RÉSUMÉ
BACKGROUND: cultivated and wild plants are used to treat different ailments. The Astragalus genus is found in temperate and dry climates; thus, it is found in Egypt and the arab world. Astragalus caprinus has a good amount of bioactive chemicals, which may help explain its therapeutic effects in reducing the risk of consequences from disease. METHOD: The phytochemical investigation of the herb and roots of Astragalus caprinus L. included the analytical characterization for the petroleum ether components by GC/MS, unsaponifiable matter (unsap. fraction), and fatty acids (FAME) investigation by GLC analysis. Main flavonoids were chromatographically isolated from ethyl acetate and n-butanol extracts. In vitro antimicrobial activity has been tested against the Gram-positive bacteria Staphylococcus aureus and Streptococcus mutans for different plant extracts, the Gram-negative bacteria Pseudomonas aeruginosa and Klebsiella pneumonia, the fungus Candida albicans and Aspergillus niger, and the Escherichia coli bacterium. Metabolite cytotoxicity was examined using the MTT assay against HepG-2 (human liver carcinoma) and MCF-7 (breast carcinoma). RESULTS: Identifying the important components of the herb and root petroleum ether extracts was achieved. Using column chromatography, luteolin, cosmosiin (apigenin-7-O-glucoside), and cynaroside (luteolin-7-O-glucoside) were separated and identified using UV, NMR, and Mass Spectroscopy. Root extracts displayed potential antimicrobial activity against most of the tested pathogens. Both extracts (herb and roots) were active against the MCF-7 cell line and HepG-2 cell line with IC50 62.5 ± 0.64 and 72.4 ± 2.3 µg/ml, and 75.9 ± 2.5 and 96.8 ± 4.2 µg/ml, respectively. CONCLUSION: Astragalus caprinus seems to be a promising source of bioactive compounds that could potentially aid in preventing disease complications and address common health issues in developing countries. Moreover, the various parts of this plant could be utilized as natural raw materials for producing health-boosting products that could address common health issues in developing countries.
Sujet(s)
Astragalus , Composés phytochimiques , Extraits de plantes , Extraits de plantes/pharmacologie , Extraits de plantes/composition chimique , Humains , Astragalus/composition chimique , Composés phytochimiques/pharmacologie , Composés phytochimiques/composition chimique , Tests de sensibilité microbienne , Cellules MCF-7 , Anti-infectieux/pharmacologie , Anti-infectieux/composition chimique , Racines de plante/composition chimique , Égypte , Cellules HepG2 , Flavonoïdes/pharmacologieRÉSUMÉ
This present study aimed to investigate the phytochemical content and antioxidant and antidiabetic activities of Curculigo latifolia leaves (CL) and C. latifolia roots (CR) found in Brunei Darussalam. Phytochemical screening showed that CL and CR extracts contain saponins, tannins, glycosides, and terpenoids. CR showed higher total phenolic content (TPC), but lower total flavonoid content (TFC) when compared to CL. The high TPC in CR contributed to its potent radical scavenging activity (RSA) against 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals and strong ferric reducing antioxidant power (FRAP). Additionally, CR exerted significant inhibition of â-glucosidase and â-amylase, suggesting a potential link between the chemical compounds and its antioxidant and antidiabetic effects. In the animal study of antihyperglycemic activity, treatment with 250 mg/kg body weight (b.w.) of the CL extract normalised the blood glucose levels and improved body weight gain of alloxan-induced diabetic rats within 14 weeks. Furthermore, our investigation into the wound-healing effects of young C. latifolia leaves (YCL) and matured C. latifolia leaves (MCL) showed a significant reduction in wound size on Day 3, 5, and 7 of the experimental study, indicating its wound-healing potential. Based on our findings, C. latifolia can be consumed as part of a balanced diet due to its antioxidant and antidiabetic properties.
Sujet(s)
Antioxydants , Curculigo , Diabète expérimental , Hypoglycémiants , Composés phytochimiques , Extraits de plantes , Cicatrisation de plaie , Animaux , Hypoglycémiants/pharmacologie , Hypoglycémiants/composition chimique , Antioxydants/pharmacologie , Antioxydants/composition chimique , Cicatrisation de plaie/effets des médicaments et des substances chimiques , Extraits de plantes/pharmacologie , Extraits de plantes/composition chimique , Curculigo/composition chimique , Rats , Composés phytochimiques/pharmacologie , Composés phytochimiques/composition chimique , Composés phytochimiques/analyse , Diabète expérimental/traitement médicamenteux , Mâle , Feuilles de plante/composition chimique , Flavonoïdes/pharmacologie , Flavonoïdes/composition chimique , Flavonoïdes/analyse , Phénols/analyse , Phénols/composition chimique , Glycémie/effets des médicaments et des substances chimiques , Glycémie/métabolisme , Rat WistarRÉSUMÉ
The purification of flavonoids using the macroporous polymer resin method has gained attention in recent years due to its simplicity, precision, cost-effectiveness, and the ability to separate flavonoids from other constituents. Several studies have been conducted to investigate the efficiency and effectiveness of macroporous polymer resin in purifying flavonoids from various plant sources. This review aims to evaluate the existing literature on macroporous polymer resin purification of flavonoids and provide a comprehensive analysis of the current research trends and advancements in this field. It also highlights the importance of optimizing the adsorption parameters and conditions such as resin type, resin concentration, pH, and temperature for efficient purification of flavonoids using macroporous polymer resin. The key findings of this review reveal that macroporous resins with weak polarity, large surface areas, and pore diameters have a stronger adsorption capacity for flavonoids compared to polar resins. Furthermore, ultrasonic-solvent assisted extraction often combines with macroporous resin for effective the extraction and purification of flavonoids.
Sujet(s)
Flavonoïdes , Plantes médicinales , Polymères , Résines synthétiques , Flavonoïdes/isolement et purification , Flavonoïdes/composition chimique , Polymères/composition chimique , Porosité , Plantes médicinales/composition chimique , Résines synthétiques/composition chimique , Adsorption , Propriétés de surfaceRÉSUMÉ
CONTEXT: The increase in bacterial resistance to currently available medications, which increases mortality rates, treatment costs is a global problem, and highlights the need for novel classes of antibacterial agents or new molecules that interact synergistically with antimicrobials. OBJECTIVE: The current work explores the potential synergistic effects of certain natural phenylpropanoids and flavonoids on ciprofloxacin (CIP), ampicillin (AMP), gentamicin (GEN), and tetracycline (TET). MATERIALS AND METHODS: The adjuvant role of cinnamic acid, p-coumaric acid, caffeic acid, ferulic acid, ferulic acid methyl ester, sinapic acid, apigenin, and luteolin was evaluated by determining the MIC (minimal inhibitory concentration) values of antibiotics in the presence of subinhibitory concentrations (200, 100, and/or 50 µM) of the compounds in Gram-positive and Gram-negative bacterial strains using a 2-fold broth microdilution method. The 96-well plates were incubated at 37 °C for 18 h, and dimethyl sulfoxide was used as a solvent control. RESULTS: The combination of luteolin with CIP, reduced the MIC values of the antibiotic from 0.625 to 0.3125 µM and to 0.078 µM in 100 and 200 µM concentration, respectively, in sensitive Staphylococcus aureus. Sinapic acid decreased the MIC value of CIP from 0.625 to 0.3125 µM in S. aureus, from 1.56 to 0.78 µM in Klebsiella pneumoniae, and the MIC of GEN from 0.39 to 0.095 µM in Pseudomonas aeruginosa strains. DISCUSSION AND CONCLUSIONS: These findings are useful in delaying the development of resistance, as the required antibacterial effect can be achieved with the use of lower concentrations of antibiotics.
Sujet(s)
Antibactériens , Synergie des médicaments , Flavonoïdes , Bactéries à Gram négatif , Bactéries à Gram positif , Tests de sensibilité microbienne , Antibactériens/pharmacologie , Bactéries à Gram négatif/effets des médicaments et des substances chimiques , Flavonoïdes/pharmacologie , Bactéries à Gram positif/effets des médicaments et des substances chimiques , Relation dose-effet des médicamentsRÉSUMÉ
BACKGROUND: Dorema aucheri gum (DAG) is a bitter flavonoid gum widely used for numerous medicinal purposes including wound recovery. The present work investigates the acute toxicity and wound-healing effects of DAG in excisional skin injury in rats. MATERIALS AND METHODS: Sprague Dawley rats (24) were clustered into four groups, each rat had a full-thickness excisional dorsal neck injury (2.00 cm) and addressed with 0.2 mL of the following treatments for 15 days: Group A (vehicle), rats addressed with normal saline; Group B, rats received intrasite gel; C and D, rats addressed with 250 and 500 mg/kg of DAG, respectively. RESULTS: The results revealed the absence of any toxic signs in rats who received oral dosages of 2 and 5 g/kg of DAG. Wound healing was significantly accelerated following DAG treatments indicated by smaller open areas and higher wound contraction percentages compared to vehicle rats. Histological evaluation revealed higher fibroblast formation, collagen deposition, and noticeably lower inflammatory cell infiltration in granulated skin tissues of DAG-addressed rats compared to vehicle rats. DAG treatment caused significant modulation of immunohistochemical proteins (decreased Bax and increased HSP 70) and inflammatory mediators (reduced TNF-α, IL-6, and magnified IL-10), which were significantly varied compared to vehicle rats. Moreover, topical DAG treatment led to significant upregulation of the hydroxyproline (HDX) (collagen) and antioxidant content. At the same time, decreased the lipid peroxidation (MDA) levels in healed tissues obtained from DAG-treated rats. CONCLUSION: The present wound contraction by DAG might be linked with the modulatory effect of its phytochemicals (polysaccharides, flavonoids, and phenolic) on the cellular mechanisms, which justify their folkloric use and provokes further investigation as therapeutic drug additives for wound contraction.
Sujet(s)
Flavonoïdes , Rat Sprague-Dawley , Peau , Cicatrisation de plaie , Protéine Bax , Animaux , Cicatrisation de plaie/effets des médicaments et des substances chimiques , Rats , Flavonoïdes/pharmacologie , Peau/effets des médicaments et des substances chimiques , Peau/traumatismes , Peau/anatomopathologie , Peau/métabolisme , Protéine Bax/métabolisme , Protéines du choc thermique HSP70/métabolisme , Hydroxyproline/métabolisme , Mâle , Gommes végétales/pharmacologieRÉSUMÉ
Diospyros lotus has been traditionally used in Asia for medicinal purposes, exhibiting a broad spectrum of pharmacological effects including antioxidant, neuroprotective and antiinflammatory properties. While the antiitch effect of D. lotus leaves has been reported, studies on the detailed mechanism of action in microglia and astrocytes, which are members of the central nervous system, have yet to be revealed. The present study aimed to investigate effects of D. lotus leaf extract (DLE) and its main component myricitrin (MC) on itchrelated cytokines and signaling pathways in lipopolysaccharide (LPS)stimulated microglia. The effect of DLE and MC on activation of astrocyte stimulated by microglia was also examined. Cytokine production was evaluated through reverse transcription PCR and western blot analysis. Signaling pathway was analyzed by performing western blotting and immunofluorescence staining. The effect of microglia on astrocytes activation was evaluated via western blotting for receptors, signaling molecules and itch mediators and confirmed through gene silencing using short interfering RNA. DLE and MC suppressed the production of itchrelated cytokine IL6 and IL31 in LPSstimulated microglia. These inhibitory effects were mediated through the blockade of NFκB, MAPK and JAK/STAT pathways. In astrocytes, stimulation by microglia promoted the expression of itchrelated molecules such as oncostatin M receptor, interleukin 31 receptor a, inositol 1,4,5trisphosphate receptor 1, lipocalin2 (LCN2), STAT3 and glial fibrillary acidic protein. However, DLE and MC significantly inhibited these receptors. Additionally, astrocytes stimulated by microglia with IL6, IL31, or both genes silenced did not show activation of LCN2 or STAT3. The findings of the present study demonstrated that DLE and MC could suppress pruritic activity in astrocytes induced by microgliaderived IL6 and IL31. This suggested the potential of DLE and MC as functional materials capable of alleviating pruritus.
Sujet(s)
Astrocytes , Diospyros , Flavonoïdes , Interleukine-6 , Microglie , Extraits de plantes , Feuilles de plante , Prurit , Astrocytes/effets des médicaments et des substances chimiques , Astrocytes/métabolisme , Microglie/effets des médicaments et des substances chimiques , Microglie/métabolisme , Extraits de plantes/pharmacologie , Extraits de plantes/composition chimique , Animaux , Flavonoïdes/pharmacologie , Flavonoïdes/composition chimique , Souris , Interleukine-6/métabolisme , Interleukine-6/génétique , Feuilles de plante/composition chimique , Prurit/traitement médicamenteux , Prurit/métabolisme , Diospyros/composition chimique , Lipopolysaccharides , Transduction du signal/effets des médicaments et des substances chimiques , Inflammation/métabolisme , Inflammation/traitement médicamenteux , InterleukinesRÉSUMÉ
Purpose: The present study aimed to develop a lipid nanoplatform, denoted as "BAL-PTX-LN", co-loaded with chiral baicalin derivatives (BAL) and paclitaxel (PTX) to promote the anti-lung cancer efficacy of paclitaxel and reduce the toxicity of chemotherapeutic drugs. Methods: BAL-PTX-LN was optimized through central composite design based on a single-factor experiments. BAL-PTX-LN was evaluated by TEM, particle size, encapsulation efficiency, hemolysis rate, release kinetics and stability. And was evaluated by pharmacokinetics and the antitumor efficacy studied both in vitro and in vivo. The in vivo safety profile of the formulation was assessed using hematoxylin and eosin (HE) staining. Results: BAL-PTX-LN exhibited spherical morphology with a particle size of 134.36 ± 3.18 nm, PDI of 0.24 ± 0.02, and with an encapsulation efficiency exceeding 90%, BAL-PTX-LN remained stable after 180 days storage. In vitro release studies revealed a zero-order kinetic model of PTX from the liposomal formulation. No hemolysis was observed in the preparation group. Pharmacokinetic analysis of PTX in the BAL-PTX-LN group revealed an approximately three-fold higher bioavailability and twice longer t1/2 compared to the bulk drug group. Furthermore, the IC50 of BAL-PTX-LN decreased by 2.35 times (13.48 µg/mL vs 31.722 µg/mL) and the apoptosis rate increased by 1.82 times (29.38% vs 16.13%) at 24 h compared to the PTX group. In tumor-bearing nude mice, the BAL-PTX-LN formulation exhibited a two-fold higher tumor inhibition rate compared to the PTX group (62.83% vs 29.95%), accompanied by a ten-fold decrease in Ki67 expression (4.26% vs 45.88%). Interestingly, HE staining revealed no pathological changes in tissues from the BAL-PTX-LN group, whereas tissues from the PTX group exhibited pathological changes and tumor cell infiltration. Conclusion: BAL-PTX-LN improves the therapeutic effect of poorly soluble chemotherapeutic drugs on lung cancer, which is anticipated to emerge as a viable therapeutic agent for lung cancer in clinical applications.
Sujet(s)
Tumeurs du poumon , Paclitaxel , Paclitaxel/composition chimique , Paclitaxel/pharmacocinétique , Paclitaxel/pharmacologie , Paclitaxel/administration et posologie , Animaux , Tumeurs du poumon/traitement médicamenteux , Tumeurs du poumon/anatomopathologie , Humains , Flavonoïdes/composition chimique , Flavonoïdes/pharmacologie , Flavonoïdes/pharmacocinétique , Flavonoïdes/administration et posologie , Taille de particule , Nanoparticules/composition chimique , Souris , Liposomes/composition chimique , Liposomes/pharmacocinétique , Cellules A549 , Lipides/composition chimique , Mâle , Souris de lignée BALB C , Lignée cellulaire tumorale , Libération de médicament , Antinéoplasiques d'origine végétale/pharmacologie , Antinéoplasiques d'origine végétale/administration et posologie , Antinéoplasiques d'origine végétale/composition chimique , Antinéoplasiques d'origine végétale/pharmacocinétique , Souris nude , Hémolyse/effets des médicaments et des substances chimiques , Antinéoplasiques/composition chimique , Antinéoplasiques/pharmacologie , Antinéoplasiques/pharmacocinétique , Antinéoplasiques/administration et posologieRÉSUMÉ
Ainsliaea fragrans Champ, a strong heat-clearing and detoxifying traditional Chinese medicine, has been effectively used for treating chronic cervicitis, endometritis, pelvic inflammatory diseases, and other conditions caused by damp heat. It shows a good effect in the treatment of cervicitis and has broad clinical application prospects. Nevertheless, there is no comprehensive study on its in vivo and in vitro chemical analysis. UHPLC-QTOF-MS/MS combined with the non-targeted characteristic filter analysis were used to conjecture and characterize the chemical components and in vivo metabolites of rats following oral administration of Ainsliaea fragrans Champ. In this study, A total of 85 compounds were identified in Ainsliaea fragrans Champ, including 29 flavonoids, 14 sesquiterpenoids, 25 chlorogenic acids, and 17 other compounds. In the plasma of rats after administration of Ainsliaea fragrans Champ, 160 compounds were deduced (19 prototype compounds and 141 metabolites). The 141 metabolites consist of 50 flavonoids, 80 phenolic acids and 11 Chlorogenic acids. The related metabolic pathways mainly involved demethylation, reduction, sulfonation, decarboxylation, hydroxylation, methylation, and glucuronide conjunction. In summary, the chemical components and metabolites of Ainsliaea fragrans Champ were comprehensively identified by using a rapid and accurate analysis method, which laid a foundation for dissecting its bioactive substances. In addition, it provides a scientific basis for the in-depth study of the material basis of Ainsliaea fragrans Champ efficacy and theoretical support for illustrating the mechanism of medical action and its clinical application.
Sujet(s)
Médicaments issus de plantes chinoises , Flavonoïdes , Rat Sprague-Dawley , Spectrométrie de masse en tandem , Animaux , Chromatographie en phase liquide à haute performance/méthodes , Spectrométrie de masse en tandem/méthodes , Rats , Médicaments issus de plantes chinoises/administration et posologie , Médicaments issus de plantes chinoises/métabolisme , Médicaments issus de plantes chinoises/composition chimique , Médicaments issus de plantes chinoises/pharmacocinétique , Administration par voie orale , Flavonoïdes/sang , Flavonoïdes/composition chimique , Femelle , Acide chlorogénique/sang , Acide chlorogénique/composition chimique , Acide chlorogénique/administration et posologie , Acide chlorogénique/métabolisme , Asteraceae/composition chimique , Hydroxybenzoates/sang , Hydroxybenzoates/analyse , Hydroxybenzoates/métabolismeRÉSUMÉ
The exclusion mechanism of food contaminants such as bisphenol A (BPA), Flavonoids (FLA), and Goitrin (GOI) onto the novel gallium-metal organic framework (MOF) and functionalized MOF with oxalamide group (MOF-OX) is evaluated by utilizing molecular dynamics (MD) and Metadynamics simulations. The atoms in molecules (AIM) analysis detected different types of atomic interactions between contaminant molecules and substrates. To assess this procedure, a range of descriptors including interaction energies, root mean square displacement, radial distribution function (RDF), density, hydrogen bond count (HB), and contact numbers are examined across the simulation trajectories. The most important elements in the stability of the systems under examination are found to be stacking π-π and HB interactions. It was confirmed by a significant value of total interaction energy for BPA/MOF-OX (- 338.21 kJ mol-1) and BPA/MOF (- 389.95 kJ mol-1) complexes. Evaluation of interaction energies reveals that L-J interaction plays an essential role in the adsorption of food contaminants on the substrates. The free energy values for the stability systems of BPA/MOF and BPA/MOF-OX complexes at their global minima reached about BPA/MOF = - 254.29 kJ mol-1 and BPA/MOF-OX = - 187.62 kJ mol-1, respectively. Nevertheless, this work provides a new strategy for the preparation of a new hierarchical tree-dimensional of the Ga-MOF hybrid material for the adsorption and exclusion of food contaminates and their effect on human health.
Sujet(s)
Contamination des aliments , Gallium , Réseaux organométalliques , Simulation de dynamique moléculaire , Réseaux organométalliques/composition chimique , Gallium/composition chimique , Contamination des aliments/analyse , Phénols/composition chimique , Phénols/analyse , Composés benzhydryliques/composition chimique , Composés benzhydryliques/analyse , Liaison hydrogène , Adsorption , Flavonoïdes/composition chimique , Flavonoïdes/analyseRÉSUMÉ
Flavin-dependent monooxygenases (FMOs) are a valuable group of biocatalysts that can regioselectively introduce a hydroxy group for the targeted modification of biologically active compounds. Here, we present the fdeE, the FMO from Herbaspirillum seropedicae SmR1 that is a part of the naringenin degradation pathway and is active towards a wide range of flavonoids-flavanones, flavones, isoflavones, and flavonols. Bioinformatics and biochemical analysis revealed a high similarity between the analyzed enzyme and other F8H FMOs what might indicate convergent evolutionary mechanism of flavonoid degradation pathway emergence by microorganism. A simple approach with the manipulation of the reaction environment allowed the stable formation of hydroxylation products, which showed very high reactivity in both in vivo and in vitro assays. This approach resulted in an 8-hydroxyquercetin-gossypetin titer of 0.16 g/L and additionally it is a first report of production of this compound.
Sujet(s)
Flavonols , Isoflavones , Isoflavones/métabolisme , Isoflavones/composition chimique , Isoflavones/biosynthèse , Flavonols/métabolisme , Flavonoïdes/métabolisme , Flavonoïdes/composition chimique , Flavonoïdes/biosynthèse , Hydroxylation , Spécificité du substratRÉSUMÉ
A novel 3D magnetic nanocomposite material based on covalent organic polymers was successfully synthesized and utilized as an efficient sorbent for magnetic solid-phase extraction. It exhibited a regular core-shell structure, large specific surface area, superior stability, and paramagnetism. To evaluate its extraction efficiency, six flavonoids were tested, demonstrating maximum adsorption capacities ranging from 90 to 218 mg/g. Additionally, the material exhibited remarkable reusability and mechanical stability, maintaining its original state over eight cycles with consistent recovery. An analytical strategy combining magnetic solid-phase extraction with high performance liquid chromatography and tandem mass spectrometry was developed for the determination of flavonoids in orange, honey, soybean, and Dioscorea bulbifera L. samples. The low limits of detection (0.01-0.1 ng/mL) and limits of quantification (0.05-0.5 ng/mL), as well as satisfactory recovery (80.4-114.8%), were obtained. The linear range started from the limits of quantification to 500 ng/mL with R2 ≥ 0.9929. These results suggest that the prepared adsorbent possesses excellent adsorption capabilities for flavonoids, highlighting its significant potential for detecting these compounds in complex sample matrices.
Sujet(s)
Flavonoïdes , Limite de détection , Nanocomposites , Polymères , Extraction en phase solide , Flavonoïdes/composition chimique , Flavonoïdes/isolement et purification , Adsorption , Nanocomposites/composition chimique , Extraction en phase solide/méthodes , Polymères/composition chimique , Chromatographie en phase liquide à haute performance , Spectrométrie de masse en tandem , Glycine max/composition chimique , Miel/analyse , Citrus sinensis/composition chimique , Nanoparticules de magnétite/composition chimiqueRÉSUMÉ
In consideration of several serious side effects induced by the classical AF-2 involved "lock" mechanism, recently disclosed PPARγ-Ser273 phosphorylation mode of action has become an alternative and mainstream mechanism for currently PPARγ-based drug discovery and development with an improved therapeutic index. In this study, by virtue of structure-based virtual high throughput screening (SB-VHTS), structurally chemical optimization by targeting the inhibition of the PPARγ-Ser273 phosphorylation as well as in vitro biological evaluation, which led to the final identification of a chrysin-based potential hit (YGT-31) as a novel selective PPARγ modulator with potent binding affinity and partial agonism. Further in vivo evaluation demonstrated that YGT-31 possessed potent glucose-lowering and relieved hepatic steatosis effects without involving the TZD-associated side effects. Mechanistically, YGT-31 presented such desired therapeutic index, mainly because it effectively inhibited the CDK5-mediated PPARγ-Ser273 phosphorylation, selectively elevated the level of insulin sensitivity-related Glut4 and adiponectin but decreased the expression of insulin-resistance-associated genes PTP1B and SOCS3 as well as inflammation-linked genes IL-6, IL-1ß and TNFα. Finally, the molecular docking study was also conducted to uncover an interesting hydrogen-bonding network of YGT-31 with PPARγ-Ser273 phosphorylation-related key residues Ser342 and Glu343, which not only gave a clear verification for our targeting modification but also provided a proof of concept for the abovementioned molecular mechanism.
Sujet(s)
Stéatose hépatique , Flavonoïdes , Récepteur PPAR gamma , Récepteur PPAR gamma/métabolisme , Récepteur PPAR gamma/agonistes , Flavonoïdes/pharmacologie , Flavonoïdes/composition chimique , Flavonoïdes/synthèse chimique , Relation structure-activité , Stéatose hépatique/traitement médicamenteux , Stéatose hépatique/métabolisme , Humains , Structure moléculaire , Diabète de type 2/traitement médicamenteux , Animaux , Hypoglycémiants/pharmacologie , Hypoglycémiants/composition chimique , Hypoglycémiants/synthèse chimique , Simulation de docking moléculaire , Relation dose-effet des médicaments , Souris , Mâle , Évaluation préclinique de médicamentRÉSUMÉ
Diabetes mellitus, characterized by dysregulated glucose metabolism, oxidative stress, and the formation of advanced glycation end products, poses a significant global health burden. In this study, we explored the potential of sorghum (Sorghum bicolor) seeds, known for their abundant phytochemical composition, as a natural remedy for diabetes and its associated damage. High-performance liquid chromatography/high-resolution mass spectrometry analysis revealed a remarkable phenolic richness in sorghum grains, including gallic acid, quercetin, and the predominant procyanidin B-1, with ecotype-specific variations in flavonoid distribution. Elemental analysis by ICP showed an abundance of macro-elements (Ca, K, Mg), trace elements (Fe, Mn, Si, Zn), and ultra-trace elements (B, Co, Cr, Cu, Mo, Se, V) essential for human health, supporting its therapeutic and nutritional potential. Additionally, the results demonstrated variable total phenolic contents (188-297 mg GAE/g dE) and total flavonoid contents (66-78 mg QE/g dE), with corresponding differences in antioxidant activities across the five ecotypes. Treatment with sorghum seed extract (SE1) significantly reduced oxidative stress markers, such as malondialdehyde (MDA)by 40% and hydrogen peroxide (H2O2) by 63%, in diabetic mice, compared to untreated diabetic controls. Moreover, sorghum extracts exhibited a remarkable increase in antioxidant enzyme activities, including a 50% increase in superoxide dismutase (SOD) activity and a 60% increase in glutathione peroxidase (GPx) activity, indicating their potential to bolster antioxidant defenses against diabetes-induced oxidative stress. These findings underscore the therapeutic potential of sorghum seeds in diabetes management and prevention, paving the way for the development of functional foods with enhanced health benefits.
Sujet(s)
Antioxydants , Stress oxydatif , Extraits de plantes , Graines , Sorghum , Sorghum/composition chimique , Stress oxydatif/effets des médicaments et des substances chimiques , Graines/composition chimique , Animaux , Souris , Extraits de plantes/pharmacologie , Extraits de plantes/composition chimique , Antioxydants/pharmacologie , Hyperglycémie/traitement médicamenteux , Hyperglycémie/métabolisme , Diabète expérimental/traitement médicamenteux , Diabète expérimental/métabolisme , Produits terminaux de glycation avancée/métabolisme , Flavonoïdes/pharmacologie , Mâle , Glycosylation/effets des médicaments et des substances chimiquesRÉSUMÉ
Previous studies have indicated that there may be differences among the varieties of lemon flavonoids, but the details have not yet been made clear, which limits the comprehensive use of different cultivated lemon varieties. In this study, ultra-performance liquid chromatography-quadrupole-time-of-flight-mass spectrometry (UPLC-Q-TOF-MS) and ultraviolet-visible spectroscopy (UV-Vis) were used to investigate the types and contents of flavonoids in the flesh of the main cultivated variety (Eureka) and five common lemon varieties, as well as their in vitro antioxidant activity. A total of 21 compounds were identified, five of which were common compounds. Among them, Verna, Lisbon, and Bearss each have characteristic components that can serve as potential criteria for variety identification. Each of the six varieties of lemon has strong antioxidant activity. The antioxidant activity of different lemon varieties is related to flavonoids. Therefore, Eureka and the other five varieties of lemon are good natural antioxidants, and the cultivation and industrial production of lemons should consider the needs and selection of suitable varieties.
Sujet(s)
Antioxydants , Citrus , Flavonoïdes , Flavonoïdes/analyse , Flavonoïdes/composition chimique , Antioxydants/composition chimique , Antioxydants/analyse , Citrus/composition chimique , Chromatographie en phase liquide à haute performance/méthodes , Extraits de plantes/composition chimique , Extraits de plantes/analyse , Spectrométrie de masse/méthodes , Fruit/composition chimiqueRÉSUMÉ
Citrus medica L. is a traditional citrus fruit that is rich in bioactive compounds and has the potential to be used as a natural source of food additives. This study aims to evaluate the antioxidant capacity and characterize the phenolic compounds present in the peels (including flavedo and albedo), pulp, and seeds of citron. The results showed that, compared to the other parts, the pulp had a substantially higher Antioxidant Activity Coefficient (AAC) of 168.2. The albedo and the seeds had significantly lower AAC values, while the green and yellow flavedo showed noteworthy results. O-coumaric acid was the predominant phenolic acid in all of the citron fractions; it was found in the highest concentration in albedo (37.54 µg/g FW). Flavanones and flavanols were the primary flavonoids in the pulp, peel, and seeds, with total flavonoid concentration ranging from ~9 µg/g FW in seeds to 508 µg/g FW in the pulp. This research offers significant insights into the antioxidant properties of this ancient fruit, emphasizing its potential applications as a natural source of antioxidants to be used in different applications.
Sujet(s)
Antioxydants , Citrus , Flavonoïdes , Fruit , Phénols , Extraits de plantes , Graines , Citrus/composition chimique , Antioxydants/composition chimique , Antioxydants/pharmacologie , Phénols/analyse , Phénols/composition chimique , Graines/composition chimique , Fruit/composition chimique , Flavonoïdes/analyse , Flavonoïdes/composition chimique , Extraits de plantes/composition chimiqueRÉSUMÉ
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.
Sujet(s)
Anti-inflammatoires , Eupatorium , Spectrométrie de masse en tandem , Eupatorium/composition chimique , Anti-inflammatoires/pharmacologie , Anti-inflammatoires/composition chimique , Chromatographie en phase liquide à haute performance/méthodes , Spectrométrie de masse en tandem/méthodes , Feuilles de plante/composition chimique , Animaux , Flavonoïdes/composition chimique , Flavonoïdes/pharmacologie , Flavonoïdes/analyse , Métabolome , Métabolomique/méthodes , Souris , Extraits de plantes/composition chimique , Extraits de plantes/pharmacologie , Cellules RAW 264.7 , Fleurs/composition chimique , Tiges de plante/composition chimique , Plantes médicinales/composition chimiqueRÉSUMÉ
Human DNA topoisomerase I (Topo I) is an essential enzyme in regulating DNA supercoiling during transcription and replication, and it is an important therapeutic target for anti-tumor agents. Bidens pilosa L. is a medicinal herb that is used as a folk medicine for cancers in China. A new flavonoid (1) and a new polyacetylene (20), along with eighteen flavonoids (2-19) and nine polyacetylenes (21-29), were isolated and identified from the methanol extract of the whole plant of B. pilosa, and some of the compounds (4, 5, 6 and 7) exhibited potent cytotoxicity against a panel of five human cancer cell lines. The DNA relaxation assay revealed that some flavonoids and polyacetylenes exerted inhibitory activities on human DNA Topo I, among them compounds 1, 2, 5, 6, 7, 8, 15, 19, 20, 22, and 24 were the most active ones, with IC50 values of 393.5, 328.98, 145.57, 239.27, 224.38, 189.84, 89.91, 47.5, 301.32, 178.03, and 218.27 µM, respectively. The structure-activity analysis of flavonoids was performed according to the results from the Topo I inhibition assay. The DNA content analysis revealed that 5, 6, and 7 potently arrested cell cycle at the G1/S and G2/M phases in human colon cancer cell DLD-1 depending on the concentration of the inhibitors. The levels of protein expression related to the G1/S and G2/M cell cycle checkpoints were in accordance with the results from the DNA content analysis. These findings suggest that flavonoids are one of the key active ingredients accounting for the anti-tumor effect of B. pilosa.
Sujet(s)
Bidens , ADN topoisomérases de type I , Flavonoïdes , Polyynes , Inhibiteurs de la topoisomérase-I , Humains , Flavonoïdes/pharmacologie , Flavonoïdes/composition chimique , Flavonoïdes/isolement et purification , Bidens/composition chimique , ADN topoisomérases de type I/métabolisme , Lignée cellulaire tumorale , Inhibiteurs de la topoisomérase-I/pharmacologie , Inhibiteurs de la topoisomérase-I/composition chimique , Inhibiteurs de la topoisomérase-I/isolement et purification , Polyynes/pharmacologie , Polyynes/composition chimique , Polyynes/isolement et purification , Extraits de plantes/pharmacologie , Extraits de plantes/composition chimique , Antinéoplasiques d'origine végétale/pharmacologie , Antinéoplasiques d'origine végétale/composition chimique , Antinéoplasiques d'origine végétale/isolement et purificationRÉSUMÉ
Fabiana punensis S. C. Arroyo is a subshrub or shrub that is indigenous to the arid and semiarid region of northern Argentina and is known to possess several medicinal properties. The objective of this study was to optimize the extraction conditions so as to maximize the yield of bioactive total phenolic compound (TPC) and flavonoids (F) of F. punensis' aerial parts by using non-conventional extraction methods, namely ultrasound-assisted extraction, UAE, and microwave-assisted extraction, MAE, and to compare the biological activities and toxicity of optimized extracts vs. conventional extracts, i.e., those gained by maceration. Response Surface Methodology (RSM) was used to apply factorial designs to optimize the parameters of extraction: solid-to-liquid ratio, extraction time, ultrasound amplitude, and microwave power. The experimental values for TPC and F and antioxidant activity under the optimal extraction conditions were not significantly different from the predicted values, demonstrating the accuracy of the mathematical models. Similar HPLC-DAD patterns were found between conventional and UAE- and MAE-optimized extracts. The main constituents of the extracts correspond to phenolic compounds (flavonoids and phenolic acids) and apigenin was identified. All extracts showed high scavenger capacity on ABTSâ¢+, O2â¢- and H2O2, enabling the inhibition of the pro-inflammatory enzymes xanthine oxidase (XO) and lipoxygenase (LOX). They also showed an antimutagenic effect in Salmonella Typhimurium assay and cytotoxic/anti-proliferative activity on human melanoma cells (SKMEL-28). Toxicological evaluation indicates its safety. The results of this work are important in the development of efficient and sustainable methods for obtaining bioactive compounds from F. punensis for the prevention of chronic degenerative diseases associated with oxidative stress, inflammation, and DNA damage.
Sujet(s)
Antioxydants , Micro-ondes , Phénols , Parties aériennes de plante , Extraits de plantes , Phénols/composition chimique , Phénols/pharmacologie , Phénols/isolement et purification , Extraits de plantes/pharmacologie , Extraits de plantes/composition chimique , Parties aériennes de plante/composition chimique , Antioxydants/pharmacologie , Antioxydants/composition chimique , Antioxydants/isolement et purification , Humains , Flavonoïdes/pharmacologie , Flavonoïdes/composition chimique , Flavonoïdes/isolement et purification , Chromatographie en phase liquide à haute performance , Ondes ultrasonores , Fractionnement chimique/méthodes , Xanthine oxidase/antagonistes et inhibiteurs , Xanthine oxidase/métabolismeRÉSUMÉ
The present study evaluated three green extraction methods, accelerated solvent extraction (ASE), ultrasound-assisted extraction (UAE), and laser irradiation extraction (LE), for the polyphenolic compounds and vitamin C extraction of Cornus mas L. and Crataegus monogyna fruit extracts. The polyphenols and vitamin C of extracts were quantified using HPLC-DAD, and the total phenolic content, flavonoid content, antioxidant activity (DPPH and reducing power), and antidiabetic activity were also studied. The antidiabetic activity was examined by the inhibition of α-amylase and α-glucosidase, and in vitro on a beta TC cell line (ß-TC-6). The results showed significant differentiation in the extraction yield between the methods used, with the ASE and LE presenting the highest values. The C. mas fruit extract obtained by ASE exhibited the best antioxidant activity, reaching an IC50 value of 31.82 ± 0.10 µg/mL in the DPPH assay and 33.95 ± 0.20 µg/mL in the reducing power assay. The C. mas fruit extracts obtained by ASE and LE also have the highest inhibitory activity on enzymes associated with metabolic disorders: α-amylase (IC50 = 0.44 ± 0.02 µg/mL for the extract obtained by ASE, and 0.11 ± 0.01 µg/mL for the extract obtained by LE at combined wavelengths of 1270 + 1550 nm) and α-glucosidase (IC50 of 77.1 ± 3.1 µg/mL for the extract obtained by ASE, and 98.2 ± 4.7 µg/mL for the extract obtained by LE at combined wavelengths of 1270 + 1550 nm). The evaluation of in vitro antidiabetic activity demonstrated that the treatment with C. mas and C. monogyna fruit extracts obtained using ASE stimulated the insulin secretion of ß-TC-6 cells, both under normal conditions and hyperglycemic conditions, as well. All results suggest that C. mas and C. monogyna fruit extracts are good sources of bioactive molecules with antioxidant and antidiabetic activity.
Sujet(s)
Antioxydants , Cornus , Crataegus , Fruit , Hypoglycémiants , Extraits de plantes , alpha-Amylases , Crataegus/composition chimique , Extraits de plantes/pharmacologie , Extraits de plantes/composition chimique , Antioxydants/pharmacologie , Antioxydants/composition chimique , Hypoglycémiants/pharmacologie , Hypoglycémiants/composition chimique , Cornus/composition chimique , Fruit/composition chimique , alpha-Amylases/antagonistes et inhibiteurs , alpha-Amylases/métabolisme , Inhibiteurs des glycoside hydrolases/pharmacologie , Inhibiteurs des glycoside hydrolases/composition chimique , Inhibiteurs des glycoside hydrolases/isolement et purification , Animaux , alpha-Glucosidase/métabolisme , Polyphénols/pharmacologie , Polyphénols/composition chimique , Lignée cellulaire , Flavonoïdes/pharmacologie , Flavonoïdes/composition chimique , Flavonoïdes/isolement et purification , Phénols/pharmacologie , Phénols/composition chimique , Chromatographie en phase liquide à haute performance , Acide ascorbique/pharmacologieRÉSUMÉ
Banana peels, comprising about 35% of the fruit's weight, are often discarded, posing environmental and economic issues. This research focuses on recycling banana peel waste by optimizing advanced extraction techniques, specifically microwave-assisted (MAE) and ultrasound-assisted extraction (UAE), for the isolation of phenolic compounds. A choline chloride-based deep eutectic solvent (DES) with glycerol in a 1:3 ratio with a water content of 30% (w/w) was compared to 30% ethanol. Parameters, including sample-to-solvent ratio (SSR), extraction time, and temperature for MAE or amplitude for UAE, were varied. Extracts were analyzed for hydroxycinnamic acid (HCA) and flavonoid content, and antioxidant activity using FRAP and ABTS assays. DES outperformed ethanol, with HCA content ranging from 180.80 to 765.92 mg/100 g and flavonoid content from 96.70 to 531.08 mg/100 g, accompanied by higher antioxidant activity. Optimal MAE conditions with DES were an SSR of 1:50, a temperature of 60 °C, and a time of 10 min, whereas an SSR of 1:60, time of 5 min, and 75% amplitude were optimal for UAE. The polyphenolic profile of optimized extracts comprised 19 individual compounds belonging to the class of flavonols, flavan-3-ols, and phenolic acids. This study concluded that DESs, with their superior extraction efficiency and environmental benefits, are promising solvents for the extraction of high-value bioactive compounds from banana peels and offer significant potential for the food and pharmaceutical industries.