New Natural Products as Candidates for the Discovery of Antimicrobial Drugs

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 (31 January 2024) | Viewed by 3478

Special Issue Editors


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The Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria
Interests: cytotoxicity of drugs and drug-delivery systems; experimental chemotherapy; signal transduction; pharmacodynamics
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Guest Editor
Department of Infectious Microbiology, The Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, 26 Acad. G. Bonchev Str., 1113 Sofia, Bulgaria
Interests: pathogenic bacteria; food-borne zoonozes; virulence factors; bacteria–host relationships; infectious immunology; molecular biology; ecology of pathogens; new antibacterial agents; antimicrobial resistance
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Nowadays, there is an urgent need to find and develop new compounds to fight life-threatening bacterial, fungal, and viral infections and to determine the ability of these pathogens to develop resistance to currently used treatment strategies. Currently, antibiotics are the main anti-infective strategy for patients in infectious, trauma, intensive care units. Unfortunately, their effectiveness is decreasing across the globe due to global emergence of multi-drug-resistant (MDR) bacterial pathogens, turning bacterial infections into a serious concern.

The prevention of the methicillin-resistant Staphylococcus aureus (MRSA) that is spreading in healthcare facilities is a huge infection control challenge because these infections remain a serious cause of healthcare-associated infections around the world. Although their prevalence among patients has decreased in many countries all over the world, this remains an important concern for healthcare professionals and scientists. Increased public awareness towards MRSA in the framework of various initiatives, events, еtc., may contribute to the search for new products of natural origin (plant, animal, microalgal, etc.) as candidates for anti-MRSA control and therapy. These include various essential oils, small antimicrobial peptides of animal origin, bacteriocines, and different plant compounds such as triterpenoids, alkaloids, phenols, flavonoids, etc., that have antimicrobial activity. Many studies have focused on the isolation, characterization, and improvement of their stability as well as the bioavailability, cellular uptake and internalization, pharmacokinetic profile, and reduction of the toxicity of the tested compounds. Attention has been focused on a number of nanocarriers, such as liposomes, microemulsion systems for drug delivery, nanocapsules, solid lipid nanoparticles, polymeric micelles, etc. Even if the majority of studies related to the evaluation of the biological activity are still in the in vitro or in silico stages, their internalization in nanocarriers represents the future of “green therapeutics”. 

To summarize, new compounds with well-defined activity and mechanisms against MDR pathogens, e.g., MRSA, need to be developed urgently. In this context, this Special Issue will focus on recent studies on the modern ways and future directions to search for the next generation safe and effective antimicrobial compounds, including those derived from phytochemicals, antimicrobial peptides, metalloantibiotics, efflux pump inhibitors, etc., to control the infections caused by emerging MDR pathogens.

Dr. Maya Zaharieva
Prof. Dr. Hristo Najdenski
Guest Editors

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Keywords

  • natural products
  • MRSA
  • antimicrobial mechanisms and strategies
  • combination effects
  • clinical applicability
  • in silico, in vitro and in vivo models
  • infection control

Published Papers (2 papers)

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Research

12 pages, 12893 KiB  
Article
Green Synthesis of Na abietate Obtained from the Salification of Pinus elliottii Resin with Promising Antimicrobial Action
by Aline B. Schons, Patrícia Appelt, Jamille S. Correa, Mário A. A. Cunha, Mauricio G. Rodrigues and Fauze J. Anaissi
Antibiotics 2023, 12(3), 514; https://doi.org/10.3390/antibiotics12030514 - 04 Mar 2023
Cited by 3 | Viewed by 1347
Abstract
The growing concern about the emergence of increasingly antibiotic-r4esistant bacteria imposes the need to search and develop drugs to combat these microorganisms. This, combined with the search for low-cost synthesis methods, was the motivation for the elaboration of this work. Abietic acid present [...] Read more.
The growing concern about the emergence of increasingly antibiotic-r4esistant bacteria imposes the need to search and develop drugs to combat these microorganisms. This, combined with the search for low-cost synthesis methods, was the motivation for the elaboration of this work. Abietic acid present in the resin of Pinus elliotti var. elliotti was used to generate a sodium salt by salification. The synthesis route was low-cost, consisting of only two reaction steps at mild temperatures without toxic organic solvents, and eco-friendly and easy to conduct on an industrial scale. Sodium abietate (Na-C20H29O2) was characterized by mass spectrometry, infrared spectroscopy, elemental analysis, X-ray diffraction, scanning electron microscopy, and energy-dispersive spectroscopy. To perform the antimicrobial tests, the determination of minimum inhibitory concentration and the disk diffusion assay was performed. The results obtained showed that the salt Na abietate performed an antimicrobial action against the bacterial strains S. aureus, E. coli, L.monocytogenes, and S. enterica Typhimurium and the yeast C. albicans. The disk diffusion test showed a high inhibition potential against S. enterica compared to the standard antimicrobial tetracycline, as an inhibition index of 1.17 was found. For the other bacterial strains, the inhibition values were above 40%. The MIC test showed promising results in the inhibition of E. coli, L. monocytogenes, and C. albicans, indicating bacteriostatic activity against the first microorganism and bactericidal and fungicidal activities against the others. Therefore, the results showed the action of Na abietate as a possible effective antimicrobial drug, highlighting its sustainability within a circular economy. Full article
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14 pages, 5577 KiB  
Article
Antibacterial Activity of Squaric Amide Derivative SA2 against Methicillin-Resistant Staphylococcus aureus
by Moxi Yu, Yachen Hou, Meiling Cheng, Yongshen Liu, Caise Ling, Dongshen Zhai, Hui Zhao, Yaoyao Li, Yamiao Chen, Xiaoyan Xue, Xue Ma, Min Jia, Bin Wang, Pingan Wang and Mingkai Li
Antibiotics 2022, 11(11), 1497; https://doi.org/10.3390/antibiotics11111497 - 28 Oct 2022
Cited by 1 | Viewed by 1657
Abstract
Methicillin-resistant Staphylococcus aureus (MRSA)-caused infection is difficult to treat because of its resistance to commonly used antibiotic, and poses a significant threat to public health. To develop new anti-bacterial agents to combat MRSA-induced infections, we synthesized novel squaric amide derivatives and evaluated their [...] Read more.
Methicillin-resistant Staphylococcus aureus (MRSA)-caused infection is difficult to treat because of its resistance to commonly used antibiotic, and poses a significant threat to public health. To develop new anti-bacterial agents to combat MRSA-induced infections, we synthesized novel squaric amide derivatives and evaluated their anti-bacterial activity by determining the minimum inhibitory concentration (MIC). Additionally, inhibitory activity of squaric amide 2 (SA2) was measured using the growth curve assay, time-kill assay, and an MRSA-induced skin infection animal model. A scanning electron microscope and transmission electron microscope were utilized to observe the effect of SA2 on the morphologies of MRSA. Transcriptome analysis and real-time PCR were used to test the possible anti-bacterial mechanism of SA2. The results showed that SA2 exerted bactericidal activity against a number of MRSA strains with an MIC at 4–8 µg/mL. It also inhibited the bacterial growth curve of MRSA strains in a dose-dependent manner, and reduced the colony formation unit in 4× MIC within 4–8 h. The infective lesion size and the bacterial number in the MRSA-induced infection tissue of mice were reduced significantly within 7 days after SA2 treatment. Moreover, SA2 disrupted the bacterial membrane and alanine dehydrogenase-dependent NAD+/NADH homeostasis. Our data indicates that SA2 is a possible lead compound for the development of new anti-bacterial agents against MRSA infection. Full article
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