Search Results (111)

Cancer remains a major global public health concern, driving the need for innovative therapeutic agents with intensified efficacy and safety. Growth factor receptors (GFRs), often overexpressed in cancer cells and critical in regulating cell proliferation, survival, and tumor progression, represent key targets for cancer therapy. Halophytic plants like Salicornia spp. are known for their diverse bioactive compounds with notable pharmacological properties. This study comprehensively evaluated the anti-cancer potentials of phytochemicals derived from Salicornia herbacea and Salicornia brachiata using molecular docking and ADME-Tox (absorption, distribution, metabolism, excretion, and toxicity) profiling. A total of 37 bioactive compounds from Salicornia spp. were screened against HER1, HER2, and HER4 receptors. Among them, 3,5-di-O-caffeoylquinic acid, 3-O-caffeoylquinic acid, myricetin, quercetin, stigmasterol, kaempferol, isorhamnetin, rhamnetin, and hesperitin featured strong predicted binding affinities to the HER1, HER2, and HER4 growth factor receptors, comparable to those of standard anti-cancer drugs such as gefitinib and dovitinib. Further pharmacokinetic assessments, including bioavailability and toxicity analyses, identified compounds with favorable drug-likeness properties and minimal toxicity risks, except for myricetin and quercetin. These findings underscore the potential of Salicornia-derived phytochemicals as promising candidates for the development of safe, novel, and effective anti-cancer agents targeting GFRs, contributing to the advances in precision oncology, pending further validation through in vitro and/or in vivo experiments. Full article

Carpesium cernuum L., the most widespread representative of the genus Carpesium, has been traditionally used in some regions of Asia as a remedy for various ailments or as a vegetable. Although the plant is distributed in Europe, there is no data on its medicinal use in this part of the world. The chemical composition of European Carpesium cernuum L. has remained unknown until now, except for the compositions of essential oils distilled from the roots and aerial parts of the plant. Polyphenolic profiles of hydroalcoholic extracts from C. cernuum were studied using the HPLC-MSⁿ technique. The analysis revealed the presence of 24 hydroxycinnamates, which were dominated by caffeoylquinic and caffeoylhexaric acids. Moreover, fractionation of the chloroform extracts from the plant led to the isolation of three new compounds, 8α-angeloyloxy-4β-hydroxy-5β-(3-methylbutyryloxy)-9-oxo-germacran-6α,12-olide, 9β-angeloyloxy-4β,8α-dihydroxy-5β-(3-methylbutyryloxy)-3-oxo-germacran-6α,12-olide, and a dihydrobenzofuran derivative, together with twelve known compounds. 8-Hydroxy-9,10-diisobutyryloxythymol, a monoterpenoid thymol derivative from the roots of the plant, was evaluated for potential neuroprotective and cytotoxic activities using differentiated and undifferentiated SH-SY5Y neuroblastoma cells. At a concentration range of 1–10 μM, the compound provided partial (up to 50%) protection against H₂O₂-induced cell damage in the undifferentiated cells. At concentrations higher than 25 μM, the monoterpenoid significantly reduced the viability of the cells (IC₅₀: 65.7 μM for the undifferentiated cells and 40.9 μM for the differentiated cells). Full article

Background: Aronia berry (Aronia melanocarpa) are native to North America, rich in polyphenols and antioxidants with the potential to promote human health through its anti-inflammatory properties. Methods: Through the chemical characterization of phenolic compounds from aronia berries, 11 distinct polyphenols were identified. We investigated the anti-inflammatory activity of a methanolic/acetone/water extract from freeze-dried aronia berries in LPS-stimulated colonic and macrophage cell models. Results: In colon cells, aronia polyphenols suppressed pro-inflammatory gene expression (NFkβ, TNFα, IL-6, COX2) by reducing ROS generation while enhancing LXRα expression. In macrophages, these compounds decreased NO production through ROS attenuation. Notably, aronia extracts exhibited no cytotoxicity in either cell type across concentrations from 100 to 1000 μg/mL. The whole-berry methanolic extract contained substantial levels of phenolic compounds (including 3-O- and 5-O-caffeoylquinic acids, quercetin derivatives, and cyanidin derivatives) with high ORAC values, likely contributing to their observed multifaceted anti-inflammatory effects. Conclusions: These findings suggest that freeze-dried aronia berry (AroBerry^®) may offer protection against low-grade inflammation, providing a foundation for future in vivo studies using murine models of inflammation-associated chronic diseases to establish appropriate dosage regimens. Full article

Edible chrysanthemum (Chrysanthemum morifolium Ramat.), widely consumed in Asia, is rich in bioactive compounds such as polyphenols, flavonoids, and amino acids. Optimizing cultivation temperature is critical for maximizing both yield and quality, especially under the challenges posed by climate change. This study evaluated the growth performance, photosynthetic characteristics, and metabolite accumulation of the ‘Taiwan Hangju No. 1’ variety under five day/night temperature regimes (15/13 °C, 20/15 °C, 25/20 °C, 30/25 °C, and 35/30 °C) over a 220-day period in an artificial climate greenhouse. The 25/20 °C regime promoted the best overall growth, with the highest yields of bud-leaves and flowers, and supported the highest net photosynthetic rate, indicating optimal carbon assimilation under moderate temperatures. In contrast, stomatal conductance, respiration rate, and transpiration rate increased with temperature, peaking at 35/30 °C. Water use efficiency was greatest at 15/13 °C. Bioactive compound accumulation exhibited complex and organ-specific responses to temperature. The concentration of polyphenols, luteolin, and caffeoylquinic acid derivatives (CQAs) increased with temperature in both bud-leaves and flowers, free amino acids decreased in bud-leaves with rising temperature, reaching a peak at 15/13 °C, and flavonoid concentration peaked at 35/30 °C. In flowers, free amino acids accumulated most at 20/15 °C, and flavonoids peaked at 25/20 °C. The differing yields of bud-leaves and flowers under various temperature conditions contributed to variation in the total content of functional compounds. Except for free amino acids, the total of other functional compounds in bud-leaves was highest at 30/25 °C. The total content of all functional compounds in flowers was highest at 25/20 °C. This study demonstrated that 25/20 °C provides the best balance between growth, photosynthetic efficiency, and accumulation of key bioactive compounds and is therefore recommended as the optimal cultivation temperature for ‘Taiwan Hangju No. 1’. These findings reveal temperature-dependent and organ-specific metabolic adjustments, suggesting that moderate warming may enhance crop quality if managed carefully. The results provide a scientific basis for climate-adaptive cultivation strategies of edible chrysanthemums in subtropical regions. Full article

Phenolic compounds are strong antioxidant and antibacterial agents with great pharmacological, medicinal, nutritional, and industrial value. The potential of Morus nigra in stem node culture was investigated for the production of phenolic compounds and their elicitation with CuSO₄. Individual phenolic compounds in the samples were identified and quantified by using HPLC-PDA and HPLC-MS methods, while the content of total phenolic compounds, the content of total flavonoids, and the antioxidant activity of methanolic extracts were evaluated spectrophotometrically. The highest fresh and dry weights were obtained in plantlets treated with 0.5 mM CuSO₄ for 42 days. The highest total phenolic content, total flavonoid content, and antioxidant activity of the extracts were determined in stem node cultures treated with 3 mM CuSO₄ for 42 days. Under the latter conditions, the predominant representatives of the caffeoylquinic acids, p-coumaric acid derivatives, kaempferol derivatives, and quercetin derivatives also achieved the highest content. The most abundant phenolic compound in all samples was the chlorogenic acid. The nodal culture of M. nigra elicited with CuSO₄ could potentially be used for the industrial production of phenolic compounds, especially caffeoylquinic acids. Moreover, considering the biochemical response to CuSO₄ treatment and the ability to tolerate and accumulate copper, the potential application of M. nigra in phytoremediation is also highlighted. Full article

Rhaponticum carthamoides (Willd.) Iljin. is an endemic plant species found in Siberia, Mongolia, and Kazakhstan. Its roots and rhizomes are used to treat physical fatigue and weakness following illness. The present study examines the scaling up of caffeoylquinic acid (CQA) derivative and flavonoid production in R. carthamoides transformed roots. The transformed roots were grown in shaken Erlenmeyer flasks of varying volumes (0.5–2 L), a temporary immersion system (TIS) (Rita^® and PlantForm bioreactors), and a nutrient sprinkle bioreactor (NSB) in Woody Plant medium for 35 days. The highest dry biomass production was achieved in the 0.5 L and 1 L flasks and in the NSB bioreactor, yielding 22.2 to 20.4 g/L—approximately 14 to 23 times the weight of the inoculum. The accumulation of individual specialized metabolites varied depending on the culture system used. The peak amount of CQAs (544.5 mg/L), in terms of the increase in dry weight and metabolite levels, was obtained in the NSB bioreactor. The primary CQAs were chlorogenic acid (5-CQA) and a tri-CQA 1. The highest concentration of 5-CQA (7.38 mg/g DW) was found in the roots cultivated in the NSB bioreactor. In contrast, the tri-CQA 1 dominated in the roots from 2 L shaken Erlenmeyer flasks (8.44 mg/g DW). Our findings demonstrate that transformed roots growing in an NSB bioreactor are an effective system for increasing CQA production, potentially serving as an alternative source. This biotechnological approach could help reduce the overexploitation of field-grown R. carthamoides, a currently threatened species. Full article

Ptilostemon greuteri Raimondo & Domina is a rare Sicilian paleoendemic species. The aim of study was to investigate the micro-morphological features of leaves by light and scanning electron microscopy, to elucidate the phytochemical profile of essential oil (EO), n-hexane (HE) and hydroalcoholic extract (HAE) by gas and liquid chromatographic methods, and antioxidant and anti-inflammatory properties by in vitro assays. Leaves had a large lanceolate blade, dark green on the upper side and greyish on the lower one with a dense tomentum. Epidermis showed many protruding stomata. By lipid-specific dyes, lipophilic droplets within cells surrounding the secretory ducts and within palisade cells were detected, whereas the presence of polyphenols in the mesophyll was highlighted by toluide blue O. These observations have driven the subsequent phytochemical analyses. EO showed germacrene D (29.94%), carvacrol (14.3%) and eugenol (12.93%) as the most abundant compounds. In the HE, docosane, oleic and palmit acid, and lupeol were the predominant compounds, whereas caffeoylquinic acid and quercetin derivatives were the most common polyphenols in HAE. Considering the detected mean half-inhibitory concentrations (IC₅₀), HAE showed predominant antioxidant activity (IC₅₀ 30.54 µg/mL), while EO showed predominant anti-inflammatory activity (IC₅₀ 397.59 µg/mL). Finally, HE, rich in medium-to-long fatty acids, showed the best protease inhibitory activity Full article

Artichoke (Cynara cardunculus L.) is an herbaceous perennial plant from the Mediterranean Basin, cultivated as a poly-annual crop in different countries. Artichoke produces a considerable amount of waste at the end of the harvesting season in the field (5.2 tons/ha/year, DW) and from the industrial processing of fresh-cut products during the harvesting time (800 tons/year). The qualitative and quantitative phenolic profile and inulin content of artichoke samples from the field and industrial processing waste have been investigated after green extraction. The best operative conditions were achieved using the dried biomass extracted with water at 80 °C for 120 min and a matrix-to-solvent ratio of 1:30. The data obtained showed that the concentration of total polyphenols in fresh artichokes followed this order: stems > heads > leaves > outer bracts. Chlorogenic acid and 3,4 di-O-caffeoylquinic acid were the most concentrated caffeoylquinic derivates, whereas luteolin 7-O-malonyglucoside, luteolin 7-O-glucoside and 7-O-rutinoside were the most abundant flavonoids. The artichoke by-products showed high polyphenolic and inulin values, thus representing an important source of health-promoting biomolecules for application in pharmaceutical and cosmeceutical fields. According to the principles of circular economy, the work scheme proposed in this article, the use of waste and its processing into useful products such as nutraceutical supplies could provide a practical and economic opportunity for companies and farmers involved in the cultivation and industrial processing of artichokes. Full article

The Italian Carciofo di Paestum (C. scolymus) PGI, an artichoke variety from the Campania region, was investigated for its potential to reuse by-products for food supplements. EtOH:H₂O 50:50 and 75:25 extracts of its leaves were analyzed for phenolic and flavonoid content and antioxidant activity (TEAC: 1.90 and 1.81 mM of Trolox; DPPH IC₅₀: 106.31 µg/mL and 128.21 µg/mL; FRAP: 1.68 and 1.58 mM FeSO₄/g extract). To further investigate the antioxidant potential, the ability of the two extracts to scavenge reactive species was assessed in Caco-2 cell cultures, showing a dose-dependent antioxidant capacity. To highlight metabolites responsible for the activity, LC-ESI/HRMSMS analysis was achieved, revealing 28 compounds (sesquiterpenes, megastigmanes, quinic acid and hydroxycinnamic acid derivatives, flavonoids, lignans, triterpenoid saponins, and polar fatty acids), of which structures were determined using 1D- and 2D-NMR analysis. In addition, quantitative determination of caffeoyl, dicaffeoyl, and quinic acid derivatives (CQAs) was performed through LC-ESI/QTrap/MS/MS, highlighting that the most abundant compound was 5-caffeoylquinic acid (6), with values of 9.310 and 7.603 mg/g extract in EtOH:H₂O (75:25) and EtOH:H₂O (50:50), respectively. The analysis showed that extracts were rich in bioactive compounds, suggesting their potential for development into antioxidant-based food supplements that may protect cells from oxidative stress and support overall wellness. Full article

Background/Objectives: Hemerocallis citrina Baroni (HCB) is a traditional herb for the treatment of depression in China. However, the active constituents and the underlying mechanisms of its antidepressant effects remain unclear. The aim of this study was to identify the bioactive constituents of HCB and elucidate its underlying mechanism for the treatment of depression. Methods: The constituents of HCB were systematically analyzed using UHPLC-Q-Orbitrap HRMS. Its antidepressant effect was evaluated by chronic unpredictable mild stress (CUMS)-induced depression. The mechanism of HCB in treating depression was investigated through network pharmacology and molecular docking. Subsequently, its potential mechanism for the treatment of depression was carried out by RNA sequencing. Finally, the mechanism was further verified by Western blot. Results: A total of 62 chemical constituents were identified from HCB using UHPLC-Q-Orbitrap HRMS, including 17 flavonoids, 11 anthraquinones, 11 alkaloids, 10 caffeoylquinic acid derivatives, five phenolic acids, five triterpenoids, and three phenylethanosides, 13 of which were identified as potential active constituents targeting 49 depression-associated proteins. Furthermore, HCB was found to significantly reduce cognitive impairment, anxiety-like behavior, and anhedonia-like behavior. The expression levels of 5-hydroxytryptamine (5-HT), dopamine (DA), and brain-derived neurotrophic factor (BDNF) were elevated in the hippocampal CA3 region. Results from network pharmacology and transcriptomics indicated that the PI3K/Akt/CREB signaling pathway is essential for the therapeutic effects of HCB on depression. Research in the field of molecular biology has conclusively demonstrated that HCB is associated with an increase in the expression levels of several important proteins. Specifically, there was a notable upregulation of phosphorylated PI3K (p-PI3K) relative to its unphosphorylated form PI3K, as well as an elevation in the ratio of phosphorylated Akt (p-Akt) to total Akt. Additionally, the study observed increased levels of phosphorylated CREB (p-CREB) compared to its unphosphorylated CREB. Conclusions: This study provides compelling evidence that HCB possesses the ability to mitigate the symptoms of depression through its influence on the PI3K/Akt/CREB signaling pathway. HCB could be developed as a promising therapeutic intervention for individuals struggling with depression, offering new avenues for treatment strategies that target this particular signaling mechanism. Full article

Background/Objectives: Cork oak forests have been declining due to fungal pathogens such as Diplodia corticola. However, the preventive fungicides against this fungus have restricted use due to the deleterious effects on human health and the environment, prompting the need for sustainable alternatives. Here, we describe the antifungal activity of an aqueous extract of Hedera helix L. leaves (HAE) against D. corticola and the possible mechanism of action. Results/Methods: The chemical analysis revealed compounds like the saponin hederacoside C, quinic acid, 5-O-caffeoylquinic acid, rutin, and glycoside derivatives of quercetin and kaempferol, all of which have been previously reported to possess antimicrobial activity. Remarkable in vitro antifungal activity was observed, reducing radial mycelial growth by 70% after 3 days of inoculation. Saccharomyces cerevisiae mutants, bck1 and mkk1/mkk2, affected the cell wall integrity signaling pathway were more resistant to HAE than the wild-type strain, suggesting that the extract targets kinases of the signaling pathway, which triggers toxicity. The viability under osmotic stress with 0.75 M NaCl was lower in the presence of HAE, suggesting the deficiency of osmotic protection by the cell wall. Conclusions: These results suggest that ivy extracts can be a source of new natural antifungal agents targeting the cell wall, opening the possibility of preventing fungal infections in cork oaks and improving the cork production sector using safer and more sustainable approaches. Full article

The major components of magnolia flower extracts (MFEs) were classified into four substances, such as flavonoids, phenylethanoid glycoside derivatives (PhGs), caffeoylquinic acids (CQAs), and others, in our previous study. The chemical components of MFEs, including the rutin of flavonoid, acteoside and isoacteoside of PhGs, and caffeyolquinic acids, are reported to have physiological effects on anti-obesity effects. The anti-obesity effect of fresh and browned Magnolia denudata flower extracts (FMFE and BMFE, respectively) was investigated in 3T3-L1 adipocytes. The treatment concentrations of FMFE and BMFE were 200 and 400 μg/mL, respectively, as determined with the WST-1 assay. Intracellular lipid accumulation in 3T3-L1 cells was inhibited with the treatment of MFEs, including FMFE and BMFE, as observed with an image of the culture plate, using an optical microscope and Oil red O staining. The expression of the adipogenic target genes involved in adipocyte differentiation, including PPARγ, C/EBPα, perilipin, FABP4, FAS, HSL, and SREBP-1, was suppressed with the treatment of MFEs. Additionally, the phosphorylation of AMPK and ACC in 3T3-L1 cells was significantly increased following treatment with the MFEs. These results suggest that both MFEs have a potential for physiological effects on anti-obesity activity. Full article

Chronic inflammatory diseases pose a substantial health challenge globally, significantly contributing to morbidity and mortality. Addressing this issue requires the use of effective anti-inflammatory strategies with fewer side effects than those provoked by currently used drugs. In this study, a range of phytochemicals (phenolic di-caffeoylquinic acid (Di-CQA), flavonoid cyanidin-3,5-diglucoside (Cy3,5DiG), aromatic isothiocyanate sinalbin (SNB) and aliphatic isothiocyanate sulforaphane (SFN)) sourced from vegetables and fruits underwent assessment for their potential anti-inflammatory activity. An in vitro model of human macrophage-like cells treated with a low dose of LPS to obtain a low degree of inflammation that emulates a chronic inflammation scenario revealed promising results. Cell viability and production of the key pro-inflammatory cytokines were assessed in the presence of various phytochemicals. The compounds Di-CQA and Cy-3,5-DiG, within low physiologically relevant doses, demonstrated notable anti-inflammatory effects by significantly reducing the production of key pro-inflammatory cytokines TNF-α and IL-6 without affecting cell viability. These findings underscore the potential of plant-derived bioactive compounds as valuable contributors to the prevention or treatment of chronic inflammatory diseases. These results suggest that these compounds, whether used individually or as part of natural mixtures, hold promise for their inclusion in nutritional interventions designed to mitigate inflammation in associated pathologies. Full article

Seeking food-derived antioxidants and inhibitors of α-glucosidase and α-amylase has been recognized as an effective way for managing diabetes. Coffee silver skin (CSS) is rich in phenolic compounds, which may be potential agents as antioxidants and for α-glucosidase and α-amylase inhibition. But whether phenolics in different forms show similar bioactivity remains unknown. In this study, phenolic compounds in CSS were extracted as free phenolics (FPs), esterified phenolics (EPs), and bound phenolics (BPs). The phenolic profiles and antioxidant activities of them were investigated. Their inhibitory effects on α-glucosidase and α-amylase were analyzed, and the inhibitory mechanisms were elucidated by molecular docking and molecular dynamic simulation. Results showed that FPs exhibited the best antioxidant ability and inhibitory effects on α-glucosidase and α-amylase. A total of 17 compounds were identified in FPs with 3-caffeoylquinic acid, 4-feruloylquinic acid, and dicaffeoylquinic acids as the dominant ones. Typical phenolics in FPs could bind to α-glucosidase and α-amylase through hydrogen bonds and form hydrophobic interaction with several key amino acid residues. In addition, 3,4-dicaffeoylquinic acid and 3-caffeoylquinic acid might be the principal components that account for the inhibitory effect of FPs on α-glucosidase. The results of this study may provide some scientific support for CSS utilization as a health-beneficial component in functional food development for type 2 diabetes mellitus management. Full article

Artichokes (Cynara scolymus L.) are valuable foods, thanks to their health benefits, but they generate significant waste during their production, harvesting, and processing, which poses sustainability issues. This study applied an agroprospecting approach to convert Tema artichoke biowaste (TB) into valuable resources, starting from a global perspective of the production chain to the targeted applications based on chemical and biological analysis. The major TB was identified in the outer bracts of the immature flower heads, which were collected throughout the harvesting season, extracted, and analyzed. The most abundant compounds were phenolic acids including chlorogenic acid and caffeoylquinic derivatives. Among flavonoids, cynaroside was the most abundant compound. Multivariate analysis distinguished batches by collection period, explaining 77.7% of the variance, with most compounds increasing in concentration later in the harvest season. Subsequently, TB extracts were analyzed for their potential in wound healing and anti-aging properties. Fibroblasts were used to assess the effect of selected extracts on cell migration through a scratch wound assay and on cellular senescence induced by etoposide. The results show a significant decrease in senescence-associated β-galactosidase activity, γH2AX nuclear accumulation, and both p53 and p21 protein levels. Overall, this study ascribes relevant anti-skin aging effects to TB, thus increasing its industrial value in cosmeceutical and nutraceutical applications. Full article