Search Results (34)

In this study, water residue obtained from Salvia desoleana Atzei et Picci steam distillation was evaluated for its antioxidant activity in vitro using different experimental models. In particular, the study evaluated the antiradical and antioxidant activity of Salvia desoleana extracts using CUPRAC, FRAP, DPPH^•, and ABTS^•+ assays; and tested ROS scavenging activity in Caco-2 cell cultures. Phenolic compounds were identified by (HR) LC-ESI-QTOF MS/MS and quantified with HPLC-PDA. Furthermore, Keap1-Nrf2, iNOS, and NOX enzymes involved in oxidative stress and antioxidant defences were the targets of molecular docking on key polyphenols. Hydroxycinnamic acids and flavonoids are the most important classes of compounds detected in the extracts. Among these compounds, the most significant was rosmarinic acid, followed by caffeic acid, luteolin glucuronide, and methyl rosmarinate. Although all extracts have shown encouraging results, the ethanolic extract solubilised with water (SEtOHA) was the one with the highest hydroxycinnamic acid content and total phenol content (518.64 ± 5.82 mg/g dw and 106.02 ± 6.02 mg GAE/g dw), as well as the highest antioxidant and antiradical activity. The extracts have shown anti-inflammatory activity by inhibiting NO release in LPS-stimulated Caco-2 cells. Finally, the in silico evaluation against the three selected enzymes showed interesting results for both numerical affinity ranking and predicted ligand binding models. The outcome of this study suggests this by-product as a possible ally in counteracting oxidative stress, as established by its favourable antioxidant compound profile, thus suggesting an interesting future application as a nutraceutical. Full article

Lung cancer is a prevalent and very aggressive sickness that will likely claim 1.8 million lives by 2022, with an estimated 2.2 million additional cases expected worldwide. The goal of the current investigation was to determine whether petroleum ether extract of purslane leaf could be used to treat lung cancer induced by 4-(Methylnitrosamino)-1-(3-pyridyl)-1-buta-4 none (NNK) in rats. In the in vitro extract recorded, promising anticancer effects in A540 cell lines with IC₅₀ were close to the reference drug, doxorubicin (14.3 and 13.8 μg/mL, respectively). A dose of 500 mg/kg/day orally for 20 weeks exhibited recovery effects on NNK-induced lung cancer with a good safety margin, where Intercellular Adhesion Molecule-1 (ICAM-1), the lung cancer biomarker, was significantly reduced by about 18.75% compared to cancer control. Purslane exhibited many anticancer mechanisms, including (i) anti-proliferation as a significant reduction in Ki67 level (20.42%), (ii) anti-angiogenesis as evident by a considerable decrease in Matrix metalloproteinase-9 (MMP-9) expression (79%), (iii) anti-inflammation as a remarked decline in Insulin-like growth factor 1 (IGF-1) expression (62%), (iv) pro-apoptotic effect as a significant activation in Forkhead box protein O1 (FOXO1) expression (262%), and (v) anti-oxidation as remarkable activation on antioxidant biomarkers either non-enzymatic or enzymatic concurrent with considerable depletion on oxidative stress biomarker, in comparison to cancer control. The histopathological examination revealed that Purslane extract showed markedly improved tissue structure and reduced pathological changes across all examined organs caused by NNK. The anti-lung cancer effect exhibited by the extract may be linked to the active ingredients of the extract that were characterized by LC–MS, such as α-linolenic acid, linoleic acid, palmitic acid, β-sitosterol, and alkaloids (berberine and magnoflorine). Full article

Developing new nanomaterials and performing functionalization to increase their photocatalytic capacity are essential in developing low-cost, eco-friendly, and multipurpose-capacity catalysts. In this research, SnO₂/Se-doped quantum dots (QDs) covered with glycerol (SnO₂/Se-GLY) were synthesized using microwave irradiation. Then, their cover was replaced with glutaraldehyde through a ligand exchange procedure (SnO₂/Se-GLUT). The XRD analyses confirmed a tetragonal rutile structure of SnO₂. The HR-TEM analysis confirmed the generation of QDs with a size around 8 nm, and the optical analysis evidenced low bandgap energies of 3.25 and 3.26 eV for the SnO₂/Se-GLY and SnO₂/Se-GLUT QDs, respectively. Zeta-sizer analysis showed that the hydrodynamic sizes for both nanoparticles were around 230 nm (50 mg/L), and the zeta potential confirmed that SnO₂/Se-GLUT QDs were more stable than SnO₂/Se-GLY QDs. The cover-modified QDs (SnO₂/Se-GLUT) showed a higher and faster adsorption capacity, followed by a slower photocatalytic process than the original QDs (SnO₂/Se-GLY). The QTOF-LC-MS analysis confirmed MB degradation through the identification of intermediates such as azure A, azure B, azure C, and phenothiazine. Adsorption isotherm analysis indicated Langmuir model compliance, supporting the high monolayer adsorption capacity and efficiency of these QDs as adsorbent/photocatalytic agents for organic pollutant removal. This dual capability for adsorption and photodegradation, along with the demonstrated reusability, highlights the potential of SnO₂/Se QDs in wastewater treatment and environmental remediation. Full article

This study aimed to determine the effectiveness of different green extraction techniques (GETs) on targeted bioactive compounds from artichoke leaf by-products using deep eutectic solvent extraction (DESE), supercritical CO₂ extraction (SCO₂E), subcritical water extraction (SWE), and ultrasound-assisted extraction (UAE). Moreover, (HR) LC-ESI-QTOF MS/MS and HPLC-PDA analyses were used to perform qualitative–quantitative analysis on the extracts, enabling the detection of several bioactive compounds, including luteolin, luteolin 7-O-glucoside, luteolin 7-O-rutinoside, apigenin rutinoside, chlorogenic acid, and cynaropicrin as the most representative ones. SWE showed better results than the other GETs (TPC: 23.39 ± 1.87 mg/g of dry plant, dp) and appeared to be the best choice. Regarding UAE, the highest total phenols content (TPC) was obtained with 50:50% v/v ethanol: water (7.22 ± 0.58 mg/g dp). The DES obtained with choline chloride:levulinic acid showed the highest TPC (9.69 ± 0.87 mg/g dp). Meanwhile, SCO₂E was a selective technique for the recovery of cynaropicrin (48.33 ± 2.42 mg/g dp). Furthermore, the study examined the antioxidant activity (1.10–8.82 mmol Fe²⁺/g dp and 3.37–31.12 mmol TEAC/g dp for DPPH^• and FRAP, respectively) and total phenols content via Folin–Ciocalteu’s assay (198.32–1433.32 mg GAE/g dp), of which the highest values were detected in the SWE extracts. The relationship among the GETs, antioxidant assays, and compounds detected was evaluated using Principal Component Analysis (PCA). PCA confirmed the strong antioxidant activity of SWE and showed comparable extraction yields for the antioxidant compounds between UAE and DESE. Consequently, GETs selection and extraction parameters optimization can be employed to enrich artichoke leaf by-products’ extracts with targeted bioactive compounds. Full article

Saffron (Crocus sativus) floral by-products are a source of phenolic compounds that can be recovered and used in the nutraceutical, pharmaceutical, or cosmetic industries. This study aimed to evaluate the phenolic compounds’ extraction using green extraction techniques (GETs) in saffron floral by-products and to explore the influence of selected extraction techniques on the phytochemical composition of the extracts. Specifically, ultrasound-assisted extraction (UAE), subcritical water extraction (SWE), and deep eutectic solvents extraction (DESE) were used. Phenolic compounds were identified with (HR) LC-ESI-QTOF MS/MS analysis, and the quantitative analysis was performed with HPLC-PDA. Concerning the extraction techniques, UAE showed the highest amount for both anthocyanins and flavonoids with 50:50% v/v ethanol/water as solvent (93.43 ± 4.67 mg/g of dry plant, dp). Among SWE, extraction with 96% ethanol and t = 125 °C gave the best quantitative results. The 16 different solvent mixtures used for the DESE showed the highest amount of flavonoids (110.95 ± 5.55–73.25 ± 3.66 mg/g dp), while anthocyanins were better extracted with choline chloride:butane-1,4-diol (16.0 ± 0.80 mg/g dp). Consequently, GETs can be employed to extract the bioactive compounds from saffron floral by-products, implementing recycling and reduction of waste and fitting into the broader circular economy discussion. Full article

Carlina vulgaris is a poorly understood plant in the context of biological activity, despite its widespread application in ethnomedicine in numerous European countries. The aim of this study was to assess the cytotoxic potential of the plant against human colorectal adenocarcinoma (HT29) and to isolate the plant components linked to this effect. Ultra-high performance liquid chromatography with a high-resolution/quadrupole time-of-flight mass spectrometer (UHPLC–HR/QTOF/MS–PDA) was used for the phytochemical characterization of the extract. Liquid–liquid extraction and preparative chromatography were employed for fractionation purposes. Our investigation demonstrated that the ethyl acetate fraction from C. vulgaris showed significant cytotoxicity, and a bioactivity-guided approach led to the isolation of oxylipins, including traumatic acid, pinellic acid, and 9,10-dihydroxy-8-oxsooctadec-12-enic acid. The structures of the compounds were confirmed by nuclear magnetic resonance spectroscopy. Among these compounds, the last one exhibited significant cytotoxicity, though without selectivity, and traumatic acid was characterized by mild cytotoxicity. The cytotoxicity was linked to intracellular reactive oxygen species generation. Full article

Carlina acaulis is highly valued in the traditional medicine of many European countries for its diuretic, cholagogue, anthelmintic, laxative, and emetic properties. Moreover, practitioners of natural medicine indicate that it has anti-cancer potential. However, its phytochemistry is still little known. In the present study, the polyphenolic composition of the plant was investigated using ultra-high-performance liquid chromatography coupled with a high-resolution/quadrupole time-of-flight mass spectrometer (UHPLC-HR/QTOF/MS-PDA). The fractionation of the extract was carried out using liquid-liquid extraction and preparative chromatography techniques. Cytotoxicity was assessed based on neutral red and MTT assays. The obtained data showed that the species is rich in chlorogenic acids and C-glycosides of luteolin and apigenin. The total amount of chlorogenic acids was 12.6 mg/g. Among flavonoids, kaempferol dihexosidipentose and schaftoside were the most abundant, reaching approximately 3 mg/g, followed by isoorientin, vitexin-2-O-rhamnoside, and vicenin II, each with a content of approximately 2 mg/g. Furthermore, the cytotoxic potential of the plant against human colorectal adenocarcinoma (HT29) and human cervical cancer (HeLa) cells was investigated using the normal epithelial colon cell line (CCD 841CoTr) as a reference. It has been demonstrated that the ethyl acetate fraction was the most abundant in polyphenolic compounds and had the most promising anticancer activity. Further fractionation allowed for the obtaining of some subfractions that differed in phytochemical composition. The subfractions containing polyphenolic acids and flavonoids were characterized by low cytotoxicity against cancer and normal cell lines. Meanwhile, the subfraction with fatty acids was active and decreased the viability of HeLa and HT29 with minimal negative effects on CCD 841CoTr. The effect was probably linked to traumatic acid, which was present in the fraction at a concentration of 147 mg/g of dried weight. The research demonstrated the significant potential of C. acaulis as a plant with promising attributes, thus justifying further exploration of its biological activity. Full article

In recent years, wild morel mushroom species have begun to be widely cultivated in China due to their high edible and medicinal values. To parse the medicinal ingredients, we employed the technique of liquid-submerged fermentation to investigate the secondary metabolites of Morehella importuna. Two new natural isobenzofuranone derivatives (1–2) and one new orsellinaldehyde derivative (3), together with seven known compounds, including one o-orsellinaldehyde (4), phenylacetic acid (5), benzoic acid (6), 4-hydroxy-phenylacetic acid (7), 3,5-dihydroxybenzoic acid (8), N,N′-pentane-1,5-diyldiacetamide (9), and 1H-pyrrole-2-carboxylic acid (10), were obtained from the fermented broth of M. importuna. Their structures were determined according to the data of NMR, HR Q-TOF MS, IR, UV, optical activity, and single-crystal X-ray crystallography. TLC-bioautography displayed that these compounds possess significant antioxidant activity with the half DPPH free radical scavenging concentration of 1.79 (1), 4.10 (2), 4.28 (4), 2.45 (5), 4.40 (7), 1.73 (8), and 6.00 (10) mM. The experimental results would shed light on the medicinal value of M. importuna for its abundant antioxidants. Full article

Chenopodium murale (Syn. Chenopodiastrum murale) (amaranthaceae) is used in the rural Egypt to treat oral ulcers in newborn children. The current study aimed to discover new natural products suitable for treating candidiasis disease with minimal side effects. Characterization of bioactive compounds by LC-QTOF-HR-MS/MS from Chenopodium murale fresh leaves’ juice (CMJ) was carried out in order to elucidate their potential anti-fungal and immunomodulatory effects in oral candidiasis in immunosuppressed rats. An oral ulcer candidiasis model was created in three stages: (i) immunosuppression by drinking dexamethasone (0.5 mg/L) for two weeks; (ii) Candida albicans infection (3.00 × 10⁶ viable cell/mL) for one week; and (iii) treatment with CMJ (0.5 and 1.0 g/kg orally) or nystatin (1,000,000 U/L orally) for one week. Two doses of CMJ exhibited antifungal effects, for example, through a significant reduction in CFU/Petri (236.67 ± 37.86 and 4.33 ± 0.58 CFU/Petri), compared to the Candida control (5.86 × 10⁴ ± 1.21 CFU/Petri), p ≤ 0.001. In addition, CMJ significantly induced neutrophil production (32.92% ± 1.29 and 35.68% ± 1.77) compared to the Candida control level of 26.50% ± 2.44. An immunomodulatory effect of CMJ at two doses appeared, with a considerable elevation in INF-γ (103.88 and 115.91%), IL-2 (143.50, 182.33%), and IL-17 (83.97 and 141.95% Pg/mL) compared with the Candida group. LC-MS/MS analysis operated in negative mode was used for tentative identification of secondary (SM) metabolites based on their retention times and fragment ions. A total of 42 phytoconstituents were tentatively identified. Finally, CMJ exhibited a potent antifungal effect. CMJ fought Candida through four strategies: (i) promotion of classical phagocytosis of neutrophils; (ii) activation of T cells that activate IFN-γ, IL-2, and IL-17; (iii) increasing the production of cytotoxic NO and H₂O₂ that can kill Candida; and (iv) activation of SOD, which converts superoxide to antimicrobial materials. These activities could be due to its active constituents, which are documented as anti-fungal, or due to its richness in flavonoids, especially the active compounds of kaempferol glycosides and aglycone, which have been documented as antifungal. After repetition on another type of small experimental animal, their offspring, and an experimental large animal, this study may lead to clinical trials. Full article

Background: Inflammation, endothelial dysfunction, and alterations in blood physiology are key factors contributing to atherosclerosis and other cardiovascular disorders. Hence, modulation of endothelial function and reducing its pro-inflammatory and pro-thrombotic activity is considered one of the most important cardioprotective strategies. This study aimed to evaluate the anti-inflammatory potential of rhubarb extracts isolated from petioles and underground organs of Rheum rhabarbarum L. (garden rhubarb) and R. rhaponticum L. (rhapontic rhubarb) as well as two stilbenoids, typically found in these plants, i.e., rhapontigenin (RHPG) and its glycoside, rhaponticin (RHPT). Methods: Analysis of the anti-inflammatory effects of the indicated rhubarb-derived substances involved different aspects of the endothelial cells’ (HUVECs) response: release of the inflammatory mediators; cyclooxygenase (COX-2) and 5-lipoxygenase (5-LOX) expression as well as the recruitment of leukocytes to the activated HUVECs. The ability of the rhubarb-derived extracts to inhibit COX-2 and 5-LOX activities was examined as well. The study was supplemented with the in silico analysis of major components of the analyzed extracts’ interactions with COX-2 and 5-LOX. Results: The obtained results indicated that the examined plant extracts and stilbenes possess anti-inflammatory properties and influence the inflammatory response of endothelial cells. Biochemical and in silico tests revealed significant inhibition of COX-2, with special importance of rhaponticin, as a compound abundant in both plant species. In addition to the reduction in COX-2 gene expression and enzyme activity, a decrease in the cytokine level and leukocyte influx was observed. Biochemical tests and computational analyses indicate that some components of rhubarb extracts may act as COX-2 inhibitors, with marginal inhibitory effect on 5-LOX. Full article

Polygoni Cuspidati Rhizoma et Radix (syn. rhizomes of Reynoutria japonica Houtt.) is a pharmacopoeial raw material in Europe and China. In traditional medicine, one of the applications for Reynoutria japonica rhizomes is wound healing. In a recent in vitro study, we demonstrated that ethanol and acetone extracts from this herbal drug have the potential to heal oral gum wounds. However, considering that a majority of herbal medicines have been traditionally administered as water decoctions, in the present study, a decoction of Reynoutria japonica rhizomes was prepared and detailed tests to determine its in vitro gingival wound healing activity were conducted. We used the primary human gingival fibroblasts (HGF) incubated with a decoction to determine cell viability (MTT assay), cell proliferation (the confocal laser scanning microscope—CLSM), and cell migration (wound healing assay). Moreover, the collagen type III expression was examined using immunocytochemical staining. The studied decoction was qualitatively and quantitatively characterized using the validated HPLC/DAD/ESI-HR-QTOF-MS method. The Folin–Ciocalteu assay was used to determine the total phenols and tannins content. Additionally, HPLC-RI analysis of decoction and the previously obtained ethanol and acetone extracts was used to determine the composition of saccharides. Low concentration (from 50 to 1000 µg/mL) of decoction after 24 h incubation caused a significant increase in HGF cell viability. No cytotoxic effect was observed at any tested concentration (up to 2000 µg/mL). The lowest active concentration of decoction (50 µg/mL) was selected for further experiments. It significantly stimulated human gingival fibroblasts to proliferate, migrate, and increase the synthesis of collagen III. Phytochemical analysis showed significantly fewer polyphenols in the decoction than in the ethanol and acetone extracts tested earlier. In contrast, high levels of polysaccharides were observed. In our opinion, they may have a significant effect on the oral wound healing parameters analyzed in vitro. The results obtained encourage the use of this raw material in its traditional, safe form—decoction. Full article

The genus of cyanobacteria Microcystis is one of the most recurrent in blooms and is associated with the hepatotoxin microcystin production. In addition to cyanotoxins, these bacteria produce a wide range of secondary metabolites with a wide repertoire of activities. The co-occurrence of cyanotoxins and other cyanopeptides during blooming is quite common, and the negative effects are not always limited to one class of toxins, which makes it essential to investigate the toxicity of the other compounds individually. The objective of this study was to isolate the cyanopeptide microcyclamide produced by the strain Microcystis aeruginosa LTPNA 08 by liquid chromatography coupled to high-resolution mass spectrometry with a quadrupole-time-of-flight analyzer (LC-HR-QTOF-MS/MS) and to evaluate its acute toxicity in embryos of Danio rerio through the Fish Embryo Acute Toxicity (FET) assay. The fraction containing microcyclamide (95% purity) caused lethality in 62% of the embryos after 96 h exposure (50 µg mL⁻¹), with evidence of cardiotoxicity (cardiac edema). The calculated LC₅₀ value was 42.98 µg mL⁻¹ (with a concentration range of 37.79–48.89 µg mL⁻¹). The characterization of the secondary metabolites produced by cyanobacteria and the investigation of the toxicity of these compounds individually are essential for the identification of the substances responsible for negative effects on living organisms and on the ecosystem, in addition to assisting in the development of risk management policies. Full article

Previous studies in Uncaria tomentosa have shown promising results concerning the characterization of polyphenols with leaves yielding more diverse proanthocyanidins and higher bioactivities values. However, the polyphenols-microbiota interaction at the colonic level and their catabolites avoid the beneficial effects that can be exerted by this medicinal plant when consumed. In this regard, a new generation of hybrid nanoparticles has demonstrated improvements in natural compounds’ activity by increasing their bioavailability. In this line, we report a detailed study of the characterization of a proanthocyanidin-enriched extract (PA-E) from U. tomentosa leaves from Costa Rica using UPLC-QTOF-ESI MS. Moreover, two types of hybrid nanoparticles, a polymeric-lipid (F-1) and a protein-lipid (F-2) loaded with PA-E were synthesized and their characterization was conducted by dynamic light scattering (DLS), attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FT-IR), high-resolution transmission electron microscopy (HR-TEM), and encapsulation efficiency (%EE). In addition, in vitro release, antioxidant activity through 2,2-diphenyl-1-picrylhidrazyl (DPPH) as well as in vivo delayed-type hypersensitivity (DTH) reaction was evaluated. Results allowed the identification of 50 different compounds. The PA-E loaded nanoparticles F-1 and F-2 achieved encapsulation efficiency of ≥92%. The formulations exhibited porosity and spherical shapes with a size average of 26.1 ± 0.8 and 11.8 ± 3.3 nm for F-1 and F-2, respectively. PA-E increased its release rate from the nanoparticles compared to the free extract in water and antioxidant activity in an aqueous solution. In vivo, the delayed-type hypersensitive test shows the higher immune stimulation of the flavan-3-ols with higher molecular weight from U. tomentosa when administered as a nanoformulation, resulting in augmented antigen-specific responses. The present work constitutes to our knowledge, the first report on these bioactivities for proanthocyanidins from Uncaria tomentosa leaves when administrated by nanosystems, hence, enhancing the cellular response in mice, confirming their role in immune modulation. Full article

Antrodia cinnamomea is a precious edible mushroom originating from Taiwan that has been popularly used for adjuvant hepatoprotection and anti-inflammation; however, the chemical principle for its anti-inflammatory activity has not been elucidated, which prevents the quality control of related products. Using the RAW264.7 model for the anti-inflammatory activity assay as a guide, we reported the isolation and structural elucidation of three potent anti-inflammatory compounds from isolated ergostanes (16) and lanostanes (6). Their structures were elucidated on the basis of spectroscopic data analysis including NMR and HR-QTOF-MS. Particularly, the absolute configurations of (25R)-antcin K, (25R)-antcin A, versisponic acid D, and (25R)-antcin C were determined by single crystal X-ray diffraction (XRD). The representative and most promising compound antcin A was shown to suppress pro-inflammatory biomolecule release via the down-regulation of iNOS and COX-2 expression through the NF-κB pathway while the mRNA levels of IL-1β, TNF-α and IL-6 were also decreased. The high dependency on structural variation and activity suggests that there might be special biological targets for antcin A. Our work makes it possible to develop evidence-based dietary supplements from Antrodia cinnamomea based on anti-inflammatory constituents. Full article

In this work, two vintages (2019 and 2020) of red-fleshed ‘Weirouge’ apples were processed with the innovative spiral filter press technology to investigate juice production in an oxygen-reduced atmosphere. After pressing, a more brilliant red color and appreciably higher amounts of oxidation-sensitive constituents (ascorbic acid, anthocyanins, and colorless (poly)phenols) were seen in spiral filter pressed juices compared to those produced with conventional systems (horizontal filter press and decanter). In a subsequent stability study (24 weeks storage at 4, 20, and 37 °C), the color and phenolic compounds were monitored and differences in the juices produced with the different pressing-systems were widely maintained during the storage period. The analyses of the anthocyanins and colorless (poly)phenols were conducted by UHPLC-DAD-ESI-QTOF-HR-MS/MS and UHPLC-DAD. The spiral filter press emerged as a promising technology for the production of juices with a more attractive color and a better retention of oxidation-sensitive constituents during processing and storage compared to conventional juices. Full article