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Natural Compounds: Advances in Antimicrobial Activity

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: 31 December 2024 | Viewed by 4137

Special Issue Editors


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Guest Editor
Department of Medicine and Surgery, “Kore” University of Enna, 94100 Enna, Italy
Interests: antimicrobial resistance; bacterial adhesion; biofilm; natural extracts; drug delivery systems; clinical infectious diseases
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Medicine and Surgery, “Kore” University of Enna, 94100 Enna, Italy
Interests: osteoarthritis; musculoskeletal pain; orthopedic biomaterials; orthopedic infections; biofilm; antimicrobial resistance

Special Issue Information

Dear Colleagues,

In recent decades, an increase in antimicrobial resistance (AMR) has been observed. AMR is defined as microorganisms' ability to resist antimicrobials' action, making them ineffective. AMR is a consequence of the large and inappropriate use of antimicrobials and the failure to complete the recommended treatment or self-medication. As a result, some microorganisms develop resistance mechanisms that allow them to evade the mechanisms of action of antimicrobial agents. AMR concerns the resistance to antibiotics and other chemotherapeutic agents, including antifungal, antiviral, and antiparasitic drugs. The widespread diffusion of resistant phenotypes explains the increasing prevalence of community-acquired (CA) and hospital-acquired (HA) infections caused by resistant strains. Considering the scarce response to the most common clinically used antimicrobial agents, these infections are extremely difficult and, in some cases, impossible to treat. Accordingly, AMR is associated with high morbidity and mortality rates and implicates increased costs for the management of infections. For these reasons, it represents one of the most important global public health threats. In this context, the research of new and effective natural molecules endowed with a broad spectrum of antimicrobial activities has attracted significant attention.

This Special Issue, entitled “Natural Compounds: Advances in Antimicrobial Activity”, of the International Journal of Molecular Sciences focuses on the antimicrobial effects of natural compounds, emphasizing strategies to make them more selective and effective. Furthermore, research aimed at studying and preventing infectious diseases through an artificial intelligence-based approach will be considered. Specifically, research pertaining to the following topics:

  • Nanotechnology-based delivery systems for natural compounds (polymer nanoparticles, crystal nanoparticles, solid lipid nanoparticles (SLNs), liposomes, dendrimers, and micelles);
  • Natural antimicrobial agents able to inhibit/eradicate biofilm or to block/modulate quorum sensing communication system;
  • Combinational antimicrobial chemotherapies (synergistic interaction of natural compounds and conventional drugs);
  • Machine-learning algorithm to identify natural compounds that could inhibit the growth of multidrug-resistant bacteria (e.g., Acinetobacter baumannii, Pseudomonas aeruginosa, Klebsiella pneumoniae, methicillin-resistant Staphylococcus aureus, and vancomycin-resistant Enterococcus) and predict possible clinical outcomes.

In this Special Issue, original research articles and reviews are welcome.

We look forward to receiving your contributions.

Prof. Dr. Carlo Genovese
Dr. Francesco Pegreffi
Guest Editors

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Keywords

  • natural compounds
  • multidrug-resistant microorganisms
  • biofilm
  • synergistic effect
  • nanotechnologies
  • delivery systems
  • machine learning
  • clinical infections

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Published Papers (4 papers)

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Research

20 pages, 5931 KiB  
Article
Trans, Trans-Farnesol Enhances the Anti-Bacterial and Anti-Biofilm Effect of Arachidonic Acid on the Cariogenic Bacteria Streptococcus mutans and Streptococcus sobrinus
by Farah Haj-Yahya, Doron Steinberg and Ronit Vogt Sionov
Int. J. Mol. Sci. 2024, 25(21), 11770; https://doi.org/10.3390/ijms252111770 - 1 Nov 2024
Viewed by 949
Abstract
Background: Streptococcus mutans and Streptococcus sobrinus are Gram-positive bacteria involved in the development of dental caries, as they are able to form biofilms on tooth enamel, ferment sugars into acids, and survive under acidic conditions. This ultimately leads to a local lowering of [...] Read more.
Background: Streptococcus mutans and Streptococcus sobrinus are Gram-positive bacteria involved in the development of dental caries, as they are able to form biofilms on tooth enamel, ferment sugars into acids, and survive under acidic conditions. This ultimately leads to a local lowering of the pH value on the tooth surface, which causes enamel cavities. Hypothesis: One measure to reduce caries is to limit the growth of cariogenic bacteria by using two anti-bacterial agents with different mechanisms of action. The hypothesis of this study was that the anti-bacterial activity of ω-6 polyunsaturated arachidonic acid (AA) against S. mutans and S. sobrinus can be enhanced by the sesquiterpene alcohol trans, trans-farnesol (t,t-farnesol). Methods: The anti-bacterial activity of single and combined treatment was determined by the checkerboard assay. Bacterial viability was assessed by live/dead SYTO 9/propidium iodide (PI) staining on flow cytometry. Anti-biofilm activity was determined by MTT metabolic assay, crystal violet staining of biofilm biomass, SYTO 9/PI staining by spinning disk confocal microscopy (SDCM) and high-resolution scanning electron microscopy (HR-SEM). Results: t,t-Farnesol lowered the minimum inhibitory concentration (MIC) and the minimum biofilm inhibitory concentration (MBIC) of AA at sub-MICs. AA reduced the metabolic activity of preformed mature biofilms, while t,t-farnesol had no significant effect. The enhanced anti-bacterial effect of the combined t,t-farnesol/AA treatment was further evidenced by increased PI uptake, indicating membrane perforation. The enhanced anti-biofilm effect was further verified by SDCM and HR-SEM. Gene expression studies showed reduced expression of some biofilm-related genes. Conclusions: Altogether, our study suggests a potential use of the two naturally occurring compounds arachidonic acid and t,t-farnesol for preventing biofilm formation by the cariogenic bacteria S. mutans and S. sobrinus. These findings have implications for caries prevention. Full article
(This article belongs to the Special Issue Natural Compounds: Advances in Antimicrobial Activity)
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21 pages, 6154 KiB  
Article
In Vitro Cytotoxicity and Antimicrobial Activity against Acne-Causing Bacteria and Phytochemical Analysis of Galangal (Alpinia galanga) and Bitter Ginger (Zingiber zerumbet) Extracts
by Tanat Na Nongkhai, Sarah E. Maddocks, Santi Phosri, Sarita Sangthong, Punyawatt Pintathong, Phanuphong Chaiwut, Kasemsiri Chandarajoti, Lutfun Nahar, Satyajit D. Sarker and Tinnakorn Theansungnoen
Int. J. Mol. Sci. 2024, 25(20), 10869; https://doi.org/10.3390/ijms252010869 - 10 Oct 2024
Viewed by 1289
Abstract
Galangal (Alpinia galanga (L.) Willd) and bitter ginger (Zingiber zerumbet (L.) Roscoe) are aromatic rhizomatous plants that are typically used for culinary purposes. These rhizomatous plants have many biological properties and the potential to be beneficial for pharmaceutics. In this study, [...] Read more.
Galangal (Alpinia galanga (L.) Willd) and bitter ginger (Zingiber zerumbet (L.) Roscoe) are aromatic rhizomatous plants that are typically used for culinary purposes. These rhizomatous plants have many biological properties and the potential to be beneficial for pharmaceutics. In this study, we evaluated the antioxidant and antimicrobial activities, with a specific focus on acne-causing bacteria, as well as the phytochemical constituents, of different parts of galangal and bitter ginger. The rhizomes, stems, and leaves of galangal and bitter ginger were separately dried for absolute ethanol and methanol extractions. The extracts were used to evaluate the antioxidant activity using a DPPH radical scavenging assay (0.005–5000 μg/mL), antimicrobial activity against acne-causing bacteria (0.50–31.68 mg/mL), and in vitro cytotoxicity toward human keratinocytes and fibroblasts (62.5–1000 μg/mL), as well as analyses of bioactive phytochemicals via GC-MS and LC-MS/MS (500 ppm). The ethanol and methanol extracts of bitter ginger and galangal’s rhizomes (BRhE, BRhM, GRhE, and GRhM), stems (BStE, BStM, GRhE, and GRhM), and leaves (BLeE, BLeM, GLeE, and GLeM), respectively, showed antioxidant and antimicrobial activities. The extracts of all parts of bitter ginger and galangal were greatly antioxidative with 0.06–1.42 mg/mL for the IC50 values, while most of the extracts were strongly antimicrobial against C. acnes DMST 14916, particularly BRhM, BRhE, GRhM, and GRhE (MICs: 3.96–7.92 mg/mL). These rhizome extracts had also antimicrobial activities against S. aureus TISTR 746 (MICs: 7.92–31.68 mg/mL) and S. epidermidis TISTR 518 (MICs: 7.92–15.84 mg/mL). The extracts of bitter ginger and galangal rhizomes were not toxic to HaCaT and MRC-5 even at the highest concentrations. Through GC-MS and LC-MS/MS analysis, phytochemicals in bitter ginger rhizome extracts, including zerumbone, tectorigenin, piperic acid, demethoxycurcumin, and cirsimaritin, and galangal rhizome extracts, including sweroside and neobavaisoflavone, were expected to provide the antioxidant and anti-microbial activities. Therefore, the results suggest that the bitter ginger and galangal extracts could be natural anti-acne compounds with potential for pharmaceutic, cosmetic, and aesthetic applications. Full article
(This article belongs to the Special Issue Natural Compounds: Advances in Antimicrobial Activity)
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15 pages, 4996 KiB  
Article
Antibacterial Activity and Mechanism of Taxillμs chinensis (DC.) Danser and Its Active Ingredients
by Yanjing Feng, Silu Huang, Shengying Zhu and Bo Gao
Int. J. Mol. Sci. 2024, 25(19), 10246; https://doi.org/10.3390/ijms251910246 - 24 Sep 2024
Viewed by 516
Abstract
Taxillμs chinensis (DC.) Danser is a traditional Chinese herbal medicine. It has not been reported regarding antibacterial active ingredients and mechanisms of action. However, the Chinese patent medicine Yinhua Miyanling Tablets containing Taxillμs chinensis has an obvious anti-infective effect in our patent. Therefore, [...] Read more.
Taxillμs chinensis (DC.) Danser is a traditional Chinese herbal medicine. It has not been reported regarding antibacterial active ingredients and mechanisms of action. However, the Chinese patent medicine Yinhua Miyanling Tablets containing Taxillμs chinensis has an obvious anti-infective effect in our patent. Therefore, we speculate that Taxillμs chinensis may have antibacterial activity. The purpose of this paper is to study the antibacterial effect and mechanism of Taxillμs chinensis and find active compounds with antibacterial activity and a mechanism. We studied the antibacterial effect and mechanism of Taxillμs chinensis extract. The compounds in the ethyl acetate extract of Taxillμs chinensis were preliminarily identified by UPLC-Q-Orbitrap and analyzed by mass spectrometry. Above all, the antibacterial effect and antibacterial mechanism of the active components of Taxillμs chinensis were determined. Finally, we found, for the first time, that Taxillμs chinensis has a good antibacterial effect and ethyl acetate extract has the best effect. In addition, we found, for the first time, that it has an active component, 4-indolecarbaldehyde, and the component has a good broad-spectrum antibacterial effect. Above all, the active chemical 4-indolecarbaldehyde of Taxillμs chinensis can destroy the bacterial structure, make it unable to maintain normal morphology, and significantly increase the number of deaths. In short, Taxillμs chinensis has an antibacterial effect, and one of its main antibacterial components is 4-indolecarbaldehyde. The antibacterial mechanism of Taxillμs chinensis and 4-indolecarbaldehyde is related to the change in bacterial membrane permeability. Full article
(This article belongs to the Special Issue Natural Compounds: Advances in Antimicrobial Activity)
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8 pages, 1140 KiB  
Communication
Mode of Action of Antimicrobial Potential Protease SH21 Derived from Bacillus siamensis
by Hasan Tarek, Seung Sik Cho, Kyung Bin Nam, Ji Min Lee, Sang Hun Lee and Jin Cheol Yoo
Int. J. Mol. Sci. 2024, 25(13), 7046; https://doi.org/10.3390/ijms25137046 - 27 Jun 2024
Viewed by 644
Abstract
Global public health is facing a major issue with emerging resistance to antimicrobial agents. Antimicrobial agents that are currently on the market are strong and efficient, but it has not been ruled out that these medications will eventually cause resistance to bacteria. Exploring [...] Read more.
Global public health is facing a major issue with emerging resistance to antimicrobial agents. Antimicrobial agents that are currently on the market are strong and efficient, but it has not been ruled out that these medications will eventually cause resistance to bacteria. Exploring novel bioactive compounds derived from natural sources is therefore, crucial to meet future demands. The present study evaluated the mode of action of the antimicrobial potential protease enzyme SH21. Protease SH21 exhibited antimicrobial activity, strong heat stability (up to 100 °C), and pH stability (pH 3.0 to 9.0). In terms of mode of action, we found that protease SH21 was able to disrupt the bacterial cell membrane as the results of the nucleotide leakage and cell membrane permeability assay. In addition, we also checked inner membrane permeability by PI uptake assay which suggested that protease SH21 has the ability to enter the bacterial cell membrane. Our results revealed that the antimicrobial protease SH21 might be a promising candidate for treating microbial infections. Full article
(This article belongs to the Special Issue Natural Compounds: Advances in Antimicrobial Activity)
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