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Pharmaceuticals
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Antiradical, Chemopreventive and Antimicrobial Effects of Bioactive Natural Substances
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Antiradical, Chemopreventive and Antimicrobial Effects of Bioactive Natural Substances

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (20 February 2025) | Viewed by 13156

Special Issue Editor

Dr. Grażyna Zgórka

E-Mail Website1 Website2
Guest Editor
Department of Pharmacognosy with the Medicinal Plant Garden, Faculty of Pharmacy, Medical University of Lublin, 20-093 Lublin, Poland
Interests: plant polyphenols; chemoprevention; advanced phytochemical analysis; herbal medicinal products
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues, 

Numerous phytochemical and biological studies conducted with herbal substances or foods of plant origin confirm the strong correlation between the consumption of natural products rich in antioxidant components and chemoprevention as a process of reducing the risk of carcinogenesis or delaying the recurrence of cancer. Specialised plant metabolites (mainly phenolics), showing low or minimal toxicity, play a key role in this health-promoting strategy. As effective radical scavengers, they can directly inactivate exo- and endogenous reactive forms that are harmful to the human genome and initiate tissue degeneration, especially in relation to the hepatocellular, cardiovascular, and nervous systems. In addition, natural antioxidants may also operate by activating immune defence mechanisms, showing beneficial anti-inflammatory effects at various cellular and biochemical levels or enhancing the potency of chemotherapeutics routinely used to treat cancer. A large number of herbal ingredients have also been successful in combating pathogenic microbial species, including antibiotic-resistant bacteria, or altering the profile of the gut microbiota, thereby enhancing regulatory molecular mechanisms helpful in effectively fighting various devastating diseases.

In this Special Issue, preference will be given to review and experimental papers addressing the above topics. Particularly valuable will be papers combining detailed phytochemical analysis of plant extracts/natural products containing antioxidants with biological studies on various aspects and mechanisms of these components as inhibitors of inflammatory processes promoting carcinogenesis and/or antimicrobial agents.

Dr. Grażyna Zgórka
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. Pharmaceuticals 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 radical scavengers
  • chemopreventive agents
  • antimicrobials
  • chemical and biomedical analysis
  • biological studies in vitro/in vivo

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Published Papers (5 papers)

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18 pages, 2961 KiB  
Article
Protective Capacity of Helichrysum italicum Infusion Against Intestinal Barrier Disruption and Translocation of Salmonella Infantis
by Katja Kramberger, Katja Bezek Kranjc, Zala Jenko Pražnikar, Darja Barlič-Maganja and Saša Kenig
Pharmaceuticals 2024, 17(10), 1398; https://doi.org/10.3390/ph17101398 - 19 Oct 2024
Viewed by 2283
Abstract
Background: Helichrysum italicum is a Mediterranean plant with well-known anti-inflammatory activity, but our previous whole transcriptome analysis has found that H. italicum infusion (HII) can also affect cytoskeletal rearrangement and tight junctions. The goal of the present study was to determine if HII [...] Read more.
Background: Helichrysum italicum is a Mediterranean plant with well-known anti-inflammatory activity, but our previous whole transcriptome analysis has found that H. italicum infusion (HII) can also affect cytoskeletal rearrangement and tight junctions. The goal of the present study was to determine if HII improves the intestinal barrier (IB) dysfunction and by what mechanism. Methods: Caco-2 cells on Transwell inserts were used as a model of IB permeability. Heat-killed (HKB) or live Salmonella Infantis bacteria were used to induce IB integrity disruption upon three different testing conditions: pre-, co-, and post-treatment with 0.2 v/v% HII. Transepithelial electrical resistance values were used as an indicator of monolayer integrity before and after all treatments, and RT-PCR was used to assess the expression of tight junction proteins (TJPs) and inflammatory cytokines known to regulate intestinal permeability. Results: We found that all three treatments with HII improved the HKB-induced integrity disruption and decreased the down-regulation of TJP1, OCLN, and CLDN1, with the greatest effect observed in the pre-treated cells. Treatment with HII also decreased the up-regulation of CLDN2, TNF-α, IL-1β, and IL-6. In addition, pre-treatment of Caco-2 cells with HII prevented translocation of S. Infantis but did not prevent adhesion and invasion. Conclusion: This study showed that HII can improve inflammation-disrupted IB function by indirect modulation of mRNA expression of TJPs, especially in a preventive manner. Full article
(This article belongs to the Special Issue Antiradical, Chemopreventive and Antimicrobial Effects of Bioactive Natural Substances)
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17 pages, 15173 KiB  
Article
HPLC-PDA Analysis of Polyacetylene Glucosides from Launaea capitata and Their Antibacterial and Antibiofilm Properties against Klebsiella pneumoniae
by Tariq M. Aljarba, Fatma M. Abdel Bar, Asmaa E. Sherif, Engy Elekhnawy, Galal Magdy and Reham M. Samra
Pharmaceuticals 2024, 17(9), 1214; https://doi.org/10.3390/ph17091214 - 15 Sep 2024
Viewed by 1449
Abstract
Background/Objectives: Bacterial resistance and virulence are challenges in treating bacterial infections, especially in Klebsiella pneumoniae. Plants of the Launaea Cass. genus are used traditionally to address a variety of diseases, including infections, but the potential bioactive compounds are unknown. Our goals [...] Read more.
Background/Objectives: Bacterial resistance and virulence are challenges in treating bacterial infections, especially in Klebsiella pneumoniae. Plants of the Launaea Cass. genus are used traditionally to address a variety of diseases, including infections, but the potential bioactive compounds are unknown. Our goals were to verify the potential contribution of two major polyacetylene glycosides isolated from our previous study, (3S,6E,12E)-6,12-tetradecadiene-8,10-diyne-1-ol 3-O-β-D-glucopyranoside (1) and bidensyneoside A (syn. gymnasterkoreaside A) [(3R,8E)-3-hydroxy-8-decene-4,6-diyn-1-yl β-D-glucopyranoside] (2), to the anti-infective properties of Launaea capitata and to develop a dependable HPLC method for their quantification; Methods: On a panel of K. pneumoniae clinical isolates, the antibacterial action of 1, 2, and the methanol extract of the whole L. capitata plant were evaluated by broth microdilution assay, while their antibiofilm action was evaluated by the crystal violet assay. qRT-PCR investigated luxS, mrkA, wzm, and wbbm genes that encode biofilm formation and quorum sensing (QS). The antibacterial activity of 1 was revealed by employing mice infection. Chromatographic separation was conducted using isocratic elution on a Hypersil BDS C18 column using a photodiode array (PDA) detector; Results: Compound 1 showed antibacterial activity with MIC values of 16–128 µg/mL. It remarkably reduced strong and moderate biofilm-forming bacterial isolates from 84.21% to 42.1% compared with the extract (68.42%) and 2 (78.95%). Compound 1 also downregulated the QS genes, luxS, mrkA, wzm, and wbbm, and exhibited in vivo antibacterial action through the enhancement of the histological construction of the liver and spleen, decreased TNF-α immunoreaction, bacterial burden, and the inflammatory mediators IL-1β and IL-6. A successful HPLC-PDA approach was developed to separate the binary mixture of 1 and 2 in less than 10 min with high sensitivity, with detection limits down to 0.518 and 0.095 µg/mL for 1 and 2, respectively; Conclusions: Compound 1 exhibited remarkable antibacterial and antibiofilm properties and may contribute to the anti-infectious traditional uses of L. capitata, meriting further clinical studies and serving as a reliable quality control biomarker for the plant. Full article
(This article belongs to the Special Issue Antiradical, Chemopreventive and Antimicrobial Effects of Bioactive Natural Substances)
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19 pages, 1110 KiB  
Article
The Antimicrobial Effect of Cornus mas L. and Sorbus aucuparia L. Fruit Extracts against Resistant Uropathogens in Correlation with the Prevalence of Urinary Tract Infections in Companion Animals
by Mara Aurori, Cristiana Ștefania Novac, George Cosmin Nadăș, Smaranda Crăciun, Nicodim Fiţ and Sanda Andrei
Pharmaceuticals 2024, 17(6), 814; https://doi.org/10.3390/ph17060814 - 20 Jun 2024
Cited by 2 | Viewed by 1571
Abstract
Urinary tract infections (UTIs) are a widespread condition in pets, with many antibiotics being prescribed, contributing to the rise in antimicrobial resistance, which is a worldwide threat. This study’s main objective was to analyze the in vitro antimicrobial activity of Cornus mas and [...] Read more.
Urinary tract infections (UTIs) are a widespread condition in pets, with many antibiotics being prescribed, contributing to the rise in antimicrobial resistance, which is a worldwide threat. This study’s main objective was to analyze the in vitro antimicrobial activity of Cornus mas and Sorbus aucuparia fruit hydro-ethanolic extracts towards bacteria identified in the urine of companion animals experiencing UTIs. Urine samples were collected from dogs and cats (n = 83; 47 negative, 36 positive); several bacterial strains were identified (n = 49) belonging to the Escherichia, Enterococcus, Staphylococcus, Proteus, Klebsiella, Enterobacter, Pseudomonas, Acinetobacter, Leclercia, and Kocuria genera. Bacterial susceptibility was tested using the disk diffusion method, with the majority being resistant to several beta-lactams, quinolones, trimethoprim/sulfamethoxazole, and nitrofurantoin. Subsequently, 13 resistant isolates were selected to evaluate the fruits extracts’ antimicrobial potential using the agar well diffusion and broth microdilution methods. Cornus mas exhibited the greatest activity against Gram-negatives (primarily Pseudomonas luteola), while Sorbus aucuparia showed maximum effects towards Gram-positives (particularly Enterococcus faecalis). The MIC was 0.01 μg/μL for both extracts; the MBC was 0.08 μg/μL for Cornus mas and 0.05 μg/μL for Sorbus aucuparia. However, Cornus mas showed a stronger bactericidal effect. This is the first study to investigate these fruit extracts in UTI isolates of companion animals, and these extracts might be used as substitutes or adjuvants for antibiotics, thus contributing to a reduction in antimicrobial resistance. Full article
(This article belongs to the Special Issue Antiradical, Chemopreventive and Antimicrobial Effects of Bioactive Natural Substances)
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18 pages, 2932 KiB  
Article
Potential Anti-Inflammatory and Anti-Fatigue Effects of an Oral Food Supplement in Long COVID Patients
by Annalisa Noce, Giulia Marrone, Manuela Di Lauro, Chiara Vita, Giulia Montalto, Gloria Giorgino, Carlo Chiaramonte, Cartesio D’Agostini, Sergio Bernardini and Massimo Pieri
Pharmaceuticals 2024, 17(4), 463; https://doi.org/10.3390/ph17040463 - 5 Apr 2024
Cited by 1 | Viewed by 4794
Abstract
Long coronavirus disease (COVID) syndrome leads to chronic inflammatory state onset that can have a multisystem impact and compromise organ function. Moreover, long COVID syndrome is often characterized by the presence of chronic fatigue, which affects subjects’ daily activities and worsens their quality [...] Read more.
Long coronavirus disease (COVID) syndrome leads to chronic inflammatory state onset that can have a multisystem impact and compromise organ function. Moreover, long COVID syndrome is often characterized by the presence of chronic fatigue, which affects subjects’ daily activities and worsens their quality of life. The aim of our double-blind, placebo-controlled randomized trial (protocol code RS 150.21, approved on 4 November 2021) was to evaluate the beneficial effects of the consumption of 2 cps/day, for two months, of an oral food supplement (OFS), based on Echinacea angustifolia, rosehip, propolis, royal jelly and zinc, in long COVID patients, compared to a two-month placebo period. The OFS’s vitamin C content was equal to 22.17 mg/g (8.87 mg/capsule). The OFS’s total polyphenol content was 43.98 mg/g gallic acid equivalents. At the end of the in vivo study, we highlighted a significant decrease in the inflammatory parameters in the OFS period, compared to the placebo period (neutrophil-to-lymphocyte ratio, p = 0.0455; monocyte to-lymphocyte ratio, p = 0.0005; C-reactive protein, p = 0.0145). Our study also highlighted a significant increase in vitamin D serum values (p = 0.0005) and, at the same time, an improvement in patients’ life quality and a reduction in fatigue, monitored by the fatigue severity scale. This study showed the OFS’s beneficial effects on the inflammatory state, fatigue and quality of life in long COVID patients. Full article
(This article belongs to the Special Issue Antiradical, Chemopreventive and Antimicrobial Effects of Bioactive Natural Substances)
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25 pages, 1962 KiB  
Systematic Review
Salvia verticillata (L.)—Biological Activity, Chemical Profile, and Future Perspectives
by Stanislava Ivanova, Zoya Dzhakova, Radiana Staynova and Kalin Ivanov
Pharmaceuticals 2024, 17(7), 859; https://doi.org/10.3390/ph17070859 - 1 Jul 2024
Cited by 2 | Viewed by 2307
Abstract
Species belonging to the genus Salvia, Lamiaceae, have been deeply involved in the folk medicine of different nations since ancient times. Lilac sage, or Salvia verticillata L. (S. verticillata) is a less studied species from the genus. However, it seems [...] Read more.
Species belonging to the genus Salvia, Lamiaceae, have been deeply involved in the folk medicine of different nations since ancient times. Lilac sage, or Salvia verticillata L. (S. verticillata) is a less studied species from the genus. However, it seems to have a prominent potential for the future drug discovery strategies of novel phytopharmaceuticals. This review aims to summarise the data on the biological activity and the phytochemical profile of extracts and essential oils derived from S. verticillata. This review is based on data from 57 in vitro and in vivo studies. The chemical profile of S. verticillata includes different synergic compounds like phenolic acids, flavonoids, terpenes, and salvianolic acids. Although some small amounts of salvianolic acid B were found in S. verticillata extracts, the major compound among the salvianolic acids is salvianolic acid C, a compound associated with the potential for improving liver fibrosis, cardio- and hepatoprotection, and the inhibition of SARS-CoV-2 infection. The cannabinoid type 2 receptor agonist β-caryophyllene is one of the major compounds in S. verticillata essential oils. It is a compound with a prominent potential in regenerative medicine, neurology, immunology, and other medical fields. The in vivo and the in vitro studies, regarding S. verticillata highlighted good antioxidant potential, anti-inflammatory, antibacterial, and antifungal activity. S.verticillata was also reported as a potential source of drug candidates for the treatment of neurodegenerative diseases such as Alzheimer’s disease, because of the inhibitory activity on the acetylcholinesterase. However, the number of studies in this direction is limited. Full article
(This article belongs to the Special Issue Antiradical, Chemopreventive and Antimicrobial Effects of Bioactive Natural Substances)
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