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Antibiotics
Special Issues
Research and Development of Antibiotics
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Research and Development of Antibiotics

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "The Global Need for Effective Antibiotics".

Deadline for manuscript submissions: closed (30 September 2021) | Viewed by 25218

Special Issue Editor

Prof. Dr. Jesus Simal-Gandara

grade E-Mail Website
Guest Editor
Department of Analytical and Food Chemistry, Food Science and Technology Faculty, University of Vigo, 32004 Ourense, Spain
Interests: agro-environmental; food chemistry; sustainable primary production; food quality and safety
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antimicrobial resistance, especially in the current COVID-19 crisis, has led to the wide spread of highly resistant microorganism strains that threaten the viability of the global health system. While many alternative antimicrobial methods show interesting potential, it is difficult to see how they will be useful in the near future. This particular Special Issue of antibiotics is intended to be the sum of opinions, perspectives, reviews, and unique research manuscripts that provide a view of the current state for developing antibiotics, including inputs from industry and academia. Sharing resources can increase the availability of research on natural products as drug candidates. Product development, innovation and accessibility must be prioritized around the world, along with a research agenda that addresses this issue.

Keywords

  • Natural candidates as antimicrobians
  • novel antimicrobians
  • antimicrobian resistance
  • bacterial and other infections
  • antiomicrobians innovation

Published Papers (5 papers)

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Research

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12 pages, 2316 KiB  
Article
A Mitochondria-Penetrating Peptide Exerts Potent Anti-Plasmodium Activity and Localizes at Parasites’ Mitochondria
by Sangdao Somsri, Mathirut Mungthin, Natthaporn Klubthawee, Poom Adisakwattana, Warunee Hanpithakpong and Ratchaneewan Aunpad
Antibiotics 2021, 10(12), 1560; https://doi.org/10.3390/antibiotics10121560 - 20 Dec 2021
Cited by 7 | Viewed by 2745
Abstract
Mitochondria are considered a novel drug target as they play a key role in energy production and programmed cell death of eukaryotic cells. The mitochondria of malaria parasites differ from those of their vertebrate hosts, contributing to the drug selectivity and the development [...] Read more.
Mitochondria are considered a novel drug target as they play a key role in energy production and programmed cell death of eukaryotic cells. The mitochondria of malaria parasites differ from those of their vertebrate hosts, contributing to the drug selectivity and the development of antimalarial drugs. (Fxr)3, a mitochondria-penetrating peptide or MPP, entered malaria-infected red cells without disrupting the membrane and subsequently killed the blood stage of P. falciparum parasites. The effects were more potent on the late stages than on the younger stages. Confocal microscopy showed that the (Fxr)3 intensely localized at the parasite mitochondria. (Fxr)3 highly affected both the lab-strain, chloroquine-resistant K1, and freshly isolated malaria parasites. (Fxr)3 (1 ng/mL to 10 μg/mL) was rarely toxic towards various mammalian cells, i.e., mouse fibroblasts (L929), human leukocytes and erythrocytes. At a thousand times higher concentration (100 μg/mL) than that of the antimalarial activity, cytotoxicity and hemolytic activity of (Fxr)3 were observed. Compared with the known antimalarial drug, atovaquone, (Fxr)3 exhibited more rapid killing activity. This is the first report on antimalarial activity of (Fxr)3, showing localization at parasites’ mitochondria. Full article
(This article belongs to the Special Issue Research and Development of Antibiotics)
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13 pages, 1555 KiB  
Article
Seconeolitsine, the Novel Inhibitor of DNA Topoisomerase I, Protects against Invasive Pneumococcal Disease Caused by Fluoroquinolone-Resistant Strains
by Jose Manuel Tirado-Vélez, David Carreño, David Sevillano, Luis Alou, José Yuste and Adela G. de la Campa
Antibiotics 2021, 10(5), 573; https://doi.org/10.3390/antibiotics10050573 - 13 May 2021
Cited by 2 | Viewed by 1891
Abstract
Antibiotic resistance in Streptococcus pneumoniae has increased worldwide, making fluoroquinolones an alternative therapeutic option. Fluoroquinolones inhibit the type II DNA topoisomerases (topoisomerase IV and gyrase). In this study we have evaluated the in vivo activity of seconeolitsine, an inhibitor of topoisomerase I. Levofloxacin [...] Read more.
Antibiotic resistance in Streptococcus pneumoniae has increased worldwide, making fluoroquinolones an alternative therapeutic option. Fluoroquinolones inhibit the type II DNA topoisomerases (topoisomerase IV and gyrase). In this study we have evaluated the in vivo activity of seconeolitsine, an inhibitor of topoisomerase I. Levofloxacin (12.5 to 50 mg/kg) or seconeolitsine (5 to 40 mg/kg) were administered every 12 h during two days in mice infected with a serotype 8-resistant strain. At 48 h, a 70% protection was obtained with seconeolitsine (40 mg/kg; p < 0.001). However, survival with levofloxacin was 20%, regardless of the dose. In addition, seconeolitsine decreased bacteremia efficiently. Levofloxacin had higher levels in serum than seconeolitsine (Cmax of 14.7 vs. 1.6; p < 0.01) and higher values of area under the serum concentration-time curve (AUC0-12h of 17.3 vs. 5; p < 0.01). However, seconeolitsine showed higher levels of time to peak concentration and elimination half-life. This is consistent with the higher binding of seconeolitsine to plasma proteins (40% and 80% when used at 1 µg/mL and 50 µg/mL, respectively) in comparison to levofloxacin (12% at 5 µg/mL and 33% at 50 µg/mL). Our results suggest that seconeolitsine would be a promising therapeutic alternative against pneumococcal isolates with high fluoroquinolone resistance levels. Full article
(This article belongs to the Special Issue Research and Development of Antibiotics)
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Review

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27 pages, 1840 KiB  
Review
Potential Environmental and Human Health Risks Caused by Antibiotic-Resistant Bacteria (ARB), Antibiotic Resistance Genes (ARGs) and Emerging Contaminants (ECs) from Municipal Solid Waste (MSW) Landfill
by Uttpal Anand, Bhaskar Reddy, Vipin Kumar Singh, Amit Kishore Singh, Kavindra Kumar Kesari, Pooja Tripathi, Pradeep Kumar, Vijay Tripathi and Jesus Simal-Gandara
Antibiotics 2021, 10(4), 374; https://doi.org/10.3390/antibiotics10040374 - 01 Apr 2021
Cited by 80 | Viewed by 11404
Abstract
The disposal of municipal solid waste (MSW) directly at landfills or open dump areas, without segregation and treatment, is a significant concern due to its hazardous contents of antibiotic-resistant bacteria (ARB), antibiotic resistance genes (ARGs), and metal resistance genes (MGEs). The released leachate [...] Read more.
The disposal of municipal solid waste (MSW) directly at landfills or open dump areas, without segregation and treatment, is a significant concern due to its hazardous contents of antibiotic-resistant bacteria (ARB), antibiotic resistance genes (ARGs), and metal resistance genes (MGEs). The released leachate from landfills greatly effects the soil physicochemical, biological, and groundwater properties associated with agricultural activity and human health. The abundance of ARB, ARGs, and MGEs have been reported worldwide, including MSW landfill sites, animal husbandry, wastewater, groundwater, soil, and aerosol. This review elucidates the occurrence and abundance of ARB, ARGs, and MRGs, which are regarded as emerging contaminants (ECs). Recently, ECs have received global attention because of their prevalence in leachate as a substantial threat to environmental and public health, including an economic burden for developing nations. The present review exclusively discusses the demands to develop a novel eco-friendly management strategy to combat these global issues. This review also gives an intrinsic discussion about the insights of different aspects of environmental and public health concerns caused due to massive leachate generation, the abundance of antibiotics resistance (AR), and the effects of released leachate on the various environmental reservoirs and human health. Furthermore, the current review throws light on the source and fate of different ECs of landfill leachate and their possible impact on the nearby environments (groundwater, surface water, and soil) affecting human health. The present review strongly suggests the demand for future research focuses on the advancement of the removal efficiency of contaminants with the improvement of relevant landfill management to reduce the potential effects of disposable waste. We propose the necessity of the identification and monitoring of potential environmental and human health risks associated with landfill leachate contaminants. Full article
(This article belongs to the Special Issue Research and Development of Antibiotics)
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12 pages, 663 KiB  
Review
Essential Oils as Antimicrobials in Crop Protection
by María Alonso-Gato, Gonzalo Astray, Juan C. Mejuto and Jesus Simal-Gandara
Antibiotics 2021, 10(1), 34; https://doi.org/10.3390/antibiotics10010034 - 01 Jan 2021
Cited by 42 | Viewed by 5593
Abstract
At present, organic crops have reached an important boom in a society increasingly interested in the conservation of the environment and sustainability. It is evident that a part of the population in the Western world focuses their concern on how to obtain our [...] Read more.
At present, organic crops have reached an important boom in a society increasingly interested in the conservation of the environment and sustainability. It is evident that a part of the population in the Western world focuses their concern on how to obtain our food and on doing it in a way that is as respectful as possible with the environment. In this review, we present a compilation of the work carried out with the use of essential oils as an alternative in the fight against different bacteria and fungi that attack crops and related products. Given the collected works, the efficacy of essential oils for their use as pesticides for agricultural use is evident. Full article
(This article belongs to the Special Issue Research and Development of Antibiotics)
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Other

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12 pages, 1439 KiB  
Project Report
Antibiotic Biosynthesis Pathways from Endophytic Streptomyces SUK 48 through Metabolomics and Genomics Approaches
by Mohd Shukri Baba, Noraziah Mohamad Zin, Siti Junaidah Ahmad, Noor Wini Mazlan, Syarul Nataqain Baharum, Nuraziemah Ahmad and Fazren Azmi
Antibiotics 2021, 10(8), 969; https://doi.org/10.3390/antibiotics10080969 - 12 Aug 2021
Cited by 4 | Viewed by 2698
Abstract
Streptomyces sp. has been known to be a major antibiotic producer since the 1940s. As the number of cases related to resistance pathogens infection increases yearly, discovering the biosynthesis pathways of antibiotic has become important. In this study, we present the streamline of [...] Read more.
Streptomyces sp. has been known to be a major antibiotic producer since the 1940s. As the number of cases related to resistance pathogens infection increases yearly, discovering the biosynthesis pathways of antibiotic has become important. In this study, we present the streamline of a project report summary; the genome data and metabolome data of newly isolated Streptomyces SUK 48 strain are also analyzed. The antibacterial activity of its crude extract is also determined. To obtain genome data, the genomic DNA of SUK 48 was extracted using a commercial kit (Promega) and sent for sequencing (Pac Biosciences technology platform, Menlo Park, CA, USA). The raw data were assembled and polished using Hierarchical Genome Assembly Process 4.0 (HGAP 4.0). The assembled data were structurally predicted using tRNAscan-SE and rnammer. Then, the data were analyzed using Kyoto Encyclopedia of Genes and Genomes (KEGG) database and antiSMASH analysis. Meanwhile, the metabolite profile of SUK 48 was determined using liquid chromatography-mass spectrophotometry (LC-MS) for both negative and positive modes. The results showed that the presence of kanamycin and gentamicin, as well as the other 11 antibiotics. Nevertheless, the biosynthesis pathways of aurantioclavine were also found. The cytotoxicity activity showed IC50 value was at 0.35 ± 1.35 mg/mL on the cell viability of HEK 293. In conclusion, Streptomyces sp. SUK 48 has proven to be a non-toxic antibiotic producer such as auranticlavine and gentamicin. Full article
(This article belongs to the Special Issue Research and Development of Antibiotics)
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