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Discovery and Development of Novel Therapeutic Agents in Infectious Diseases Treatment

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A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Antibiotic Therapy in Infectious Diseases".

Deadline for manuscript submissions: closed (1 August 2023) | Viewed by 16053

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Special Issue Editors

Dr. Tinchun Chu

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Guest Editor

Department of Biological Sciences, Seton Hall University, South Orange, NJ, USA
Interests: a novel approach using natural products and their derivatives as potential therapeutic agents for diseases; study of physiological response to various stress factors on bacteria; environmental probes development for prediction, early detection, and prevention of algal blooms; metagenomic characterization of phytoplankton community in Barnegat Bay; genome projects and bioinformatic analyses of cyanobacteria and cyanophage

Dr. Lee H. Lee

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Guest Editor

Department of Biology, Montclair State University, Montclair, NJ, USA
Interests: using green tea polyphenols as a novel approach to developing antiviral and antibacterial agents; monitoring the water quality using bacterial indicators and microbial source tracking; studying food safety and food handling practices of ready-to-eat foods; using microorganisms as environmental indicators to study heavy metal contamination; studying the interaction of cyanophage, cyanobacteria, and cyanobacterial algal blooms

Special Issue Information

Dear Colleagues,

Infectious diseases refer to infections caused by pathogenic microorganisms, including bacteria, viruses, fungi, and helminths. For the past few decades, many epidemics or pandemic outbreaks of emerging and re-emerging diseases have caused significant morbidity and mortality, posing a new threat to global public health. Despite medical advances with new treatments and better access to healthcare, multidrug resistance problems, including antibiotic resistance, and the discovery of new therapeutic agents for emerging diseases remain a major challenge and burden in healthcare. Thus, developing safe and effective therapeutic agents is urgently needed in this new era of infectious diseases.

For this Special Issue, we would like to invite researchers to contribute articles, either original research articles or reviews, on modern approaches to focus on the discovery and development of new anti-infectious agents. The candidates of these agents can be small molecules, natural products, or modified natural products. Furthermore, the studies can include but are not limited to antimicrobial agents' discovery, efficacy, safety, mechanisms, and therapeutic approaches to establish strategies to combat infectious diseases.

In view of your research expertise in this area, we look forward to receiving your excellent contributions.

Dr. Tinchun Chu
Dr. Lee H. Lee
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. 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

antimicrobial agent
drug resistance
natural product
small molecule
drug discovery
infectious disease

Published Papers (7 papers)

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Research

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15 pages, 2532 KiB

Open AccessArticle

Itraconazole Loaded Biosurfactin Micelles with Enhanced Antifungal Activity: Fabrication, Evaluation and Molecular Simulation

by Faisal Usman, Mudassir Farooq, Tanveer A. Wani, Hassan Ahmad, Ibrahim Javed, Mazhar Iqbal, Fatima Akbar Sheikh, Farhan Siddique, Seema Zargar and Saleh Sheikh

Antibiotics 2023, 12(10), 1550; https://doi.org/10.3390/antibiotics12101550 - 19 Oct 2023

Cited by 1 | Viewed by 1493

Abstract

Itraconazole (ITZ) is a broad-spectrum antifungal for superficial subcutaneous and systemic fungal infections. This study aimed to enhance the antifungal activity of ITZ using surfactin A (SA), a cyclic lipopeptide produced by the SA-producing Bacillus strain NH-100, possessing strong antifungal activity. SA was extracted, and ITZ-loaded SA micelles formulations were prepared via a single-pot rinsing method and characterized by particle size, zeta potential, and infrared spectroscopy. In vitro dissolution at pH 1.2, as well as hemolysis studies, was also carried out. The fabricated formulations were stable and non-spherical in shape, with an average size of about 179 nm, and FTIR spectra depicted no chemical interaction among formulation components. ITZ-loaded micelles showed decreased hemolysis activity in comparison to pure ITZ. The drug released followed the Korsmeyer–Peppas model, having R² 0.98 with the diffusion release mechanism. In an acidic buffer, drug release of all prepared formulations was in the range of 73–89% in 2 h. The molecular simulation showed the outstanding binding and stability profile of the ITZ-SA complex. The aromatic ring of the ITZ mediates a π-alkyl contact with a side chain in the SA. It can be concluded that ITZ-loaded micelles, owing to significant enhanced antifungal activity up to 6-fold due to the synergistic effect of SA, can be a promising drug delivery platform for delivery of poorly soluble ITZ. Full article

(This article belongs to the Special Issue Discovery and Development of Novel Therapeutic Agents in Infectious Diseases Treatment)

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19 pages, 3544 KiB

Open AccessArticle

Characterization of Oral Candida spp. Biofilms in Children and Adults Carriers from Eastern Europe and South America

by Anelise Maria Costa Vasconcelos Alves, Beatriz Oliveira Lopes, Ana Caroline Rocha de Melo Leite, Gabriela Silva Cruz, Érika Helena Salles de Brito, Laritza Ferreira de Lima, Lucia Černáková, Nuno Filipe Azevedo and Célia Fortuna Rodrigues

Antibiotics 2023, 12(5), 797; https://doi.org/10.3390/antibiotics12050797 - 22 Apr 2023

Cited by 2 | Viewed by 1567

Abstract

Background: Candida albicans and non-Candida albicans Candida species (NCACs) are known to colonize and invade various tissues, including the oral mucosa. In this work, we aimed to characterize mature biofilms of several Candida spp. clinical isolates (n = 33) obtained from the oral mucosa of children, adults, and elders of Eastern Europe and South America. Methods: Each strain was evaluated for its capacity to form biofilms in terms of total biomass using the crystal violet assay and for matrix components production (proteins and carbohydrates) using the BCA and phenol-sulfuric tests, respectively. The effect of different antifungals on biofilm formation was studied. Results: in the children’s group, a predominance of C. krusei (81%) was observed, while, among adults, the main species was C. albicans (59%). Most strains showed a reduced response to antimicrobial drugs when in biofilm form (p < 0.01). Moreover, it was observed that strains isolated from children produced more matrix, with higher levels of protein and polysaccharides. Conclusions: children were more likely to be infected by NCACs than adults. More importantly, these NCACs were able to form biofilms richer in matrix components. This finding is of clinical importance, particularly in pediatric care, since stronger biofilms are highly associated with antimicrobial resistance, recurrent infections, and higher therapeutic failure. Full article

(This article belongs to the Special Issue Discovery and Development of Novel Therapeutic Agents in Infectious Diseases Treatment)

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21 pages, 4327 KiB

Open AccessArticle

Scabicidal Potential of Coconut Seed Extract in Rabbits via Downregulating Inflammatory/Immune Cross Talk: A Comprehensive Phytochemical/GC-MS and In Silico Proof

by Eman Maher Zahran, Nehad M. Reda Abdel-Maqsoud, Omar. Y. Tammam, Islam M. Abdel-Rahman, Mahmoud A. Elrehany, Hussain T. Bakhsh, Faisal H. Altemani, Naseh A. Algehainy, Mubarak A. Alzubaidi, Usama Ramadan Abdelmohsen and Abeer H. Elmaidomy

Antibiotics 2023, 12(1), 43; https://doi.org/10.3390/antibiotics12010043 - 27 Dec 2022

Cited by 11 | Viewed by 2660

Abstract

Scabies is an invasive skin condition caused by Sarcoptes scabiei mites. The present study investigates the antiscabies potential of coconut seed extract (CSE) in rabbits. GC-MS analysis of the seed oil identified 17 known compounds, while CSE phytochemical investigation afforded 4 known ones. The topical application of seed extract improved all signs of infection, and the improvement started 3 days post application. However, in vitro application of the extract caused 99% mortality of mites 1 day post application. Histopathological examination revealed the absence of inflammatory infiltration and hyperkeratosis of the epidermis, compared with ivermectin-treated groups which revealed less improvement. The mRNA gene expression results revealed a suppression of IL-1β, IL-6, IL-10, MMP-9, VEGF, and MCP-1, and an upregulation of I-CAM-1, KGF as well as TIMP-1. The docking analysis emphasized a strong binding of gondoic acid with IL-1β, IL-6, and VEGF with high binding scores of −5.817, −5.291, and −8.362 kcal/mol, respectively, and a high binding affinity of 3″(1‴-O-β-D-glucopyranosyl)-sucrose with GST with −7.24 kcal/mol. Accordingly, and for the first time, our results highlighted the scabicidal potential of coconut seed extract, which opens the gate for an efficient, cost-effective as well as herbal-based alternative for the control of scabies in rabbits. Full article

(This article belongs to the Special Issue Discovery and Development of Novel Therapeutic Agents in Infectious Diseases Treatment)

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13 pages, 1230 KiB

Open AccessArticle

Bacteriocins Revitalize Non-Effective Penicillin G to Overcome Methicillin-Resistant Staphylococcus pseudintermedius

by Kirill V. Ovchinnikov, Christian Kranjec, Tage Thorstensen, Harald Carlsen and Dzung B. Diep

Antibiotics 2022, 11(12), 1691; https://doi.org/10.3390/antibiotics11121691 - 24 Nov 2022

Cited by 2 | Viewed by 2261

Abstract

The rise of antibiotic-resistant bacteria is among the biggest challenges in human and veterinary medicine. One of the major factors that contributes to resistance is use of frontline clinical antibiotics in veterinary practices. To avoid this problem, searching for antimicrobials aimed at veterinary applications is becoming especially important. Thiopeptide micrococcin P1 and leaderless peptide EntEJ97s are two different bacteriocins that are very active against many gram-positive bacteria; however, sensitive bacteria can rapidly develop resistance towards those bacteriocins. To overcome this problem, we searched for synergy between those bacteriocins and conventional antibiotics against methicillin-resistant Staphylococcus pseudintermedius (MRSP): a common pathogen in animal skin infections. The two bacteriocins acted synergistically with each other and with penicillin G against MRSP clinical isolates in both planktonic and biofilm assays; they also prevented resistance development. The therapeutic potential was further validated in a murine skin infection model that showed that a combination of micrococcin P1, EntEJ97s and penicillin G reduced cell-forming units of MRSP by 2-log₁₀ CFU/g. Taken together, our data show that a combination of bacteriocins with conventional antibiotics can not only prevent resistance development but also pave the way to revitalize some old, less useful antibiotics, such as penicillin, which by itself has no effect on methicillin-resistant pathogens. Full article

(This article belongs to the Special Issue Discovery and Development of Novel Therapeutic Agents in Infectious Diseases Treatment)

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Review

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58 pages, 11867 KiB

Open AccessReview

Recent Advances in Pharmaceutical Approaches of Antimicrobial Agents for Selective Delivery in Various Administration Routes

by Ardiyah Nurul Fitri Marzaman, Tri Puspita Roska, Sartini Sartini, Rifka Nurul Utami, Sulistiawati Sulistiawati, Cindy Kristina Enggi, Marianti A. Manggau, Latifah Rahman, Venkatram Prasad Shastri and Andi Dian Permana

Antibiotics 2023, 12(5), 822; https://doi.org/10.3390/antibiotics12050822 - 27 Apr 2023

Cited by 1 | Viewed by 3387

Abstract

Globally, the increase of pathogenic bacteria with antibiotic-resistant characteristics has become a critical challenge in medical treatment. The misuse of conventional antibiotics to treat an infectious disease often results in increased resistance and a scarcity of effective antimicrobials to be used in the future against the organisms. Here, we discuss the rise of antimicrobial resistance (AMR) and the need to combat it through the discovery of new synthetic or naturally occurring antibacterial compounds, as well as insights into the application of various drug delivery approaches delivered via various routes compared to conventional delivery systems. AMR-related infectious diseases are also discussed, as is the efficiency of various delivery systems. Future considerations in developing highly effective antimicrobial delivery devices to address antibiotic resistance are also presented here, especially on the smart delivery system of antibiotics. Full article

(This article belongs to the Special Issue Discovery and Development of Novel Therapeutic Agents in Infectious Diseases Treatment)

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88 pages, 33720 KiB

Open AccessReview

Conjugation as a Tool in Therapeutics: Role of Amino Acids/Peptides-Bioactive (Including Heterocycles) Hybrid Molecules in Treating Infectious Diseases

by Rohith Gattu, Sanjay S. Ramesh, Siddaram Nadigar, Channe Gowda D and Suhas Ramesh

Antibiotics 2023, 12(3), 532; https://doi.org/10.3390/antibiotics12030532 - 07 Mar 2023

Cited by 6 | Viewed by 2699

Abstract

Peptide-based drugs are gaining significant momentum in the modern drug discovery, which is witnessed by the approval of new drugs by the FDA in recent years. On the other hand, small molecules-based drugs are an integral part of drug development since the past several decades. Peptide-containing drugs are placed between small molecules and the biologics. Both the peptides as well as the small molecules (mainly heterocycles) pose several drawbacks as therapeutics despite their success in curing many diseases. This gap may be bridged by utilising the so called ‘conjugation chemistry’, in which both the partners are linked to one another through a stable chemical bond, and the resulting conjugates are found to possess attracting benefits, thus eliminating the stigma associated with the individual partners. Over the past decades, the field of molecular hybridisation has emerged to afford us new and efficient molecular architectures that have shown high promise in medicinal chemistry. Taking advantage of this and also considering our experience in this field, we present herein a review concerning the molecules obtained by the conjugation of peptides (amino acids) to small molecules (heterocycles as well as bioactive compounds). More than 125 examples of the conjugates citing nearly 100 references published during the period 2000 to 2022 having therapeutic applications in curing infectious diseases have been covered. Full article

(This article belongs to the Special Issue Discovery and Development of Novel Therapeutic Agents in Infectious Diseases Treatment)

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Other

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20 pages, 2665 KiB

Open AccessSystematic Review

The Efficacy and Safety of Bedaquiline in the Treatment of Pulmonary Tuberculosis Patients: A Systematic Review and Meta-Analysis

by Enyu Tong, Qian Wu, Yiming Chen, Zhengwei Liu, Mingwu Zhang, Yelei Zhu, Kunyang Wu, Junhang Pan and Jianmin Jiang

Antibiotics 2023, 12(9), 1389; https://doi.org/10.3390/antibiotics12091389 - 31 Aug 2023

Viewed by 1219

Abstract

Background: Bedaquiline (BDQ) has been designated as a Group A drug by the World Health Organization (WHO) for the management of multi-drug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB). This systematic review and meta-analysis aim to evaluate the efficacy and safety of BDQ-containing regimens for the treatment of patients with pulmonary TB. Methods: PubMed (MEDLINE), Elton B. Stephens Company (EBSCO) database, the Cochrane Register of Controlled Trials, and the China National Knowledge Infrastructure (CNKI) database were initially searched on 15 June 2022 and again on 20 March 2023. We included randomized controlled trials (RCTs) and non-randomized studies (NRSs) that administered BDQ to TB patients. The outcomes of interest were as follows: (1) efficacy, including the rate of sputum culture conversion at 8 weeks, 24 weeks, and during follow-up, as well as the rates of completion cure, death, treatment failure, and loss at follow-up and at the end of the treatment; and (2) safety, which encompassed the incidences of cardiotoxicity, hepatotoxicity, and grade 3–5 adverse events during the treatment period. Results: A total of 29 articles were included in this meta-analysis, representing 23,358 individuals. Patients who were treated with BDQ were compared with patients who were not exposed to BDQ. The use of BDQ-containing regimens demonstrated improved rates of sputum conversion in RCTs at 24 weeks (RR = 1.27, 95% CI: 1.10 to 1.46) and during follow-up (RR = 1.33, 95% CI: 1.06 to 1.66). Additionally, BDQ-containing regimens showed increased cure rates (RR = 1.60, 95% CI: 1.13 to 2.26) and decreased failure rates (RR = 0.56, 95% CI: 0.56 to 0.88). In NRSs, BDQ-containing regimens improved the sputum culture conversion rate during follow-up (RR = 1.53, 95% CI: 1.07 to 2.20), increased the rate of cure (RR = 1.86, 95% CI: 1.23 to 2.83), reduced deaths from all causes (RR = 0.68, 95% CI: 0.48 to 0.97), and reduced failure rates (RR = 0.57, 95% CI: 0.46 to 0.71). However, the use of BDQ-containing regimens was associated with increased incidences of cardiotoxicity (RR = 4.54, 95% CI: 1.74 to 11.87) and grade 3–5 adverse events (RR = 1.42, 95% CI: 1.17 to 1.73) in RCTs. NRSs also showed an association between BDQ-containing regimens and cardiotoxicity (RR = 6.00, 95% CI: 1.32 to 27.19). No significant differences were observed between intervention groups and control groups with respect to other outcomes. Conclusions: Data from both RCTs and NRSs support the efficacy of BDQ for the treatment of pulmonary tuberculosis. However, the use of BDQ is associated with a higher incidence of cardiotoxicity and serious adverse events. Comparative data on efficacy and safety are limited, and further confirmation is required, due to potential bias and discrepancies in the available studies. Full article

(This article belongs to the Special Issue Discovery and Development of Novel Therapeutic Agents in Infectious Diseases Treatment)

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