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18 pages, 631 KB  
Article
Evaluation of the Antimicrobial, Cyto-Genotoxic, and Antigenotoxic Activity of Dipteryx odorata Seed Extracts
by Margarita Dormousoglou, Ioannis Galiatsatos, Panagiota Stathopoulou, Regina Fragkouli, Maria Antonopoulou, Damian E. L. Fetzer, Marcos L. Corazza, Vasilios Triantafylidis, George Tsiamis, Dimitris Vlastos and Ioanna Efthimiou
Int. J. Mol. Sci. 2026, 27(2), 561; https://doi.org/10.3390/ijms27020561 - 6 Jan 2026
Viewed by 69
Abstract
In the present study, Dipteryx odorata seeds (tonka beans) were extracted via the Soxhlet method to acquire ethanolic (TBSE) and hexane (TBSH) extracts. Both extracts were characterized using Gas Chromatography–Mass Spectrometry (GC-MS). The antimicrobial activity was evaluated against two Gram-positive (Bacillus licheniformis [...] Read more.
In the present study, Dipteryx odorata seeds (tonka beans) were extracted via the Soxhlet method to acquire ethanolic (TBSE) and hexane (TBSH) extracts. Both extracts were characterized using Gas Chromatography–Mass Spectrometry (GC-MS). The antimicrobial activity was evaluated against two Gram-positive (Bacillus licheniformis, Staphylococcus epidermidis) and two Gram-negative (Escherichia coli, Pseudomonas aeruginosa) human pathogens using the disc diffusion test (DDT), followed by the determination of Minimum Inhibitory Concentrations (MIC). The Cytokinesis-Block Micronucleus (CBMN) assay was applied in human lymphocytes (0.1, 0.2, 0.5 µL/mL), to investigate the cyto-genotoxic activity of both extracts, while their antigenotoxic potential was evaluated against mitomycin C (MMC) (0.5 μg/mL). Coumarin was the major constituent in both extracts. TBSE exhibited remarkable antimicrobial activity, whereas TBSH was not equally potent. Cytotoxicity was reported for higher doses, while no genotoxicity was observed, except for 0.2 µL/mL for TBSE. A considerable antigenotoxic activity was shown by the lowest dose of TBSE, which was not present at the two highest concentrations. However, TBSH did not diminish the MMC mediated genotoxicity, while at the same time led to an increase in genotoxic potency. To our knowledge, this is the first comprehensive evaluation of the cyto-genotoxic and antigenotoxic profiles of tonka bean extracts. Full article
(This article belongs to the Special Issue Biological Study of Plant Bioactive Compounds)
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21 pages, 1046 KB  
Article
Aqueous Leaf Extracts of Bauhinia cheilantha (Bong.) Steud.: Phytochemical Profile, Antioxidant Activity and In Vitro Safety Evaluation
by Palloma Lima de Oliveira, José Rafael da Silva Araújo, Camila Marinho da Silva, Kyria Cilene de Andrade Bortoleti, Silvany de Sousa Araújo, Márcia Vanusa da Silva, Dráulio Costa da Silva, Marcos dos Santos Lima, Ana Paula de Oliveira and Ana Christina Brasileiro-Vidal
Drugs Drug Candidates 2025, 4(4), 54; https://doi.org/10.3390/ddc4040054 - 8 Dec 2025
Viewed by 199
Abstract
Background/Objectives: Bauhinia cheilantha Bong. Steud. (Leguminosae; “pata-de-vaca”) is traditionally used in folk medicine for its antidiabetic, anti-inflammatory, and sedative properties. This study aimed to evaluate aqueous leaf extracts of B. cheilantha, non-delipidated and delipidated, regarding their phytochemical composition, phenolic profile, antioxidant potential, [...] Read more.
Background/Objectives: Bauhinia cheilantha Bong. Steud. (Leguminosae; “pata-de-vaca”) is traditionally used in folk medicine for its antidiabetic, anti-inflammatory, and sedative properties. This study aimed to evaluate aqueous leaf extracts of B. cheilantha, non-delipidated and delipidated, regarding their phytochemical composition, phenolic profile, antioxidant potential, and cytotoxic, genotoxic, and antigenotoxic effects. Methods: Phytochemical screening was performed by TLC, and phenolic compounds were determined by HPLC. Antioxidant activity was assessed using DPPH, ABTS, and phosphomolybdenum assays. Cytotoxicity, genotoxicity, and antigenotoxicity were evaluated in L929 murine fibroblast cells using MTT and cytokinesis-block micronucleus (CBMN) assays. Results: Both extracts contained anthocyanins, phenolics, lignans, saponins, and hydrolyzable tannins. The delipidated extract showed higher total phenolic content (17.54 mg/kg) than the non-delipidated (13.76 mg/kg). Major constituents included kaempferol 3-glucoside, quercetin, hesperidin, naringenin, and t-cinnamic acid. Antioxidant assays revealed EC50 values of 25.84, 13.60, and 66.09 µg/mL for the non-delipidated extract, and 26.19, 16.34, and 52.78 µg/mL for the delipidated extract in the DPPH, ABTS, and phosphomolybdenum assays, respectively. No cytotoxicity was observed, except at 1600 µg/mL for the non-delipidated extract and 800–1600 µg/mL for the delipidated extract. Genotoxicity occurred only at 400 µg/mL. Antigenotoxic evaluation showed that the non-delipidated extract (100 µg/mL) reduced methyl methanesulfonate-induced chromosomal damage in simultaneous and post-treatment conditions, while the delipidated extract was only effective for post-treatment. Conclusions: Aqueous extracts of B. cheilantha exhibit antioxidant and antigenotoxic properties. At active concentrations, they were non-cytotoxic and non-genotoxic. The non-delipidated extract, in particular, showed the strongest genome-protective potential, supporting its traditional use and highlighting its relevance in the development of natural therapeutic agents. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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28 pages, 19684 KB  
Article
Carvacrol-Loaded Chitosan Nanoparticles as a Multifunctional Nanotherapeutic Strategy Targeting Oxidative Stress, Inflammation, Apoptosis, and Genotoxicity in Nonalcoholic Fatty Liver Disease
by M. Alfawaz, Ekramy M. Elmorsy, Ahmad Najem Alshammari, Noor A. Hakim, Najlaa M. M. Jawad, Soha A. Hassan, Manal S. Fawzy and Safya E. Esmaeel
Antioxidants 2025, 14(12), 1432; https://doi.org/10.3390/antiox14121432 - 28 Nov 2025
Viewed by 621
Abstract
Nonalcoholic fatty liver disease (NAFLD) associated with high-fat diet (HFD) intake involves oxidative stress, inflammation, apoptosis, and genotoxicity. Carvacrol, a natural monoterpenoid phenol, exhibits potent antioxidant, anti-inflammatory, and cytoprotective properties, but its clinical application is limited by poor solubility and bioavailability. Chitosan nanoparticles, [...] Read more.
Nonalcoholic fatty liver disease (NAFLD) associated with high-fat diet (HFD) intake involves oxidative stress, inflammation, apoptosis, and genotoxicity. Carvacrol, a natural monoterpenoid phenol, exhibits potent antioxidant, anti-inflammatory, and cytoprotective properties, but its clinical application is limited by poor solubility and bioavailability. Chitosan nanoparticles, known for their biocompatibility and ability to enhance drug delivery, offer a promising nanotherapeutic platform for carvacrol delivery in NAFLD. Given the limited therapeutic options for NAFLD, there is a growing interest in nanotherapeutic strategies to enhance the delivery and efficacy of natural antioxidants. This study examined carvacrol-loaded chitosan nanoparticles (CRV-CNPs) in HFD-induced NAFLD. Sixty rats were assigned to six groups: control, CRV-treated (100 mg/kg), CRV-CNP-treated (100 mg/kg), HFD-fed, and two combination groups receiving HFD with either CRV or CRV-CNPs (100 mg/kg) for six weeks after 14 weeks on HFD. Liver function, metabolic markers, oxidative stress parameters, antioxidant enzyme levels, inflammatory and fibrotic mediators, apoptotic gene expression, genotoxicity indices, and histopathological changes were evaluated. CRV-CNPs showed greater efficacy than free carvacrol in ameliorating hepatic dysfunction and metabolic disturbances in HFD-fed rats. CRV-CNPs significantly reduced malondialdehyde, upregulated Nrf2, and elevated hepatic glutathione peroxidase, superoxide dismutase, catalase, and reduced glutathione. Inflammatory markers (NF-κB, iNOS, IL-1β, CRP) and transforming growth factor-beta were suppressed. Pro-apoptotic genes (Bax, Caspase-3) were downregulated, while antiapoptotic Bcl-2 was upregulated. CRV-CNPs also reduced DNA fragmentation and 8-hydroxy-2′-deoxyguanosine levels, indicating strong antigenotoxic effects. Histopathological and ultrastructural assessments revealed mitigated steatosis, preserved hepatic architecture, and maintained mitochondrial integrity. In conclusion, CRV-CNPs provide potent hepatoprotection by targeting oxidative stress, inflammation, apoptosis, and genotoxicity in NAFLD, demonstrating enhanced bioavailability, solubility, and sustained release, which support their potential as an advanced nanotherapeutic strategy for NAFLD management. Full article
(This article belongs to the Special Issue Applications of Antioxidant Nanoparticles, 2nd Edition)
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14 pages, 1816 KB  
Article
Sage Essential Oil as a Natural Antigenotoxic Agent: Comet Assay Findings and Pharmacological Relevance
by Sara Diogo Gonçalves, Igor Koval, Rita S. Matos and Ana Caramelo
Appl. Biosci. 2025, 4(4), 54; https://doi.org/10.3390/applbiosci4040054 - 19 Nov 2025
Viewed by 510
Abstract
Oxidative stress is a major contributor to genomic instability and a key factor in the etiology of various chronic diseases. Natural compounds with antioxidant and DNA-protective properties are increasingly being explored as potential preventive agents. In this study, we investigated the antigenotoxic potential [...] Read more.
Oxidative stress is a major contributor to genomic instability and a key factor in the etiology of various chronic diseases. Natural compounds with antioxidant and DNA-protective properties are increasingly being explored as potential preventive agents. In this study, we investigated the antigenotoxic potential of Salvia sclarea L. (sage) essential oil in human peripheral blood mononuclear cells exposed to hydrogen peroxide-induced oxidative stress. The DNA damage was assessed using the in vivo Comet assay, and five concentrations of sage essential oil (0.2–3%) were evaluated, both with and without co-exposure to H2O2. The results show a dose-dependent reduction in DNA damage in cells treated with the essential oil, with significant protection observed at all tested concentrations. Chemical characterization of the essential oil revealed a high content of linalyl acetate (62.63%) and linalool (22.22%), compounds known for their antioxidant activities. These findings demonstrate the antigenotoxic capacity of S. sclarea essential oil and strengthen the evidence supporting its role as a natural agent capable of protecting human cells from oxidative DNA damage. The study contributes to the growing body of evidence on essential oils as multifunctional bioactive agents and highlights the importance of incorporating natural compounds into strategies aimed at mitigating oxidative DNA damage. Full article
(This article belongs to the Special Issue Plant Natural Compounds: From Discovery to Application (2nd Edition))
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30 pages, 768 KB  
Review
Lactoferrin, a Natural Protein with Multiple Functions in Health and Disease
by Manuela Rizzi, Paolo Manzoni, Chiara Germano, Maria Florencia Quevedo and Pier Paolo Sainaghi
Nutrients 2025, 17(21), 3403; https://doi.org/10.3390/nu17213403 - 29 Oct 2025
Viewed by 4915
Abstract
Lactoferrin is a multifunctional glycoprotein showing multiple biological properties (antimicrobial, antiviral, antioxidant, antigenotoxic, prebiotic, probiotic) that play an essential role in maintaining host physiological homeostatic condition by exerting immunomodulatory and anti-inflammatory activities. Thanks to these biological properties, lactoferrin has widely been studied as [...] Read more.
Lactoferrin is a multifunctional glycoprotein showing multiple biological properties (antimicrobial, antiviral, antioxidant, antigenotoxic, prebiotic, probiotic) that play an essential role in maintaining host physiological homeostatic condition by exerting immunomodulatory and anti-inflammatory activities. Thanks to these biological properties, lactoferrin has widely been studied as a therapeutic agent in gastroenteric diseases, neonatal sepsis and necrotizing enterocolitis, lung diseases, and COVID-19, showing very heterogeneous results based on the disease considered and the population studied. Since lactoferrin is one of the main components of neutrophils’ secondary granules, it has also been investigated as a potential disease-monitoring biomarker, especially for diseases in which inflammation is a key component. This narrative review offers updated and comprehensive insights into the available literature on lactoferrin biology, biological properties, and clinical utility. Full article
(This article belongs to the Section Nutritional Immunology)
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39 pages, 7417 KB  
Article
Development of a Collagen–Cerium Oxide Nanohydrogel for Wound Healing: In Vitro and In Vivo Evaluation
by Ekaterina Vladimirovna Silina, Natalia Evgenievna Manturova, Victor Ivanovich Sevastianov, Nadezhda Victorovna Perova, Mikhail Petrovich Gladchenko, Alexey Anatolievich Kryukov, Aleksandr Victorovich Ivanov, Victor Tarasovich Dudka, Evgeniya Valerievna Prazdnova, Sergey Alexandrovich Emelyantsev, Evgenia Igorevna Kozhukhova, Vladimir Anatolievich Parfenov, Alexander Vladimirovich Ivanov, Mikhail Alexandrovich Popov and Victor Alexandrovich Stupin
Biomedicines 2025, 13(11), 2623; https://doi.org/10.3390/biomedicines13112623 - 26 Oct 2025
Cited by 1 | Viewed by 1187
Abstract
Background: Effective regenerative therapeutics for acute and chronic wounds remain a critical unmet need in biomedicine. Objectives: This study aimed to develop novel collagen–cerium oxide nanoparticle hydrogels designed to enhance cellular metabolism, proliferation, and antioxidant/antimutagenic activity, accelerating wound regeneration in vivo. [...] Read more.
Background: Effective regenerative therapeutics for acute and chronic wounds remain a critical unmet need in biomedicine. Objectives: This study aimed to develop novel collagen–cerium oxide nanoparticle hydrogels designed to enhance cellular metabolism, proliferation, and antioxidant/antimutagenic activity, accelerating wound regeneration in vivo. Methods: Collagen–nanocerium composites were synthesized by combining a collagen extract with cerium oxide nanoparticles at defined concentrations. In vitro assays using human fibroblasts identified two formulations that enhanced proliferation and metabolic activity by 42–50%. FTIR spectroscopy confirmed chemical interactions within the composite matrix. Toxicity, antioxidant, and antigenotoxic effects were evaluated using Escherichia coli MG1655 lux-biosensors to assess their general toxicity, antioxidant and pro-oxidant activities, and antigenotoxic and promutagenic effects. In vivo efficacy was tested in Wistar rats with full-thickness skin wounds. Treated groups were compared to untreated controls and Dexpanthenol-treated positive controls. On days 3, 7, and 14, healing was assessed clinically, histologically, and morphometrically. Results: Biosensor analysis demonstrated non-toxicity and antigenotoxic activity of the nanocomposites, reduced DNA damage by up to 45%, providing 31–49% protection against H2O2 and 15–23% against O2 radicals. The animal study results demonstrated significantly accelerated healing with both nanocomposites versus control and comparison groups, evidenced by improved tissue regeneration, reduced inflammation, and increased fibroblast infiltration. Conclusions: The developed hydrogels exhibit promising pharmacological profiles, including antioxidant, antimutagenic, anti-inflammatory, and pro-regenerative effects validated across in vitro and in vivo models. Full article
(This article belongs to the Special Issue Medicinal Chemistry in Drug Design and Discovery, 2nd Edition)
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17 pages, 923 KB  
Article
Assessment of Antioxidant Activity and Dose-Dependent Effect on Genotoxicity/Antigenotoxicity of Pulmonaria officinalis Ethanolic Extract
by Ana Ignjatijević, Tamara Anđić, Marija Lješević, Biljana Nikolić, Tea Ganić, Stefana Spasović and Stefana Vuletić
Pharmaceutics 2025, 17(9), 1134; https://doi.org/10.3390/pharmaceutics17091134 - 29 Aug 2025
Viewed by 1257
Abstract
Background/Objectives: Pulmonaria officinalis L., commonly known as lungwort, is a medicinal plant traditionally used for respiratory ailments, but its biological activities have not yet been sufficiently researched. The aim of this study was to investigate the antioxidant and dose-dependent genotoxic/antigenotoxic properties of [...] Read more.
Background/Objectives: Pulmonaria officinalis L., commonly known as lungwort, is a medicinal plant traditionally used for respiratory ailments, but its biological activities have not yet been sufficiently researched. The aim of this study was to investigate the antioxidant and dose-dependent genotoxic/antigenotoxic properties of a 70% ethanolic extract. Methods: Quantification of polyphenols and GC–MS analysis were performed in order to chemically characterize the extract. Antioxidant activity was evaluated through DPPH, PFRAP, total antioxidant capacity (TAC), and ferrous ion chelating assay (FIC). MTT and alkaline comet assay were used for investigation of cytotoxicity and geno/antigenotoxicity on normal fetal fibroblast cells (MRC-5). Results: The chemical analysis of the extract showed that the extract is rich in polyphenolics and that phytol is the most abundant compound, accompanied by terpenoids, fatty acids, alcohols, polyketides, and alkaloids. In addition, notable antioxidant capacity was detected in all tests applied. The extract reduced cell viability only at the highest concentration tested (33.7%). Furthermore, a dual dose-dependent effect was recorded since the genotoxic effect of the tested extract was observed at higher concentrations, while non-genotoxic concentrations showed protective effects against oxidative damage of DNA. Namely, pretreatment with lungwort extract reduced the DNA damage induced by H2O2, with the highest protective effect at the lowest tested concentration, indicating a hormetic mode of action. Conclusions: These results provide a solid foundation for future research into this medicinal plant, with the aim of its potential therapeutic use in the prevention of diseases associated with oxidative stress. Full article
(This article belongs to the Section Biopharmaceutics)
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27 pages, 425 KB  
Review
Green Preservation Strategies: The Role of Essential Oils in Sustainable Food Preservatives
by Sara Diogo Gonçalves, Maria das Neves Paiva-Cardoso and Ana Caramelo
Sustainability 2025, 17(16), 7326; https://doi.org/10.3390/su17167326 - 13 Aug 2025
Cited by 5 | Viewed by 3431
Abstract
Essential oils (EOs) have gained increasing attention as natural alternatives to synthetic food preservatives due to their broad-spectrum antimicrobial, antioxidant, and antigenotoxic properties. Derived from aromatic plants, EOs possess complex chemical compositions rich in bioactive compounds such as terpenes, phenolics, and aldehydes, which [...] Read more.
Essential oils (EOs) have gained increasing attention as natural alternatives to synthetic food preservatives due to their broad-spectrum antimicrobial, antioxidant, and antigenotoxic properties. Derived from aromatic plants, EOs possess complex chemical compositions rich in bioactive compounds such as terpenes, phenolics, and aldehydes, which contribute to their effectiveness against foodborne pathogens, oxidative spoilage, and genotoxic contaminants. This review provides a comprehensive examination of the potential of EOs in food preservation, highlighting their mechanisms of action, including membrane disruption, efflux pump inhibition, and reactive oxygen species scavenging. Standard assays such as disk diffusion, MIC/MBC, time-kill kinetics, and comet and micronucleus tests are discussed as tools for evaluating efficacy and safety. Additionally, the use of EOs in diverse food matrices and the reduction in reliance on synthetic additives support cleaner-label products and improved consumer health. The review also examines the sustainability outlook, highlighting the potential for extracting EOs from agricultural byproducts, their integration into green food processing technologies, and alignment with the circular economy and the Sustainable Development Goals. Despite promising results, challenges remain in terms of sensory impact, regulatory approval, and dose optimization. Overall, EOs represent a multifunctional and sustainable solution for modern food preservation systems. Full article
(This article belongs to the Special Issue Future Trends in Food Processing and Food Preservation Techniques)
15 pages, 302 KB  
Review
Pruritus in Palliative Care: A Narrative Review of Essential Oil-Based Strategies to Alleviate Cutaneous Discomfort
by Sara Diogo Gonçalves
Diseases 2025, 13(8), 232; https://doi.org/10.3390/diseases13080232 - 23 Jul 2025
Cited by 2 | Viewed by 2779
Abstract
Pruritus is a common and distressing symptom in palliative care, often resulting from complex underlying conditions such as cancer, chronic kidney disease, and liver failure. Conventional pharmacological treatments frequently offer limited relief and may produce undesirable side effects in this medically fragile population. [...] Read more.
Pruritus is a common and distressing symptom in palliative care, often resulting from complex underlying conditions such as cancer, chronic kidney disease, and liver failure. Conventional pharmacological treatments frequently offer limited relief and may produce undesirable side effects in this medically fragile population. Despite the high prevalence and impact of pruritus in palliative care, there is a lack of consolidated evidence on integrative non-pharmacological approaches. This narrative review explores the potential role of essential oils as a complementary approach to managing pruritus in palliative settings. A review of the literature was conducted to examine the mechanisms of action, safety considerations, and clinical outcomes associated with the use of essential oils, with a particular focus on their anti-inflammatory, neuromodulatory, and soothing properties. Evidence suggests that essential oils may provide symptom relief and enhance quality of life when integrated into multidisciplinary care; however, small sample sizes, heterogeneity, and methodological weaknesses often limit the findings of these studies. Furthermore, the long-term safety and antigenotoxic potential of essential oils remain underexplored. This narrative review concludes that while essential oils appear promising as adjunct therapies for pruritus, further rigorous research, particularly well-designed clinical trials and toxicological assessments, is needed to support their safe and effective use in palliative care. Full article
17 pages, 1126 KB  
Article
Argovit™ Silver Nanoparticles Mitigate Sodium Arsenite-Induced Cytogenotoxicity Effects in Cultured Human Lymphocytes
by María del Carmen Jauregui Romo, Balam Ruiz Ruiz, Francisco Casilas-Figueroa, Nayeli Guadalupe Girón Vázquez, Roberto Luna Vázquez Gómez, Olivia Torres-Bugarín, Idalia Yazmín Castañeda Yslas, Alexey Pestryakov, Nina Bogdanchikova and María Evarista Arellano García
Toxics 2025, 13(7), 539; https://doi.org/10.3390/toxics13070539 - 27 Jun 2025
Viewed by 1251
Abstract
Exposure to arsenic, a known environmental and occupational genotoxicant, poses significant health risks. Identifying agents capable of mitigating its effects is crucial for public health. This study evaluates the protective potential of Argovit™ silver nanoparticles (AgNPs) against cytotoxic and genotoxic damage induced by [...] Read more.
Exposure to arsenic, a known environmental and occupational genotoxicant, poses significant health risks. Identifying agents capable of mitigating its effects is crucial for public health. This study evaluates the protective potential of Argovit™ silver nanoparticles (AgNPs) against cytotoxic and genotoxic damage induced by sodium arsenite in ex vivo cultured human lymphocytes obtained from the whole blood of healthy donors. Lymphocytes were exposed to sodium arsenite (3.7 × 10−3 µg/mL) and Argovit™ AgNPs (3.6 × 10−3 µg/mL). The cytokinesis-block micronucleus (CBMN) assay was performed using a modified 144 h protocol to assess delayed effects across two cell cycles. Four groups were analyzed: untreated control, sodium arsenite only, AgNPs only, and sodium arsenite followed by AgNPs. Arsenite exposure increased cytotoxic and genotoxic biomarkers. In contrast, post-treatment with AgNPs significantly reduced these effects. All treatments were performed in duplicate, and data were analyzed using the Kruskal–Wallis test with Dunn’s post hoc comparison (p < 0.05). Statistical analysis confirmed the antigenotoxic and cytoprotective properties of Argovit™. These findings support its potential application as a mitigating agent in scenarios of environmental or occupational exposure to genotoxic compounds. Full article
(This article belongs to the Section Human Toxicology and Epidemiology)
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17 pages, 1433 KB  
Article
Insights into Chemopreventive Effects of Rosmarinic Acid Against Aflatoxin B1-Induced Genotoxic Effects
by Veronika Furlan, Matjaž Novak, Martina Štampar, Alja Štern, Bojana Žegura and Urban Bren
Foods 2025, 14(12), 2111; https://doi.org/10.3390/foods14122111 - 16 Jun 2025
Viewed by 1072
Abstract
In this study, the chemopreventive effects of rosmarinic acid (RA), a major phenolic acid of the plant Rosmarinus officinalis L., against the carcinogenic naturally occurring mycotoxin aflatoxin B1 (AFB1) were investigated using both in silico and in vitro approaches. The in silico investigation [...] Read more.
In this study, the chemopreventive effects of rosmarinic acid (RA), a major phenolic acid of the plant Rosmarinus officinalis L., against the carcinogenic naturally occurring mycotoxin aflatoxin B1 (AFB1) were investigated using both in silico and in vitro approaches. The in silico investigation of the chemical reactions between rosmarinic acid and the carcinogenic metabolite of AFB1, aflatoxin B1 exo-8,9-epoxide (AFBO), was conducted by activation free energies calculations with DFT functionals M11-L and MN12-L, in conjunction with the 6-311++G(d,p) flexible basis set and implicit solvation model density (SMD), according to a newly developed quantum mechanics-based protocol for the evaluation of carcinogen scavenging activity (QM-CSA). Following the computational analyses, the chemoprotective effects of RA were further studied in vitro in human hepatocellular carcinoma HepG2 cells by analyzing its influence on AFB1-induced genotoxicity using a comet assay, γH2AX, and p-H3, while its impact on cell proliferation and cell cycle modulation was assessed using flow cytometry. Our computational results revealed that the activation free energy required for the reaction of RA with AFBO (14.86 kcal/mol) is significantly lower than the activation free energy for the competing reaction of AFBO with guanine (16.88 kcal/mol), which indicates that RA acts as an efficient natural scavenger of AFBO, potentially preventing AFB1-specific DNA adduct formation. The chemoprotective activity of RA was confirmed through in vitro experiments, which demonstrated a statistically significant (p < 0.05) reduction in AFB1-induced single- and double-strand breaks in HepG2 cells exposed to a mixture of AFB1 and RA at non-cytotoxic concentrations. In addition, RA reversed the AFB1-induced reduction in cell proliferation. Full article
(This article belongs to the Special Issue Potential Health Benefits of Plant Food-Derived Bioactive Compounds)
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16 pages, 1011 KB  
Article
Preventive Capacity of Citrus paradisi Juice for Male Reproductive Damage Induced by Cadmium Chloride in Mice
by Isela Álvarez-González, José David García-García, Beatriz A. Espinosa-Ahedo, Luis S. Muñoz-Carrillo, José A. Morales-González, Eduardo O. Madrigal-Santillán, Felipe de Jesús Carrillo-Romo, Antonieta García-Murillo, Rogelio Paniagua-Pérez and Eduardo Madrigal-Bujaidar
Appl. Sci. 2025, 15(11), 6071; https://doi.org/10.3390/app15116071 - 28 May 2025
Cited by 1 | Viewed by 1043
Abstract
Previous studies have shown mouse antigenotoxic and chemopreventive potential with the administration of Citrus paradisi juice (GJ). To evaluate another activity, the aim of the present report was to determine the beneficial effect of GJ on male mouse reproductive damage induced by cadmium [...] Read more.
Previous studies have shown mouse antigenotoxic and chemopreventive potential with the administration of Citrus paradisi juice (GJ). To evaluate another activity, the aim of the present report was to determine the beneficial effect of GJ on male mouse reproductive damage induced by cadmium chloride (CC). Seven groups of mice were intragastrically (IG) administered for 11 days. A control group was administered purified water daily, three groups were administered GJ daily (4.1, 16.6, and 33.2 µL/g), plus a single administration of CC (3 mg/kg) on the fifth day of the assay, another group was treated daily with 33.2 µL/g GJ, and a positive control group was treated with 3 mg/kg of CC on day 5 of the experiment. The results with the high GJ dose on the CC-treated mice showed a mean reduction of 88% in sperm quality endpoints (viability, motility, malformations) and a 94% sperm concentration increase. With the same dose, we also determined an 81% reduction in the DNA breaking potential and in the number of micronuclei in the spermatids. We also found an 87% decrease in lipoperoxidation and a 68% decrease in protein oxidation with respect to the CC damage, and a strong DPPH scavenging ability. Our results suggest the potential involvement of the GJ antioxidant in the observed effect. Full article
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23 pages, 1563 KB  
Article
Bioactive Compounds, Antioxidant, Cytotoxic, and Genotoxic Investigation of the Standardized Liquid Extract from Eugenia involucrata DC. Leaves
by Monatha Nayara Guimarães Teófilo, Leonardo Gomes Costa, Jamira Dias Rocha, Fernando Gomes Barbosa, Anielly Monteiro de Melo, Grazzielle Guimarães de Matos, Cristiane Maria Ascari Morgado, Amanda Silva Fernandes, Lucas Barbosa Ribeiro de Carvalho, Clayson Moura Gomes, Milton Adriano Pelli de Oliveira, Joelma Abadia Marciano de Paula, Elisa Flávia Luiz Cardoso Bailão and Leonardo Luiz Borges
Pharmaceuticals 2025, 18(5), 764; https://doi.org/10.3390/ph18050764 - 21 May 2025
Cited by 1 | Viewed by 1670
Abstract
Background: Eugenia involucrata DC., a Cerrado native plant, is recognized for its medicinal properties. However, its bioactive compounds remain inadequately explored. Objectives: This study investigated bioactive compounds from a standardized liquid extract from E. involucrata leaves that can act with antioxidant, [...] Read more.
Background: Eugenia involucrata DC., a Cerrado native plant, is recognized for its medicinal properties. However, its bioactive compounds remain inadequately explored. Objectives: This study investigated bioactive compounds from a standardized liquid extract from E. involucrata leaves that can act with antioxidant, cytogenotoxic, cytoprotective, and genoprotective effects. Methods: The phenolic compounds in the standardized liquid extract from E. involucrata leaves were screened by HPLC-DAD. The capture of the free radicals DPPH, ABTS+, and the metal reduction power FRAP determined the antioxidant potential. Cytotoxicity was evaluated in RAW 264.7 macrophages (MTT assay), and (anti)cytotoxic and (anti)genotoxic effects were assessed in human lymphocytes using the Trypan blue exclusion method and comet assay, respectively. Results: The extracts present key phenolic compounds, such as ellagic acid, myricitrin, and epicatechin gallate. The standardized extract demonstrated antioxidant capacity, evidenced by its ability to reduce iron and scavenge free radicals. The liquid extract from E. involucrata leaves exhibited cytotoxic effects on RAW 264.7 macrophages at higher concentrations, while demonstrating (anti)cytotoxic activity on human lymphocytes from all tested concentrations. The highest concentration tested of the standardized liquid extract from E. involucrata leaves (250 µg/mL) showed genotoxicity against human lymphocytes compared to the negative control. In contrast, the lowest concentration (62.5 µg/mL) exhibited an antigenotoxic effect on human lymphocytes, reducing the genotoxicity of doxorubicin by approximately 27%. Conclusions: The bioactive compounds in the standardized liquid extract from E. involucrata leaves exhibited antioxidant and antigenotoxic properties, suggesting potential value for nutraceutical and pharmaceutical applications, particularly those related to oxidative stress associated withaging and disease progression. Full article
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21 pages, 3711 KB  
Article
Metabolomic Profiling and In Vitro Evaluation of Cytotoxic, Genotoxic, and Antigenotoxic Effects of Staphylea pinnata L. Extract from Italian Flora
by Ghanya Al-Naqeb, Fabio Pietrolucci, Mauro Commisso, Aliki Kalmpourtzidou, Amanda Oldani, Sara Boussetta, Beatrice Maccarini, Rachele De Giuseppe and Hellas Cena
Biomolecules 2025, 15(3), 385; https://doi.org/10.3390/biom15030385 - 6 Mar 2025
Cited by 1 | Viewed by 1701
Abstract
Staphylea pinnata L., (S. pinnata), has long been recognized in Europe as both a wild food source and a traditional medicinal. This study aimed to characterize the metabolomic profile of the leaf extract of S. pinnata and assess its cytotoxic, genotoxic, [...] Read more.
Staphylea pinnata L., (S. pinnata), has long been recognized in Europe as both a wild food source and a traditional medicinal. This study aimed to characterize the metabolomic profile of the leaf extract of S. pinnata and assess its cytotoxic, genotoxic, and antigenotoxic effects in vitro for the first time. The methanolic extract of the leaves was analyzed using Ultra-Performance Liquid Chromatography–High-Resolution Mass Spectrometry (UPLC-HRMS). To evaluate its cytotoxic, genotoxic, and antigenotoxic properties, the cytokinesis block micronucleus assay was performed on Chinese hamster ovarian K1 cells. The analysis revealed a wide variety of metabolites in the extract, with B-type procyanidins and prodelphinidins being the most abundant. The genotoxicity of the extract varied depending on its concentration; at the lowest concentration (75 μg/mL), it showed no genotoxic effects and exhibited antigenotoxic properties by reducing the frequency of micronuclei induced by mitomycin C. However, at the highest concentration (300 μg/mL), the extract demonstrated genotoxic effects. In conclusion, the S. pinnata extract displayed both genotoxic and antigenotoxic properties, which may be attributed to its phytochemical composition. These findings highlight the complex nature of the plant’s bioactive compounds, suggesting potential therapeutic applications with careful consideration of dosage. Additional research is necessary to understand the mechanisms underlying these properties. Full article
(This article belongs to the Special Issue Natural Bioactives as Leading Molecules for Drug Development)
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Article
Bioactivity Assessment of Functionalized TiO2 Powder with Dihydroquercetin
by Valentina Nikšić, Andrea Pirković, Biljana Spremo-Potparević, Lada Živković, Dijana Topalović, Jovan M. Nedeljković and Vesna Lazić
Int. J. Mol. Sci. 2025, 26(4), 1475; https://doi.org/10.3390/ijms26041475 - 10 Feb 2025
Cited by 1 | Viewed by 1328
Abstract
Biological activities, including cell viability, oxidative stress, genotoxicity/antigenotoxicity, and antimicrobial activity, were evaluated for a visible-light-responsive TiO2-based ICT complex with dihydroquercetin (DHQ) and compared with pristine TiO2, its inorganic component. Pristine TiO2 did not induce cytotoxicity in MRC-5 [...] Read more.
Biological activities, including cell viability, oxidative stress, genotoxicity/antigenotoxicity, and antimicrobial activity, were evaluated for a visible-light-responsive TiO2-based ICT complex with dihydroquercetin (DHQ) and compared with pristine TiO2, its inorganic component. Pristine TiO2 did not induce cytotoxicity in MRC-5 or HeLa cells within the tested concentration range (1–20 mg/mL), while TiO2/DHQ displayed a significant reduction in cell viability in both cell lines at higher concentrations (≥10 mg/mL). The analysis of reactive oxygen species (ROS) production revealed that TiO2/DHQ significantly reduced ROS levels in both cell types (MRC-5 and HeLa), with HeLa cells showing a more substantial reduction at lower concentrations. Genotoxicity assessment using the comet assay demonstrated that TiO2 induced DNA damage in MRC-5 cells, while TiO2/DHQ did not, indicating that DHQ mitigates the genotoxic potential of TiO2. Furthermore, TiO2/DHQ exhibited antigenotoxic effects by reducing H2O2-induced DNA damage in MRC-5 cells, supporting its protective role against oxidative stress. Preliminary antimicrobial tests revealed that TiO2/DHQ exhibits antimicrobial activity against E. coli under visible-light excitation, while TiO2 does not. These findings suggest that the TiO2-based ICT complex with DHQ with enhanced antioxidant properties can potentially serve as a safe, non-toxic biocide agent. Full article
(This article belongs to the Special Issue Novel Nanoparticle Composites: Functionalization and Application)
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