RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Viral pneumonia is the leading cause of death after SARS-CoV-2 infection. Despite effective at early stage, long-term treatment with glucocorticoids can lead to a variety of adverse effects and limited benefits. The Chinese traditional herb Pogostemonis Herba is the aerial part of Pogostemon Cablin (Blanco) Benth., which has potent antiviral, antibacterial, anti-inflammatory, and anticancer effects. It was used widely for treating various throat and respiratory diseases, including COVID-19, viral infection, cough, allergic asthma, acute lung injury and lung cancer. AIM OF THE STUDY: To investigate the antiviral and anti-inflammatory effects of chemical compounds from Pogostemonis Herba in SARS-CoV-2-infected hACE2-overexpressing mouse macrophage RAW264.7 cells and hACE2 transgenic mice. MATERIALS AND METHODS: The hACE2-overexpressing RAW264.7 cells were exposed with SARS-CoV-2. The cell viability was detected by CCK8 assay and cell apoptotic rate was by flow cytometric assay. The expressions of macrophage M1 phenotype markers (TNF-α and IL-6) and M2 markers (IL-10 and Arg-1) as well as the viral loads were detected by qPCR. The mice were inoculated intranasally with SARS-CoV-2 omicron variant to induce viral pneumonia. The levels of macrophages, neutrophils, and T cells in the lung tissues of infected mice were analyzed by full spectrum flow cytometry. The expressions of key proteins were detected by Western blot assay. RESULTS: Diosmetin-7-O-ß-D-glucopyranoside (DG) presented the strongest anti-SARS-CoV-2 activity. Intervention with DG at the concentrations of 0.625-2.5 µM not only reduced the viral replication, cell apoptosis, and the productions of inflammatory cytokines (IL-6 and TNF-α) in SARS-CoV-2-infected RAW264.7 cells, but also reversed macrophage polarity from M1 to M2 phenotype. Furthermore, treatment with DG (25-100 mg/kg) alleviated acute lung injury, and reduced macrophage infiltration in SARS-COV-2-infected mice. Mechanistically, DG inhibited SARS-COV-2 gene expression and HK3 translation via targeting YTHDF1, resulting in the inactivation of glycolysis-mediated NF-κB pathway. CONCLUSIONS: DG exerted the potent antiviral and anti-inflammatory activities. It reduced pneumonia in SARS-COV-2-infected mice via inhibiting the viral replication and accelerating M2 macrophage polarization via targeting YTHDF1, indicating its potential for COVID-19 treatment.
Assuntos
Antivirais , Tratamento Farmacológico da COVID-19 , COVID-19 , Macrófagos , SARS-CoV-2 , Replicação Viral , Animais , Camundongos , Células RAW 264.7 , Replicação Viral/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Macrófagos/virologia , SARS-CoV-2/efeitos dos fármacos , Antivirais/farmacologia , Camundongos Transgênicos , Pogostemon/química , Citocinas/metabolismo , Apoptose/efeitos dos fármacos , Pulmão/efeitos dos fármacos , Pulmão/virologia , Pulmão/patologia , Glucosídeos/farmacologia , Glucosídeos/isolamento & purificação , Flavonoides/farmacologia , Flavonoides/isolamento & purificação , Flavonoides/uso terapêutico , Enzima de Conversão de Angiotensina 2/metabolismo , Anti-Inflamatórios/farmacologia , Masculino , Pneumonia Viral/tratamento farmacológico , Pneumonia Viral/virologia , HumanosRESUMO
Grape processing generates large amounts of by-products, including seeds rich in hydrophilic and lipophilic antioxidants. This study demonstrates, for the first time, that subjecting grape seeds to a single ultrasound-assisted extraction (UAE) with aqueous ethanolic solutions yields both flavan-3-ols and tocochromanols in the final extract. Notably, the water content in ethanol significantly influences the extractability of tocochromanols more than flavan-3-ols. Solid-to-solvent ratios of 1:50 to 1:2 were tested for both analytical and industrial applications. A sustainable analytical approach for recovering flavan-3-ols and tocochromanols using 60% and 96.4% ethanol extractions was validated and employed to profile nineteen genotypes of lesser-studied interspecific grape crosses (Vitis spp.). Different genotypes showed a wide range of concentrations of tocopherols (1.6-6.3 mg/100 g), tocotrienols (1.0-17.4 mg/100 g), and flavan-3-ols (861-9994 mg/100 g). This indicated that the genetic background and maturity of the plant material are crucial factors from an industrial perspective due to the initial concentration of bioactive compounds. Finally, the study also discussed the fundamental aspects of hydrophobic antioxidant extractability from the lipid matrix with aqueous ethanol solutions and the limitations of the workflow, such as the non-extractable tocochromanols and their esters and the losses of these lipophilic antioxidants during extraction.
Assuntos
Flavonoides , Sementes , Vitis , Vitis/química , Sementes/química , Flavonoides/isolamento & purificação , Flavonoides/química , Flavonoides/análise , Antioxidantes/química , Antioxidantes/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Tocoferóis/isolamento & purificação , Tocoferóis/química , Tocoferóis/análise , Tocotrienóis/análise , Tocotrienóis/isolamento & purificação , Tocotrienóis/químicaRESUMO
The extraction of bioactive compounds is based on the application of various extraction techniques. Therefore, the stem and root bark of the plant species Morinda lucida L. were used in this research, while the extraction procedure was performed using three extraction techniques: HAE (homogenizer extraction), UAE (ultrasound extraction) as modern, and MAC (maceration) as conventional extraction technique. The presence of different classes of secondary metabolites was determined using the UHPLC method, while the content of total phenols and flavonoids was determined spectrophotometrically. The biological potential was investigated by in vitro antioxidant and enzyme assays. Different extraction technologies showed significant differences in only two classes of phenols, namely lignans and phenolic acids, which were significantly higher in HAE than in UAE and MAC. These findings highlight the significant effect of stem and bark extracts of M. lucida, opening the way for innovative industrial exploitation of these matrices.
Assuntos
Antioxidantes , Morinda , Fenóis , Extratos Vegetais , Morinda/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Fenóis/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Cromatografia Líquida de Alta Pressão , Flavonoides/química , Flavonoides/isolamento & purificação , Casca de Planta/química , Fracionamento Químico/métodos , Caules de Planta/química , Raízes de Plantas/químicaRESUMO
AIM: The aim of the present investigation is to study HPLC process to evaluate Some Active Flavonoids in Ethyl Acetate Extract of Leaves of Butea monosperma Linn. MATERIAL AND METHODS: Using a soxhlation device, the leaves of Butea monosperma Linn. were extracted in stages. Each powdered batch (500g) was extracted in stages with polarity-graded solvents such as petroleum ether (Pet. Et) (60-80º), chloroform (CHCl3), ethyl acetate (EtOAc) using a soxhlet extractor. Alkaloids, flavonoids, glycosides, tannins, phenols, and steroids, among other chemical families of components, were identified through qualitative phytochemical screenings of each extract. To make a 10 g/ml stock, standard phenolic markers like quercetin, rutin, catechin, gallic acid, and chlorogenic acid were dissolved in methanol. Phytoconstituents were separated and identified from extracts using various solvents and combinations of solvents, which were chosen after consulting the literature. RESULTS AND DISCUSSION: Preliminary phytochemical screening showed the revealed that the leaves contain steroid, triterpenoids, fatty acid and alkaloids. While the ethyl acetate extract found to contain therapeutically important phytoconstitutes such as steroids, triterpenoids, saponins, flavonoids, and tannins. Bioactive extracts of Butea monosperma were found to include flavonoids and phenolic substances. In ethyl acetate extract, various flavonoids and phenolic compounds were discovered. CONCLUSION: This is a preliminary report on the identification of phytochemical and HPLC evaluation of ethyl acetate extract of leaves of Butea monosperma Linn. and to unravel the mechanisms driving bioactive qualities and the existence of putative synergy among these substances, more research is needed on the isolation and characterization of individual Flavonoids or phenolic compounds.
Assuntos
Acetatos , Flavonoides , Extratos Vegetais , Folhas de Planta , Flavonoides/análise , Flavonoides/química , Flavonoides/isolamento & purificação , Folhas de Planta/química , Cromatografia Líquida de Alta Pressão/métodos , Extratos Vegetais/química , Acetatos/química , Solventes/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/isolamento & purificação , Taninos/análise , Taninos/isolamento & purificação , Taninos/químicaRESUMO
Diabetes mellitus is a metabolic disorder. Synthetic antidiabetics are the commonly used treatment options associated with complications. The objective of this study was to explore the antioxidative and antidiabetic potential of Euphorbia helioscopia whole plant ethanolic extract using in vitro and in vivo models. For that purpose, the antioxidative potential was explored by using 2,2-diphenyl-1-picrylhydrazyl analysis. In vitro antidiabetic potential of the extract was evaluated using amylase inhibitory analysis. In vivo antidiabetic activity of the extract was assessed in diabetic rats using streptozotocin/nicotinamide (60 mg/kg/120 mg/kg) as an inducing agent. Metformin was used as standard. The results indicated the presence of significant quantities of phenolic 82.18 ± 1.28 mgg-1 gallic acid equivalent (GAE) and flavonoid 66.55±1.22 mgg-1 quercetin equivalent (QE) contents in the extract. Quantitation of phytoconstituents exhibited the presence of sinapic acid, myricetin, and quercetin using HPLC analysis. The extract inhibited α-amylase by 84.71%, and an antiglycemic potential of 50.34% was assessed in the OGTT assay. Biochemical analysis demonstrated a reduction in urea, creatinine, cholesterol, low-density lipoprotein, and alkaline phosphatase (p < 0.001) as compared to diabetic control rats at the dose of 500 mg/kg. An upregulation in the expressions of glucokinase, glucose transporter 4, peroxisome proliferator-activated receptor γ, and insulin-like growth factor was observed in treated rats in contrast to G6P expression, which was downregulated upon treatment. In conclusion, this study provided evidence of the antioxidative and antidiabetic potential of E. helioscopia whole plant ethanolic extract through in vitro and in vivo analysis and emphasized its promising role as a natural alternative.
Assuntos
Antioxidantes , Glicemia , Diabetes Mellitus Experimental , Euphorbia , Glucoquinase , Transportador de Glucose Tipo 4 , Hipoglicemiantes , Extratos Vegetais , Animais , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Extratos Vegetais/farmacologia , Euphorbia/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Hipoglicemiantes/isolamento & purificação , Masculino , Ratos , Glucoquinase/metabolismo , Transportador de Glucose Tipo 4/metabolismo , Antioxidantes/farmacologia , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Glucose-6-Fosfatase/metabolismo , Ratos Wistar , Folhas de Planta/química , Estreptozocina , Etanol/química , Flavonoides/farmacologia , Flavonoides/isolamento & purificaçãoRESUMO
Three new dihydroflavonols, gloverinols A-C (1-3), a new flavon-3-ol, gloverinol D (4), two new isoflavans, gloveriflavan A (5) and B (6), and seven known compounds were isolated from the root bark of Dalbergia gloveri. The structures of the isolates were elucidated by using NMR, ECD, and HRESIMS data analyses. Among the isolated compounds, gloverinol B (2), gloveriflavan B (6), and 1-(2,4-dihydroxyphenyl)-3-hydroxy-3-(4-hydroxyphenyl)-1-propanone (10) were the most active against Staphylococcus aureus, with MIC values of 9.2, 18.4, and 14.2 µM, respectively.
Assuntos
Dalbergia , Testes de Sensibilidade Microbiana , Casca de Planta , Raízes de Plantas , Staphylococcus aureus , Casca de Planta/química , Raízes de Plantas/química , Estrutura Molecular , Staphylococcus aureus/efeitos dos fármacos , Dalbergia/química , Antibacterianos/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Flavonoides/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Isoflavonas/farmacologia , Isoflavonas/química , Isoflavonas/isolamento & purificaçãoRESUMO
This study aimed to enrich ï¬avonoids from Euphorbia hirta L. (E. hirta) extracts, and the enrichment parameters were optimized by adsorption and desorption tests. The HPD-300 resin was chosen after a comparison of the flavonoids from E. hir15ta's adsorption and desorption capabilities on nine different types of macro porous resin. The optimal enrichment for purification of E. hirta extracts were determined as sample concentration of 3.0mg/mL, pH of 2.0 and a desorption solvent of 50% ethanol. The optimal dynamic parameters were loading 2.5 BV of sample at a feeding flow rate of 2 BV/h, cleaning the column with 5 BV of water and then eluting 50.0% ethanol at a 2 BV/h elution flow rate using 5 BV of eluent. Following a single treatment cycle with HPD-300 resin, the product's total flavonoid content rose from 6.32% to 28.8%, with an 80.01% recovery yield. Then, 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-Azinobis-(3-ethylbenzthiazoline-6-sulphonate) (ABTS) and hydroxyl radical scavenging ability were used to evaluate the antioxidant properties of the purified flavonoids. The main chemical components of purified flavonoids from E. hirta are astragalin, quercetin-3ß-D-glucoside, 9,16-dioxo-10,12,14-octadeca-trienoic acid and gallic acid. The results showed that purified ï¬avonoids from E. hirta had a strong antioxidant effect, which indicated that it represented a valuable natural antioxidant source.
Assuntos
Antioxidantes , Euphorbia , Flavonoides , Extratos Vegetais , Euphorbia/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Flavonoides/química , Antioxidantes/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/isolamento & purificação , Adsorção , Picratos/química , Compostos de Bifenilo/químicaRESUMO
This study was conducted to determine and compare the phenolic compounds, glucosinolate contents and antidiabetic effects of the extracts obtained by ultrasonic and conventional extraction method of the leaves and flowers of the Crambe tataria. The highest antioxidant activity (12.95 mg/mL IC50 value) and total phenolic content (1313.57 mg GAE/100 g fw) were detected in the ultrasonic flower extract. In total flavonoid results, extracts obtained from the flower part of C. tataria had higher values than that of extracts obtained from the leaf part. The most abundant phenolic component in the flower extract was catechin. The highest catechin content in all samples was detected in the ultrasonic flower extract with a value of 374.37 mg/kg. Rutin was the dominant phenolic component in the leaf extract. Rutin values were 654.38 mg/kg and 757.30 mg/kg for conventional and ultrasonic extraction, respectively. In glucosinolate analysis, the highest glucoraphanin content was obtained in flower samples and by conventional extraction method (3466.84 mg/kg). The highest contents of sinigrin (689.97 mg/kg), glucotropaeolin (420.89 mg/kg), glucoerucin (357.27 mg/kg), glucoraphasatin (181.11 mg/kg) and gluconasturtin (66.07 mg/kg) were detected in ultrasonic flower extracts. The highest α-amylase and α-glucosidase enzyme inhibition effects belonged to the ultrasonic flower extract with values of 3.70 mg/mL and 4.89 mg/mL, respectively. As a result, this study determined for the first time that ultrasonic extraction of C. tataria flowers has much higher bioactive components and antidiabetic effects, revealing the potential use of this plant in the fields of medicine, pharmacology and chemistry.
Assuntos
Antioxidantes , Flores , Glucosinolatos , Hipoglicemiantes , Extratos Vegetais , Folhas de Planta , Glucosinolatos/isolamento & purificação , Glucosinolatos/análise , Flores/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Hipoglicemiantes/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Antioxidantes/análise , Fenóis/análise , Fenóis/isolamento & purificação , Fenóis/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Flavonoides/análise , Flavonoides/isolamento & purificação , UltrassomRESUMO
The subcritical water extraction of Undaria pinnatifida (blade, sporophyll, and root) was evaluated to determine its chemical properties and biological activities. The extraction was conducted at 180 °C and 3 MPa. Root extracts exhibited the highest phenolic content (43.32 ± 0.19 mg phloroglucinol/g) and flavonoid content (31.54 ± 1.63 mg quercetin/g). Sporophyll extracts had the highest total sugar, reducing sugar, and protein content, with 97.35 ± 4.23 mg glucose/g, 56.44 ± 3.10 mg glucose/g, and 84.93 ± 2.82 mg bovine serum albumin (BSA)/g, respectively. The sporophyll contained the highest fucose (41.99%) and mannose (10.37%), whereas the blade had the highest galactose (48.57%) and glucose (17.27%) content. Sporophyll had the highest sulfate content (7.76%). Key compounds included sorbitol, glycerol, L-fucose, and palmitic acid. Root extracts contained the highest antioxidant activity, with IC50 values of 1.51 mg/mL (DPPH), 3.31 mg/mL (ABTS+), and 2.23 mg/mL (FRAP). The root extract exhibited significant α-glucosidase inhibitory activity with an IC50 of 5.07 mg/mL, indicating strong antidiabetic potential. The blade extract showed notable antihypertensive activity with an IC50 of 0.62 mg/mL. Hence, subcritical water extraction to obtain bioactive compounds from U. pinnatifida, supporting their use in functional foods, cosmetics, and pharmaceuticals is highlighted. This study uniquely demonstrates the variation in bioactive compound composition and bioactivities across different parts of U. pinnatifida, providing deeper insights. Significant correlations between chemical properties and biological activities emphasize the use of U. pinnatifida extracts for chronic conditions.
Assuntos
Antioxidantes , Extratos Vegetais , Undaria , Antioxidantes/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/química , Undaria/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Água/química , Raízes de Plantas/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Flavonoides/química , Anti-Hipertensivos/farmacologia , Anti-Hipertensivos/isolamento & purificação , Anti-Hipertensivos/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Fenóis/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Algas ComestíveisRESUMO
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.
Assuntos
Flavonoides , Limite de Detecção , Nanocompostos , Polímeros , Extração em Fase Sólida , Flavonoides/química , Flavonoides/isolamento & purificação , Adsorção , Nanocompostos/química , Extração em Fase Sólida/métodos , Polímeros/química , Cromatografia Líquida de Alta Pressão , Espectrometria de Massas em Tandem , Glycine max/química , Mel/análise , Citrus sinensis/química , Nanopartículas de Magnetita/químicaRESUMO
The fruits of Alpinia oxyphylla (Alpiniae Oxyphyllae Fructus, AOF) are one of the "Four Famous South Medicines" in China. In this study, beta-site amyloid protein precursor cleaving enzyme 1 (BACE1) was applied to explore the active components in AOF responsible for type 2 diabetes mellitus (T2DM)-related cognitive disorder. As a result, 24 compounds including three unreported ones (1, 3, 4) were isolated from AOF. Compound 1 is an unusual carboncarbon linked diarylheptanoid dimer, and compound 4 is the first case of 3,4-seco-eudesmane sesquiterpenoid with a 5/6-bicyclic skeleton. Four diarylheptanoids (3, 5-7), one flavonoid (9) and two sesquiterpenoids (14 and 20) showed BACE1 inhibitory activity, of which the most active 6 was revealed to be a non-competitive and anti-competitive mixed inhibitor. Docking simulation suggested that OH-4' of 6 played important roles in maintaining activity by forming hydrogen bonds with Ser36 and Ile126 residues. Compounds 3, 5, 9 and 20 displayed neuroprotective effects against amyloid ß (Aß)-induced damage in BV2 cells. Mechanism study revealed that compounds 5 and 20 downregulated the expression of BACE1 and upregulated the expression of Lamp2 to exert effects. Thus, the characteristic diarylheptanoids and sesquiterpenoids in AOF had the efficacy to alleviate T2DM-related cognitive disorder by inhibiting BACE1 activity and reversing Aß-induced neuronal damage.
Assuntos
Alpinia , Secretases da Proteína Precursora do Amiloide , Ácido Aspártico Endopeptidases , Diabetes Mellitus Tipo 2 , Frutas , Sesquiterpenos , Alpinia/química , Ácido Aspártico Endopeptidases/antagonistas & inibidores , Ácido Aspártico Endopeptidases/metabolismo , Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores , Frutas/química , Estrutura Molecular , Diabetes Mellitus Tipo 2/tratamento farmacológico , Sesquiterpenos/farmacologia , Sesquiterpenos/isolamento & purificação , Simulação de Acoplamento Molecular , Diarileptanoides/farmacologia , Diarileptanoides/isolamento & purificação , Diarileptanoides/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Humanos , Animais , China , Flavonoides/farmacologia , Flavonoides/isolamento & purificação , Flavonoides/química , Transtornos Cognitivos/tratamento farmacológico , Camundongos , Extratos VegetaisRESUMO
BACKGROUND: The traditional Chinese medicine Tetrastigma Hemsleyanum (TH) is employed in treating respiratory diseases; however, the aerial parts by which its total flavonoids alleviate acute lung injury (ALI) are still unknown. This study investigated the protective effect and mechanism of Tetrastigma Hemsleyanum flavonoids (THF) in lipopolysaccharide (LPS)-induced ALI in mice. METHODS: Firstly, the total flavonoids from the above-ground part of TH were extracted. Subsequently, the composition of THF was analyzed using LC-MS. In vivo, the impact of THF on ALI mice was assessed through lung histopathology and the evaluation of various inflammatory factors' expression in mice. After treating RAW264.7 cells with THF in vitro, changes in inflammatory markers were examined upon LPS stimulation, and mRNA expression levels of inflammatory factors were detected using RT-qPCR. Finally, Western blot analysis was performed to determine TLR4/NF-κB pathway-associated proteins expression. RESULTS: In summary, a total of 24 flavonoids have been identified in THF. In vivo and vitro results show that THF effectively reduces the damage caused by LPS inflammation by blocking the expression and release of inflammatory factors. THF alleviates inflammatory injury by modulating the TLR4/NF-KB pathway. CONCLUSION: The results suggest that flavonoids exhibit a potent anti-inflammatory effect and effectively mitigate LPS-induced injury both in vivo and in vitro. We suggested that these flavonoids exert their therapeutic effects by modulating the TLR4/NF-KB pathway. In conclusion, the development of THF is anticipated to represent a promising new pharmaceutical for treatingALI.
Assuntos
Lesão Pulmonar Aguda , Flavonoides , Lipopolissacarídeos , Componentes Aéreos da Planta , Transdução de Sinais , Vitaceae , Animais , Masculino , Camundongos , Lesão Pulmonar Aguda/induzido quimicamente , Lesão Pulmonar Aguda/tratamento farmacológico , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/isolamento & purificação , China , Flavonoides/farmacologia , Flavonoides/isolamento & purificação , Estrutura Molecular , NF-kappa B/metabolismo , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Componentes Aéreos da Planta/química , Células RAW 264.7 , Transdução de Sinais/efeitos dos fármacos , Receptor 4 Toll-Like/metabolismo , Vitaceae/químicaRESUMO
Intestinal inflammation is one of the main health challenges affecting the quality of life of millions of people worldwide. Accumulating evidence introduces several flavonoids with multifaceted therapeutic properties in inflammatory diseases including intestinal inflammation. Herein, we examined potential anti-inflammatory properties of 5,4'-dihydroxy-6,8-dimethoxy7-O-rhamnosylflavone (DDR) flavone derived from Indigofera aspalathoides Vahl (I. aspalathoides Vahl) on lipopolysaccharide (LPS)-induced intestinal inflammation and injury in mice. Oral DDR treatment decreased serum levels of pro-inflammatory cytokines including TNF-α, IL-6, and IL-1ß. It reduced oxidative stress through augmenting the activities of catalase (CAT) and superoxide dismutase (SOD) and reducing the level of malondialdehyde (MDA) in the duodenum and colon tissues. Moreover, DDR enhanced the activities of digestive enzymes including trypsin, pancreatic lipase, and amylase, and increased the production of short-chain fatty acids (SCFAs) by colon microbiota. Histopathological investigation of duodenum and colon revealed that DDR inhibited inflammatory infiltration and largely restored mucosal architecture and protected lining integrity. Importantly, DDR suppressed activation of nuclear factor-κB (NF-κB) signaling pathway through reduced expression of Toll-like receptor 4 (TLR4) and expression and phosphorylation of P65. The current study identified DDR as anti-inflammatory flavonoid capable of ameliorating LPS-induced intestinal inflammation through suppression of NF-κB signaling.
Assuntos
Anti-Inflamatórios , Indigofera , Lipopolissacarídeos , Estresse Oxidativo , Animais , Camundongos , Masculino , Anti-Inflamatórios/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Indigofera/química , NF-kappa B/metabolismo , Flavonas/farmacologia , Citocinas/metabolismo , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Intestinos/efeitos dos fármacos , Receptor 4 Toll-Like/metabolismo , Flavonoides/farmacologia , Flavonoides/isolamento & purificaçãoRESUMO
Fridericia chica is an Amazonian plant used to treat stomach disorders. However, the pharmacological activity of flavonoids in the extract has yet to be investigated. Therefore, we considered that a flavonoid-rich F. chica subfraction (FRS) has gastroprotective functions. For this, before the induction of gastric ulcers with ethanol or piroxicam, the rats received vehicle (water), omeprazole (30 mg/kg), or FRS (30 mg/kg), and the ulcer area was measured macro and microscopically, and the antisecretory action was investigated in pylorus-ligated rats. In addition, the roles of nitric oxide (NO) and nonprotein sulfhydryl compounds (NP-SH) in the gastroprotective effects of FRS were studied. FRS reduced ethanol- and piroxicam-induced ulcerations by 81% and 77%, respectively, as confirmed histologically. Antioxidant effects were observed for FRS through the maintenance of GSH and LPO levels, and the SOD and CAT activity similar to those found in the nonulcerated group. Moreover, FRS avoided the increase in MPO activity and TNF, IL-6, IL-4 and IL-10 levels. Moreover, mucin staining increased in ulcerated rats receiving FRS, and the pharmacological mechanism gastroprotective seems to involve the NO and NP-SH in addition to antisecretory actions. The chemical study by mass spectrometry confirmed the presence of flavonoids in FRS, and molecular docking studies have shown that these compounds interact with cyclooxygenase-1 and NO synthase. Furthermore, there was no indication that FRS had cytotoxic effects. Our results support the popular use of F. chica, and we conclude that the gastroprotection effect promoted by FRS can be attributed to the combined effect of the flavonoids.
Assuntos
Antiulcerosos , Antioxidantes , Flavonoides , Extratos Vegetais , Plantas Medicinais , Ratos Wistar , Úlcera Gástrica , Animais , Flavonoides/farmacologia , Flavonoides/isolamento & purificação , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/prevenção & controle , Ratos , Extratos Vegetais/farmacologia , Masculino , Antiulcerosos/farmacologia , Antiulcerosos/isolamento & purificação , Plantas Medicinais/química , Antioxidantes/farmacologia , Óxido Nítrico/metabolismo , Fabaceae/química , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Simulação de Acoplamento MolecularRESUMO
Sophora flavescens, a traditional Chinese herb, produces a wide range of secondary metabolites with a broad spectrum of biological activities. In this study, we isolated six isopentenyl flavonoids (1-6) from the roots of S. flavescens and evaluated their activities against phytopathogenic fungi. In vitro activities showed that kurarinone and sophoraflavanone G displayed broad spectrum and superior activities, among which sophoraflavanone G displayed excellent activity against tested fungi, with EC50 values ranging from 4.76 to 13.94 µg/mL. Notably, kurarinone was easily purified and showed potential activity against Rhizoctonia solani, Botrytis cinerea, and Fusarium graminearum with EC50 values of 16.12, 16.55, and 16.99 µg/mL, respectively. Consequently, we initially investigated the mechanism of kurarinone against B. cinerea. It was found that kurarinone disrupted cell wall components, impaired cell membrane integrity, increased cell membrane permeability, and affected cellular energy metabolism, thereby exerting its effect against B. cinerea. Therefore, kurarinone is expected to be a potential candidate for the development of plant fungicides.
Assuntos
Botrytis , Flavonoides , Fungicidas Industriais , Fusarium , Doenças das Plantas , Raízes de Plantas , Rhizoctonia , Sophora , Botrytis/efeitos dos fármacos , Botrytis/crescimento & desenvolvimento , Sophora/química , Flavonoides/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Fusarium/efeitos dos fármacos , Fungicidas Industriais/farmacologia , Fungicidas Industriais/química , Raízes de Plantas/química , Doenças das Plantas/microbiologia , Rhizoctonia/efeitos dos fármacos , Rhizoctonia/crescimento & desenvolvimento , Prenilação , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Sophora flavescensRESUMO
In this study, it is the first that the Viticis Fructus (VF) was used as the raw material for extracting total flavonoids using the ultrasound-assisted enzyme extraction (UAE) method. Response surface methodology was employed to determine the optimal extraction parameters. The optimal conditions were as follows: 60 % ethanol solution as the extract solvent, material-liquid ratio of 1:25, pH value of 4, enzyme addition amount of 1.5 %, enzymatic hydrolysis time of 30 min, enzymatic hydrolysis temperature of 40 â, and ultrasonic time of 50 min. Comparing the total flavonoid yield of VF and processed VF (PVF) extracted using different methods, it was observed that UAE resulted in a higher total flavonoid yield compared to traditional ultrasound extraction and enzyme extraction. Additionally, the total flavonoid yield of PVF extracted by all three methods was generally higher than that of VF. The PVF solution extracted by UAE also demonstrated better in vitro antioxidant activity compared to VF. These results suggest that UAE is an effective method to enhance the activity of natural total flavonoids. The study of the physicochemical properties and in vitro antioxidant activity of VF and PVF showed that the total flavonoid yield and antioxidant activity significantly increased after VF stir-frying, indicating that their efficacy can also be enhanced.
Assuntos
Antioxidantes , Fracionamento Químico , Flavonoides , Ondas Ultrassônicas , Flavonoides/isolamento & purificação , Flavonoides/química , Antioxidantes/isolamento & purificação , Antioxidantes/química , Antioxidantes/farmacologia , Fracionamento Químico/métodos , Hidrólise , Temperatura , Enzimas/metabolismo , Concentração de Íons de Hidrogênio , Frutas/químicaRESUMO
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.
Assuntos
Bidens , DNA Topoisomerases Tipo I , Flavonoides , Poli-Inos , Inibidores da Topoisomerase I , Humanos , Flavonoides/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Bidens/química , DNA Topoisomerases Tipo I/metabolismo , Linhagem Celular Tumoral , Inibidores da Topoisomerase I/farmacologia , Inibidores da Topoisomerase I/química , Inibidores da Topoisomerase I/isolamento & purificação , Poli-Inos/farmacologia , Poli-Inos/química , Poli-Inos/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificaçãoRESUMO
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.
Assuntos
Antioxidantes , Micro-Ondas , Fenóis , Componentes Aéreos da Planta , Extratos Vegetais , Fenóis/química , Fenóis/farmacologia , Fenóis/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Componentes Aéreos da Planta/química , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Humanos , Flavonoides/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Ondas Ultrassônicas , Fracionamento Químico/métodos , Xantina Oxidase/antagonistas & inibidores , Xantina Oxidase/metabolismoRESUMO
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.
Assuntos
Antioxidantes , Cornus , Crataegus , Frutas , Hipoglicemiantes , Extratos Vegetais , alfa-Amilases , Crataegus/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antioxidantes/farmacologia , Antioxidantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Cornus/química , Frutas/química , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Animais , alfa-Glucosidases/metabolismo , Polifenóis/farmacologia , Polifenóis/química , Linhagem Celular , Flavonoides/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Fenóis/farmacologia , Fenóis/química , Cromatografia Líquida de Alta Pressão , Ácido Ascórbico/farmacologiaRESUMO
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.