its pathway regulators (VDR, CYP27B1 and CYP24A1) on plasma RF concentrations in TB patients on antitubercular therapy. Available reports to date have shown that there is a lack of any association of ABCB1, PXR, CAR, CES1 and AADAC genetic variants with plasma concentrations of RF. Further evidence is required from a more comprehensive exploration of the association of SLCO1B1, CES2 and Vitamin D pathway gene variants with RF pharmacokinetics in distinct ethnic groups and a larger population to reach conclusive information. Full article
(This article belongs to the Special Issue Synthesis and Pharmacokinetics of Antibiotics)
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