Search Results (45)

Chirality plays a key role in the effectiveness and toxicity of bioactive compounds. Usnic acid (UA), a lichen metabolite, exists as two enantiomers. Despite numerous studies on its biological properties, enantioselective aspects remain poorly recognized. This study assessed the cytotoxicity of UA enantiomers against colon, prostate, thyroid, brain, and breast cancer cell lines, as well as non-cancerous cells. Cell viability was determined by the MTT assay after 24, 48, and 72 h. Colon cancer HCT116 cells were the most sensitive (IC₅₀ ~10 µg/mL, 72 h), with no enantiomeric dominance. In prostate cancer PC3 cells, (+)-UA was more effective. Moderate cytotoxic effect was noted for thyroid cancer cells; however, this was evaluated for the first time. MDA-MB-231 breast cancer cells were strongly affected (IC₅₀ 15.8 and 20.2 µg/mL for (+)- and (−)-UA, 72 h), as compared to MCF7 cells. Brain cancer cells were the least affected, as so were normal astrocytes. UA had no effect on normal colon epithelial cells but showed moderate toxicity in prostate, thyroid, and breast cells. To conclude, the overall cytotoxicity of (+)-UA was stronger than its (−)-enantiomer, while the latter compound was more toxic to normal cells. These findings highlight the advantage of (+)-UA, especially in chemopreventive strategies. Full article

Objectives: Iodine and selenium are key elements for thyroid. There is also evidence of their immunoregulatory potential. However, the current state of knowledge of potential interactions among iodine—selenium—thyroid—immune system is not sufficient. The aim of the study was to evaluate iodine and selenium statuses and examine the relationship between them and the functioning of the thyroid and immune system in a group of women of reproductive age, without previously diagnosed disease. Methods: The study involved a group of 60 women aged 19–40 from southern Poland. The concentrations of iodine and selenium were determined in serum samples using the ICP-MS and AAS methods, respectively. Thyroid function was assessed by determining serum levels of thyroid-stimulating hormone (TSH), free thyroxine (fT4), and anti-thyroid peroxidase antibodies (anti-TPO) by electrochemiluminescence methods. Glutathione peroxidase 3 (GPX3) and ferric ion reducing antioxidant power (FRAP) in serum were measured by spectrophotometric methods. Immune functions were evaluated by analyzing cytokine levels using ELISA tests, including interferon-γ, interleukin-4, interleukin-17, and transforming growth factor-β. Results: No significant correlations between selenium and thyroid or immunological parameters were observed. The level of iodine in serum positively correlated with free thyroxine, indicating its importance for maintaining normal thyroid function, as well as with FRAP in serum, suggesting a protective role of iodine-mediated antioxidant activity on thyroid function. Conclusions: Our results underline the complexity of the system of correlations between iodine–selenium–thyroid–immune function. Nevertheless, understanding them may turn out to be crucial for developing preventive and therapeutic strategies in the context of thyroid diseases. Full article

Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder characterized by impaired glucose regulation. This study evaluated the antioxidant and antidiabetic potential of aqueous extracts from four plant species from the southern Algarve: Aristolochia baetica, Chelidonium majus, Dittrichia viscosa, and Lavandula viridis, using non-cellular in vitro assays. HPLC/PDA was used to identify active compounds. Antioxidant activity was assessed by using TAA, FRAP, RP, and DPPH assays; antidiabetic potential through α-glucosidase and α-amylase inhibition; and wound healing relevance through elastase, collagenase, and lipoxygenase inhibition. D. viscosa showed the highest antioxidant activity (FRAP: 1132.99 ± 19.54 mg TE/g dw; DPPH IC₅₀ = 25.85 ± 0.75 μg/mL) and total phenolic/flavonoid content, with a diverse profile including caffeic and chlorogenic acids, isoquercetin, and quercetin. It also exhibited potent α-glucosidase inhibition (IC₅₀ = 0.61 ± 0.06 mg/mL), outperforming acarbose. L. viridis had the highest total phenolic content (39.04 mg/g), while A. baetica demonstrated the strongest anti-elastase, anti-collagenase, and lipoxygenase activity, suggesting wound-healing potential. C. majus showed the weakest effects. A strong correlation was observed between phenolic content and antioxidant/antidiabetic activity. These findings support further in vivo studies on D. viscosa and A. baetica for potential use in T2DM management and diabetic wound healing. Full article

The Fabaceae family is known for the presence of isoflavones—phytoestrogens with potential chemopreventive effects against hormone-dependent cancers. This study aimed to optimize isoflavones extraction using a fractional factorial design and to quantitatively and qualitatively analyze 32 Fabaceae species native to Polish flora by HPLC-UV-VIS to indicate new, rich plant sources of isoflavones. The optimal extraction method was a 60 min reflux with 50% methanol and a plant material-to-solvent ratio of 1:125. The highest isoflavone levels were found in Trifolium medium (26.70 mg/g d.m.), Genista tinctoria (19.65 mg/g d.m.), and Trifolium pratense (12.56 mg/g d.m.). The obtained extracts were further evaluated for cytotoxic and antiproliferative activity against MCF7 and MDA-MB-231 human breast cancer cells. Genista tinctoria showed the highest cytotoxicity against MCF7, while Cytisus scoparius and Ononis arvensis were most effective against MDA-MB-231 at a dose of 500 µg/mL. The extracts were also characterized by varied, potent antioxidant properties, important in chemoprevention. A strong correlation was observed between isoflavone content and cytotoxic and antiproliferative activity exclusively in the estrogen receptor-positive MCF7 cell line. Importantly, the tested extracts demonstrated no toxic effects on normal human liver (HepG2), thyroid (Nthy-ori 3-1), or breast (MCF10A) cells, indicating a favorable safety profile. Full article

Meripilus giganteus (Pers.) P. Karst. is a basidiomycete fungus known for its bioactive properties, including antioxidant, antimicrobial, and cytotoxic effects. Although research has largely focused on fruiting bodies, mycelium obtained through in vitro culture offers a sustainable and potentially scalable source of bioactive metabolites. This study aimed to compare the chemical composition and biological activity of extracts from the fruiting bodies and mycelium of M. giganteus. Key compound groups were analyzed using high-performance liquid chromatography (HPLC), and biological activity was assessed through DPPH and ABTS antioxidant assays and MTT-based cytotoxicity testing on human gastrointestinal cancer and normal colon epithelial cell lines. The results revealed distinct metabolite profiles between fungal forms and demonstrated that solvent type strongly influenced extraction efficiency. Cytotoxicity assays indicated moderate activity of both extract types, with some selectivity towards colorectal cancer cell lines. These findings suggest that M. giganteus mycelium may serve as a promising alternative to fruiting bodies for the production of antioxidant and potentially chemopreventive compounds. Further studies are recommended to optimize cultivation and extraction conditions to enhance both metabolite yield and biological activity. Full article

Background: Breast milk is the most important nutrition for newborns. Growth factors such as insulin-like growth factor 1 (IGF-1), epidermal growth factor (EGF), transforming growth factor-β (TGF-β), and nerve growth factor (NGF) are among its components that play pivotal roles in neonatal development, immune system priming, and gastrointestinal maturation. This study examined the effects of gestational diabetes mellitus (GDM), maternal hypothyroidism, and method of delivery on the concentrations of these factors in colostrum collected at three distinct postpartum time points. Methods: A group of 39 women was included, 20 of whom gave birth vaginally, whereas caesarean section was performed in 19 patients. A total of 18 volunteers were diagnosed with GDM, and 17 suffered from hypothyroidism. Colostrum samples were collected from the volunteers in the first 3 days after birth under hospital conditions. Growth factors like IGF-1, EGF, NGF, and TGF-β were measured in the samples using commercial immunoenzymatic assays. Results: No significant differences were observed in the values of these parameters between the groups of women (with GDM or hypothyroidism and healthy, as well as giving birth naturally and by caesarean section). In addition, the growth factors exhibited good stability within the first few postpartum days (CVs for all studied parameters: in the range of 0.7–5.0%). Conclusions: The pregnancy disorders that were properly controlled and treated by specialists appeared not to affect the levels of the analyzed growth factors—just like the type of delivery and the day of colostrum collection. Full article

Wheat germ oil (WGO), derived from the nutrient-dense germ of wheat kernels, is a functional bioactive product, known for its rich composition of essential fatty acids, sterols, tocopherols, and polyphenols. This study aimed to comprehensively profile the molecular and therapeutic properties of WGO, focusing on its antioxidant, cytotoxic, and anti-inflammatory activity. Using advanced analytical techniques such as gas chromatography-mass spectrometry (GC-MS), Fourier Transform Infrared (FTIR) spectroscopy, and fluorescence analysis, WGO was shown to contain high levels of linoleic acid (45.3%), squalene (2.52 g/100 g), and polyphenols. WGO displayed selective cytotoxicity, inhibiting cancer cells’ viability in melanoma, prostate, and colorectal cancer cell lines, but not normal cells, highlighting its chemoprevention potential. Furthermore, WGO significantly reduced LPS-induced nitric oxide and IL-6 production in macrophages, with effects plateauing at higher doses. The 3D fluorescence spectra showed a significant decrease in fluorescence intensity when human serum albumin interacted with the WGO polyphenol fraction, indicating a strong binding affinity and stable complex formation. These findings emphasize the nutritional and therapeutic potential of WGO as a natural bioactive agent, warranting further mechanistic investigation and broader applications in health and disease management. Full article

γ-Polyglutamic acid (γ-PGA) is a biodegradable and non-toxic biopolymer with numerous potential applications in agriculture, food, and health sciences due to its antioxidant and antimicrobial properties. This study evaluated the cytotoxic and antioxidant properties of kale (Brassica oleracea var. sabellica) and lupine (Lupinus luteus) sprouts supplemented with different concentrations of γ-PGA. The sprouts were cultivated for various durations (6–10 days), and their bioactive compound profiles were analyzed using HPLC with a PDA 100 UV-VIS detector. Antioxidant activity was assessed via DPPH and FRAP assays, while cytotoxicity was tested against cancer and normal colon cell lines. Results demonstrated that kale sprouts had significantly higher antioxidant activity compared to lupine, with the highest levels observed in kale sprouts supplemented with 0.01% γ-PGA on day 8 (DPPH: 63.6 ± 0.4 μM TEAC/g dw; FRAP: 181.8 ± 2.1 μM/Fe²⁺/g dw). In contrast, supplementation of lupine sprouts with γ-PGA showed mixed effects, with antioxidant activity depending on concentration and cultivation duration (DPPH in the range 6.5 ± 0.2 ÷ 12.4 ± 0.2 μM TEAC/g dw; FRAP in the range 14.3 ± 0.4 ÷ 25.2 ± 0.9 μM/Fe²⁺/g dw). Cytotoxicity assays revealed that neither kale nor lupine extracts were toxic to normal colon cells (approx. 100% of alive cells), suggesting selectivity in their action, but fortification with γ-PGA resulted in a weaker or even unfavorable effect on the cytotoxic activity of the examined sprouts. The findings highlight the potential of γ-PGA to enhance the bioactive properties of sprouts, although its effects are influenced by species and cultivation conditions. These results provide a foundation for developing functional foods and sustainable agricultural practices. Full article

Background/Objectives: Developing antifungal drugs with lower potential for interactions with food may help to optimize treatment and reduce the risk of antimicrobial resistance. Chemometrics uses statistical and mathematical methods to analyze multivariate chemical data, enabling the identification of key correlations and simplifying data interpretation. We used the partial least squares (PLS) approach to explore the correlations between various characteristics of oral antifungal drugs (including antifungal antibiotics) and dietary interventions, aiming to identify patterns that could inform the optimization of antifungal therapy. Methods: We analyzed 15 oral antifungal drugs, including azoles (8), antifungal antibiotics (4), antifungal antimetabolites (1), squalene epoxidase inhibitors (1), and glucan synthase inhibitors (1). The input dataset comprised information from published clinical trials, chemical records, and calculations. We constructed PLS models with changes in the pharmacokinetic parameters (∆AUC, area under the curve; ∆C_max, maximum drug concentration; and ∆T_max, time to reach maximum drug concentration) after dietary intervention as the response parameters and eight groups of molecular descriptors (M1–M8) as the predictor parameters. We performed separate analyses for the different nutritional interventions. Results: In the final PLS model with food as an intervention, we effectively reduced the dimensionality of the dataset while retaining a substantial percentage of the original information (variance), as significant components explained 69.8% and 17.5% of the predictor and response parameter variances, respectively. The PLS model was significant because its components met the cross-validation criteria. We obtained six significant positive and negative correlations between the descriptors related to atoms and the postprandial ∆T_max. Conclusions: The PLS method is valuable for investigating interactions between antifungal drugs (including antifungal antibiotics) and food. The correlations obtained can be used in drug modeling to predict interactions with dietary interventions based on the antifungal drug’s chemical structure. Incorporating chemometric techniques into the early drug development stages could facilitate the design of antifungal antibiotics and other antifungal agents with optimized absorption in the presence of dietary components. Full article

The aim of this review is to explore how diet and dietary supplements influence the activity of key multidrug resistance (MDR) transporters—MRP2, BCRP, and P-gp. These transporters play a crucial role in drug efflux from cancer cells and significantly affect chemotherapy outcomes. This review focuses on how dietary phytochemicals, such as catechins and quercetin, impact the expression and function of these transporters. Both in vitro and in vivo experiments were examined to assess changes in drug bioavailability and intracellular drug accumulation. The findings show that certain dietary components—such as catechins, flavonoids, resveratrol, curcumin, terpenoids, sterols, and alkaloids—can either inhibit or induce MDR transporter activity, thus influencing the effectiveness of chemotherapy. These results highlight the importance of understanding diet–drug interactions in cancer therapy to improve treatment outcomes and reduce side effects. In conclusion, dietary modifications and supplements should be carefully considered in cancer treatment plans to optimize therapeutic efficacy. Full article

This study investigates the phytochemical composition and biological activities of hemp (Cannabis sativa L.) leaves, flowers’ methanolic extracts from the Sofia variety, and its sprouts cultivated under different light conditions (natural light, darkness, blue, and white LED light for 5, 7, and 9 days). Phytochemical analysis using HPLC identified four key polyphenolic compounds in sprouts’ extracts: chlorogenic, caffeic, and gallic acids, and myricetin, with a predomination of the chlorogenic acid. In contrast, leaves and flowers’ extracts contained cannflavins A and B and chlorogenic, p-coumaric, and ferulic acids, with a significant presence of isochlorogenic acid. Antioxidant capacity, assessed by FRAP method, revealed higher antioxidant potential in leaves compared to flowers and sprouts, with sprouts grown under blue and white LED lights exhibiting the highest activity. Cytotoxic activity was evaluated on human colon cancer cell lines (HT29, HCT116, DLD-1) and normal colon epithelial cells (CCD 841 CoN). Results demonstrated significant and selective cytotoxicity against cancer cell lines, with leaves showing more pronounced effects than flowers, and sprouts only moderate activity. All samples revealed an anti-inflammatory effect in vitro. To conclude, sprouts, leaves, and flowers of the Sofia hemp may be considered promising products for chemoprevention in the future. Full article

The hepatoprotective effects of natural products have been a significant focus in recent decades due to the growing demand for the help in the treatment of hepatic impairments. This review specifically delves into the findings of clinical trials involving 13 selected natural products, namely plants and their derived compounds (e.g., artichoke, berberine, and turmeric), algae (e.g., spirulina), probiotics, and other products like phospholipids and vitamin D. A literature search was performed in the Scopus database, PubMed, and Google Scholar, covering all articles found up to June 2024. Artichoke, berberine, chlorella, chicory, green tea, probiotics, phospholipids, schisandra, silymarin, spirulina, and vitamin D caused a decrease in liver enzymes, while for cinnamon and turmeric such an effect was either not observed or not convincing. The presented results indicate that some natural products might satisfactorily improve hepatic outcomes in NAFLD, NASH, and other liver disorders; however, further studies and metanalyses are needed to clearly demonstrate their effectiveness. Full article

Considering the spectrum of benefits of breast milk feeding, determining the essential components of an infant’s only food-mother’s milk-seems justified, especially in the case of those whose deficiency (e.g., iodine) may result in developmental disorders. The main aim of this study was the determination of the total iodine content of breast milk (including colostrum and mature milk). A secondary objective was to assess the influence of factors such as the type of delivery, hypothyroidism, gestational diabetes or the stage of lactation on this parameter. The study materials were colostrum and milk after 1 (n = 14), 2 and 3 months (n = 8) of lactation with a range of iodine concentrations (µg/L): 195–1648 and 170–842, 174–650 and 273–751, respectively. Iodine was determined using the inductively coupled plasma mass spectrometry (ICP-MS). Multivariate statistical analysis revealed, e.g., that delivery by caesarean section or dose of L-thyroxine taken by women to normalise thyroid hormones, had a significant effect on iodine concentrations in breast milk. Further research aimed at assessing the quality of breast milk should also include determining the factors influencing it. Full article

Plants from the Fabaceae family are widely distributed around the world, especially in Europe, Asia and North America. They are a rich source of isoflavones, compounds with estrogen-like activity, which are suspected of having a chemopreventive effect against hormone-dependent cancers. Following the PRISMA guidelines, we conducted a systematic review aimed at assessing the impact of Fabaceae plant extracts on hormone-dependent cancer cells and the content of active compounds in plant raw materials. We analyzed the results of 63 articles from in vitro and in vivo studies describing the effect of plant extracts containing isoflavones on cancer cells, along with their anti-inflammatory and antioxidant potential. In the process, we determined the research limitations and future research directions. The collected results indicate the plant species with potentially high contents of phytoestrogens and anti-inflammatory, antioxidant and cytotoxic properties. They point to the potential use of plants in the diet as a source of compounds offering cancer prevention. Full article

Sprouts’ consumption has become popular due to their wide availability, easy cultivation process, and proven biological activity. Moreover, stress factors, such as limited access to light or disturbed gravity during growth, may contribute to the increased activity and the synthesis of bioactive compounds. In this study, for the first time, the examination of the impact of darkness and simulated microgravity conditions on the white clover sprouts from the Fabaceae family was conducted. Among several species, used in the preliminary attempts, only white clover was satisfactory sprouting in the disturbed gravity conditions, and thus was chosen for further examination. A random positioning machine setup was used during the cultivation process to simulate microgravity conditions. Additionally, the sprouts were cultivated in total darkness. Simulated microgravity and/or darkness during the first few days of the sprouts’ growth caused biomass reduction, the increased synthesis of bioactive compounds (isoflavones and phenolics), and changes in the level of abscisic acid and phenylalanine ammonia-lyase. Moreover, it increased the antioxidant properties of the sprouts, while the enhancement of their cytotoxic impact was observed only for androgen-dependent prostate cancer LNCaP cells. To conclude, the presented results are promising in searching for novel functional food candidates and further studies are necessary, directed at other plant families. Full article