Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 23.571
Filtrar
1.
Molecules ; 29(9)2024 Apr 25.
Artículo en Inglés | MEDLINE | ID: mdl-38731467

RESUMEN

Flavonoids are important secondary metabolites found in Juglans mandshurica Maxim., which is a precious reservoir of bioactive substances in China. To explore the antitumor actions of flavonoids (JMFs) from the waste branches of J. mandshurica, the following optimized purification parameters of JMFs by macroporous resins were first obtained. The loading concentration, flow rate, and loading volume of raw flavonoid extracts were 1.4 mg/mL, 2.4 BV/h, and 5 BV, respectively, and for desorption, 60% ethanol (4 BV) was selected to elute JMFs-loaded AB-8 resin at a flow rate of 2.4 BV/h. This adsorption behavior can be explained by the pseudo-second-order kinetic model and Langmuir isotherm model. Subsequently, JMFs were identified using Fourier transform infrared combined with high-performance liquid chromatography and tandem mass spectrometry, and a total of 156 flavonoids were identified. Furthermore, the inhibitory potential of JMFs on the proliferation, migration, and invasion of HepG2 cells was demonstrated. The results also show that exposure to JMFs induced apoptotic cell death, which might be associated with extrinsic and intrinsic pathways. Additionally, flow cytometry detection found that JMFs exposure triggered S phase arrest and the generation of reactive oxygen species in HepG2 cells. These findings suggest that the JMFs purified in this study represent great potential for the treatment of liver cancer.


Asunto(s)
Apoptosis , Proliferación Celular , Flavonoides , Juglans , Juglans/química , Humanos , Flavonoides/farmacología , Flavonoides/química , Flavonoides/aislamiento & purificación , Proliferación Celular/efectos de los fármacos , Células Hep G2 , Apoptosis/efectos de los fármacos , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/farmacología , Movimiento Celular/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Antineoplásicos/farmacología , Antineoplásicos/química
2.
Molecules ; 29(9)2024 Apr 26.
Artículo en Inglés | MEDLINE | ID: mdl-38731493

RESUMEN

The aim of this study was to investigate the potential of Amaranthus cruentus flavonoids (quercetin, kaempferol, catechin, hesperetin, naringenin, hesperidin, and naringin), cinnamic acid derivatives (p-coumaric acid, ferulic acid, and caffeic acid), and benzoic acids (vanillic acid and 4-hydroxybenzoic acid) as antioxidants, antidiabetic, and antihypertensive agents. An analytical method for simultaneous quantification of flavonoids, cinnamic acid derivatives, and benzoic acids for metabolomic analysis of leaves and inflorescences from A. cruentus was developed with HPLC-UV-DAD. Evaluation of linearity, limit of detection, limit of quantitation, precision, and recovery was used to validate the analytical method developed. Maximum total flavonoids contents (5.2 mg/g of lyophilized material) and cinnamic acid derivatives contents (0.6 mg/g of lyophilized material) were found in leaves. Using UV-Vis spectrophotometry, the maximum total betacyanin contents (74.4 mg/g of lyophilized material) and betaxanthin contents (31 mg/g of lyophilized material) were found in inflorescences. The leaf extract showed the highest activity in removing DPPH radicals. In vitro antidiabetic activity of extracts was performed with pancreatic α-glucosidase and intestinal α-amylase, and compared to acarbose. Both extracts exhibited a reduction in enzyme activity from 57 to 74%. Furthermore, the in vivo tests on normoglycemic murine models showed improved glucose homeostasis after sucrose load, which was significantly different from the control. In vitro antihypertensive activity of extracts was performed with angiotensin-converting enzyme and contrasted to captopril; both extracts exhibited a reduction of enzyme activity from 53 to 58%. The leaf extract induced a 45% relaxation in an ex vivo aorta model. In the molecular docking analysis, isoamaranthin and isogomphrenin-I showed predictive binding affinity for α-glucosidases (human maltase-glucoamylase and human sucrase-isomaltase), while catechin displayed binding affinity for human angiotensin-converting enzyme. The data from this study highlights the potential of A. cruentus as a functional food.


Asunto(s)
Amaranthus , Antihipertensivos , Hipoglucemiantes , Metabolómica , Extractos Vegetales , Hojas de la Planta , Amaranthus/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Cromatografía Líquida de Alta Presión , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Antihipertensivos/farmacología , Antihipertensivos/química , Metabolómica/métodos , Animales , Antioxidantes/farmacología , Antioxidantes/química , Masculino , Ratas , Flavonoides/química , Flavonoides/farmacología , Flavonoides/análisis
3.
Molecules ; 29(9)2024 Apr 26.
Artículo en Inglés | MEDLINE | ID: mdl-38731498

RESUMEN

Natural products and their bioactive compounds have been used for centuries to prevent and treat numerous diseases. Kaempferol, a flavonoid found in vegetables, fruits, and spices, is recognized for its various beneficial properties, including its antioxidant and anti-inflammatory potential. This molecule has been identified as a potential means of managing different pathogenesis due to its capability to manage various biological activities. Moreover, this compound has a wide range of health-promoting benefits, such as cardioprotective, neuroprotective, hepatoprotective, and anti-diabetic, and has a role in maintaining eye, skin, and respiratory system health. Furthermore, it can also inhibit tumor growth and modulate various cell-signaling pathways. In vivo and in vitro studies have demonstrated that this compound has been shown to increase efficacy when combined with other natural products or drugs. In addition, kaempferol-based nano-formulations are more effective than kaempferol treatment alone. This review aims to provide detailed information about the sources of this compound, its bioavailability, and its role in various pathogenesis. Although there is promising evidence for its ability to manage diseases, it is crucial to conduct further investigations to know its toxicity, safety aspects, and mechanism of action in health management.


Asunto(s)
Antiinflamatorios , Inflamación , Quempferoles , Quempferoles/farmacología , Humanos , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/uso terapéutico , Animales , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Flavonoides/farmacología , Flavonoides/uso terapéutico , Flavonoides/química
4.
Molecules ; 29(9)2024 Apr 27.
Artículo en Inglés | MEDLINE | ID: mdl-38731503

RESUMEN

This current article was dedicated to the determination of the composition of phenolic compounds in extracts of four species of the genus Filipendula in order to establish a connection between the composition of polyphenols and biological effects. A chemical analysis revealed that the composition of the extracts studied depended both on the plant species and its part (leaf or flower) and on the extractant used. All four species of Filipendula were rich sources of phenolic compounds and contained hydrolyzable tannins, condensed tannins, phenolic acids and their derivatives, and flavonoids. The activities included data on those that are most important for creating functional foods with Filipendula plant components: the influence on blood coagulation measured by prothrombin and activated partial thromboplastin time, and on the activity of the digestive enzymes (pancreatic amylase and lipase). It was established that plant species, their parts, and extraction methods contribute meaningfully to biological activity. The most prominent result is as follows: the plant organ determines the selective inhibition of either amylase or lipase; thus, the anticoagulant activities of F. camtschatica and F. stepposa hold promise for health-promoting food formulations associated with general metabolic disorders.


Asunto(s)
Fenoles , Extractos Vegetales , Extractos Vegetales/química , Extractos Vegetales/farmacología , Fenoles/química , Fenoles/análisis , Fenoles/farmacología , Lipasa/antagonistas & inhibidores , Lipasa/metabolismo , Flavonoides/química , Flavonoides/farmacología , Flavonoides/análisis , Polifenoles/química , Polifenoles/farmacología , Polifenoles/análisis , Amilasas/antagonistas & inhibidores , Amilasas/metabolismo , Coagulación Sanguínea/efectos de los fármacos , Humanos , Anticoagulantes/farmacología , Anticoagulantes/química , Hojas de la Planta/química
5.
Nat Prod Res ; 38(11): 1956-1960, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38739565

RESUMEN

Magonia pubescens is a natural species from the Brazilian cerrado biome. Its fruits and seeds are used in the treatment of seborrheic dermatitis, a common inflammatory skin disease. In this work, the known compounds lapachol, stigmasterol, maniladiol and scopoletin were isolated from hexane and dichloromethane extracts of M. pubescens branches. The aqueous extract of this material was fractioned through a liquid-liquid partition and the obtained fractions were analyzed by UHPLC-MS/MS. The results obtained were compared with data from three databases, leading to the putative identification of 51 compounds from different classes, including flavonoids, saponins and triterpenes. The cytotoxicity of aqueous fractions was assayed against breast cancer (MDA-MB-231) and leukemia (THP-1 and K562) cells. The best activity was observed for fraction AE3 against MDA-MB-231 cells (IC50 30.72 µg.mL-1).


Asunto(s)
Antineoplásicos Fitogénicos , Neoplasias de la Mama , Fitoquímicos , Extractos Vegetales , Humanos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Neoplasias de la Mama/tratamiento farmacológico , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/química , Línea Celular Tumoral , Femenino , Fitoquímicos/farmacología , Fitoquímicos/química , Triterpenos/farmacología , Triterpenos/química , Brasil , Leucemia/tratamiento farmacológico , Flavonoides/farmacología , Flavonoides/química , Células K562 , Cromatografía Líquida de Alta Presión , Espectrometría de Masas en Tándem , Saponinas/farmacología , Saponinas/química , Células THP-1 , Estructura Molecular
6.
Sci Rep ; 14(1): 10528, 2024 05 08.
Artículo en Inglés | MEDLINE | ID: mdl-38719861

RESUMEN

The current study aimed to assess the effect of the germination process of wild mustard seeds on the phenolic profile, antioxidant, antibacterial, and antidiabetic properties, and some relevant enzyme activities. The total phenolic and flavonoid contents increased 5- and 10-fold, respectively, and were maximized on 5-days sprouts. One new phenolic compound was identified on 5-days sprout extract using HPLC. The concentrations of the identified phenolic compounds increased 1.5-4.3 folds on 5-days sprouts compared with dry seeds. The total antioxidant activity multiplied 17- and 21-fold on 5-days sprouts using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) assays, respectively. The activity of carbohydrate-cleaving, phenolic-synthesizing and antioxidant enzymes also increased during germination. On 5-days sprouts, there was a substantial correlation between the highest ß-glucosidase and peroxidase activities with highest phenolic and flavonoid levels and maximum antioxidant activity. The phenolic extract of 5-days sprouts exhibited antimicrobial activities against Escherichia coli and Staphylococcus aureus and showed potent antidiabetic activity established by its inhibitory effect against α-amylase and α-glucosidase compared to dry seeds.


Asunto(s)
Antioxidantes , Germinación , Planta de la Mostaza , Fenoles , Extractos Vegetales , Semillas , Fenoles/análisis , Fenoles/farmacología , Fenoles/química , Antioxidantes/farmacología , Antioxidantes/química , Germinación/efectos de los fármacos , Semillas/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Planta de la Mostaza/química , Antibacterianos/farmacología , Antibacterianos/química , Flavonoides/análisis , Flavonoides/farmacología , Flavonoides/química , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Cromatografía Líquida de Alta Presión
7.
Sci Rep ; 14(1): 10561, 2024 05 08.
Artículo en Inglés | MEDLINE | ID: mdl-38719884

RESUMEN

This study focuses on understanding the structural and molecular changes in lipid membranes under the influence of six halogenated flavonoid derivatives differing in the number and position of substitution of chlorine and bromine atoms (D1-D6). Utilizing various analytical techniques, including fluorometric methods, dynamic light scattering (DLS), attenuated Fourier transform infrared spectroscopy (ATR- FTIR), and FT-Raman spectroscopy, the research aims to elucidate the mechanisms underlying the interaction of flavonoids with cell membranes. Additionally, the study includes in silico analyses to explore the physicochemical properties of these compounds and their potential pharmaceutical applications, along with toxicity studies to assess their effects on cancer, normal, and red blood cells. Our study showed the ability of halogenated derivatives to interact mostly with the outer part of the membrane, especially in the lipid heads region however, some of them were able to penetrate deeper into the membrane and affect the fluidity of hydrocarbon chains. The potential to reduce cancer cell viability, the lack of toxicity towards erythrocytes, and the favourable physicochemical and pharmacokinetic properties suggest these halogenated flavonoids potential candidates for exploring their potential for medical use.


Asunto(s)
Flavonoides , Lípidos de la Membrana , Flavonoides/química , Flavonoides/farmacología , Flavonoides/metabolismo , Humanos , Lípidos de la Membrana/metabolismo , Lípidos de la Membrana/química , Membrana Celular/metabolismo , Halogenación , Citotoxinas/química , Citotoxinas/farmacología , Citotoxinas/metabolismo , Eritrocitos/efectos de los fármacos , Eritrocitos/metabolismo , Supervivencia Celular/efectos de los fármacos , Espectrometría Raman , Espectroscopía Infrarroja por Transformada de Fourier , Antineoplásicos/farmacología , Antineoplásicos/química , Antineoplásicos/metabolismo , Línea Celular Tumoral
8.
Food Res Int ; 186: 114404, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38729686

RESUMEN

Autism spectrum disorder (ASD) is a neurodevelopmental disorder with an unknown etiology. It is associated with various factors and causes great inconvenience to the patient's life. The gut-brain axis (GBA), which serves as a bidirectional information channel for exchanging information between the gut microbiota and the brain, is vital in studying many neurodegenerative diseases. Dietary flavonoids provide anti-inflammatory and antioxidant benefits, as well as regulating the structure and function of the gut microbiota. The occurrence and development of ASD are associated with dysbiosis of the gut microbiota. Modulation of gut microbiota can effectively improve the severity of ASD. This paper reviews the links between gut microbiota, flavonoids, and ASD, focusing on the mechanism of dietary flavonoids in regulating ASD through the GBA.


Asunto(s)
Trastorno del Espectro Autista , Eje Cerebro-Intestino , Flavonoides , Microbioma Gastrointestinal , Microbioma Gastrointestinal/efectos de los fármacos , Humanos , Trastorno del Espectro Autista/microbiología , Trastorno del Espectro Autista/metabolismo , Trastorno del Espectro Autista/dietoterapia , Flavonoides/farmacología , Dieta , Disbiosis , Encéfalo/metabolismo , Animales , Antioxidantes/farmacología
9.
PLoS One ; 19(5): e0302015, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38728332

RESUMEN

Nature has proven to be a treasure resource of bioactive metabolites. In this regard, Tamarix aphylla (F. Tamaricaceae) leaves crude extract was investigated for its gastroprotective effect against indomethacin-induced damage to the gastric mucosa. Additionally, phytochemical investigation of the methanolic extract afforded eight flavonoids' derivatives (1-8). On pharmacology networking study, the isolated compounds identified 123 unique targets where only 45 targets were related to peptic ulcer conditions, these 45 targets include 11 targets specifically correlate to gastric ulcer. The protein-protein interaction defined the PTGS2 gene as one of the highly interacted genes and the complete pharmacology network defined the PTGS2 gene as the most represented gene. The top KEGG signaling pathways according to fold enrichment analysis was the EGFR tyrosine kinase inhibitor resistance pathway. As a result, these findings highlighted the significance of using T. aphylla leaves crude extract as an anti-gastric ulcer candidate, which provides a safer option to chemical antisecretory medicines, which are infamous for their negative side effects. Our findings have illuminated the potent anti-inflammatory and antioxidant effects of T. aphylla, which are likely mediated by suppressing IL-1ß, IL-6, TNF-α, and MAPK signaling pathways, without compromising gastric acidity.


Asunto(s)
Indometacina , Sistema de Señalización de MAP Quinasas , Estrés Oxidativo , Extractos Vegetales , Úlcera Gástrica , Tamaricaceae , Úlcera Gástrica/tratamiento farmacológico , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patología , Animales , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Indometacina/efectos adversos , Indometacina/toxicidad , Ratas , Tamaricaceae/química , Sistema de Señalización de MAP Quinasas/efectos de los fármacos , Masculino , Hojas de la Planta/química , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Inflamación/inducido químicamente , Ratas Sprague-Dawley , Farmacología en Red , Mucosa Gástrica/metabolismo , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/patología , Antiulcerosos/farmacología , Antiulcerosos/uso terapéutico , Antiulcerosos/química , Flavonoides/farmacología , Flavonoides/química
10.
Mol Biol Rep ; 51(1): 653, 2024 May 11.
Artículo en Inglés | MEDLINE | ID: mdl-38734766

RESUMEN

Prostate cancer is a malignant epithelial tumor of the prostate gland and is the most common malignant tumor of the male genitourinary system. Pharmacological therapies, including chemotherapy and androgen deprivation therapy, play a key role in the treatment of prostate cancer. However, drug resistance and side effects limit the use of these drugs and so there is a need for new drug therapies for prostate cancer patients. Flavonoids, with their wide range of sources and diverse biological activities, have attracted much attention in the field of anti-tumor drug screening. In 2016, at least 58 flavonoids were reported to have anti-prostate cancer activity. In recent years, six additional flavonoid compounds have been found to have anti-prostate cancer potential. In this review, we have collected a large amount of evidence on the anti-prostate cancer effects of these six flavonoids, including a large number of cellular experiments and a small number of preclinical animal experiments. In addition, we predicted their drug-forming properties using Schrödinger's QikProp software and ADMETlab due to the lack of in vivo pharmacokinetic data for the six compounds. In conclusion, this review has fully confirmed the anti-prostate cancer effects of these six flavonoids, summarized their mechanisms of action and predicted their druggability. It provides a reference for the further development of these compounds into anti-prostate cancer drugs.


Asunto(s)
Flavonoides , Neoplasias de la Próstata , Masculino , Flavonoides/farmacología , Flavonoides/uso terapéutico , Neoplasias de la Próstata/tratamiento farmacológico , Neoplasias de la Próstata/patología , Humanos , Animales , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico
11.
Food Res Int ; 187: 114458, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38763690

RESUMEN

This study examines the antimicrobial and antibiofilm effectiveness of baicalin and carvacrol against Salmonella enterica ser. Typhimurium on food contact surfaces and chicken meat. The minimum inhibitory concentrations (MIC) for baicalin and carvacrol were found to be 100 µg/mL and 200 µg/mL, respectively, which aligns with findings from previous studies. The compounds exhibited a concentration-dependent decrease in microbial populations and biofilm formation. When used together, they displayed a remarkable synergistic effect, greatly augmenting their antibacterial activity. The assessment of food quality demonstrated that these treatments have no negative impact on the sensory characteristics of chicken meat. The impact of the structure on biofilms was observed through the use of Field Emission Scanning Electron Microscopy (FE-SEM) and Confocal Laser Scanning Microscopy (CLSM), revealing disrupted biofilm architectures and decreased cell viability. Crucially, RT-PCR analysis revealed a marked downregulation of quorum sensing (luxS), virulence (hilA), and stress response (rpoS) genes, highlighting the multifaceted antimicrobial mechanism of action. This gene-specific suppression suggests a targeted disruption of bacterial communication and virulence pathways, offering insight into the comprehensive antibiofilm strategy. This provides further insight into the molecular mechanisms that contribute to their antibiofilm effects.


Asunto(s)
Antibacterianos , Biopelículas , Pollos , Cimenos , Flavonoides , Microbiología de Alimentos , Pruebas de Sensibilidad Microbiana , Salmonella typhimurium , Biopelículas/efectos de los fármacos , Cimenos/farmacología , Salmonella typhimurium/efectos de los fármacos , Flavonoides/farmacología , Antibacterianos/farmacología , Animales , Percepción de Quorum/efectos de los fármacos , Carne/microbiología , Monoterpenos/farmacología , Microscopía Electrónica de Rastreo
12.
Pak J Pharm Sci ; 37(2): 321-326, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38767099

RESUMEN

Fatigue is a serious disturbance to human health, especially in people who have a severe disease such as cancer, or have been infected with COVID-19. Our research objective is to evaluate the anti-fatigue effect and mechanism of icariin through a mouse experimental model. Mice were treated with icariin for 30 days and anti-fatigue effects were evaluated by the weight-bearing swimming test, serum urea nitrogen test, lactic acid accumulation and clearance test in blood and the amount of liver glycogen. The protein expression levels of adenosine monophosphate-activated protein kinase (AMPK) and peroxisome proliferator-activated receptor-gamma coactivator-1alpha (PGC1-α) in the skeletal muscle of mice in each group were measured by western blotting. Results showed that icariin prolonged the weight-bearing swimming time of animals, reduced the serum urea nitrogen level after exercise, decreased the blood lactic acid concentration after exercise and increased the liver glycogen content observably. Compared to that in the control group, icariin upregulated AMPK and PGC1-α expression in skeletal muscle. Icariin can improve fatigue resistance in mice and its mechanism may be through improving the AMPK/PGC-1α pathway in skeletal muscle to enhance energy synthesis, decreasing the accumulation of metabolites and slowing glycogen consumption and decomposition.


Asunto(s)
Nitrógeno de la Urea Sanguínea , Fatiga , Flavonoides , Ácido Láctico , Músculo Esquelético , Coactivador 1-alfa del Receptor Activado por Proliferadores de Peroxisomas gamma , Animales , Flavonoides/farmacología , Coactivador 1-alfa del Receptor Activado por Proliferadores de Peroxisomas gamma/metabolismo , Músculo Esquelético/efectos de los fármacos , Músculo Esquelético/metabolismo , Ratones , Masculino , Ácido Láctico/sangre , Ácido Láctico/metabolismo , Fatiga/tratamiento farmacológico , Fatiga/metabolismo , Natación , Proteínas Quinasas Activadas por AMP/metabolismo , Glucógeno/metabolismo , Hígado/efectos de los fármacos , Hígado/metabolismo , Glucógeno Hepático/metabolismo
13.
BMC Vet Res ; 20(1): 212, 2024 May 20.
Artículo en Inglés | MEDLINE | ID: mdl-38764041

RESUMEN

BACKGROUND: Acinetobacter lwoffii (A.lwoffii) is a serious zoonotic pathogen that has been identified as a cause of infections such as meningitis, bacteremia and pneumonia. In recent years, the infection rate and detection rate of A.lwoffii is increasing, especially in the breeding industry. Due to the presence of biofilms, it is difficult to eradicate and has become a potential super drug-resistant bacteria. Therefore, eradication of preformed biofilm is an alternative therapeutic action to control A.lwoffii infection. The present study aimed to clarify that baicalin could eradicate A.lwoffii biofilm in dairy cows, and to explore the mechanism of baicalin eradicating A.lwoffii. RESULTS: The results showed that compared to the control group, the 4 MIC of baicalin significantly eradicated the preformed biofilm, and the effect was stable at this concentration, the number of viable bacteria in the biofilm was decreased by 0.67 Log10CFU/mL. The total fluorescence intensity of biofilm bacteria decreased significantly, with a reduction rate of 67.0%. There were 833 differentially expressed genes (367 up-regulated and 466 down-regulated), whose functions mainly focused on oxidative phosphorylation, biofilm regulation system and trehalose synthesis. Molecular docking analysis predicted 11 groups of target proteins that were well combined with baicalin, and the content of trehalose decreased significantly after the biofilm of A.lwoffii was treated with baicalin. CONCLUSIONS: The present study evaluated the antibiofilm potential of baicalin against A.lwoffii. Baicalin revealed strong antibiofilm potential against A.lwoffii. Baicalin induced biofilm eradication may be related to oxidative phosphorylation and TCSs. Moreover, the decrease of trehalose content may be related to biofilm eradication.


Asunto(s)
Acinetobacter , Antibacterianos , Biopelículas , Flavonoides , Leche , Biopelículas/efectos de los fármacos , Animales , Flavonoides/farmacología , Acinetobacter/efectos de los fármacos , Bovinos , Leche/microbiología , Antibacterianos/farmacología , Pruebas de Sensibilidad Microbiana , Simulación del Acoplamiento Molecular , Femenino , Infecciones por Acinetobacter/veterinaria , Infecciones por Acinetobacter/tratamiento farmacológico , Infecciones por Acinetobacter/microbiología
14.
J Tradit Chin Med ; 44(3): 437-447, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38767627

RESUMEN

OBJECTIVE: To evaluate the analgesic effects of total flavonoids of Longxuejie (Resina Dracaenae Cochinchinensis) (TFDB) and explore the possible analgesic mechanism associated with transient receptor potential vanilloid 1 (TRPV1). METHODS: Whole-cell patch clamp technique was used to observe the effects of TFDB on capsaicin-induced TRPV1 currents. Rat experiments in vivo were used to observe the analgesic effects of TFDB. Western blot and immunofluorescence experiments were used to test the change of TRPV1 expression in DRG neurons induced by TFDB. RESULTS: Results showed that TFDB inhibited capsaicin-induced TRPV1 receptor currents in acutely isolated dorsal root ganglion (DRG) neurons of rats and the half inhibitory concentration was (16.7 ± 1.6) mg/L. TFDB (2-20 mg/kg) showed analgesic activity in the phase Ⅱ of formalin test and (0.02-2 mg per paw) reduced capsaicin-induced licking times of rats. TFDB (20 mg/kg) was fully efficacious on complete Freund's adjuvant (CFA)-induced inflammatory thermal hyperalgesia and capsaicin could weaken the analgesic effects. The level of TRPV1 expressions of DRG neurons was also decreased in TFDB-treated CFA-inflammatory pain rats. CONCLUSION: All these results indicated that the analgesic effect of TFDB may contribute to their modulations on both function and expression of TRPV1 channels in DRG neurons.


Asunto(s)
Analgésicos , Flavonoides , Ganglios Espinales , Ratas Sprague-Dawley , Canales Catiónicos TRPV , Animales , Canales Catiónicos TRPV/genética , Canales Catiónicos TRPV/metabolismo , Ratas , Flavonoides/farmacología , Analgésicos/farmacología , Analgésicos/química , Masculino , Ganglios Espinales/efectos de los fármacos , Ganglios Espinales/metabolismo , Ganglios Espinales/citología , Humanos , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/química , Neuronas/efectos de los fármacos , Neuronas/metabolismo , Dolor/tratamiento farmacológico , Dolor/metabolismo
15.
Int J Mol Sci ; 25(9)2024 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-38732097

RESUMEN

The olive oil sector is a fundamental food in the Mediterranean diet. It has been demonstrated that the consumption of extra virgin olive oil (EVOO) with a high content of phenolic compounds is beneficial in the prevention and/or treatment of many diseases. The main objective of this work was to study the relationship between the content of phenolic compounds and the in vitro neuroprotective and anti-inflammatory activity of EVOOs from two PDOs in the province of Granada. To this purpose, the amounts of phenolic compounds were determined by liquid chromatography coupled to mass spectrometry (HPLC-MS) and the inhibitory activity of acetylcholinesterase (AChE) and cyclooxygenase-2 (COX-2) enzymes by spectrophotometric and fluorimetric assays. The main families identified were phenolic alcohols, secoiridoids, lignans, flavonoids, and phenolic acids. The EVOO samples with the highest total concentration of compounds and the highest inhibitory activity belonged to the Picual and Manzanillo varieties. Statistical analysis showed a positive correlation between identified compounds and AChE and COX-2 inhibitory activity, except for lignans. These results confirm EVOO's compounds possess neuroprotective potential.


Asunto(s)
Fármacos Neuroprotectores , Aceite de Oliva , Fenoles , Aceite de Oliva/química , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/química , Fenoles/análisis , Fenoles/química , Fenoles/farmacología , España , Ciclooxigenasa 2/metabolismo , Acetilcolinesterasa/metabolismo , Cromatografía Líquida de Alta Presión , Inhibidores de la Colinesterasa/farmacología , Inhibidores de la Colinesterasa/química , Inhibidores de la Ciclooxigenasa 2/farmacología , Inhibidores de la Ciclooxigenasa 2/química , Flavonoides/análisis , Flavonoides/farmacología , Flavonoides/química
16.
Nutrients ; 16(9)2024 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-38732608

RESUMEN

Flavonoids exert vasculoprotective effects in humans, but interindividual variability in their action has also been reported. This study aims to identify genes that are associated with vascular health effects of flavonoids and whose polymorphisms could explain interindividual variability in response to their intake. Applying the predetermined literature search criteria, we identified five human intervention studies reporting positive effects of flavonoids on vascular function together with global genomic changes analyzed using microarray methods. Genes involved in vascular dysfunction were identified from genome-wide association studies (GWAS). By extracting data from the eligible human intervention studies, we obtained 5807 differentially expressed genes (DEGs). The number of identified upstream regulators (URs) varied across the studies, from 227 to 1407. The search of the GWAS Catalog revealed 493 genes associated with vascular dysfunction. An integrative analysis of transcriptomic data with GWAS genes identified 106 candidate DEGs and 42 candidate URs, while subsequent functional analyses and a search of the literature identified 20 top priority candidate genes: ALDH2, APOE, CAPZA1, CYP11B2, GNA13, IL6, IRF5, LDLR, LPL, LSP1, MKNK1, MMP3, MTHFR, MYO6, NCR3, PPARG, SARM1, TCF20, TCF7L2, and TNF. In conclusion, this integrated analysis identifies important genes to design future nutrigenetic studies for development of precision nutrition for polyphenols.


Asunto(s)
Flavonoides , Estudio de Asociación del Genoma Completo , Nutrigenómica , Humanos , Nutrigenómica/métodos , Flavonoides/farmacología , Flavonoides/administración & dosificación , Polifenoles/farmacología , Polifenoles/administración & dosificación , Medicina de Precisión/métodos , Genómica/métodos
17.
CNS Neurosci Ther ; 30(5): e14740, 2024 05.
Artículo en Inglés | MEDLINE | ID: mdl-38715318

RESUMEN

AIMS: γ-aminobutyric acid (GABA) from reactive astrocytes is critical for the dysregulation of neuronal activity in various neuroinflammatory conditions. While Scutellaria baicalensis Georgi (S. baicalensis) is known for its efficacy in addressing neurological symptoms, its potential to reduce GABA synthesis in reactive astrocytes and the associated neuronal suppression remains unclear. This study focuses on the inhibitory action of monoamine oxidase B (MAO-B), the key enzyme for astrocytic GABA synthesis. METHODS: Using a lipopolysaccharide (LPS)-induced neuroinflammation mouse model, we conducted immunohistochemistry to assess the effect of S. baicalensis on astrocyte reactivity and its GABA synthesis. High-performance liquid chromatography was performed to reveal the major compounds of S. baicalensis, the effects of which on MAO-B inhibition, astrocyte reactivity, and tonic inhibition in hippocampal neurons were validated by MAO-B activity assay, qRT-PCR, and whole-cell patch-clamp. RESULTS: The ethanolic extract of S. baicalensis ameliorated astrocyte reactivity and reduced excessive astrocytic GABA content in the CA1 hippocampus. Baicalin and baicalein exhibited significant MAO-B inhibition potential. These two compounds downregulate the mRNA levels of genes associated with reactive astrogliosis or astrocytic GABA synthesis. Additionally, LPS-induced aberrant tonic inhibition was reversed by both S. baicalensis extract and its key compounds. CONCLUSIONS: In summary, baicalin and baicalein isolated from S. baicalensis reduce astrocyte reactivity and alleviate aberrant tonic inhibition of hippocampal neurons during neuroinflammation.


Asunto(s)
Astrocitos , Flavanonas , Flavonoides , Lipopolisacáridos , Neuronas , Extractos Vegetales , Scutellaria baicalensis , Ácido gamma-Aminobutírico , Animales , Astrocitos/efectos de los fármacos , Astrocitos/metabolismo , Flavanonas/farmacología , Scutellaria baicalensis/química , Ratones , Ácido gamma-Aminobutírico/metabolismo , Neuronas/efectos de los fármacos , Neuronas/metabolismo , Masculino , Flavonoides/farmacología , Extractos Vegetales/farmacología , Lipopolisacáridos/toxicidad , Lipopolisacáridos/farmacología , Ratones Endogámicos C57BL , Monoaminooxidasa/metabolismo , Inhibición Neural/efectos de los fármacos , Hipocampo/efectos de los fármacos , Hipocampo/metabolismo
18.
Sci Rep ; 14(1): 10745, 2024 05 10.
Artículo en Inglés | MEDLINE | ID: mdl-38730240

RESUMEN

Gastric cancer is one of the most common malignant tumors, and chemotherapy is the main treatment for advanced gastric cancer. However, chemotherapy resistance leads to treatment failure and poor prognosis in patients with gastric cancer. Multidrug resistance (MDR) is a major challenge that needs to be overcome in chemotherapy. According to recent research, ferroptosis activation is crucial for tumor therapeutic strategies. In this work, we explored the solution to chemoresistance in gastric cancer by investigating the effects of the Chinese medicine monomer baicalin on ferroptosis. Baicalin with different concentrations was used to treat the parent HGC27 and drug-resistant HGC27/L cells of gastric cancer. Cell viability was measured by CCK8, and synergistic effects of baicalin combined with oxaliplatin were evaluated using Synergy Finder software. The effects of baicalin on organelles and cell morphology were investigated using projective electron microscopy. Iron concentration, MDA production and GSH inhibition rate were measured by colorimetry. ROS accumulation was detected by flow cytometry. The ferroptosis-related genes (IREB2, TfR, GPX4, FTH1), P53, and SLC7A11 were analysed by Western blot, and the expression differences of the above proteins between pretreatment and pretreatment of different concentrations of baicalin, were assayed in both parental HGC27 cells and Oxaliplatin-resistant HGC27/L cells. Mechanically, Baicalin disrupted iron homeostasis and inhibits antioxidant defense, resulting in iron accumulation, lipid peroxide aggregation, and specifically targeted and activated ferroptosis by upregulating the expression of tumor suppressor gene p53, thereby activating the SLC7A11/GPX4/ROS pathway mediated by it. Baicalin activates ferroptosis through multiple pathways and targets, thereby inhibiting the viability of oxaliplatin-resistant gastric cancer HGC27/L cells and enhancing the sensitivity to oxaliplatin chemotherapy.


Asunto(s)
Resistencia a Antineoplásicos , Ferroptosis , Flavonoides , Oxaliplatino , Neoplasias Gástricas , Proteína p53 Supresora de Tumor , Ferroptosis/efectos de los fármacos , Humanos , Flavonoides/farmacología , Neoplasias Gástricas/tratamiento farmacológico , Neoplasias Gástricas/metabolismo , Neoplasias Gástricas/patología , Neoplasias Gástricas/genética , Oxaliplatino/farmacología , Resistencia a Antineoplásicos/efectos de los fármacos , Proteína p53 Supresora de Tumor/metabolismo , Proteína p53 Supresora de Tumor/genética , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Antineoplásicos/farmacología , Sinergismo Farmacológico , Especies Reactivas de Oxígeno/metabolismo , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos
19.
Int J Mol Sci ; 25(9)2024 Apr 24.
Artículo en Inglés | MEDLINE | ID: mdl-38731845

RESUMEN

Moringa oleifera leaves are rich sources of bioactive compounds with potential health benefits, including antioxidants and anti-inflammatory agents. Pressurized liquid extraction (PLE) stands out as a promising technique for effectively extracting valuable compounds from natural sources. In this study, we aimed to optimize PLE parameters, such as temperature, extraction duration, and pressure, to maximize bioactive compound (polyphenols, flavonoids, and ascorbic acid) yield from M. oleifera leaves and evaluate their antioxidant and anti-inflammatory activities. According to the outcomes of this research, the maximum achieved total polyphenol content was 24.10 mg gallic acid equivalents (GAE)/g of dry weight (dw), and the total flavonoid content was increased up to 19.89 mg rutin equivalents (RtE)/g dw. Moreover, after HPLC-DAD analysis, neochlorogenic and chlorogenic acids, catechin and epicatechin, rutin, and narirutin were identified and quantified. As far as the optimum ascorbic acid content is concerned, it was found to be 4.77 mg/g dw. The antioxidant activity was evaluated by three different methods: ferric reducing antioxidant power (FRAP), the DPPH method, and the anti-hydrogen peroxide activity (AHPA) method, resulting in 124.29 µmol ascorbic acid equivalent (AAE)/g dw, 131.28 µmol AAE/g dw, and 229.38 µmol AAE/g dw values, respectively. Lastly, the albumin denaturation inhibition was found to be 37.54%. These findings underscore the potential of PLE as an efficient extraction method for preparing extracts from M. oleifera leaves with the maximum content of bioactive compounds.


Asunto(s)
Antioxidantes , Moringa oleifera , Extractos Vegetales , Hojas de la Planta , Moringa oleifera/química , Hojas de la Planta/química , Antioxidantes/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Extractos Vegetales/farmacología , Extractos Vegetales/química , Flavonoides/aislamiento & purificación , Flavonoides/análisis , Flavonoides/química , Flavonoides/farmacología , Polifenoles/aislamiento & purificación , Polifenoles/farmacología , Polifenoles/análisis , Polifenoles/química , Ácido Ascórbico/farmacología , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Cromatografía Líquida de Alta Presión/métodos , Presión , Extracción Líquido-Líquido/métodos , Fitoquímicos/química , Fitoquímicos/farmacología , Fitoquímicos/aislamiento & purificación
20.
Colloids Surf B Biointerfaces ; 238: 113928, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38692175

RESUMEN

In this research, four water-insoluble flavonoid compounds were utilized and reacted with arginine to prepare four carbonized polymer dots with good water-solubility in a hydrothermal reactor. Structural characterization demonstrated that the prepared carbonized polymer dots were classic core-shell structure. Effect of the prepared carbonized polymer dots on protein amyloid aggregation was further investigated using hen egg white lysozyme and human lysozyme as model protein in aqueous solution. All of the prepared carbonized polymer dots could retard the amyloid aggregation of hen egg white lysozyme and human lysozyme in a dose-depended manner. All measurements displayed that the inhibition ratio of luteolin-derived carbonized polymer dots (CPDs-1) was higher than that of the other three carbonized polymer dots under the same dosage. This result may be interpreted by the highest content of phenolic hydroxyl groups on the periphery. The inhibition ratio of CPDs-1 on hen egg white lysozyme and human lysozyme reached 88 % and 83 % at the concentration of 0.5 mg/mL, respectively. CPDs-1 also could disaggregate the formed mature amyloid fibrils into short aggregates.


Asunto(s)
Amiloide , Flavonoides , Muramidasa , Polímeros , Agregado de Proteínas , Muramidasa/química , Muramidasa/metabolismo , Humanos , Polímeros/química , Polímeros/farmacología , Amiloide/química , Amiloide/antagonistas & inhibidores , Flavonoides/química , Flavonoides/farmacología , Agregado de Proteínas/efectos de los fármacos , Animales , Pollos , Carbono/química
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA