Search Results (110)

Background:Becium grandiflorum is a fragrant perennial shrub of the Lamiaceae family. Objectives: The current study aimed to explore the cytotoxic potential of the n-hexane fraction from Becium grandiflorum aerial parts and, further, isolate its major diterpene and conduct in vitro and in vivo anticancer activities along with its molecular mechanism and synergy with doxorubicin. Methods: The hydroalcoholic extract of Becium grandiflorum aerial parts was fractionated, and the n-hexane fraction was analyzed via GC-MS. The major isolated diterpene, 18-epoxy-pimara-8(14),15-diene (epoxy-pimaradiene), was quantified using UPLC-PDA. Cytotoxicity assays were conducted on HCT-116, MCF-7, MDA-MB-231, and HepG2 cell lines. The synergistic effect with doxorubicin was tested on HepG2 cells. In vivo anticancer activity was evaluated using the Ehrlich ascites carcinoma model, and molecular docking analyzed Bax-Bcl2 interactions. Results: The n-hexane fraction contained 21 compounds, mainly oxygenated diterpenes, and the major isolated compound was epoxy-pimaradiene, with a quantity of 0.3027 mg/mg. N-Hexane fraction and epoxy-pimaradiene exhibited strong cytotoxicity against HepG2 cells, induced apoptosis, and G2/M arrest. The combination of epoxy-pimaradiene with doxorubicin lowered the IC₅₀ of doxorubicin from 4 µM to 1.78 µM. In vivo, both reduced tumor growth and increased necrotic tumor areas. Molecular docking revealed disruption of Bax-Bcl2. Conclusions: The findings suggest that B. grandiflorum and its major diterpene, epoxy-pimaradiene, exhibit potent anticancer activity, particularly against liver cancer cells. Epoxy-pimaradiene enhances doxorubicin’s efficacy, induces apoptosis, and inhibits tumor progression. Further studies are needed to explore their therapeutic potential. Full article

Oak infusions enriched with agavins may offer nutraceutical benefits in the development of iced teas. This study evaluated infusions of Quercus sideroxyla and Quercus eduardii leaves formulated with different concentrations of agavins (0, 2, 6, and 10%), analyzing their physicochemical and sensory properties, chemical stability, and antioxidant capacity. The incorporation of agavins resulted in substantial modifications to physicochemical parameters, including pH, titratable acidity, and soluble solids, thereby enhancing product stability and consistency. Notable distinctions were observed between the two species with respect to their acidogenic response and soluble solid concentration. Interactions between agavins and phenolic compounds, as discerned by UPLC-PDA-ESI-MS/MS and FT-IR, exerted a significant influence on bioactivity of the phenolic constituents, thereby affecting the nutraceutical potential of the infusions. These interactions, facilitated by hydrogen bonds, led to reduction in phenolic acids, such as quinic acid (↓ 43%), and alteration in antioxidant capacity at high concentrations of agavins. The findings underscore the significance of meticulously designing balanced formulations that optimize chemical stability, functionality, and sensory acceptance, thereby ensuring the quality of the final product. Full article

Triticum aestivum L. subsp. spelta (cv. Rokosz) and common winter wheat Triticum aestivum L. subsp. aestivum (cv. Arktis, Belissa, Estivus, Fidelius, Hondia, Jantarka, KWS Ozon, Linus, Markiza, Ostka Strzelecka, Pokusa) grown in an organic farming system were analyzed and compared. Furthermore, the productivity of four common wheat cultivars (cv. Fidelius, Hondia, Jantarka, KWS Ozon) grown under four different (organic, conventional integrated, and monoculture) farming systems was compared. Using UPLC-DAD-MS, UPLC-PDA-MS/MS, and TLC-DPPH^•, nine phenolic acids, nine alkylresorcinols, and their antiradical activity were identified and quantified. In the organic farming system, the highest yield was observed for T. aestivum L. subsp. aestivum cv. Fidelius (4.17 t/ha). Infections of wheat cultivars were low or at a medium level. The highest resistance to Fusarium fungi was shown by cv. Fidelius, which also exhibited the highest alkylresorcinol content and antioxidant capacity. The total phenolic acid content was highest in cv. Rokosz (1302.3 µg/g), followed by common winter wheat cultivars cv. Linus (1135.1 µg/g) and cv. Markiza (1089.6 µg/g). The potential of winter wheat cultivars for human health and their suitability for cultivation in different production systems was determined, showing significant differences in bioactive compounds depending on cultivars, systems, and years. Full article

Sustainable agricultural practices increasingly focus on natural bioactive agents for managing phytopathogens. This study investigates the antifungal and phytotoxic properties of methanolic bioextracts derived from Plantago major leaves (MBPm) and Sambucus nigra roots (MBSn) to explore their potential applications. Bioextracts were prepared through methanolic maceration, with yields of 6.02% (P. major) and 6.42% (S. nigra). Antifungal assays evaluated inhibitory effects on Fusarium oxysporum, Corynespora cassiicola, and Penicillium oxalicum, while phytotoxicity assays assessed concentration-dependent impacts on Solanum lycopersicum seed germination. A qualitative evaluation of major polyphenolic compounds was conducted using Ultra-Performance Liquid Chromatography coupled with a Photodiode Array Detector and Electrospray Ionization Mass Spectrometry (UPLC-PDA-ESI-MS) to identify bioactive compounds known for their significant biological activity. P. major bioextracts demonstrated significant inhibition of F. oxysporum (90.06%) and C. cassiicola (83.19%), while S. nigra bioextracts achieved 89.65% and 92.16% inhibition, respectively. Both bioextracts showed minimal impact on P. oxalicum, with effects observed only at 50 mg/mL. Low concentrations of S. nigra bioextract enhanced seed germination, whereas higher doses inhibited it. Identified bioactive compounds included acteoside, isoacteoside, chlorogenic acid, and dicaffeoylquinic acid isomers. The findings highlight the potential of these bioextracts as biocontrol agents and modulators of seed germination processes, contributing to sustainable agricultural strategies. While this study was conducted under controlled laboratory conditions, these results provide a strong foundation for future evaluations in field settings to explore their broader agricultural applications. Full article

Cistus monspeliensis L. (C. monspeliensis) is used in Italian folk medicine. This study was performed to determine genotoxic and antigenotoxic effects of C. monspeliensis leaf extract against mitomycin C (MMC) using an in vitro cytokinesis-block micronucleus assay (CBMN) in the Chinese Hamster Ovarian K1 (CHO-K1) cell line. The phytochemical composition of C. monspeliensis extract was evaluated using an untargeted metabolomic approach by employing UPLC-PDA-ESI/MS. The automated in vitro CBMN assay was carried out using image analysis systems with a widefield fluorescence microscope and the ImageStreamX imaging flow cytometer. The phytochemical profile of C. monspeliensis extract showed, as the most abundant metabolites, punicalagin, myricetin, gallocathechin, and a labdane-type diterpene. C. monspeliensis, at the tested concentrations of 50, 100, and 200 μg/mL, did not induce significant micronuclei frequency, thus indicating the absence of a genotoxic potential. When testing the C. monspeliensis extract for antigenotoxicity in the presence of MMC, we observed a hormetic concentration-dependent effect, where low concentrations resulted in a significant protective effect against MMC-induced micronuclei frequency, and higher concentrations resulted in no effect. In conclusion, our findings demonstrate that C. monspeliensis extract is not genotoxic and, at low concentration, exhibits an antigenotoxic effect. In relation to this final point, C. monspeliensis may act as a potential chemo-preventive against genotoxic agents. Full article

Designing new forms of food, food additives, and nutraceuticals is necessary due to the growing needs of consumers, as well as the inflammation of civilization diseases, the prevention and treatment of which can be significantly supported by dietary intervention. For this reason, this study aimed to obtain highly bioactive preparations in the form of powders from the fruits, leaves, and flowers of six species of hawthorn (Crataegus L.) using solid phase extraction (SPE). Ultra-performance liquid chromatography analysis (UPLC-PDA-MS/MS) showed a high concentration of phenolic compounds (in the range from 31.50 to 66.06 mg/g), including the highest concentration in hawthorn fruit preparations. Fruit preparations also showed the highest antioxidant activity (through scavenging of O₂˙⁻ and OH˙ radicals), antidiabetic activity (inhibition of α-amylase and α-glucosidase), and anticancer activity, mainly against colon cancer cells (Caco-2). At the same time, hawthorn flower preparations showed the highest biocompatibility against normal colon cells (CCD841CoN) and anti-inflammatory activity (trypsin inhibition). Correlation and principal component analysis (PCA) showed that the health-promoting potential was most influenced by the content of falavan-3-ols. The above findings provide a basis for the industrial use of the developed preparations, which is in line with the current trend in food technology related to the search for new sources of bioactive compounds and the design of highly bioactive food. Full article

Background/Objectives: Horseradish (Armoracia rusticana L.) roots—largely used in traditional medicine for their multiple therapeutic effects—are a rich source of health-promoting phytochemicals. However, their efficacy can be compromised by low chemical stability and poor bioavailability. Incorporation into phospholipid vesicles is often proposed to tackle this problem. Methods: In this study, a hydroalcoholic extract was produced from horseradish roots. The extract was characterized by UPLC-MS and HPLC-PDA and formulated in conventional liposomes and Penetration Enhancer-containing Vesicles (PEVs) for skin application. Results: The obtained nanovesicles were small in size (<100 nm), negatively charged, uni/bilamellar, and with high values of entrapment efficiency (>85%) for the flavonoids identified in the extract. Both the free and the nanoformulated extract showed optimal biocompatibility, measured as the absence of hemolysis of erythrocytes and absence of cytotoxicity in skin cell lines. Furthermore, the nanoformulations displayed antioxidant activity in vitro. Conclusions: The proposed nananoformulations could be exploited to counteract oxidative stress involved in the pathogenesis and progression of numerous skin disorders. Full article

Salix species have been used in traditional medicine to treat fever and inflammation. However, there is no reported information on the antibacterial activities of S. aurita and S. pyrolifolia, and little is known about the phytochemistry of S. aurita. In this study, winter-dormant twig extracts of S. aurita, S. caprea, and S. pyrolifolia were screened for their antibacterial activities against Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus cereus, and Escherichia coli. The antibacterial effects were evaluated using agar diffusion and turbidimetric microplate methods. Time-kill effects were measured using the microplate optical density (OD620) method. UPLC-PDA-QTOF/MS analysis was conducted to identify the polyphenols present in a methanol extract of S. aurita. The antibacterial results show that methanol and hot and cold water twig extracts of S. aurita, S. caprea, and S. pyrolifolia have significant antibacterial effects against P. aeruginosa, S. aureus, and B. cereus with the diameters of the inhibition zones (IZDs) ranging from 16.17 to 30.0 mm and the MICs between 1250 and 2500 µg/mL. Only the cold water extract of S. caprea was moderately active against E. coli. Proanthocyanidins, procyanidin B1 (m/z 577), and procyanidin C1 (m/z 865) were identified as the major polyphenols present in the methanol extract of S. aurita twigs for the first time. Additionally, salicin-7-sulfate was present in S. aurita twigs. Procyanidin B-1, taxifolin, trans-p-hydroxycinnamic acid, and catechin showed growth inhibitory activity against B. cereus with a MIC value of 250 µg/mL. Full article

Abiotic elicitation with heavy metals has demonstrated considerable potential to stimulate the production of industrially important secondary metabolites in plant in vitro cultures. The present study investigates the effect of exogenous silver nitrate and cadmium chloride supplementation on flavonoid and phenolic acid production, as well as other indicators of oxidative stress, in shoot cultures of Dracocephalum ruyschiana L. Owing to the presence of bioactive polyphenolic compounds, this Mongolian medicinal plant is traditionally used as an anti-inflammatory, antibacterial and antipyretic agent. The shoots were cultured for three weeks, and then, cadmium (Cd²⁺) and silver (Ag⁺) ions (50 or 100 µM) were added to the medium. The maximum proliferation rate was observed in the presence of 100 µM Ag⁺ (almost 5), the highest chlorophyll content in the presence of 100 µM Cd²⁺ (0.6 mg/g FW) and the highest biomass was observed with both these treatments (73.4–75.7 g FW and 7.53–7.72 g DW). UPLC-PDA-ESI-MS analysis revealed four phenolic acids and five flavonoid derivatives in the hydromethanolic extract of D. ruyschiana shoots. All treatments stimulated the production of rosmarinic acid (RA), which was the dominant compound in the analyzed culture; the highest level of RA, i.e., about three times higher than the control, was noted in shoots exposed to 50 µM Cd²⁺ (14.72 mg/g DW), whereas the level of most flavonoids in the culture increased most significantly when exposed to Cd²⁺ at a concentration of 100 µM. Moreover, the shoots grown in the presence of 100 µM Cd²⁺ exhibited significantly higher antioxidant potential in comparison to the control. Our findings indicate that heavy metals are able to stimulate phenolic compound biosynthesis in Dracocephalum shoots without any negative impact on their growth. These results could be of significant importance for the medical, nutraceutical and agronomic industries. Full article

The aim of the study was to assess the effect of water infusion of dried and crushed ground ivy (GH) on the fermentation properties of wheat flour (WF), farinographic properties of flour and dough (WD) and the quality of the obtained bread. In the tested systems, tap water was replaced with water infusion with GH (m/v) at a concentration of 1% (A), 3% (B) and 5% (C). As part of the research methodology, the fermentation properties of flour and rheological properties of dough were assessed using a farinograph, and bread was obtained using a single-phase method using yeast and its quality was assessed. As part of this, the antioxidant potential and the profile and level of polyphenol content were determined. It was shown that replacing water with GH infusions shortened the total fermentation time of the dough and reduced the fermentation capacity of the dough. In the farinographic evaluation, an increase in flour water absorption (54.0–57.0%), dough development time (2.3–7.6 min), dough stability and softening were observed with an increase in the concentration of the added GH infusion. In turn, the volume of the loaf and the specific volume of the bread decreased with increasing the concentration of the GH infusion. The bread crumb darkened, and the elasticity and chewiness of the crumb decreased in relation to the control sample. In turn, the presence of GH infusion did not significantly affect the hardness of the crumb. As the concentration of the added GH infusion increased, an increase in the antioxidant potential of bread and the content of polyphenols and flavonoids was observed, and the UPLC-PDA-MS/MS analysis allowed the identification of 11 polyphenols in the bread. Full article

The aim of this study was to investigate the qualitative and quantitative fruit profiles of ten cultivars (cvs.) of haskap berry (Lonicera caerulea var. kamtschatica Sevast.) to determine their antioxidant activity (ABTS test, CUPRAC test, ability to capture superoxide (O₂˙⁻) and hydroxyl radicals (OH˙)), cytotoxic activity (against cancer cell lines breast, MCF-7; colon, HT-29; and melanoma, SK-Mel-28) and physicochemical properties. Most of the selected cultivars had not previously been analyzed for these properties. A total of 19 polyphenolic compounds were identified in the fruits of the tested genotypes, with a quantitative range of 2166.3–3597.0 µg/g. The polyphenol profile was dominated by anthocyanins (90.0–92.4%), and the remaining classes occurred in the following order: phenolic acids > flavonols > flavan-3-ols. The highest concentrations of these polyphenol groups were found in the cultivars ‘Honeybee’, ‘Sinij Uties’ and ‘Usłada’. The fruits of these cultivars were also characterized by the highest antioxidant activity (546.6–683.5 µg/mL for O₂˙⁻ and 541.2–652.1 µg/mL for OH˙) and cytotoxic activity (103.6–649.2 µg/mL). The data obtained indicate that the fruits of the new haskap cultivars are a good source of bioactive compounds with possible health-promoting properties. Full article

In food authentication, it is important to compare different analytical procedures and select the best method. The aim of this study was to determine the fingerprints of Zweigelt and Rondo wines through headspace analysis using ultra-fast gas chromatography (ultra-fast GC) and to compare the effectiveness of this approach at classifying wines based on grape variety and type of malolactic fermentation (MLF) as well as its greenness and practicality with three other chromatographic methods such as headspace solid-phase microextraction/gas chromatography-mass spectrometry with carboxen-polydimethylosiloxane fiber (SPME/GC-MS with CAR/PDMS fiber), headspace solid-phase microextraction/gas chromatography-mass spectrometry with polyacrylate fiber (SPME/GC-MS with PA fiber), and ultra performance liquid chromatography–photodiode array detector-tandem mass spectrometry (UPLC-PDA-MS/MS). Principal Component Analysis (PCA) revealed that fingerprints obtained using all four chromatographic methods were suitable for classification using machine learning (ML). Random Forest (RF) and Support Vector Machines (SVM) yielded accuracies of at least 99% in the varietal classification of Zweigelt and Rondo wines and therefore proved suitable for robust fingerprinting-based Quality Assurance/Quality Control (QA/QC) procedures. In the case of wine classification by the type of MLF, the classifiers performed slightly worse, with the poorest accuracy of 91% for SVM and SPME/GC-MS with CAR/PDMS fiber, and no less than 93% for the other methods. Ultra-fast GC is the greenest and UPLC-PDA-MS/MS is the most practical of the four chromatographic methods. Full article

Glioblastoma (GBM) is the most aggressive cancer originating in the brain, but unfortunately combination treatments with resection, radiation, and chemotherapy are relatively ineffective. Therefore, novel methods of adjuvant therapy are critically needed. Cyclotides are plant-derived circular peptides that chemosensitize drug-resistant breast cancer to doxorubicin. We analyzed naturally occurring and synthetic cyclotides (Cycloviolacin O3, Cycloviolacin O19, natural Kalata B1, synthetic Kalata B1, and Vitri E) alone and in co-exposure treatments with the drug temozolomide (TMZ) in human glioblastoma cells. The cyclotides were identified by UPLC-PDA and HPLC-UV. The synthetic Kalata B1 sequence was verified with orbitrap LC-MS, and structural confirmation was provided by NMR spectroscopy. The cyclotides displayed dose-dependent cytotoxicity (IC₅₀ values 2.4–21.1 µM) both alone and as chemosensitizers of U-87 MG and T 98 cells to TMZ. In fact, a 16-fold lower concentration of TMZ (100 µM) was needed for significant cytotoxicity in U-87 MG cells co-exposed to synthetic Kalata B (0.5 µM). Similarly, a 15-fold lower concentration of TMZ (75 µM) was required for a significant reduction in cell viability in T 98 cells co-exposed to synthetic Kalata B1 (0.25 µM). Kalata B1 remained stable in human serum stability assays. The data support the assertion that cyclotides may chemosensitize glioblastoma cells to TMZ. Full article

Eupatorium lindleyanum DC. (EL) is a traditional Chinese herb known for its phlegm-reducing, cough-relieving and asthma-calming properties. It is widely used for treating cough and bronchitis. However, preliminary experiments have revealed wide variations in the composition of its different medicinal parts (flowers, leaves and stems), and the composition and efficacy of its different medicinal parts remain largely underexplored at present. In this study, non-targeted rapid resolution liquid chromatography coupled with a quadruple time-of-flight mass spectrometry (RRLC-Q-TOF-MS)-based metabolomics approach was developed to investigate the differences in the chemical composition of different medicinal parts of EL. We identified or tentatively identified 9 alkaloids, 11 flavonoids, 14 sesquiterpene lactones, 3 diterpenoids and 24 phenolic acids. In addition, heatmap visualization, quantitative analysis by high-performance liquid chromatography (HPLC-PDA) and ultra-high-performance liquid chromatography–triple quadrupole tandem mass spectrometry (UPLC-MS/MS) showed particularly high levels of sesquiterpene lactones, flavonoids and phenolic acids in the flowers, such as eupalinolide A and B and chlorogenic acid, among others. The leaves also contained some flavonoid sesquiterpene lactones and phenolic acids, while the stems were almost absent. The findings of in vitro activity studies indicated that the flowers exhibited a notable inhibitory effect on the release of the inflammatory factors TNF-α and IL-6, surpassing the anti-inflammatory efficacy observed in the leaves. Conversely, the stems demonstrated negligible anti-inflammatory activity. The variations in anti-inflammatory activity among the flowers, leaves and stems of EL can primarily be attributed to the presence of flavonoids, phenolic acids and sesquiterpene lactones in both the flowers and leaves. Additionally, the flowers contain a higher concentration of these active components compared to the leaves. These compounds mediate their anti-inflammatory effects through distinct biochemical pathways. The results of this study are anticipated to provide a scientific basis for the rational and effective utilization of EL resources. Full article

Sea buckthorn and Japanese knotweed are known in many traditional medicine systems to be a great source of bioactive substances. This research aims to compare the bioactivity and protective effects of the phenolic extracts of leaves from sea buckthorn and roots and leaves from the Japanese knotweed on erythrocytes. The polyphenol composition of the extract was analyzed using UPLC-PDA-ESI-MS/MS. The extracts’ toxicity and impact on the erythrocytes’ osmotic fragility were measured spectrophotometrically. The antioxidant activity was determined based on the inhibition of oxidation of erythrocytes and their membrane induced by 2,2′-Azobis(2-methylpropionamidine) dihydrochloride (AAPH),measured spectrophotometrically and using fluorimetry. To find the possible mechanism of the extracts’ action, extract-modified cells were observed under a microscope, and the potential localization of the extract’s phytochemical composition was checked using fluorescent probes. The results showed that the used extracts are not toxic to erythrocytes, increase their osmotic resistance, and successfully protect them against free radicals. Extract components localize on the outer part of the membrane, where they can scavenge the free radicals from the environment. Altogether, the presented extracts can greatly protect living organisms against free radicals and can be used to support the treatment of diseases caused by excess free radicals. Full article