Search Results (75)

The Inula japonica flower is traditionally used to alleviate lung inflammatory symptoms. While the therapeutic effect of the I. japonica flower on lung diseases has been suggested, the efficacy of the I. japonica flower in treating atopic dermatitis (AD) remains unknown. We investigated the effects of a water extract of the I. japonica flower (WEIF) on Dermatophagoides farinae extract (DfE)-induced AD-like inflammation in NC/Nga mice. Histological analysis of the epidermal structure, mast cell infiltration, and barrier protein expression were examined. Serum inflammatory mediator levels were assessed. To elucidate the regulatory pathway of WEIF, the effects of 1,5-dicaffeoylquinic acid (DCQA) and 1-O-acetylbritannilactone (ABL) in WEIF on the JAK/STAT pathway were evaluated in interferon-γ/tumor necrosis factor (TNF)-α-stimulated human adult epidermal keratinocytes. WEIF ameliorated DfE-induced skin inflammation by reducing dermatitis scores, mast cell infiltration, skin structural damage, and serum inflammatory mediator levels. Additionally, DCQA and ABL significantly inhibited JAK/STAT activation in interferon-γ/TNF-α-treated keratinocytes. Furthermore, ligand-binding analysis revealed high binding affinities of DCQA and ABL for JAK. These results suggest the pharmacological potential of WEIF to alleviate DfE-induced skin inflammation by inhibiting the JAK/STAT signaling pathway. In conclusion, these findings support the development of WEIF as a therapeutic treatment for AD-like skin inflammatory diseases. Full article

This study compares the antioxidant properties and phytochemical profiles of three pairs of widely used medicinal plant species to their counterparts from Provence, France: Arnica montana with Pentanema montanum (formerly known as Inula montana), Helichrysum italicum with Helichrysum stoechas, and Satureja hortensis with Satureja montana. Phytochemical composition has been investigated using UHPLC-HRMS/MS and molecular networking, revealing chemical profiles dominated by phenylpropanoids and flavonoids, with lignans, sesquiterpene lactones, or polyketides aside. Well-plate DPPH/ABTS assays were used to evaluate the antioxidant activity of extracts, and post-column assays were used to identify antioxidant compounds. The three Provence species demonstrated comparable or superior antioxidant activities to their counterparts, primarily attributed to phenolic compounds such as mono- and di-caffeoylquinic acids, quercetagetin-7-O-glucoside, and myricetin acetylhexoside. These findings show the potential of Provence species to be substituted for some overharvested medicinal plants. This research supports biodiversity conservation while promoting the integration of these local species into pharmaceutical, nutraceutical, cosmetic, and food industries. Full article

Holoparasitic plants of the genus Cuscuta are generally considered prominent agricultural pests. In addition to their negative economic effect on agriculture and their impact on natural plant societies, they have also been long known in East Asian as medicinal plants with beneficial properties. This underlines the fact that Cuscuta spp. are particularly rich in specialized metabolites, flavonoids, alkaloids, and cumarines, among others. In addition to several well-characterized species, most of the species variety within the genus remains largely unstudied. In the present study we aimed to compare the flavonoid profiles of natural populations of two of the most abundant Cuscuta species in Bulgaria—the native C. epithymum, and the naturalized C. campestris. Based on HPLC-MS/MS analysis, a total of 13 polyphenolics compounds were annotated, with hyperoside and isoquercitrin being some of the most abundant. Some notable differences were found, like the complete absence of dicaffeoylquinic acid in C. campestris, and kaempferol-3,7-O-diglucoside and kaempferol 3-O-β-(6′′-O-trans-p-coumaroyl)-glucopyranoside in C. epithymum. The population of the two species clustered separately from each other, with some variations, but with no clear pattern of dependence on the locality or host species. Based on the results it can be concluded that flavonoids may be used as chemotaxonomical markers within the genus, showing that even in different climatic conditions and different host ranges, the two studied species clearly differed from each other. Also, their rich content emphasizes the potential of these parasites as a source of bioactive compounds. Full article

Fennel waste is rich in compounds that may have beneficial effects on human health. For this reason, the most abundant metabolites in fennel were isolated as the following: quercetin-3-O-glucoside, quinic acid, 1,5-dicaffeoylquinic acid, kaempferol-3-O-glucuronide, and quercetin-3-O-glucuronide. After inducing inflammation in human bronchial epithelial cells by stimulating them with IL-1β, the cells were treated with the specialized Foeniculum vulgare metabolites at different concentrations to assess their anti-inflammatory effect. Eicosanoids, fatty acids, and sphingolipids were extracted from the cell medium and quantified by UPLC-ESI-QTRAP-MS/MS analysis. The anti-inflammatory activity of the metabolites isolated from fennel waste was demonstrated. They were able to alleviate the inflammatory state in human bronchial epithelium by modulating the metabolic expression of both pro- and anti-inflammatory eicosanoids, fatty acids, and sphingolipids. These findings suggest the potential use of fennel waste in the production of dietary supplements to alleviate the symptoms of chronic inflammatory diseases like asthma, chronic obstructive pulmonary disease (COPD), and idiopathic pulmonary fibrosis (IPF), where the continuous use of antiphlogistics may have significant side effects. Full article

Capirona macrophylla is a Rubiaceae known as “mulateiro”. Ethnobotanical extracts have been used for skin treatment and in the management of leishmaniasis and malaria. Objectives: The metabolites in aqueous extracts from wood bark, leaves, and stems were identified, and their in silico docking and in vitro cellular efficacy against Leishmania amazonensis and Plasmodium falciparum were evaluated. Methods: The extracts were analyzed by UHPLC/HRMSⁿ using untargeted metabolomics approach with MSDial, MSFinder, and GNPS software for metabolite identification and spectra clustering. The most abundant metabolites underwent molecular docking using AutoDock via PyRx, targeting the dihydroorotate dehydrogenase from Leishmania and P. falciparum, and evaluated through molecular dynamics simulations using Gromacs. In vitro biological assays were conducted on 60 HPLC-fractions against these parasites. Results: Metabolomics analysis identified 5100 metabolites in ESI+ and 2839 in ESI− spectra among the “mulateiro” samples. GNPS clustering highlighted large clusters of quercetin and chlorogenic acid groups. The most abundant metabolites were isofraxidin, scopoletin, 5(S)-5-carboxystrictosidine, loliolide, quercetin, quinic acid, caffeoylquinic acid (and isomers), chlorogenic acid, neochlorogenic acid, tryptophan, N-acetyltryptophan, epicatechin, procyanidin, and kaempferol-3-O-robinoside-7-O-rhamnoside. Molecular docking pointed to 3,4-dicaffeoylquinic acid and kaempferol as promising inhibitors. The in vitro assays yielded four active HPLC-fractions against L. amazonensis with IC50 values ranging from 175.2 μg/mL to 194.8 μg/mL, and fraction G29 showed an IC50 of 119.8 μg/mL against P. falciparum. Conclusions: The ethnobotanical use of “mulateiro” wood bark tea as an antimalarial and antileishmanial agent was confirmed through in vitro assays. We speculate that these activities are attributed to linoleic acids and quinic acids. Full article

The incidence of various inflammatory diseases has remained high. Inula cappa is a kind of Chinese herbal medicine with a wide range of pharmacological uses and application value. It has anti-inflammatory, antibacterial, antioxidant, hepatoprotective and other pharmacological activities. The monomeric compounds that have been confirmed to have anti-inflammatory effects are luteolin, chrysoerilol, artemetin, chlorogenic acid, neochlorogenic acid, cryptchlorogenic acid, isochlorogenic acid A, isochlorogenic acid B, isochlorogenic acid C and 1,3-O-dicaffeoylquinic acid. This article introduces the relationship between Inula cappa and inflammation, the anti-inflammatory components of I. cappa, the modulation of each component on the inflammatory transduction signal pathway, and the TLR2/MyD88/NF-KB anti-inflammatory signaling pathway, providing a theoretical basis for anti-inflammatory research on and clinical medication using Inula cappa. Full article

Astragali Radix (AR), a traditional food and medicinal herb used for thousands of years, is widely recognized for its role in enhancing immunity, particularly when combined with adjuvant chemotherapy. The two primary types of AR available in the market are imitation wild AR (grown for seven years) and cultivated AR (grown for two years). However, whether differences exist in their immune-enhancing effects and chemical constituents remains unclear. In this study, a comparative analysis was performed to evaluate the immune activity and chemical composition of cultivated and imitation wild AR. Immune activity was assessed through in vivo animal studies, while metabolomic analysis was used to characterize their chemical profiles. The results demonstrate that AR possesses significant antitumor and immune-enhancing activities, with imitation wild AR showing superior efficacy compared with cultivated AR. Following 16 days of daily AR treatment, both the thymus and spleen coefficients were significantly increased, effectively reversing the immune dysfunction induced by cyclophosphamide (CTX). Moreover, the administration of AR showed no significant toxicity, as evidenced by the stable liver and kidney function indicators, including ALT, UREA, and CRE levels. To investigate chemical differences, a customized chemotaxonomic-based in-house library containing 215 compounds was developed and integrated with the Progenesis QI informatics platform for metabolite annotation. Using multivariate analysis, 48 constituents were identified in total: 46 unique to the imitation wild AR and 45 specific to the cultivated AR. The correlation between chemical constituents and the pharmacological effects of AR was evaluated. Based on orthogonal partial least-squares discriminant analysis (OPLS-DA) and S-plot analysis, five potential biomarkers were identified, including Calycosin-7-glucoside, Rhamnocitrin-3-O-β-D-glucopyranoside, Ononin, 3,5-Dicaffeoylquinic acid, and Acetylastragaloside I. These biomarkers likely account for the differences in immune-enhancing effects between the two AR types. This study provides a scientific foundation for the rational use of Astragali Radix. Full article

Gynura divaricata (L.) DC is a long-used medicinal and edible plant in China folk. Its hyperglycemic effects have garnered increasing public attention in recent years. This study revealed that the ethyl acetate (EtOAc) and butanol (BuOH) partition fractions of G. divaricata crude extract exhibited significantly higher α-glucosidase inhibition activity and enhanced glucose uptake ability compared to other fractions. Guided by the hypoglycemic bioassay, these two fractions were subjected to isolation of active compounds using high-speed countercurrent chromatography (HSCCC). A two-phase solvent system composed of hexane-methyl tert-butyl ether (MtBE)-methanol-0.1% TFA water was employed for the separation of the EtOAc fraction by conventional HSCCC through a gradient elution strategy. Five major compounds were obtained and identified as chlorogenic acid (1), 3,4-dicaffeoylquinic acid (2), 3,5-dicaffeoylquinic acid (3), 4,5-dicaffeoylquinic acid (4), and kaempferol-3-O-β-D-glucopyranoside (5) by ESI-MS, ¹HNMR, and ¹³CNMR. The chlorogenic acid and the three dicaffeoylquinic acids were found to display higher inhibitory activities against α-glucosidase compared to the flavonoid. Considering their acidic nature, pH-zone-refining CCC (PHZCCC) was then applied for further scale-up separation using a solvent system MtBE: n-butanol: acetonitrile: water with trifluoroacetic acid (TFA) as a retainer and ammonium hydroxide (NH₄OH) as an eluter. A significantly higher yield of chlorogenic acid was obtained from the BuOH fraction by PZRCCC. Molecular docking between the caffeoylquinic acids and α-glucosidase confirmed their hypoglycemic activities. This study demonstrates that CCC is a powerful tool for preparative separation of active constituents in natural products. This research presents a novel and effective method for the preparative isolation of hypoglycemic compounds from Gynura divaricata. Full article

This study developed a structured fruit cube (FC) snack using only natural ingredients, specifically red grape and apple, without hydrocolloids and sucrose. After development, physicochemical characterization and analysis of phenolic compounds (PCs), including anthocyanins, flavonols, and hydroxycinnamic acid derivatives, using HPLC-DAD-ESI-MS/MS, were conducted. Sensory quality was also assessed through an acceptance and sensory profile analysis using the rate-all-that-apply methodology. The results showed that the FC had physicochemical characteristics similar to other structured fruits that use hydrocolloids. Additionally, they presented a complex composition of PCs, predominantly including anthocyanins derived from malvidin (tri-substituted methoxylated anthocyanins), notably cumarylated ones. Flavonols compounds comprised the 3-glucoside series of myricetin, quercetin, laricitrin, kaempferol, isorhamnetin, and syringetin; the 3-galactoside series of myricetin and quercetin; and the 3-glucuronic acid series of myricetin and quercitin, along with rutin. The presence of caftaric acid, coutaric acid, fertaric acid, and p-coumaroyl-glucose was also detected, alongside caffeic acid-O-glucoside 1, caffeic acid-O-glucoside 2, chlorogenic acid, 4-O-p-coumaroylquinic acid, and dicaffeoylquinic acid. In conclusion, the selection of natural ingredients was technologically suitable for obtaining an FC. Despite using conventional drying at 60 °C, the product showed notable concentrations of PCs and also achieved great sensory acceptance. Full article

Ceratonia siliqua L. is a medicinal plant that has long been used in traditional Moroccan medicine to treat many diseases. This study aimed to assess the impact of the stages of the immature phase of carob pulp (M1, M2, M3, M4, and M5) on phytochemical composition, antioxidant activity, and antidiabetic activity of Ceratonia siliqua L. The identification of the phenolic profile by HPLC-UV/MS-MS and the study of the antidiabetic effect by in silico, in vitro, and in vivo studies were carried out for extracts with high contents of phenolic compounds from immature wild carob pulp from the communes of Timoulit (TM), Bin Elouidane (AW), and Ouaouizerth (TG) in the province of Azilal in the Béni Mellal-Khénifra region. The results revealed a gradual increase in total sugar content over the pulp’s ripening period, reaching a value of 2134 ± 56.23 mg GE/100 g fresh weight (FW) for TG. The three locations showed peak values for total polyphenol content (TPC), total flavonoid content (TFC), and total condensed tannin (TCT) at the M2 stage. AW had the highest concentrations of TPC (3819 ± 226.4 mg GAE/100 g FM), TFC (1034 ± 57.08 mg QE/100 g FM), and TCT (1472 ± 28.46 mg CE/100 g FM). The DPPH assay (7892 ± 296.1 mg TE/100 g FM) and the FRAP assay (278.2 ± 7.85 mg TE/100 g FM) both demonstrated that the TG zone is a highly potent antioxidant zone. In contrast, the AW site exhibited a markedly elevated value of 725.4 ± 103.6 mg TE/100 g FM in the ABTS assay. HPLC-UV-MS/MS analysis showed that the methanolic extracts of immature carob pulp (MEICP) from the three areas contained several different chemical compounds. The most prevalent were 3-O-p-coumaroyl-5-O-caffeoylquinic acid, quercetin 3-methyl ether, gallic acid, and galloylquinic acid. Immature carob pulp extract (ICPE) from AW showed the strongest in vitro inhibition of pancreatic α-amylase (IC₅₀ = 0.405 µg/mL) and TG extracts were most potent against intestinal α-glucosidase (IC₅₀ = 0.063 µg/mL). In vivo, AW, TG, and TM extracts significantly reduced postprandial glycemia in rats, with AW having the greatest effect. These results highlight the antidiabetic potential of ICPE. The 3-O-p-Coumaroyl-5-O-caffeoylquinic acid showed better affinity for α-amylase compared to acarbose and interacted significantly with several amino acid residues of the enzyme. Similarly, this molecule and 3,4-Dicaffeoylquinic acid demonstrated a strong affinity for α-glucosidase, suggesting their potential as natural inhibitors of enzymes involved in carbohydrate metabolism. Most of the compounds are not substrates of P-glycoprotein and exhibited high intestinal absorption. Furthermore, the majority of these compounds did not act as inhibitors or substrates of CYP450 enzymes, reinforcing their suitability for development as oral medications. These results underscore the potential of immature carob pulp as a promising antidiabetic agent. Full article

Chrysanthemum morifolium cv. Fubaiju (CMF) is regarded as one of the three most renowned varieties of white Chrysanthemum in China, and different extraction methods have significant effects on its composition and activities. Therefore, six extractions were used in this study to assess the effects on extracts. The basic chemical composition showed that hot water extract (Hw) had the highest total phenolic content, alkali water immersion-assisted hot water extract (Al) had the highest content of protein, and enzyme-assisted hot water extract (Enz) had the highest content of carbohydrate. The UPLC-Q-Exactive-MS results evinced the presence of 19 small-molecule compounds, including chlorogenic acid, caffeic acid, tuberonic acid glucoside, luteolin-7-O-rutinoside, and other substances. In addition, the antioxidant test found that the Hw exhibited the best 1,1-diphenyl-2-picrylhydrazyl (DPPH) (82.05 ± 1.59 mM TE/mg) and 2,2’-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) (61.91 ± 0.27 mM TE/mg) scavenging ability. The anti-glycation test demonstrated that Enz possessed the most pronounced inhibitory effect on glycation products, including fructosamine and advanced glycation end products (AGEs). Additionally, the Enz also exhibited the most significant inhibitory effect on the protein oxidation product N’-formylkynurenine. The correlation analysis revealed that there was a close relationship between antioxidant properties and glycation resistance of extracts, and tuberonic acid glucoside, 1,3-di-O-caffeoylquinic acid, 1,4-Dicaffeoylquinic acid, quercetin-7-O-β-D-glucopyranoside, and isochlorogenic acid B were key small molecule components that affected activities. In summary, the extracts of CMF can be regarded as an excellent antioxidant and anti-glycosylation agent. Full article

Oxidative stress exerts multiple disruptive effects on cellular morphology and function and is a major detriment to age-related and pathological neurodegenerative processes. The present study introduces an evaluative and comparative investigation of the antioxidant and cytoprotective properties of a Prenanthes purpurea extract and its major constituent 3,5-dicaffeoylquinic acid (DiCQA) in an in vitro model of H₂O₂-induced neurotoxicity. Using validated in vitro and in silico approaches, we established the presence and concentration dynamics of cellular protection in a 24 h pretreatment regimen with the natural products. The conducted cytotoxicity studies and the automated Chou–Talalay analysis for studying drug interactions demonstrated a strong antagonistic effect of the tested substances against oxidative stimuli in an “on demand” manner, prevailing at the higher end of the concentration range. These findings were further supported by the proteomic characterization of the treatment samples, accounting for a more distinct neuroprotection provided by the pure polyphenol 3,5-DiCQA. Full article

Chrysanthemum morifolium is a perennial herbaceous plant in the Asteraceae family that is used as a medicine and food owing to its superior pharmacological properties. Irrespective of its application, C. morifolium must be dried before use. Shade drying (YG) and heat drying (HG) are the two drying methods used in most origins. Given the abundance of flavonoids, phenolic acids, and terpenoids, the primary medicinal active constituents of C. morifolium, it is important to determine whether the composition and content of these compounds are altered during the drying processes. To test this, the changes in the chemical composition of C. morifolium flowers after YG and HG using full-spectrum, non-targeted LC/GC–MS−based metabolomics and, subsequently, the three indicator components of C. morifolium—chlorogenic acid, 3,5−dicaffeoylquinic acid, and luteolin−7−O−glucoside—were accurately quantified by HPLC. The results of the non-targeted metabolomics analysis revealed that YG- and HG-processed C. morifolium differed significantly with respect to chemical contents, especially flavonoids, phenolic acids, and terpenoids. The levels of the indicator components and their precursors also differed significantly between the YG and HG treatments. The contents of most of the flavonoids and key phenolic acids, terpenoids, and carbohydrates were higher with YG than with HG pre-treatment. These results revealed the changes in the chemical composition of C. morifolium during the YG and HG processes, thus providing a reference for the further optimization of the production and processing of chrysanthemums. Full article

This study aimed to investigate the leaves of six cultivars of Ipomoea batatas L. from the USA, focusing on their Total Polyphenol Content (TPC), Total Flavonoid Content (TFC), antioxidant, and antimicrobial activities. TPC and TFC ranged from 7.29 ± 0.62 to 10.49 ± 1.04 mg TAE/g Dw, and from 2.30 ± 0.04 to 4.26 ± 0.23 mg QE/g Dw, respectively, with the highest values found in the ‘O’Henry’ variety. RP-High-Performance Liquid Chromatography identified six phenolic and flavonoid compounds: caffeic acid, chlorogenic acid, 3,5-dicaffeoylquinic acid, 3,4-dicaffeoylquinic acid, and quercetin, excluding gallic acid. The highest levels of these compounds were found in acidified methanolic extracts. Antioxidant activities, measured by ABTS and DPPH assays, showed low IC₅₀ values ranging from 94.6 ± 2.76 to 115.17 ± 7.65 µg/mL, and from 88.83 ± 1.94 to 147.6 ± 1.22 µg/mL. Ferric Ion-Reducing Antioxidant Potential (FRAP) measurements indicated significant antioxidant levels, varying from 1.98 ± 0.14 to 2.83 ± 0.07, with the ‘O’Henry’ variety exhibiting the highest levels. The antimicrobial activity test included five Gram-positive bacteria, three Gram-negative bacteria, and two pathogenic fungi. S. aureus, S. mutans, L. monocytogenes, E. coli, S. dysenteriae, and C. albicans were most susceptible to the methanolic extract. This study underscores the impressive antioxidant and antimicrobial activities of sweet potato leaves, often discarded, making them a valuable source of natural antioxidants, antimicrobials, and other health-promoting compounds. Full article

Lonicerae japonicae Flos (LJF) is a natural plant containing abundant antioxidant ingredients. In order to extract more antioxidants from LJF, in this study, a novel strategy was proposed for optimizing the extraction factor level by response surface methodology with a tailored deep eutectic solvent (DES) as the extraction solvent and antioxidant ability as the evaluation index. After optimizing the composition of DES and the extraction condition, the extracts obtained by our proposed method yielded better antioxidant ability (229.1–249.1 μmol TE/g DW) and higher antioxidant contents (34.2–36.5 mg GAE/g DW for total phenolics and 119.6–123.0 mg RE/g DW for total flavonoids) from LJF in 5 min without organic solvent consumption that were significantly superior to the Chinese Pharmacopoeia extraction method. The K-T solvation parameter and a scanning electron microscope were adopted to explore the extraction mechanism, and the results showed that the polarity and damage effect on plant cells of DES were crucial for the extraction of antioxidants. In addition, after combining the HPLC fingerprint and partial least squares model, chlorogenic acid, rutin, and 3,5-O-Dicaffeoylquinic acid were screened as the antioxidant Q-markers of LJF. This work demonstrates that an optimization strategy based on antioxidant ability and tailored DES has the potential to extract more antioxidants from natural plants. Full article