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Antibiotics
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Synthetic and Natural Products-Based Antimicrobial and Antiparasitic Agents
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Synthetic and Natural Products-Based Antimicrobial and Antiparasitic Agents

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Novel Antimicrobial Agents".

Deadline for manuscript submissions: 30 November 2024 | Viewed by 3256

Special Issue Editor

Prof. Dr. Antonio Eduardo Miller Crotti

E-Mail Website
Guest Editor
Department of Chemistry, Faculty of Philosophy, Sciences, and Letters at Ribeirão Preto, University of São Paulo, Ribeirão Preto 14040-901, Brazil
Interests: natural products; organic synthesis; biological and pharmacological activities; mass spectrometry; structural elucidation; reaction mechanisms
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Microbial and parasites are responsible for a wide diversity of diseases in humans and animals. The need for novel antimicrobials and antiparasitic agents has emerged as the current drugs have become less efficient due to resistance development. The potential of synthetic, semi-synthetic, and natural products as alternative antimicrobial (antibacterial, antifungal, and antiviral) and antiparasitic (especially antileishmanial, anti-trypanosomal, antischistosomal, and anti-toxoplasma, but not limited to them) agents will be addressed in this Special Issue. This issue will cover the discovery and design of new synthetic and semi-synthetic compounds, as well as their mechanisms of action, and structure–activity relationship (SAR) studies. Studies on bioactive microbial and plant-derived natural products and/or their semi-synthetic derivatives, as well as essential oils and their constituents, are also welcome. Authors are invited to contribute their submissions as reviews, research papers, or communications.

Prof. Dr. Antonio Eduardo Miller Crotti
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 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.

Prof. Dr. Antonio Eduardo Miller Crotti
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 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

  • antibacterial
  • antifungal
  • antiviral
  • Candida
  • Chagas's disease
  • essential oils
  • Helicobacter
  • Leishmania
  • Schistosoma
  • Staphylococcus
  • Streptococcus
  • Toxoplasma
  • Trypanosoma

Published Papers (5 papers)

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Research

Jump to: Review

14 pages, 1996 KiB  
Article
Cytocompatibility and Antibiofilm Activity of Calcium Hydroxide Mixed with Cyperus articulatus Essential Oil and Bio-C Temp Bioceramic Intracanal Medicament
by Cláudia Fernandes de Magalhães Silveira, Carlos Eduardo da Silveira Bueno and Angélica Zaninelli Schreiber
Antibiotics 2024, 13(7), 637; https://doi.org/10.3390/antibiotics13070637 - 10 Jul 2024
Viewed by 479
Abstract
Calcium hydroxide represents the most commonly used intracanal dressing between sessions; however, it may not be effective against all types of microorganisms. Several compounds of plant origin have attracted increasing attention from researchers in recent years. The objective of this study was to [...] Read more.
Calcium hydroxide represents the most commonly used intracanal dressing between sessions; however, it may not be effective against all types of microorganisms. Several compounds of plant origin have attracted increasing attention from researchers in recent years. The objective of this study was to evaluate the cytocompatibility and antimicrobial activity of calcium hydroxide associated with the essential oil of Cyperus articulatus and the new bioceramic intracanal medicament Bio-C Temp®. Five experimental groups were designed: group Ca–C. articulatus essential oil; group CHPG-calcium hydroxide associated with propylene glycol; group CHCa-essential oil of C. articulatus associated with calcium hydroxide; and group U-UltraCal® XS; group BCT-Bio-C Temp®. The control group was a culture medium. Cytocompatibility was assessed by the methyltetrazolium (MTT) assay after exposure of the Saos-2 human osteoblast-like cell line to dilutions of commercial products/associations for 24 h and 72 h. The antimicrobial activity against mature Enterococcus faecalis biofilm was evaluated by the crystal violet assay. All commercial products/associations showed a cell viability similar to or even higher than the control group (p > 0.05) for both periods evaluated. C. articulatus essential oil associated or not with calcium hydroxide showed better antibiofilm capacity. C. articulatus associated or not with calcium hydroxide showed superior cytocompatibility and antimicrobial capacity, representing a promissory intracanal medicament. Full article
(This article belongs to the Special Issue Synthetic and Natural Products-Based Antimicrobial and Antiparasitic Agents)
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26 pages, 10235 KiB  
Article
In Vitro Evaluation of Colistin Conjugated with Chitosan-Capped Gold Nanoparticles as a Possible Formulation Applied in a Metered-Dose Inhaler
by Narumon Changsan, Apichart Atipairin, Poowadon Muenraya, Rutthapol Sritharadol, Teerapol Srichana, Neelam Balekar and Somchai Sawatdee
Antibiotics 2024, 13(7), 630; https://doi.org/10.3390/antibiotics13070630 - 6 Jul 2024
Viewed by 676
Abstract
Inhaled colistin is used to treat pneumonia and respiratory infections through nebulization or dry powder inhalers. Nevertheless, the development of a metered-dose inhaler (MDI) for colistin, which could enhance patient convenience and treatment efficacy, has not yet been developed. Colistin is known for [...] Read more.
Inhaled colistin is used to treat pneumonia and respiratory infections through nebulization or dry powder inhalers. Nevertheless, the development of a metered-dose inhaler (MDI) for colistin, which could enhance patient convenience and treatment efficacy, has not yet been developed. Colistin is known for its ability to induce cellular toxicity. Gold nanoparticles (AuNPs) can potentially mitigate colistin toxicity. Therefore, this study aimed to evaluate the antimicrobial effectiveness of colistin conjugated with chitosan-capped gold nanoparticles (Col-CS-AuNPs) and their potential formulation for use with MDIs to deliver the aerosol directly to the deep lung. Fourier-transform infrared spectroscopy, nuclear magnetic resonance, and elemental analysis were used to characterize the synthesized Col-CS-AuNPs. Drug release profiles fitted with the most suitable release kinetic model were evaluated. An MDI formulation containing 100 µg of colistin per puff was prepared. The aerosol properties used to determine the MDI performance included the fine particle fraction, mass median aerodynamic diameter, and geometric standard deviation, which were evaluated using the Andersen Cascade Impactor. The delivered dose uniformity was also determined. The antimicrobial efficacy of the Col-CS-AuNP formulation in the MDI was assessed. The chitosan-capped gold nanoparticles (CS-AuNPs) and Col-CS-AuNPs had particle sizes of 44.34 ± 1.02 and 174.50 ± 4.46 nm, respectively. CS-AuNPs effectively entrapped 76.4% of colistin. Col-CS-AuNPs exhibited an initial burst release of up to 60% colistin within the first 6 h. The release mechanism was accurately described by the Korsmeyer–Peppas model, with an R2 > 0.95. The aerosol properties of the Col-CS-AuNP formulation in the MDI revealed a high fine particle fraction of 61.08%, mass median aerodynamic diameter of 2.34 µm, and geometric standard deviation of 0.21, with a delivered dose uniformity within 75–125% of the labeled claim. The Col-CS-AuNP MDI formulation completely killed Escherichia coli at 5× and 10× minimum inhibitory concentrations after 6 and 12 h of incubation, respectively. The toxicity of CS-AuNP and Col-CS-AuNP MDI formulations in upper and lower respiratory tract cell lines was lower than that of free colistin. The stability of the Col-CS-AuNP MDI formulation was maintained for at least 3 months. The Col-CS-AuNP MDI formulation effectively eradicated bacteria over a 12-h period, showing promise for advancing lung infection treatments. Full article
(This article belongs to the Special Issue Synthetic and Natural Products-Based Antimicrobial and Antiparasitic Agents)
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11 pages, 2383 KiB  
Article
Therapeutic Potential of Mangosteen Pericarp Extract-Loaded Liposomes against Superficial Skin Infection Caused by Staphylococcus pseudintermedius in a Murine Model
by Seong-Yeop Kim, Seong-Yong Park, Jung-Hwa Lee, Nayeong Kim, Ha-Na Oh, So-Young Yoo, Dae-Sung Lee and Je-Chul Lee
Antibiotics 2024, 13(7), 612; https://doi.org/10.3390/antibiotics13070612 - 1 Jul 2024
Viewed by 469
Abstract
α-mangostin (α-MG) demonstrates antibacterial activity against Staphylococcus species. Therefore, this study aimed to explore the antibacterial activity of α-MG-rich mangosteen pericarp extract (MPE)-loaded liposomes against Staphylococcus isolates from companion animal skin diseases in vitro and evaluated their therapeutic potential in a murine model [...] Read more.
α-mangostin (α-MG) demonstrates antibacterial activity against Staphylococcus species. Therefore, this study aimed to explore the antibacterial activity of α-MG-rich mangosteen pericarp extract (MPE)-loaded liposomes against Staphylococcus isolates from companion animal skin diseases in vitro and evaluated their therapeutic potential in a murine model of superficial skin infection caused by S. pseudintermedius. α-MG-rich extract was purified from mangosteen pericarp and then complexed with γ-cyclodextrin (γ-CD), forming the inclusion complexes. Nanoliposomes containing MPE and γ-CD complexes were prepared by adding lecithin and casein. Minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) of MPE-loaded liposomes were determined using agar dilution and broth microdilution methods. The therapeutic potential of MPE-loaded liposomes was evaluated in vivo on tape-stripped skin lesions infected with S. pseudintermedius. Purified MPE and MPE-loaded liposomes contained 402.43 mg/g and 18.18 mg/g α-MG, respectively. MPE-loaded liposomes showed antibacterial activity against clinical Staphylococcus isolates in vitro but did not show antibacterial activity against Gram-negative bacterial isolates. MPE-loaded liposomes demonstrated consistent MICs and MBCs against Staphylococcus isolates. These liposomes significantly reduced bacterial numbers and lesional sizes in a superficial skin infection model. Moreover, they reconstructed the epidermal barrier in skin lesions. The therapeutic concentrations of MPE-loaded liposomes did not induce cytotoxicity in canine progenitor epidermal keratinocyte cells. In conclusion, MPE-loaded liposomes hold promise for the development of a prospective topical formulation to treat superficial pyoderma in companion animals. Full article
(This article belongs to the Special Issue Synthetic and Natural Products-Based Antimicrobial and Antiparasitic Agents)
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11 pages, 1536 KiB  
Article
Antimicrobial and Antibiofilm Effects of Bithionol against Mycobacterium abscessus
by Dan Cao, Xin Yuan, Xiuzhi Jiang, Tiantian Wu, Yanghui Xiang, Zhongkang Ji, Jiaying Liu, Xu Dong, Kefan Bi, Tone Tønjum, Kaijin Xu and Ying Zhang
Antibiotics 2024, 13(6), 529; https://doi.org/10.3390/antibiotics13060529 - 5 Jun 2024
Viewed by 719
Abstract
Mycobacterium abscessus (M. abscessus) is a multidrug-resistant nontuberculous mycobacterium (NTM) that is responsible for a wide spectrum of infections in humans. The lack of effective bactericidal drugs and the formation of biofilm make its clinical treatment very difficult. The FDA-approved drug [...] Read more.
Mycobacterium abscessus (M. abscessus) is a multidrug-resistant nontuberculous mycobacterium (NTM) that is responsible for a wide spectrum of infections in humans. The lack of effective bactericidal drugs and the formation of biofilm make its clinical treatment very difficult. The FDA-approved drug library containing 3048 marketed and pharmacopeial drugs or compounds was screened at 20 μM against M. abscessus type strain 19977 in 7H9 medium, and 62 hits with potential antimicrobial activity against M. abscessus were identified. Among them, bithionol, a clinically approved antiparasitic agent, showed excellent antibacterial activity and inhibited the growth of three different subtypes of M. abscessus from 0.625 μM to 2.5 μM. We confirmed the bactericidal activity of bithionol by the MBC/MIC ratio being ≤4 and the time–kill curve study and also electron microscopy study. Interestingly, it was found that at 128 μg/mL, bithionol could completely eliminate biofilms after 48h, demonstrating an outstanding antibiofilm capability compared to commonly used antibiotics. Additionally, bithionol could eliminate 99.9% of biofilm bacteria at 64 μg/mL, 99% at 32 μg/mL, and 90% at 16 μg/mL. Therefore, bithionol may be a potential candidate for the treatment of M. abscessus infections due to its significant antimicrobial and antibiofilm activities. Full article
(This article belongs to the Special Issue Synthetic and Natural Products-Based Antimicrobial and Antiparasitic Agents)
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Review

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25 pages, 2344 KiB  
Review
Vitis vinifera L. Leaf Extract, a Microbiota Green Ally against Infectious and Inflammatory Skin and Scalp Diseases: An In-Depth Update
by Marta Armari, Elisa Zavattaro, Cesar Francisco Trejo, Alice Galeazzi, Alessia Grossetti, Federica Veronese, Paola Savoia and Barbara Azzimonti
Antibiotics 2024, 13(8), 697; https://doi.org/10.3390/antibiotics13080697 - 26 Jul 2024
Abstract
The skin microbiota, with its millions of bacteria, fungi, and viruses, plays a key role in balancing the health of the skin and scalp. Its continuous exposure to potentially harmful stressors can lead to abnormalities such as local dysbiosis, altered barrier function, pathobiont [...] Read more.
The skin microbiota, with its millions of bacteria, fungi, and viruses, plays a key role in balancing the health of the skin and scalp. Its continuous exposure to potentially harmful stressors can lead to abnormalities such as local dysbiosis, altered barrier function, pathobiont overabundance, and infections often sustained by multidrug-resistant bacteria. These factors contribute to skin impairment, deregulation of immune response, and chronic inflammation, with local and systemic consequences. In this scenario, according to the needs of the bio-circular-green economy model, novel harmless strategies, both for regulating the diverse epidermal infectious and inflammatory processes and for preserving or restoring the host skin eubiosis and barrier selectivity, are requested. Vitis vinifera L. leaves and their derived extracts are rich in plant secondary metabolites, such as polyphenols, with antioxidant, anti-inflammatory, antimicrobial, and immunomodulatory properties that can be further exploited through microbe-driven fermentation processes. On this premise, this literature review aims to provide an informative summary of the most updated evidence on their interactions with skin commensals and pathogens and on their ability to manage inflammatory conditions and restore microbial biodiversity. The emerging research showcases the potential novel beneficial ingredients for addressing various skincare concerns and advancing the cosmeceutics field as well. Full article
(This article belongs to the Special Issue Synthetic and Natural Products-Based Antimicrobial and Antiparasitic Agents)
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Planned Papers

The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.

Title: In vitro antifungal activity of Gymnemic acid on Candida Albicans
Authors: Riaan Mulde
Affiliation: 0
Abstract: Natural medicine is an emerging field and is being explored to overcome drug resistance and reduce side effects in the management of oral candidiasis. Gymnemagenin (which is also known as Gymnemic acid; GA) is a purified extract from Gymnema sylvestre known for its potency against microbial and fungal activity. The study aimed to determine the effectiveness of Gymnemic acid in the inhibition of Candida growth and hyphae development. Disc diffusion tests were carried out on the agar plates containing the prepared Candida (3 plates each week). Samples of Candida albicans were transferred using a sterile loop from underneath and at the edge of each disc (NYS, CHX, GA and DH2O), for each medicament, and transferred to bovine serum vials (n=24). This was repeated for week 2 and week 3 (n=72). There was no zone of inhibition around GA and DH20 discs, while CHX and NYS discs exhibited significantly large inhibition zones. Meanwhile, there is an increase in bud size (2-4 hours) with the highest in NYS, followed by GA and CHX. The bud size significantly decreased (p>0.05) at 4-6 hours for all medicaments. Only GA progressively decreased in bud size from 6 to 24 hours. NYS increased in bud size from 6-24 hours and CHX showed little change in bud surface area. At hour 0, hyphae length base-line readings showed no hyphal growth across all treatments. Over the 24-hour period for three weeks, GA treatment significantly reduced the hyphal growth as compared to CHX and NYS treatments (p=0.05). There were no significant differences found in the hyphal length of GA over the three weeks. GA reduced the hyphae length and bud size of Candida, but unlike NYS and CHX, did not inhibit the Candidal growth. The reduction in bud size and hyphae length may indicate that GA reduced the pathogenic potential of Candida albicans, rendering it less virulent.

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