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Antibiotics
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The Search for Antimicrobial Agents from Natural Products
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The Search for Antimicrobial Agents from Natural Products

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Plant-Derived Antibiotics".

Deadline for manuscript submissions: 15 May 2025 | Viewed by 12159

Special Issue Editors

Dr. Carolina P. Reyes

E-Mail Website
Guest Editor
Instituto Universitario de Bio-Orgánica “Antonio González”, Departamento de Bioquímica, Microbiología, Biología Celular y Genética, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez, La Laguna, Spain
Interests: natural products; medicinal chemistry; antimicrobial agents; microalgae; phylogeny
Dr. Antonio Francioso

E-Mail Website
Guest Editor
Department of Bioscience and Technology for Food Agriculture and Environment, University of Teramo, Teramo, Italy
Interests: natural bioactive compounds; bio-organic chemistry; analytical biochemistry; ethnopharmacology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Traditionally, there has been a growing interest in exploring natural products as a reservoir of unique chemical structures that have been finely honed by evolution for their capacity to interact with biological molecular targets. Derived from diverse sources such as plants, fungi, marine organisms, and microorganisms, these natural compounds offer a treasure trove of bioactive molecules with the potential to serve as potent antimicrobial agents. This exploration into the therapeutic potential of natural products not only provides a promising avenue for combating antimicrobial resistance but also presents opportunities to circumvent the limitations associated with conventional antibiotics.

This Special Issue underscores the interdisciplinary nature of natural product research, drawing upon insights from chemistry, biochemistry, microbiology, pharmacology, and bioinformatics to accelerate the discovery and development of novel antimicrobial agents. Moreover, this Special Issue delves into the underlying mechanisms of action driving the antimicrobial efficacy of natural products, providing insights into their molecular interactions and therapeutic potential. By unraveling the intricate interplay between these compounds and microbial targets, researchers aim to harness their full therapeutic potential while minimizing the risk of resistance development. By highlighting the unique chemical structures and evolutionary adaptations of these compounds, we hope to inspire further exploration and innovation in this dynamic field, ultimately paving the way for the development new antimicrobial agents.

Dr. Carolina P. Reyes
Dr. Antonio Francioso
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

  • natural products
  • antimicrobial agents
  • drug discovery
  • mechanism of action
  • pharmacology

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Published Papers (6 papers)

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Research

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19 pages, 4004 KiB  
Article
Antioxidant: Antimycobacterial and Antibiofilm Activities of Acetone Extract and Subfraction Artemisia afra Jacq. ex Willd. Against Mycobacterium smegmatis
by Mabasa Precious Matlala, Mashilo Mash Matotoka, Wanda Shekwa and Peter Masoko
Antibiotics 2024, 13(11), 1027; https://doi.org/10.3390/antibiotics13111027 - 31 Oct 2024
Cited by 1 | Viewed by 1206
Abstract
Tuberculosis is a worldwide prevalent and recurring disease that contributes significantly to high mortality rates. This study aimed to investigate the antioxidant, anti-mycobacterial, and antibiofilm activities of Artemisia afra acetone crude extract. Methodology: The crude acetone extract was fractionated using column chromatography and [...] Read more.
Tuberculosis is a worldwide prevalent and recurring disease that contributes significantly to high mortality rates. This study aimed to investigate the antioxidant, anti-mycobacterial, and antibiofilm activities of Artemisia afra acetone crude extract. Methodology: The crude acetone extract was fractionated using column chromatography and characterized by liquid chromatography–mass spectroscopy (LC-MS). A 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay was used to assess the antioxidant activity. The antimycobacterial activity against Mycobacterium smegmatis was screened using bioautography, broth microdilution, and growth curve assays. Molecular docking was used to predict the possible mechanisms of action of the LC-MS-identified ligands. Crystal violet was used to screen for anti-cell adherence and biofilm inhibition activities. Results: The crude extract scavenged 77% of the free radical at 16 μg/mL. The subfraction had a lower minimum inhibitory concentration (MIC) (0.078 mg/mL) compared to the crude extract (0.313–0.833 mg/mL). The subfraction had a concentration-dependent inhibition effect (>50%) on mycobacterial cell adherence and early biofilms. However, the mature biofilms were resistant. Two propanoate compounds, [(2S)-3-[6-acetyl-4,6-dihydroxy-3-[(1R)-1-hydroxyethyl]tetrahydropyran-2-yl]-2-hydroxy-propyl] (2R)-2-amino-3-(1H-imidazol-5-yl)propanoate and 3-(6-aminopurin-9-yl)propyl 3-(2,4-dioxo-1,3-diazaspiro[4.5]decan-3-yl) propanoate, had binding energies of −5.4 kcal/mol and −6.3 kcal/mol, respectively, against the RNA polymerase binding protein. Conclusions: The results show that A. afra acetone crude extract has antioxidant and antimycobacterial activities that can be improved by fractionation. Full article
(This article belongs to the Special Issue The Search for Antimicrobial Agents from Natural Products)
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9 pages, 276 KiB  
Communication
Sustainable Bacterial Control of Hatching Eggshells Using Essential Oils
by Igor Rafael Ribeiro Vale, Gabriel da Silva Oliveira, Luana Maria de Jesus, Marcio Botelho de Castro, Concepta McManus and Vinícius Machado dos Santos
Antibiotics 2024, 13(11), 1025; https://doi.org/10.3390/antibiotics13111025 - 31 Oct 2024
Cited by 1 | Viewed by 1028
Abstract
Background: Decontamination of poultry surfaces through appropriate hygiene and sanitation measures can partially mitigate bacterial problems, as this process does not result in the complete elimination of bacteria. Thus, the remaining bacteria can persist and contaminate eggshells. Therefore, regardless of the rigor of [...] Read more.
Background: Decontamination of poultry surfaces through appropriate hygiene and sanitation measures can partially mitigate bacterial problems, as this process does not result in the complete elimination of bacteria. Thus, the remaining bacteria can persist and contaminate eggshells. Therefore, regardless of the rigor of the sanitary standards applied on farms, it is suggested that hatching eggs be subjected to the sanitization process. Here, we investigated the effectiveness of essential oil-based antibacterial agents in sanitizing eggs. Results: The results indicated that essential oils from Cinnamomum cassia (L.) J. Presl. (CCEO), Syzygium aromaticum (L.) Merr. & L.M. Perry (SAEO) and Cymbopogon nardus (L.) Rendle (CNEO), at specific concentrations, have antibacterial effects in vitro, reducing the load of mesophilic bacteria and enterobacteria in the eggshell by at least 3 and 2 log10 CFU/mL, respectively. Conclusion: The adoption of CCEO, SAEO and CNEO to reduce the bacterial load on eggshells could be a favorable change to the conventional protocol of egg sanitization with formaldehyde, especially on farms where sanitary standards are insufficient. Full article
(This article belongs to the Special Issue The Search for Antimicrobial Agents from Natural Products)
12 pages, 3111 KiB  
Article
Antibacterial and Antibiofilm Potential of Chlorophyllin Against Streptococcus mutans In Vitro and In Silico
by Seemrose Khan, Ihtisham Ul Haq, Imran Ali, Abdul Rehman, Mazen Almehmadi, Meshari A. Alsuwat, Tariq Zaman and Muhammad Qasim
Antibiotics 2024, 13(9), 899; https://doi.org/10.3390/antibiotics13090899 - 20 Sep 2024
Cited by 3 | Viewed by 2241
Abstract
Background: Streptococcus mutans is a leading causative agent of dental caries and exerts pathogenicity by forming biofilms. Dental caries continues to be a significant public health issue worldwide, affecting an estimated 2.5 billion people, showing a 14.6% increase over the past decade. Herein, [...] Read more.
Background: Streptococcus mutans is a leading causative agent of dental caries and exerts pathogenicity by forming biofilms. Dental caries continues to be a significant public health issue worldwide, affecting an estimated 2.5 billion people, showing a 14.6% increase over the past decade. Herein, the antibacterial potential of Chlorophyllin extracted from Spinacia oleracea was evaluated against biofilm-forming S. mutans via in vitro and in silico studies. Methodology: The antimicrobial activity of chlorophyllin extract against S. mutans isolates was tested using the agar well diffusion method. Chlorophyllin extract was also tested against biofilm-forming isolates of S. mutans. Chlorophyllin was docked with the antigen I/II (AgI/II) protein of S. mutans to evaluate its antimicrobial mechanism. The chemical structure and canonical SMILES format of Chlorophyllin were obtained from PubChem. Additionally, adsorption, distribution, metabolism, excretion, and toxicity (ADMET) analyses of Chlorophyllin were performed using ADMETlab 2.0 to assess its pharmacokinetic properties. Results: An agar well diffusion assay revealed that all S. mutans isolates were susceptible to Chlorophyllin extract and showed a variety of inhibition zones ranging from 32 to 41 mm. Chlorophyllin reduces the biofilm strength of four isolates from strong to moderate and six from strong to weak. The antibiofilm potential of Chlorophyllin was measured by a reduction in the number of functional groups observed in the Fourier Transform Infrared Spectrometer (FTIR) spectra of the extracellular polymeric substance (EPS) samples. Chlorophyllin showed binding with AgI/II proteins of S. mutans, which are involved in adherence to the tooth surface and initiating biofilm formation. The ADMET analysis revealed that the safety of Chlorophyllin exhibited favorable pharmacokinetic properties. Conclusions: Chlorophyllin stands out as a promising antibacterial and antibiofilm agent against biofilm-forming S. mutans, and its safety profile highlights its potential suitability for further investigation as a therapeutic agent. Full article
(This article belongs to the Special Issue The Search for Antimicrobial Agents from Natural Products)
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Review

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42 pages, 8074 KiB  
Review
Antibacterial Activity of Selected Essential Oil Components and Their Derivatives: A Review
by Vuyolwethu Khwaza and Blessing A. Aderibigbe
Antibiotics 2025, 14(1), 68; https://doi.org/10.3390/antibiotics14010068 - 10 Jan 2025
Cited by 2 | Viewed by 3037
Abstract
Essential oils (EOs) are gaining ground and have been intensively studied due to their widespread use in the pharmaceutical, food, and cosmetics industries. The essential components of EOs have been recognized for diverse therapeutic activities and have gained significant attention for their potential [...] Read more.
Essential oils (EOs) are gaining ground and have been intensively studied due to their widespread use in the pharmaceutical, food, and cosmetics industries. The essential components of EOs have been recognized for diverse therapeutic activities and have gained significant attention for their potential antibacterial activities. Despite the popularity of EOs and potent biological properties, their bioactive components and their derivatives are still not comprehensively characterized. This review explores the antibacterial efficacy of selected EO components and their derivatives, focusing on monoterpenes chosen (i.e., carvacrol, menthol, and thymol) and phenylpropanoids (i.e., cinnamaldehyde and eugenol). Furthermore, this review highlights recent advancements in developing derivatives of these EO components, which have shown improved antibacterial activity with reduced toxicity. By summarizing recent studies, this review reveals the potential of these natural compounds and their derivatives as promising candidates for pharmaceuticals, food preservation, and as alternatives to synthetic antibiotics in combating bacterial resistance. Full article
(This article belongs to the Special Issue The Search for Antimicrobial Agents from Natural Products)
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19 pages, 1749 KiB  
Review
Biochemistry and Future Perspectives of Antibiotic Resistance: An Eye on Active Natural Products
by Giulia Caioni, Carolina Pérez Reyes, Davide Laurenti, Carmen Chiaradia, Enrico Dainese, Roberto Mattioli, Daniel Di Risola, Eleonora Santavicca and Antonio Francioso
Antibiotics 2024, 13(11), 1071; https://doi.org/10.3390/antibiotics13111071 - 11 Nov 2024
Cited by 2 | Viewed by 1890
Abstract
Antibiotic resistance poses a serious threat to the current healthcare system, negatively impacting the effectiveness of many antimicrobial treatments. The situation is exacerbated by the widespread overuse and abuse of available antibiotics, accelerating the evolution of resistance. Thus, there is an urgent need [...] Read more.
Antibiotic resistance poses a serious threat to the current healthcare system, negatively impacting the effectiveness of many antimicrobial treatments. The situation is exacerbated by the widespread overuse and abuse of available antibiotics, accelerating the evolution of resistance. Thus, there is an urgent need for novel approaches to therapy to overcome established resistance mechanisms. Plants produce molecules capable of inhibiting bacterial growth in various ways, offering promising paths for the development of alternative antibiotic medicine. This review emphasizes the necessity of research efforts on plant-derived chemicals in the hopes of finding and creating novel drugs that can successfully target resistant bacterial populations. Investigating these natural chemicals allows us to improve our knowledge of novel antimicrobial pathways and also expands our antibacterial repertoire with novel molecules. Simultaneously, it is still necessary to utilize present antibiotics sparingly; prudent prescribing practices must be encouraged to extend the effectiveness of current medications. The combination of innovative drug research and responsible drug usage offers an integrated strategy for managing the antibiotic resistance challenge. Full article
(This article belongs to the Special Issue The Search for Antimicrobial Agents from Natural Products)
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21 pages, 1656 KiB  
Review
Antibacterial and Antifungal Activity of Metabolites from Basidiomycetes: A Review
by Valeria Lysakova, Larissa Krasnopolskaya, Maria Yarina and Mayya Ziangirova
Antibiotics 2024, 13(11), 1026; https://doi.org/10.3390/antibiotics13111026 - 31 Oct 2024
Cited by 2 | Viewed by 2042
Abstract
Background/Objectives: The search for new antimicrobial molecules is important to expand the range of available drugs, as well as to overcome the drug resistance of pathogens. One of the promising sources of antibacterial and antifungal metabolites is basidial fungi, which have wide [...] Read more.
Background/Objectives: The search for new antimicrobial molecules is important to expand the range of available drugs, as well as to overcome the drug resistance of pathogens. One of the promising sources of antibacterial and antifungal metabolites is basidial fungi, which have wide biosynthetic capabilities. Methods: The review summarized the results of studying the antimicrobial activity of extracts and metabolites from basidiomycetes published from 2018–2023. Results: In all studies, testing for antibacterial and antifungal activity was carried out in in vitro experiments. To obtain the extracts, mainly the fruiting bodies of basidiomycetes, as well as their mycelia and culture liquid were used. Antimicrobial activity was found in aqueous, methanol, and ethanol extracts. Antimicrobial metabolites of basidiomycetes were isolated mainly from the submerged culture of basidiomycetes. Metabolites active against Gram-positive and Gram-negative bacteria and mycelial and yeast-like fungi were identified. Conclusions: Basidiomycete extracts and metabolites have shown activity against collectible strains of bacteria and fungi and multi-resistant and clinical strains of pathogenic bacteria. The minimum inhibitory concentration (MIC) values of the most active metabolites ranged from 1 to 16.7 µg/mL. Full article
(This article belongs to the Special Issue The Search for Antimicrobial Agents from Natural Products)
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