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Search Results (459)

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20 pages, 493 KiB  
Review
Glucosinolates in Cruciferous Vegetables: Genetic and Environmental Regulation, Metabolic Pathways, and Cancer-Preventive Mechanisms
by Sujata Kattel and George F. Antonious
Int. J. Plant Biol. 2025, 16(2), 58; https://doi.org/10.3390/ijpb16020058 - 29 May 2025
Abstract
We investigated the genetic and environmental variables determining the glucosinolate (GSL) content of cruciferous vegetables and the implications for cancer prevention. The enzyme myrosinase hydrolyzes GSLs, which are sulfur-containing chemicals found mostly in cruciferous vegetables, producing isothiocyanates (ITCs), which are physiologically active molecules. [...] Read more.
We investigated the genetic and environmental variables determining the glucosinolate (GSL) content of cruciferous vegetables and the implications for cancer prevention. The enzyme myrosinase hydrolyzes GSLs, which are sulfur-containing chemicals found mostly in cruciferous vegetables, producing isothiocyanates (ITCs), which are physiologically active molecules. GSL breakdown products have considerable anti-carcinogenic, antioxidant, and anti-inflammatory capabilities, making them vital to human health. The review dives into genetic heterogeneity among cruciferous species, the importance of individual genes in GSL manufacturing, and breeding techniques for increasing GSL content. It also examines how environmental variables like soil type, pH, plant, nutrient availability, and temperature affect GSL levels. This report also covers the function of GSLs in plant defense, their bioavailability in humans, and their mechanisms in cancer prevention, emphasizing the chemicals’ potential for lowering cancer risk through cruciferous vegetable consumption. The findings highlight the necessity of optimizing both genetic and environmental variables required to increase the nutritional content and medicinal potential of cruciferous vegetables. Full article
(This article belongs to the Section Plant Biochemistry and Genetics)
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21 pages, 1053 KiB  
Review
Benefits of Probiotics—Biodetoxification
by Barbara Sionek, Aleksandra Szydłowska, Danuta Jaworska and Danuta Kołożyn-Krajewska
Appl. Sci. 2025, 15(10), 5297; https://doi.org/10.3390/app15105297 - 9 May 2025
Viewed by 367
Abstract
The rapid growth of the world’s population is generating escalating demands for food production. Global food demand is expected to increase by 35% to 56% between 2010 and 2050. Therefore, food mass production is becoming more challenging. The chemicalization of food production, processing, [...] Read more.
The rapid growth of the world’s population is generating escalating demands for food production. Global food demand is expected to increase by 35% to 56% between 2010 and 2050. Therefore, food mass production is becoming more challenging. The chemicalization of food production, processing, transport, packaging, and storage is almost impossible to avoid. These factors, along with environmental pollution, contribute to the increase in food product contamination. Xenobiotics appearing in food, including a variety of toxic substances (heavy metals, acrylamide, polycyclic aromatic hydrocarbons), and pathogens (pathogenic bacteria, fungi, molds, and yeast-producing mycotoxins) can threaten consumers’ safety and have negative economic implications. In this regard, the introduction of effective detoxification methods appears to be very important. It can be accomplished by physical, chemical, and biological means. Many reports have proved that probiotics are useful in food biodetoxification. Probiotics effectively reduce food contamination (at various stages of food production) and, moreover, annihilate toxins present in the human body. Many in vitro studies have confirmed the biodetoxification properties of probiotics, demonstrating that they diminish the toxic effects of the main types of food contaminants (heavy metals, polycyclic aromatic hydrocarbons, pesticides, mycotoxins, nitrates and nitrites, acrylamide, alkylphenols, biogenic amines, and dioxins). Probiotics produce various bioactive compounds, including antimutagenic, antioxidant, and anti-carcinogenic compounds. Their protective and beneficial influence on human microbiota can modulate host inflammatory processes, inhibit carcinogenesis, and modify immune resistance. Detoxification with probiotics is environment-friendly and, unlike physical and chemical methods, does not adversely affect the nutritional value and quality of food. In addition, probiotics in food are associated with well-known human health benefits; therefore, as a functional food, they have gained common consumer acceptance. The large-scale application of biodetoxification methods in both agriculture and the food industry is a challenge for the future. Based on contemporary research, this review provides the mechanism of probiotic biodetoxification, possible applications of various probiotics, and future trends. Full article
(This article belongs to the Section Applied Biosciences and Bioengineering)
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24 pages, 5739 KiB  
Article
Multifaceted Biological Activities of Culinary Herb and Spice Extracts: In Vitro and In Silico Simulation Insights into Inflammation-Related Targets
by Nance Hontman, Jéssica Gonçalves, José S. Câmara and Rosa Perestrelo
Foods 2025, 14(9), 1456; https://doi.org/10.3390/foods14091456 - 23 Apr 2025
Viewed by 314
Abstract
Culinary herbs and spices are valued worldwide for their flavor, aroma, and medicinal benefits. They encompass diverse bioactive metabolites, such as polyphenols and terpenoids, which contribute to plant defense and offer anticarcinogenic, anti-inflammatory, antioxidant, and cognitive-enhancing effects. This study aimed to establish the [...] Read more.
Culinary herbs and spices are valued worldwide for their flavor, aroma, and medicinal benefits. They encompass diverse bioactive metabolites, such as polyphenols and terpenoids, which contribute to plant defense and offer anticarcinogenic, anti-inflammatory, antioxidant, and cognitive-enhancing effects. This study aimed to establish the volatile fingerprint of culinary herbs (lemon verbena, chives, basil, sage, coriander, and parsley) and spices (curcuma, nutmeg, cumin, black pepper, Jamaica pepper, and juniper berry) using headspace solid-phase microextraction combined with gas chromatography-mass spectrometry (HS-SPME/GC-MS). The predominant volatile organic metabolites (VOMs) identified were subjected to in silico molecular docking simulations of anti-Alzheimer’s (e.g., acetylcholinesterase (AChE), butyrylcholinesterase (BChE)), antioxidants (e.g., monoamine oxidase B (MAO-B), inducible nitric oxide synthase (iNOS)), and anti-inflammatory receptors (e.g., 5-lipoxygenase (5-LOX), cyclooxygenase-2 (COX-2)). The culinary herb and spice extracts were also subjected to in vitro assays to evaluate their potential as antioxidant (DPPH, ABTS, and ORAC) and anti-inflammatory (% protein denaturation) agents. A total of 121 VOMs were identified in the culinary herbs and spices, with the predominant chemical families being monoterpenoids (48.3%), sesquiterpenoids (14.0%), esters (11.9%), and carbonyl compounds (8.8%). In silico molecular docking simulations revealed that cuminaldehyde, β-caryophyllene, γ-curcumene, germacrene D, and τ-cadinol exhibited the strongest inhibitory activities against the selected receptors. Among the extracts, Jamaica pepper showed the highest antioxidant and anti-inflammatory activities, while lemon verbena exhibited the lowest ones. These findings highlight the promising potential of the studied culinary herbs and spices in the modulation of inflammatory processes related to Alzheimer’s disease. However, further investigations, particularly clinical studies, are recommended to validate these results and explore their therapeutic applications. Full article
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21 pages, 1169 KiB  
Review
Dichloroacetate and Salinomycin as Therapeutic Agents in Cancer
by Sunny Hunt, Anita Thyagarajan and Ravi P. Sahu
Med. Sci. 2025, 13(2), 47; https://doi.org/10.3390/medsci13020047 - 23 Apr 2025
Viewed by 595
Abstract
Cancer is the second leading cause of mortality worldwide. Despite the available treatment options, a majority of cancer patients develop drug resistance, indicating the need for alternative approaches. Repurposed drugs, such as antiglycolytic and anti-microbial agents, have gained substantial attention as potential alternative [...] Read more.
Cancer is the second leading cause of mortality worldwide. Despite the available treatment options, a majority of cancer patients develop drug resistance, indicating the need for alternative approaches. Repurposed drugs, such as antiglycolytic and anti-microbial agents, have gained substantial attention as potential alternative strategies against different disease pathophysiologies, including lung cancer. To that end, multiple studies have suggested that the antiglycolytic dichloroacetate (DCA) and the antibiotic salinomycin (SAL) possess promising anticarcinogenic activity, attributed to their abilities to target the key metabolic enzymes, ion transport, and oncogenic signaling pathways involved in regulating cancer cell behavior, including cell survival and proliferation. We used the following searches and selection criteria. (1) Biosis and PubMed were used with the search terms dichloroacetate; salinomycin; dichloroacetate as an anticancer agent; salinomycin as an anticancer agent; dichloroacetate side effects; salinomycin side effects; salinomycin combination therapy; dichloroacetate combination therapy; and dichloroacetate or salinomycin in combination with other agents, including chemotherapy and tyrosine kinase inhibitors. (2) The exclusion criteria included not being related to the mechanisms of DCA and SAL or not focusing on their anticancer properties. (3) All the literature was sourced from peer-reviewed journals within a timeframe of 1989 to 2024. Importantly, experimental studies have demonstrated that both DCA and SAL exert promising anticarcinogenic properties, as well as having synergistic effects in combination with other therapeutic agents, against multiple cancer models. The goal of this review is to highlight the mechanistic workings and efficacy of DCA and SAL as monotherapies, and their combination with other therapeutic agents in various cancer models, with a major emphasis on non-small-cell lung cancer (NSCLC) treatment. Full article
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31 pages, 1870 KiB  
Review
Enhancing Bone Health with Conjugated Linoleic Acid: Mechanisms, Challenges, and Innovative Strategies
by Khandoker Hoque, Zayana Ali, Asma Maliha, Mohammad A. Al-Ghouti, Chiara Cugno, Shaikh Mizanoor Rahman and Md Mizanur Rahman
Nutrients 2025, 17(8), 1395; https://doi.org/10.3390/nu17081395 - 21 Apr 2025
Viewed by 469
Abstract
Conjugated linoleic acid (CLA) is a bioactive compound known for its anti-inflammatory, anti-carcinogenic, and metabolic effects, with growing interest in its role in supporting bone health. Preclinical studies, particularly those involving the t10c12 isomer, have shown that CLA can enhance bone mineral density [...] Read more.
Conjugated linoleic acid (CLA) is a bioactive compound known for its anti-inflammatory, anti-carcinogenic, and metabolic effects, with growing interest in its role in supporting bone health. Preclinical studies, particularly those involving the t10c12 isomer, have shown that CLA can enhance bone mineral density (BMD) by enhancing bone formation and reducing bone resorption, indicating its potential as a therapeutic agent to improve bone health. However, clinical trials have yielded inconsistent results, underscoring the difficulty in translating animal model successes to human applications. A major challenge is CLA’s low water solubility, poor absorption, and limited bioavailability, which restrict its therapeutic effectiveness. To address these issues, nanoparticle-based delivery systems have been proposed to improve its solubility, stability, and resistance to oxidative damage, thereby enhancing its bioactivity. Recent studies also suggest that electrical stimulation can stimulate bone regeneration by promoting bone cell proliferation, differentiation, and adherence to scaffolds. This review explores the combined use of CLA supplementation and electrical stimulation as a novel approach to improving bone health, particularly in osteoporosis management. By integrating CLA’s biological effects with the regenerative potential of electrical stimulation, this multimodal strategy offers a promising method for enhancing bone restoration, with significant implications for clinical applications in bone health. Full article
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25 pages, 1732 KiB  
Review
Pt(IV) Complexes as Anticancer Drugs and Their Relationship with Oxidative Stress
by Vlad Iova, Radu Ciprian Tincu, Ioana Scrobota and Mihail Silviu Tudosie
Biomedicines 2025, 13(4), 981; https://doi.org/10.3390/biomedicines13040981 - 17 Apr 2025
Viewed by 435
Abstract
Despite continuous research, cancer is still a leading cause of death worldwide; therefore, new methods of cancer management improvement are emerging. It is well known that in the pathophysiology of cancer, oxidative stress (OS) is a significant factor. Nevertheless, there is currently no [...] Read more.
Despite continuous research, cancer is still a leading cause of death worldwide; therefore, new methods of cancer management improvement are emerging. It is well known that in the pathophysiology of cancer, oxidative stress (OS) is a significant factor. Nevertheless, there is currently no quick or easy way to identify OS in cancer patients using blood tests. Currently, in cancer treatments, Pt(IV) complexes are preferred to Pt(II) complexes in terms of adverse effects, drug resistance, and administration methods. Intracellular reductants convert Pt(IV) complexes to their Pt(II) analogs, which are Pt compounds with anti-carcinogenic effects. Our aim was to find out if Pt(IV) complexes could be used to assess blood oxidative stress indicators and, consequently, monitor the development of cancer. In this review, we analyzed previous research using the PubMed and Google Scholar public databases to verify the potential use of Pt(IV) complexes in cancer management. We found that two main serum antioxidants, glutathione and ascorbic acid, which are easily measured using conventional methods, react favorably with Pt(IV) complexes. Our research results suggest Pt(IV) complexes as therapeutic anticancer drugs and potential diagnosis agents. However, further research must be conducted to verify this hypothesis. Full article
(This article belongs to the Section Cancer Biology and Oncology)
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30 pages, 2626 KiB  
Review
Gut Microbiota and Colorectal Cancer: A Balance Between Risk and Protection
by Vlad Alexandru Ionescu, Camelia Cristina Diaconu, Gina Gheorghe, Mara-Madalina Mihai, Carmen Cristina Diaconu, Marinela Bostan and Coralia Bleotu
Int. J. Mol. Sci. 2025, 26(8), 3733; https://doi.org/10.3390/ijms26083733 - 15 Apr 2025
Viewed by 932
Abstract
The gut microbiome, a complex community of microorganisms residing in the intestinal tract, plays a dual role in colorectal cancer (CRC) development, acting both as a contributing risk factor and as a protective element. This review explores the mechanisms by which gut microbiota [...] Read more.
The gut microbiome, a complex community of microorganisms residing in the intestinal tract, plays a dual role in colorectal cancer (CRC) development, acting both as a contributing risk factor and as a protective element. This review explores the mechanisms by which gut microbiota contribute to CRC, emphasizing inflammation, oxidative stress, immune evasion, and the production of genotoxins and microbial metabolites. Fusobacterium nucleatum, Escherichia coli (pks+), and Bacteroides fragilis promote tumorigenesis by inducing chronic inflammation, generating reactive oxygen species, and producing virulence factors that damage host DNA. These microorganisms can also evade the antitumor immune response by suppressing cytotoxic T cell activity and increasing regulatory T cell populations. Additionally, microbial-derived metabolites such as secondary bile acids and trimethylamine-N-oxide (TMAO) have been linked to carcinogenic processes. Conversely, protective microbiota, including Lactobacillus, Bifidobacterium, and Faecalibacterium prausnitzii, contribute to intestinal homeostasis by producing short-chain fatty acids (SCFAs) like butyrate, which exhibit anti-inflammatory and anti-carcinogenic properties. These beneficial microbes enhance gut barrier integrity, modulate immune responses, and inhibit tumor cell proliferation. Understanding the dynamic interplay between pathogenic and protective microbiota is essential for developing microbiome-based interventions, such as probiotics, prebiotics, and fecal microbiota transplantation, to prevent or treat CRC. Future research should focus on identifying microbial biomarkers for early CRC detection and exploring personalized microbiome-targeted therapies. A deeper understanding of host–microbiota interactions may lead to innovative strategies for CRC management and improved patient outcomes. Full article
(This article belongs to the Special Issue Gut Microbiota in Human Disease and Health)
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20 pages, 4662 KiB  
Article
Bioencapsulation of Hesperidinase from Penicillium sp. Toward Biocompounds with Enhanced Bioactivity
by Diogo F. Ribeiro, Ana Catarina Severo and Maria H. L. Ribeiro
Compounds 2025, 5(2), 12; https://doi.org/10.3390/compounds5020012 - 14 Apr 2025
Viewed by 216
Abstract
Natural polyphenols, especially the ones in their glycosylated form like hesperidin, rutin, and anthocyanins, are the most abundant phenolic compounds in citric fruits, apples, and red fruits, respectively. They stand out for their high nutraceutical potential, with various reported properties, like antioxidant, anti-inflammatory, [...] Read more.
Natural polyphenols, especially the ones in their glycosylated form like hesperidin, rutin, and anthocyanins, are the most abundant phenolic compounds in citric fruits, apples, and red fruits, respectively. They stand out for their high nutraceutical potential, with various reported properties, like antioxidant, anti-inflammatory, anticarcinogenic, and cardioprotective. Nevertheless, these compounds have low bioavailability and are rapidly excreted and released by the organism. Therefore, the main goal of this work was to obtain polyphenols with increased bioactivity by functionalizing biocompounds in fruit juices, namely, orange, apple, and red fruits. This modification was achieved via hesperidinase, an enzyme that catalyzes the hydrolysis of several natural bioactive compounds. Hesperidinase was produced with Penicillium sp. The activity and stability of the produced enzyme, in its free and immobilized form, using the sol–gel method, were assessed, as well as the bioactivity of the bioprocessed juices. Moreover, after immobilizing hesperidinase in sol–gel lens-shaped particles, the activity and operational stability of the bioencapsulates were evaluated by measuring the residual activity over several runs. Using the specific substrate p-NPG, β-D-glucosidase retained 31% of its activity in the second run, 22.6% in the third, and 35% in the fourth. For α-L-rhamnosidase, using the substrate p-NPR, residual activity was 31.1% in both the fourth and fifth runs. In fruit juices, the bioencapsulates exhibited residual activities around 100% in the second run, approximately 81% in the third, and around 90% in the fourth. The antioxidant and anti-inflammatory activities of the bioprocessed juices were evaluated, and an increase in the anti-inflammatory activity was observed when compared with the non-processed juices. Full article
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67 pages, 6303 KiB  
Review
Bioactive Compounds of Marine Algae and Their Potential Health and Nutraceutical Applications: A Review
by Emin Cadar, Antoanela Popescu, Ana-Maria-Laura Dragan, Ana-Maria Pesterau, Carolina Pascale, Valentina Anuta, Irina Prasacu, Bruno Stefan Velescu, Cezar Laurentiu Tomescu, Claudia Florina Bogdan-Andreescu, Rodica Sirbu and Ana-Maria Ionescu
Mar. Drugs 2025, 23(4), 152; https://doi.org/10.3390/md23040152 - 31 Mar 2025
Cited by 1 | Viewed by 2499
Abstract
Currently, marine algae are still an under-exploited natural bioresource of bioactive compounds. Seaweeds represent a sustainable source for obtaining bioactive compounds that can be useful for the fabrication of new active products with biomedical benefits and applications as biomedicinals and nutraceuticals. The objective [...] Read more.
Currently, marine algae are still an under-exploited natural bioresource of bioactive compounds. Seaweeds represent a sustainable source for obtaining bioactive compounds that can be useful for the fabrication of new active products with biomedical benefits and applications as biomedicinals and nutraceuticals. The objective of this review is to highlight scientific papers that identify biocompounds from marine macroalgae and emphasize their benefits. The method used was data analysis to systematize information to identify biocompounds and their various benefits in pharmaceuticals, cosmetics, and nutraceuticals. The research results demonstrate the multiple uses of seaweeds. As pharmaceuticals, seaweeds are rich sources of bioactive compounds like polysaccharides, protein compounds, pigments, and polyphenols, which have demonstrated various pharmacological activities such as antioxidant, antibacterial, anti-inflammatory, antiviral, anticoagulant, and potentially anticarcinogenic effects. Seaweed has gained recognition as a functional food and offers a unique set of compounds that promote body health, including vitamins, minerals, and antioxidants. In conclusion, the importance of this review is to expand the possibilities for utilizing natural resources by broadening the areas of research for human health and marine nutraceuticals. Full article
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29 pages, 9171 KiB  
Article
Anti-Tumor Potential of Frankincense Essential Oil and Its Nano-Formulation in Breast Cancer: An In Vivo and In Vitro Study
by Nouran Mohamed, Hisham Ismail, Ghada M. Nasr, Shaimaa Abdel-Ghany, Borros Arneth and Hussein Sabit
Pharmaceutics 2025, 17(4), 426; https://doi.org/10.3390/pharmaceutics17040426 - 27 Mar 2025
Viewed by 753
Abstract
Background/Objective: Breast cancer remains the most common malignancy among women worldwide, contributing to high morbidity and mortality rates. Many anti-cancer drugs have been derived from medicinal plants, and frankincense from Boswellia carterii is notable for its anti-inflammatory, anti-neoplastic, and anti-carcinogenic properties. Using gas [...] Read more.
Background/Objective: Breast cancer remains the most common malignancy among women worldwide, contributing to high morbidity and mortality rates. Many anti-cancer drugs have been derived from medicinal plants, and frankincense from Boswellia carterii is notable for its anti-inflammatory, anti-neoplastic, and anti-carcinogenic properties. Using gas chromatography/mass spectrometry (GC/MS), 48 components were identified in B. carterii essential oil, and the major constituent was α-pinene (35.81%). Method: In this study, we investigated the anti-tumor effects of frankincense essential oil (FEO) and its nano-formulation with chitosan (FEO-CSNPs) using in vitro breast cancer models (MCF-7, MDA-MB-231, and 4T1 cells) and in vivo mouse mammary carcinoma (4T1) models (Balb/c). Results: The results showed significant reductions in cell viability. At 10 μg/mL, the FEO showed the highest reduction in the C-166 cells, while at 100 μg/mL, the FEO exhibited a stronger cytotoxicity in the MDA-MB-231 and 4T1 cells compared to the FEO-CSNPs and CSNPs. The FEO-CSNPs exhibited cell growth arrest in the S, G2/M, and G1/S phases in the MCF-7, MDA-MB-231, and 4T1 cell lines (36.91%, 23.12%, and 33.58%), in addition to increased apoptosis rates in the MCF-7, MDA-MB-231, and 4T1 cell lines (33.04%, 36.39%, and 42.19%). The wound healing assays revealed a decreased migratory ability in the treated cells. The in vivo experiments in the balb/c mice demonstrated a reduction in the tumor volume, with a histopathological analysis confirming extensive tumor necrosis. Moreover, the FEO and FEO-CSNPs showed notable antioxidant and arginase activity. The gene expression analysis via qPCR indicated the upregulation of tumor suppressor genes and the downregulation of oncogenes. Conclusions: These findings suggest that FEO and its nano-formulation, particularly in the form of FEO-CSNPs as an oral formulation, display enhanced efficacy, warranting further preclinical and clinical research to develop innovative treatment strategies. Full article
(This article belongs to the Special Issue Natural Nanoparticle for Cancer Diagnosis and Treatment, 2nd Edition)
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29 pages, 2069 KiB  
Article
Extraction of Bioactive Compounds from Larrea cuneifolia Cav. Using Natural Deep Eutectic Solvents: A Contribution to the Plant Green Extract Validation of Its Pharmacological Potential
by Agostina Conta, Mario Juan Simirgiotis, José Martínez Chamás, María Inés Isla and Iris Catiana Zampini
Plants 2025, 14(7), 1016; https://doi.org/10.3390/plants14071016 - 24 Mar 2025
Viewed by 423
Abstract
A sustainable alternative to replace the use of toxic and non-biodegradable conventional solvents for the extraction of active principles from plants is natural deep eutectic solvents (NADESs). Larrea cuneifolia Cav. (Zygophyllaceae) is a plant widely distributed in semiarid areas of western Argentina. Several [...] Read more.
A sustainable alternative to replace the use of toxic and non-biodegradable conventional solvents for the extraction of active principles from plants is natural deep eutectic solvents (NADESs). Larrea cuneifolia Cav. (Zygophyllaceae) is a plant widely distributed in semiarid areas of western Argentina. Several studies validate its popular medicinal use by demonstrating its biological activities such as antibacterial, antifungal, antioxidant, anti-inflammatory, and anticarcinogenic properties, among others. The aim of this work was to compare the bioactive compounds and the in vitro antioxidant and antibacterial activity of L. cuneifolia extracts using non-conventional vs. conventional solvents. Aqueous, ethanolic, and four NADES extracts were prepared. The extracts were phytochemically characterized, and extracted compounds were identified by UHPLC-MS/MS. Antioxidant activity was determined by evaluating the hydrogen peroxide and free radical scavenging capacity using ABTS•+. The antibacterial activity of the extracts and NADESs was evaluated against Gram-positive and Gram-negative multidrug-resistant strains. The extracts of L. cuneifolia presented a variable content of total phenolic compounds between 4163.4 and 24,371.63 µg GAE/mL. Phenolic acids, flavonoid glycosides, flavanones, flavones, flavonols, alkaloids, lignans (nordihydroguaiaretic acid and its derivatives), and other compounds were tentatively identified in extracts of L. cuneifolia obtained with conventional and non-conventional solvents. A heatmap cluster and a bubble plot were created to compare the diversity and relative abundance of identified compounds, and the extracts were classified into two major groups. All extracts were able to scavenge > 40% of hydrogen peroxide and the ABTS radical cation (ABTS•+) (CD50 = 3.15–5.13 µg GAE/mL). The LAS extract exhibited the highest bacterial growth inhibition (MIC = 75–37.5 µg GAE/mL). In conclusion, the results show that NADESs represent a sustainable alternative for the extraction of compounds with antioxidant and antibacterial activity and could therefore replace traditional solvents in the pharmaceutical, cosmetic, or food industries. Full article
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22 pages, 4201 KiB  
Article
Trend in Detection of Anthocyanins from Fresh Fruits and the Influence of Some Factors on Their Stability Impacting Human Health: Kinetic Study Assisted by UV–Vis Spectrophotometry
by Cătălina Ionescu, Adriana Samide and Cristian Tigae
Antioxidants 2025, 14(2), 227; https://doi.org/10.3390/antiox14020227 - 17 Feb 2025
Viewed by 1003
Abstract
Anthocyanins (ANTHs) are polyphenolic compounds with health promoting properties, being known for their strong antioxidant effects as well as for their antimicrobial properties, obesity and cardiovascular disease prevention, and anticarcinogenic activity. Being main dietary components, it is important to know the content of [...] Read more.
Anthocyanins (ANTHs) are polyphenolic compounds with health promoting properties, being known for their strong antioxidant effects as well as for their antimicrobial properties, obesity and cardiovascular disease prevention, and anticarcinogenic activity. Being main dietary components, it is important to know the content of anthocyanins in various dietary sources and their stability in time. The total anthocyanin content (TAC) of various fresh fruits has been spectrophotometrically determined using the pH differential method. The results showed that in the analyzed samples, the TAC increased in the order: blackcurrants > blackberries > blueberries > raspberries > strawberries > plums. The degradation degree of anthocyanins extracted from blueberries (BBEs) in an ethanol/water solution in four experimental conditions was studied. Kinetic studies have been approached, fitting the experimental data recorded by UV–Vis spectrophotometric analysis in agreement with some kinetic models verified for the ANTH degradation reaction. Therefore, zero-order kinetics for BBE extract degradation exposed to sunlight were identified, while for the other storage conditions (shadow, dark, cold), the first-order kinetics were respected. The results indicate that the stability decreased as follows: (ANTH stability)sunlight test << (ANTH stability)shadow test ≈ (ANTH stability)dark test < (ANTH stability)cold test. A mechanism for BBE anthocyanin degradation was proposed and the impact on human health of the degradation products is discussed. Full article
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9 pages, 1858 KiB  
Communication
Role of Human DNA Ligases in Mediating Pharmacological Activities of Flavonoids
by Daekyu Sun and Vijay Gokhale
Int. J. Mol. Sci. 2025, 26(4), 1456; https://doi.org/10.3390/ijms26041456 - 10 Feb 2025
Viewed by 578
Abstract
Dietary flavonoids are a group of polyphenol compounds originating from plants that have drawn much attention in the last few decades. Flavonoid-rich foods and dietary supplements are used worldwide due to their health benefits, including antioxidative, anti-inflammatory, immunity-enhancing, anticarcinogenic, estrogenic, and favorable cardiovascular [...] Read more.
Dietary flavonoids are a group of polyphenol compounds originating from plants that have drawn much attention in the last few decades. Flavonoid-rich foods and dietary supplements are used worldwide due to their health benefits, including antioxidative, anti-inflammatory, immunity-enhancing, anticarcinogenic, estrogenic, and favorable cardiovascular effects. The main objective of our study was to explore the molecular targets of flavonoids to gain insight into the mechanism of action behind their biological effects. In this study, a novel class of resorcinol-based flavonoid compounds was identified as a potent inhibitor of human DNA ligase activity. Human DNA ligases are crucial in the maintenance of genetic integrity and cell fate determination. Thus, our results strongly suggest that this activity against human DNA ligases is responsible, at least in part, for the cellular effects of flavonoid compounds. We anticipate that the results from our studies will improve our understanding of how interactions with human DNA ligases cascade into the recognized health benefits of flavonoids, particularly their wide variety of anticancer effects. Full article
(This article belongs to the Special Issue The Role of Natural Products in Drug Discovery)
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21 pages, 2703 KiB  
Article
Gallic Acid Enhances Olaparib-Induced Cell Death and Attenuates Olaparib Resistance in Human Osteosarcoma U2OS Cell Line
by Mehmet Kadir Erdogan and Ayse Busra Usca
Curr. Issues Mol. Biol. 2025, 47(2), 104; https://doi.org/10.3390/cimb47020104 - 7 Feb 2025
Viewed by 1087
Abstract
Cancer remains one of the most formidable diseases globally and continues to be a leading cause of mortality. While chemotherapeutic agents are crucial in cancer treatment, they often come with severe side effects. Furthermore, the development of acquired drug resistance poses a significant [...] Read more.
Cancer remains one of the most formidable diseases globally and continues to be a leading cause of mortality. While chemotherapeutic agents are crucial in cancer treatment, they often come with severe side effects. Furthermore, the development of acquired drug resistance poses a significant challenge in the ongoing battle against cancer. Combining these chemotherapeutic agents with plant-derived phenolic compounds offers a promising approach, potentially reducing side effects and counteracting drug resistance. Phytochemicals, the bioactive compounds found in plants, exhibit a range of health-promoting properties, including anticarcinogenic, antimutagenic, antiproliferative, antioxidant, antimicrobial, neuroprotective, and cardioprotective effects. Their ability to enhance treatment, coupled with their non-toxic, multi-targeted nature and synergistic potential when used alongside conventional drugs, underscores the growing importance of natural therapeutics. In this study, we investigated the anticancer effects of olaparib (OL), a small-molecule PARP inhibitor that has shown promising results in both preclinical and clinical trials, and gallic acid (GA), a phenolic compound, in olaparib-resistant human osteosarcoma U2OS cells (U2OS-PIR). Both parental U2OS and U2OS-PIR cell lines were treated with increasing concentrations of olaparib and gallic acid, and their cytotoxic effects were assessed using the WST-1 cell viability assay. The synergistic potential of OL and GA, based on their determined IC50 values, was further explored in combination treatment. A colony survival assay revealed the combination’s ability to significantly reduce the colony-forming capacity of cancer cells. Additionally, the apoptotic effects of OL and GA, both individually and in combination, were examined in U2OS-PIR cells using acridine orange/ethidium bromide dual staining. The anti-angiogenic properties were assessed through a VEGF ELISA, while the expression of proteins involved in DNA damage and apoptotic signaling pathways was analyzed via Western blot. The results of this study demonstrate that gallic acid effectively suppresses cell viability and colony formation, particularly when used in combination therapy to combat OL resistance. Additionally, GA inhibits angiogenesis and induces DNA damage and apoptosis by modulating key apoptosis-related proteins, including cPARP, Bcl-2, and Bax. These findings highlight gallic acid as a potential compound for enhancing therapeutic efficacy in overcoming acquired drug resistance. Full article
(This article belongs to the Special Issue The Role of Natural Compounds in Cancer Therapy)
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24 pages, 1711 KiB  
Review
Anticancer Properties of Macroalgae: A Comprehensive Review
by Sara Frazzini and Luciana Rossi
Mar. Drugs 2025, 23(2), 70; https://doi.org/10.3390/md23020070 - 7 Feb 2025
Viewed by 2149
Abstract
In recent years, the exploration of bioactive molecules derived from natural sources has gained interest in several application fields. Among these, macroalgae have garnered significant attention due to their functional properties, which make them interesting in therapeutic applications, including cancer treatment. Cancer constitutes [...] Read more.
In recent years, the exploration of bioactive molecules derived from natural sources has gained interest in several application fields. Among these, macroalgae have garnered significant attention due to their functional properties, which make them interesting in therapeutic applications, including cancer treatment. Cancer constitutes a significant global health burden, and the side effects of existing treatment modalities underscore the necessity for the exploration of novel therapeutic models that, in line with the goal of reducing drug treatments, take advantage of natural compounds. This review explores the anticancer properties of macroalgae, focusing on their bioactive compounds and mechanisms of action. The key findings suggest that macroalgae possess a rich array of bioactive compounds, including polysaccharides (e.g., fucoidans and alginates), polyphenols (e.g., phlorotannins), and terpenoids, which exhibit diverse anticancer activities, such as the inhibition of cell proliferation, angiogenesis, induction of apoptosis, and modulation of the immune system. This review provides an overview of the current understanding of macroalgae’s anticancer potential, highlighting the most promising compounds and their mechanisms of action. While preclinical studies have shown promising results, further research is necessary to translate these findings into effective clinical applications. Full article
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