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Studies on the Cytotoxicity and Antimicrobial Effects of Synthetic and Natural Compounds

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A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: 20 May 2024 | Viewed by 5645

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Special Issue Editors

Prof. Dr. Jelena Antić-Stanković

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Guest Editor

Department of Microbiology and Immunology, Faculty of Pharmacy, University of Belgrade, 11 000 Belgrade, Serbia
Interests: antimicrobial effects; cytotoxicity effects

Dr. Anja Klančnik

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Guest Editor

Department of Food Microbiology, Biotechnical Faculty, University of Ljubljana, Ljubljana, Slovenia
Interests: campylobacter jejuni; bacterial stress response; host-pathogen interactions; antibacterial resistance mechanism; biofilm-specific resistant phenotype; virulence factors; bacterial communication
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Dr. Dragana Božić

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Department of Microbiology and Immunology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia
Interests: antimicrobial resistance; biofilm; multi-resistant bacteria; methicillin-resistant staphylococcus aureus; antibiotics; natural and synthetic antimicrobial compounds; plant extracts and essential oils; chalcones; anticancer activity; anti-inflammatory activity; cytotoxicity assays; in vivo animal models of autoimmune diseases, sepsis, and inflammation; one health; microbiological quality control of medicines; GMP
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Organisms such as microorganisms, fungi, and animals (including insects) can supply us with valuable, biologically active products. A majority of contemporary studies on the biological activity of natural products are devoted to the search for natural compounds, particularly those demonstrating anticancer and antimicrobial effects.

Natural products still present a major source of new drug molecules. Plants and other natural sources can provide a huge range of complex and structurally diverse compounds. Many researchers have therefore focused on the investigation of plant extracts, microbial products, and new synthetized molecules as potential antimicrobial and antiproliferative agents. Many molecules of natural origin act as starting compounds for the synthesis of new molecules with antimicrobial or cytotoxic effects.

This Special Issue looks to collect original research articles and review articles addressing recent advances in the investigation of antimicrobial and/or cytotoxicity effects of synthetic and natural compounds.

We look forward to receiving your papers.

Prof. Dr. Jelena Antić-Stanković
Dr. Anja Klančnik
Dr. Dragana Božić
Guest Editors

Manuscript Submission Information

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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. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

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Keywords

antimicrobial activity
cytotoxicity effect
natural products
synthetic compounds
plant essential oil

Published Papers (4 papers)

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Research

23 pages, 1495 KiB

Open AccessArticle

Phytochemical Profile, Antioxidant and Cytotoxic Potential of Capsicum annuum (L.) Dry Hydro-Ethanolic Extract

by Ionuț Mădălin Ivan, Violeta Popovici, Carmen Lidia Chițescu, Liliana Popescu, Emanuela Alice Luță, Elena Iuliana Ilie, Lorelei Irina Brașoveanu, Camelia Mia Hotnog, Octavian Tudorel Olaru, George Mihai Nițulescu, Rica Boscencu and Cerasela Elena Gîrd

Pharmaceutics 2024, 16(2), 245; https://doi.org/10.3390/pharmaceutics16020245 - 07 Feb 2024

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Abstract

Capsicum annuum (L.) is one of the essential spices most frequently used in our daily routine and has remarkable ethnobotanical and pharmacological properties. Its fruits are rich in vitamins, minerals, carotenoids, and numerous other phenolic metabolites with a well-known antioxidant activity. Regular consumption of chili fruits may have a positive influence on human health. Therefore, we investigated a commercially available chili fruit powder in the present study, extracting it with 50% ethanol. The dried hydro-ethanolic extract (CAE) was thoroughly analyzed using ultra-high-performance liquid chromatography coupled with high-resolution mass spectrometry (UHPLC–HRMS/MS), and 79 bioactive phenolic constituents were identified. Then, we quantified the main phenolic compounds and found a polyphenol content of 4.725 ± 1.361 mg Eq tannic acid/100 g extract and a flavonoid amount of 1.154 ± 0.044 mg Eq rutin/100 g extract. Phenolic secondary metabolites are known for their dual redox behavior as antioxidants/pro-oxidants, underlying their numerous benefits in health and disease. Thus, the antioxidant potential of CAE was evaluated using three methods; our results could explain the protective effects of chili fruits: IC₅₀DPPH = 1.669 mg/mL, IC₅₀ABTS = 0.200 mg/mL, and EC₅₀FRAP = 0.561 mg/mL. The pro-oxidant potential of phenolic compounds could be a basis for CAE cytotoxicity, investigated in vitro on tumor cell lines and in vivo on Daphnia sp. Results demonstrated the dose- and time-dependent CAE’s cytotoxic activity; the highest antiproliferative activity was recorded on colon (LoVo) and breast (MDA-MB-231) cancer cell lines after 48 h of exposure (IC₅₀ values < 200 µg/mL). In vivo testing on Daphnia sp. reported a potent CAE cytotoxicity after 48 h and embryonic developmental delays. Extensive data analyses support our results, showing a significant correlation between the CAE’s concentration, phenolic compound content, antioxidant activity, exposure time, and the viability rate of different tested cell lines. Full article

(This article belongs to the Special Issue Studies on the Cytotoxicity and Antimicrobial Effects of Synthetic and Natural Compounds)

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18 pages, 7208 KiB

Open AccessEditor’s ChoiceArticle

Antibiotics against Pseudomonas aeruginosa on Human Skin Cell Lines: Determination of the Highest Non-Cytotoxic Concentrations with Antibiofilm Capacity for Wound Healing Strategies

by María I. Quiñones-Vico, Ana Fernández-González, Ana Ubago-Rodríguez, Kirsten Moll, Anna Norrby-Teglund, Mattias Svensson, José Gutiérrez-Fernández, Jesús M. Torres and Salvador Arias-Santiago

Pharmaceutics 2024, 16(1), 117; https://doi.org/10.3390/pharmaceutics16010117 - 17 Jan 2024

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Abstract

Pseudomonas aeruginosa is one of the most common microorganisms causing infections of severe skin wounds. Antibiotic or antiseptic treatments are crucial to prevent and curb these infections. Antiseptics have been reported to be cytotoxic to skin cells and few studies evaluate the impact of commonly used antibiotics. This study evaluates how clinical antibiotics affect skin cells’ viability, proliferation, migration, and cytokine secretion and defines the highest non-cytotoxic concentrations that maintain antibacterial activity. Cell proliferation, viability, and migration were evaluated on cell monolayers. Cytokines related to the wound healing process were determined. The minimum inhibitory concentrations and the impact on bacterial biofilm were assessed. Results showed that 0.02 mg/mL ciprofloxacin and 1 mg/mL meropenem are the highest non-cytotoxic concentrations for fibroblasts and keratinocytes while 1.25 mg/mL amikacin and 0.034 mg/mL colistin do not affect fibroblasts’ viability and cytokine secretion but have an impact on keratinocytes. These concentrations are above the minimum inhibitory concentration but only amikacin could eradicate the biofilm. For the other antibiotics, cytotoxic concentrations are needed to eradicate the biofilm. Combinations with colistin at non-cytotoxic concentrations effectively eliminate the biofilm. These results provide information about the concentrations required when administering topical antibiotic treatments on skin lesions, and how these antibiotics affect wound management therapies. This study set the basis for the development of novel antibacterial wound healing strategies such as antibiotic artificial skin substitutes. Full article

(This article belongs to the Special Issue Studies on the Cytotoxicity and Antimicrobial Effects of Synthetic and Natural Compounds)

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26 pages, 10345 KiB

Open AccessArticle

Antibiofilm, Antimicrobial, Anti-Quorum Sensing, and Antioxidant Activities of Saudi Sidr Honey: In Vitro and Molecular Docking Studies

by Abdulrahman S. Bazaid, Ahmed Alsolami, Mitesh Patel, Aiah Mustafa Khateb, Abdu Aldarhami, Mejdi Snoussi, Shekah M. Almusheet and Husam Qanash

Pharmaceutics 2023, 15(9), 2177; https://doi.org/10.3390/pharmaceutics15092177 - 22 Aug 2023

Cited by 7 | Viewed by 1716

Abstract

Sidr honey is a valuable source of bioactive compounds with promising biological properties. In the present study, antimicrobial, antioxidant, and anti-quorum sensing properties of Saudi Sidr honey were assessed, along with phytochemical analysis, via gas chromatography–mass spectrometry (GC-MS). In silico study was also carried out to study the drug-likeness properties of the identified compounds and to study their affinity with known target proteins assessed using molecular docking approach. The results showed that Saudi Sidr honey exhibited promising antibacterial activity, with MIC values ranging from 50 to 400 mg/mL and MBC values from 50 to >450 mg/mL. Interestingly, the Saudi Sidr honey was active against Candida auris and Candida neoformans, with an MIC value of about 500 mg/mL. Moreover, the Sidr honey showed important antioxidant activities (ABTS assay: IC50 5.41 ± 0.045 mg/mL; DPPH assay: IC50 7.70 ± 0.065 mg/mL) and β-carotene bleaching test results (IC50 ≥ 20 mg/mL). In addition, the Saudi Sidr honey was able to inhibit biofilm formation on glass slides at 1/2 MIC by 77.11% for Bacillus subtilis, 70.88% for Staphylococcus aureus, 61.79% for Escherichia coli, and 56.64% for Pseudomonas aeruginosa. Similarly, violacein production by Chromobacterium violaceum was reduced by about 56.63%, while the production of pyocyanin by P. aeruginosa was decreased to 46.27% at a low concentration of Saudi Sidr honey. ADMET properties showed that five identified compounds, namely, 1-cyclohexylimidazolidin-2-one, 3-Butyl-3-methylcyclohexanone, 4-butyl-3-methoxy-2-cyclo penten-1-one, 2,2,3,3-Tetramethyl cyclopropane carboxylic acid, and 3,5-dihydroxy-2-(3-methylbut-2-en-1-yl showed promising drug-likeness properties. The compound 3,5-dihydroxy-2-(3-methylbut-2-en-1-yl exhibited the highest binding energy against antimicrobial and antioxidant target proteins (1JIJ, 2VAM, 6B8A, 6F86, 2CDU, and 1OG5). Overall, the obtained results highlighted the promising potential of Saudi Sidr honey as a rich source of bioactive compounds that can be used as food preservatives and antimicrobial, antioxidant, and anti-quorum sensing molecules. Full article

(This article belongs to the Special Issue Studies on the Cytotoxicity and Antimicrobial Effects of Synthetic and Natural Compounds)

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13 pages, 2659 KiB

Open AccessEditor’s ChoiceArticle

Natural Antimicrobials Block the Host NF-κB Pathway and Reduce Enterocytozoon hepatopenaei Infection Both In Vitro and In Vivo

by Iulia Adelina Bunduruș, Igori Balta, Eugenia Butucel, Todd Callaway, Cosmin Alin Popescu, Tiberiu Iancu, Ioan Pet, Lavinia Stef and Nicolae Corcionivoschi

Pharmaceutics 2023, 15(7), 1994; https://doi.org/10.3390/pharmaceutics15071994 - 20 Jul 2023

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Abstract

The objective of this work was to investigate, for the first time, the antioxidant effect of a mixture of natural antimicrobials in an Enterocytozoon hepatopenaei (EHP) shrimp-gut model of infection and the biological mechanisms involved in their way of action. The study approach included investigations, firstly, in vitro, on shrimp-gut primary (SGP) epithelial cells and in vivo by using EHP-challenged shrimp. Our results show that exposure of EHP spores to 0.1%, 0.5%, 1%, and 2% AuraAqua (Aq) significantly reduced spore activity at all concentrations but was more pronounced after exposure to 0.5% Aq. The Aq was able to reduce EHP infection of SGP cells regardless of cells being pretreated or cocultured during infection with Aq. The survivability of SGP cells infected with EHP spores was significantly increased in both scenarios; however, a more noticeable effect was observed when the infected cells were pre-exposed to Aq. Our data show that infection of SGP cells by EHP activates the host NADPH oxidases and the release of H₂O₂ produced. When Aq was used during infection, a significant reduction in H₂O₂ was observed concomitant with a significant increase in the levels of CAT and SOD enzymes. Moreover, in the presence of 0.5% Aq, the overproduction of CAT and SOD was correlated with the inactivation of the NF-κB pathway, which, otherwise, as we show, is activated upon EHP infection of SGP cells. In a challenge test, Aq was able to significantly reduce mortality in EHP-infected shrimp and increase the levels of CAT and SOD in the gut tissue. Conclusively, these results show, for the first time, that a mixture of natural antimicrobials (Aq) can reduce the EHP-spore activity, improve the survival rates of primary gut-shrimp epithelial cells and reduce the oxidative damage caused by EHP infection. Moreover, we show that Aq was able to stop the H₂O₂ activation of the NF-κB pathway of Crustins, Penaeidins, and the lysozyme, and the CAT and SOD activity both in vitro and in a shrimp challenge test. Full article

(This article belongs to the Special Issue Studies on the Cytotoxicity and Antimicrobial Effects of Synthetic and Natural Compounds)

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