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1.
Food Microbiol ; 87: 103377, 2020 May.
Artículo en Inglés | MEDLINE | ID: mdl-31948618

RESUMEN

The present study explored the effect of quercetin on the expression of virulence genes actA, inlA, inlC, and their regulatory components, sigB and prfA, in L. monocytogenes. Furthermore, the physicochemical changes on the surface, membrane permeability, and biofilm formation of quercetin-treated bacteria were evaluated. An inhibitory dose-dependent effect of quercetin (0.1-0.8 mM) was observed on the cell attachment on stainless steel at 2 and 6 h at 37 °C. Quercetin at 0.8 mM prevented the biofilm formation on stainless steel surfaces after 6 h of incubation at 37 °C, while the untreated bacteria formed biofilms with a cell density of 5.1 Log CFU/cm2. The microscopic analysis evidenced that quercetin at 0.2 mM decreased the biovolume and covered area of the attached micro-colonies. Also, sigB, prfA, inlA, inlC, and actA genes were downregulated by 7-29 times lower compared to untreated bacteria. In addition, quercetin decreased the superficial cell charge, increased the membrane permeability, and its surface hydrophobicity. These results demonstrated that quercetin prevented biofilm formation, repressed the genes of stress and virulence of L. monocytogenes and also altered the physicochemical cell properties.


Asunto(s)
Adhesión Bacteriana/efectos de los fármacos , Proteínas Bacterianas/genética , Biopelículas/efectos de los fármacos , Listeria monocytogenes/efectos de los fármacos , Quercetina/farmacología , Factores de Virulencia/genética , Proteínas Bacterianas/metabolismo , Regulación Bacteriana de la Expresión Génica/efectos de los fármacos , Listeria monocytogenes/genética , Listeria monocytogenes/fisiología , Acero Inoxidable/química , Factores de Virulencia/metabolismo
2.
Food Chem Toxicol ; 135: 110985, 2020 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-31765700

RESUMEN

Investigation of antiviral and cytotoxic effect of quercetin 3-glucoside (Q3G) from Dianthus superbus L over influenza virus infection and replication were studied. Moreover, anti-influenza mechanism was screened by time-dependent antiviral assay, virus-induced symptoms and related gene expressions. The blockade of cap-binding domain of polymerase basic protein subunit were analysed by molecular docking study. The Q3G demonstrated potent antiviral activity showing 4.93, 6.43, 9.94, 8.3, and 7.1 µg/mL of IC50 for A/PR/8/34, A/Victoria/3/75, A/WS/33, B/Maryland/1/59, and B/Lee/40, respectively. The cellular toxicity of Q3G and oseltamivir (control) were tested and >100 µg/mL of CC50 value considered as nontoxic. Influenza A virus infection induced a higher ROS production, however potentially reduced by Q3G treatment and significantly blocked virus infection induced acidic vesicular organelles (AVO). Moreover, Q3G has no inhibitory effect for neuraminidase activity but blocked virus replication through time dependent assay and showed more competitive binding affinity (-8.0 kcal/mal) than GTP (-7.0 kcal/mol) to block polymerase basic protein-2 subunit of influenza virus. Q3G from D. superbus showed potent antiviral activity against influenza A and B viruses with suppressive effect on virus-induced cellular ROS generation and AVO formation. Thus, this study provided a new line of research for Q3G to develop possible natural anti-influenza drug.


Asunto(s)
Antivirales/farmacología , Dianthus/química , Virus de la Influenza A/efectos de los fármacos , Virus de la Influenza B/efectos de los fármacos , Gripe Humana/tratamiento farmacológico , Quercetina/análogos & derivados , Animales , Antivirales/toxicidad , Supervivencia Celular/efectos de los fármacos , Simulación por Computador , Perros , Humanos , Técnicas In Vitro , Virus de la Influenza A/genética , Virus de la Influenza A/fisiología , Virus de la Influenza B/genética , Virus de la Influenza B/fisiología , Gripe Humana/virología , Células de Riñón Canino Madin Darby , Simulación del Acoplamiento Molecular , Quercetina/farmacología , Quercetina/toxicidad , ARN Viral/biosíntesis , Especies Reactivas de Oxígeno/metabolismo , Replicación Viral/efectos de los fármacos
3.
Artículo en Inglés | MEDLINE | ID: mdl-31648051

RESUMEN

We aimed to ascertain whether ubiquitous plant-based polyphenolic flavonoid compound quercetin (Q) was capable of alleviating deltamethrin (DM) stress in a freshwater teleost, Channa punctata, with emphasis on levels of acetylcholinesterase (AChE), reduced glutathione (GSH), glutathione-S-transferase (GST), DNA/RNA contents and hematological parameters. We measured these parameters in various tissues of fish at 7 and 21 days of exposure to DM doses (0.03 and 0.15 µL L-1), Q (0.14 g L-1) and their combinations (0.03 µL DM L-1 + 0.14 g Q L-1 and 0.15 µL DM L-1 + 0.14 g Q L-1). Both the DM doses altered blood parameters, lowered DNA/RNA contents, AchE activities, GSH levels and augmented GST activities as a mark of neurotoxicity and oxidative stress in fish tissues. We found that 0.14 g L-1 Q ameliorated oxidative stress and AchE inhibitory effects, recovered DM-induced nucleic acid damage and alterations in blood parameters, with some tissue specificity and in duration-dependent manner. Thus, the results indicated that Q was capable of neuroprotection and enhancing the function of antioxidants in fish, which could be predicted to be useful for providing better protection to fish under aquaculture settings with improved Q-rich diets. Through this study with multiple biomarkers in several tissues of fish, valuable information for devising better strategies regarding pesticide risk assessment was obtained and it was recognized that an appropriate dose of Q was essential for its better functioning.


Asunto(s)
Peces/metabolismo , Nitrilos/toxicidad , Piretrinas/toxicidad , Quercetina/farmacología , Estrés Fisiológico/efectos de los fármacos , Animales , Antioxidantes/farmacología , Biomarcadores/sangre , Inhibidores de la Colinesterasa/toxicidad , Agua Dulce , Insecticidas/toxicidad , Contaminantes Químicos del Agua/toxicidad
4.
BMC Complement Altern Med ; 19(1): 346, 2019 Dec 02.
Artículo en Inglés | MEDLINE | ID: mdl-31791311

RESUMEN

BACKGROUND: Influenza A virus (IAV) is still a major health threat. The clinical manifestations of this infection are related to immune dysregulation, which causes morbidity and mortality. The usage of traditional medication with immunomodulatory properties against influenza infection has been increased recently. Our previous study showed antiviral activity of quercetin-3-O-α-L-rhamnopyranoside (Q3R) isolated from Rapanea melanophloeos (RM) (L.) Mez (family Myrsinaceae) against H1N1 (A/PR/8/34) infection. This study aimed to confirm the wider range of immunomodulatory effect of Q3R on selective pro- and anti-inflammatory cytokines against IAV in vitro, to evaluate the effect of Q3R on apoptosis pathway in combination with H1N1, also to assess the physical interaction of Q3R with virus glycoproteins and RhoA protein using computational docking. METHODS: MDCK cells were exposed to Q3R and 100CCID50/100 µl of H1N1 in combined treatments (co-, pre- and post-penetration treatments). The treatments were tested for the cytokines evaluation at RNA and protein levels by qPCR and ELISA, respectively. In another set of treatment, apoptosis was examined by detecting RhoA GTPase protein and caspase-3 activity. Molecular docking was used as a tool for evaluation of the potential anti-influenza activity of Q3R. RESULTS: The expressions of cytokines in both genome and protein levels were significantly affected by Q3R treatment. It was shown that Q3R was much more effective against influenza when it was applied in co-penetration treatment. Q3R in combination with H1N1 increased caspase-3 activity while decreasing RhoA activation. The molecular docking results showed strong binding ability of Q3R with M2 transmembrane, Neuraminidase of 2009 pandemic H1N1, N1 and H1 of PR/8/1934 and Human RhoA proteins, with docking energy of - 10.81, - 10.47, - 9.52, - 9.24 and - 8.78 Kcal/mol, respectively. CONCLUSIONS: Quercetin-3-O-α-L-rhamnopyranoside from RM was significantly effective against influenza infection by immunomodulatory properties, affecting the apoptosis pathway and binding ability to viral receptors M2 transmembrane and Neuraminidase of 2009 pandemic H1N1 and human RhoA cellular protein. Further research will focus on detecting the detailed specific mechanism of Q3R in virus-host interactions.


Asunto(s)
Antivirales , Glicósidos , Subtipo H1N1 del Virus de la Influenza A , Myrsine/química , Fitoquímicos , Quercetina/análogos & derivados , Animales , Antivirales/química , Antivirales/metabolismo , Antivirales/farmacología , Apoptosis/efectos de los fármacos , Citocinas/metabolismo , Perros , Glicósidos/química , Glicósidos/metabolismo , Glicósidos/farmacología , Células de Riñón Canino Madin Darby , Simulación del Acoplamiento Molecular , Neuraminidasa/química , Neuraminidasa/metabolismo , Fitoquímicos/química , Fitoquímicos/metabolismo , Fitoquímicos/farmacología , Quercetina/química , Quercetina/metabolismo , Quercetina/farmacología , Proteínas de la Matriz Viral/química , Proteínas de la Matriz Viral/metabolismo
5.
Int J Nanomedicine ; 14: 8943-8959, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31819411

RESUMEN

Objective: The study was designed to investigate the therapeutic potential of lactobionic acid (LA) conjugated quercetin (Q) loaded organically modified silica nanoparticles (LA-Q-ORMOSIL) with bulk quercetin to mitigate cyclophosphamide (CP) induced liver injury. Methodology: Q-ORMOSIL nanoparticles were synthesized and characterized using UV-Vis spectroscopy, TEM, Zeta sizer, FTIR and EDX. Further, encapsulation efficiency and in vitro release kinetic study was done. Q-ORMOSIL nanoparticles surface were modified with lactobionic acid, a ligand for the asialoglycoprotein receptor on the hepatocyte surface. The hepatoprotective effects of Q-ORMOSIL and LA-Q-ORMOSIL nanoparticles were evaluated in vivo. Cyclophosphamide (20 mg/kg/day, i.p) was co-administered for seven days with bulk quercetin (50mg/kg/day) and quercetin nanoparticles (50µg/kg/day). After seven days, the number of biomarkers for liver function test and oxidative stress were determined in liver homogenate. Histopathological changes were also analyzed in control and treated liver tissues. Results: Physiochemical characterization of LA-Q-ORMOSIL nanoparticles depicts that the particles formed were of approx. 80 nm, spherical, monodispersed in nature and showed sustain drug release in in vitro study. Our results further suggested that Q-ORMOSIL and LA-Q-ORMOSIL nanoparticles significantly decreased tissue TBARS, ROS levels and ALT, AST, and ALP activities compared to CP induced group. On the other hand, tissue antioxidant levels (GSH, GST, and catalase) showed a significant increase in LA-Q-ORMOSIL treated group compared to the CP treated group confirming its high therapeutic efficacy during liver injury. Conclusion: Targeted nanoquercetin demonstrated a significant hepatoprotective effect compared to bulk quercetin against CP-induced hepatotoxicity and it considerably reduced bulk quercetin dose level to many folds. Bulk quercetin has low bioavailability and thus, from obtained data we suggest that LA-Q-ORMOSIL nanoparticles provide high therapeutic value in protecting experimental animals against CP-induced liver injury. We also propose multifunctional dye-doped LA-modified ORMOSIL nanoparticles for future studies in facilitating nanoparticles uptake to hepatocytes for liver diagnosis and treatment.


Asunto(s)
Ciclofosfamida/efectos adversos , Disacáridos/química , Hígado/patología , Nanopartículas/química , Quercetina/farmacología , Dióxido de Silicio/química , Alanina Transaminasa/metabolismo , Fosfatasa Alcalina/metabolismo , Animales , Antioxidantes/farmacología , Aspartato Aminotransferasas/metabolismo , Catalasa/metabolismo , Liberación de Fármacos , Cinética , Hígado/efectos de los fármacos , Masculino , Nanopartículas/ultraestructura , Estrés Oxidativo/efectos de los fármacos , Tamaño de la Partícula , Ratas Wistar , Especies Reactivas de Oxígeno/metabolismo , Espectrofotometría Ultravioleta , Espectroscopía Infrarroja por Transformada de Fourier , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismo
6.
Int J Nanomedicine ; 14: 9173-9184, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31819425

RESUMEN

Background: As an active ingredient of Chinese herbal medicine, quercetin (QU) can significantly induce apoptosis of tumor cells and give play to other effect such as decreasing both fibroblast population and collagen in cancer cell nest. However, the antitumor efficacy of quercetin was mostly evaluated at cellular level and rarely developed in vivo by intravenous injection, which may be ascribed to its inferior physicochemical properties including water insolubility, short plasma half-time, and insufficient enrichment in the tumor tissues. Methods: The DSPE-PEG was used to construct quercetin-loaded micelles, and the integrin ligand cRGDfK was grafted to modify the nanocarrier for enhancing its cancer-specific homing. The MALDI-TOF-MS, DLS, TEM, and UV were orderly operated to characterize guidance molecules and micelles by morphology, size distribution, Zeta potential, and drug encapsulation efficiency. In addition, the surface plasmon resonance study and real-time confocal analysis were employed to demonstrate αvß3 integrin-overexpressing B16 cells-specific binding and uptake. After further pharmacodynamics studies in vitro and in vivo, we also evaluate systemic toxicity about cRGDfK-PM-QU. Results: The cRGDfK was successfully stitched with DSPE-PEG and modified on the surface of micelles. The ligand modification enhanced the negative charges of the micelles, but it did not induce significant changes in particle size. The quercetin micelles were about 15 nm in size and negatively charged, and had spherical morphology and high drug encapsulation efficiency. In vitro, the cRGDfK-modified micelles (cRGDfK-PM) showed αvß3 integrin-overexpressing B16 cells-specific binding and uptake, and cRGDfK-PM-QU (QU loaded in cRGDfK-PM) induced more significant cell apoptosis and cytotoxic effects against B16 tumor cells than counterpart micelles (PM-QU). In vivo, the cRDGfK modification enhanced enrichment in B16 tumor tissue, improved the therapeutic efficacy of the quercetin-loaded micelles against B16 tumor, and exhibited lower systemic and pulmonary toxicity compared with counterpart micelles in the mouse mode. Conclusion: Quercetin as a natural product has triggered increasing interest in the antitumor field. In this study, cRGDfK-modified DSPE-PEG micelles significantly optimized quercetin therapeutic efficacy and pulmonary toxicity as well as lowered systemic toxicity.


Asunto(s)
Medicamentos Herbarios Chinos/uso terapéutico , Micelas , Tamaño de la Partícula , Péptidos Cíclicos/química , Quercetina/farmacología , Animales , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Humanos , Integrina alfaVbeta3/metabolismo , Masculino , Melanoma Experimental/tratamiento farmacológico , Melanoma Experimental/patología , Ratones Desnudos , Fosfatidiletanolaminas/química , Polietilenglicoles/química
7.
Ceska Slov Farm ; 68(4): 173-179, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31822110

RESUMEN

The article presents the results of the study of the nephroprotective effect of N-acetylglucosamine (NAG) under the development of experimental acute kidney injury (AKI). The study was conducted on a model of acute glycerol nephrosis in rats. NAG was studied at a dose of 50 mg/kg at daily parenteral administration during 1 week compared to quercetin, which was administered intraperitoneally at a dose of 34 mg/kg. The efficiency of the drugs was assessed by the functional state of animals, the renal excretory function and the nitrogen metabolism indices. The NAG effect on rats with AKI caused a reduction of the mortality rate, an increase in diuresis, a reduction of proteinuria, an increase in creatinine and urea excretion, which indicates the normalization of the renal excretory function and nitrogen metabolism. At the same time, NAG has statistically significantly exceeded the effect of quercetin in the majority of indices and, therefore, the level of efficiency. Thus, NAG is an efficient agent for AKI treatment, which can be used at parenteral route of administration.


Asunto(s)
Acetilglucosamina/farmacología , Lesión Renal Aguda/tratamiento farmacológico , Animales , Creatinina/orina , Diuresis , Proteinuria , Quercetina/farmacología , Ratas , Urea/orina
8.
Int. j. morphol ; 37(4): 1422-1428, Dec. 2019. graf
Artículo en Inglés | LILACS | ID: biblio-1040148

RESUMEN

Paracetamol (also called acetaminophen, or APAP) overdose causes acute damage to the liver and kidneys in both humans and experimental animal models via the induction of the oxidative stress pathway. We sought to determine whether the combined antioxidants and anti-inflammatory compounds, resveratrol (RES) and quercetin (QUR) can protect against kidney injury induced by a toxic dose of APAP in a rat model of APAP-induced acute kidney injury. Rats were either received a single dose of APAP (2 g/kg) before being sacrificed after 24 hours or were pre-treated for 7 days with combined doses of RES (30 mg/kg) and QUR (50 mg/kg) before being given a single dose of APAP and then sacrificed 24 hours post APAP ingestion. Harvested kidney tissues were prepared for light microscopy staining, and tissue samples were assayed for (i) biomarkers of oxidative stress and antioxidant, malondialdehyde (MDA) and superoxide dismutase (SOD); and (ii) biomarkers of inflammation, tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6). Hematoxylin and eosin (H&E) stained images showed that APAP overdose induced acute kidney injury as demonstrated by widening of glomeruli space (Bowman space), tubular dilatation, numerous cellular debris in the renal tubules with tubular epithelial degeneration, and vacuolization, which were effectively protected by RES+QUR except a partial protection of the glomeruli space was observed. In addition, APAP significantly (p<0.05) modulated tissue levels of MDA, SOD, TNF-α, and IL-6, which were protected by RES+QUR. Furthermore, a significant (p<0.0001) positive correlation was observed between glomeruli space and TNF-α, (r=0.8899), IL-6 (r=0.8986), and MDA (r=0.8552), whereas glomeruli space scoring versus SOD showed negative correlation (r= - 0.7870). We conclude that resveratrol plus quercetin substantially protects against APAP-induced acute kidney injury in rats, possibly via the augmentation of antioxidants and inhibition of oxidative stress and inflammation.


La sobredosis de paracetamol (también llamado acetaminofen o APAP) causa un daño agudo en el hígado y los riñones, tanto en humanos como en modelos animales experimentales, a través de la inducción de la vía del estrés oxidativo. Intentamos determinar si los antioxidantes y los compuestos antiinflamatorios combinados, el resveratrol (RES) y la quercetina (QUR) pueden proteger contra la lesión renal inducida por una dosis tóxica de APAP en un modelo de rata de lesión renal aguda inducida por APAP. Las ratas recibieron una dosis única de APAP (2 g / kg) antes de ser sacrificadas después de 24 horas o se trataron previamente durante 7 días con dosis combinadas de RES (30 mg / kg) y QUR (50 mg / kg), antes de ser tratadas, se administró una dosis única de APAP y luego fueron sacrificadas 24 horas después de la ingestión. Los tejidos renales recolectados se tiñeron con H-E y fueron observados a través de microscopía óptica. Las muestras de tejido se analizaron para (i) biomarcadores de estrés oxidativo y antioxidante, malondialdehído (MDA) y superóxido dismutasa (SOD); y (ii) biomarcadores de inflamación, factor de necrosis tumoral alfa (TNF-α) e interleucina-6 (IL-6). Las imágenes teñidas con H & E mostraron que la sobredosis de APAP indujo daño renal agudo como lo demuestra la ampliación del espacio glomerular, la dilatación tubular, numerosos desechos celulares en los túbulos renales con degeneración epitelial tubular y la vacuolización, que se protegieron eficazmente con RES + QUR Se observó una protección parcial del espacio glomerular. Además, APAP modificó significativamente (p <0.05) los niveles tisulares de MDA, SOD, TNF-α e IL-6, que estaban protegidos por RES + QUR. Además, se observó una correlación positiva significativa (p <0,0001) entre el espacio glomerular y el TNF-α, (r = 0,8899), IL-6 (r = 0,8986) y MDA (r = 0,8552), mientras que la puntuación del espacio glomerular versus SOD mostró correlación negativa (r = - 0,7870). Concluimos que el resveratrol más quercetina protege sustancialmente contra la lesión renal aguda inducida por APAP en ratas, posiblemente a través del aumento de antioxidantes y la inhibición del estrés oxidativo y la inflamación.


Asunto(s)
Animales , Ratas , Quercetina/uso terapéutico , Lesión Renal Aguda/tratamiento farmacológico , /uso terapéutico , Acetaminofén/toxicidad , Quercetina/farmacología , Estrés Oxidativo/efectos de los fármacos , Modelos Animales de Enfermedad , Quimioterapia Combinada , Lesión Renal Aguda/inducido químicamente , /farmacología , Acetaminofén/antagonistas & inhibidores , Antiinflamatorios/uso terapéutico , Antioxidantes/uso terapéutico
9.
Sichuan Da Xue Xue Bao Yi Xue Ban ; 50(5): 684-687, 2019 Sep.
Artículo en Chino | MEDLINE | ID: mdl-31762238

RESUMEN

OBJECTIVE: To explore the protective effects of quercetin (QE) on triptolide (TP) induced liver injury and the relevant mechanism. METHODS: Forty C57BL/6 mice were equally divided into 4 groups, control group, TP model group, 20 mg/kg QE treatment group and 80 mg/kg QE treatment group randomly. The 20 mg/kg and 80 mg/kg QE groups were gastrointestinal administration with QE at the dose of 0.2 mL/10 g for 10 d, twice daily, while other groups were administrated with equivalent normal saline. Four hours post the last dose, animals were gastrointestinal administered with TP at a dose of 500 µg/kg per mouse, except for NS control. All the mice were sacrificed 22 h later, blood and liver tissue samples were collected. The pathologic change of liver tissue was detected by HE staining. The level of aminotransferase (AST) and aspartate alanine aminotransferase (ALT) in serum, and the level of glutathione (GSH), malondialdehyde (MDA) and superoxide dismutase (SOD) in liver tissue homogenates were detected using the commercial kits. The level of interleukin (IL)-17, IL-10 and IL-6 in liver tissue homogenates was measured by ELISA. Hepatic expression of Toll-like receptor 4 (TLR4) was detected by Western blot. RESULTS: Compared with the control group, in the TP model group, hepatic lobule structure atrophied and even disappeared, hepatic cell necrosis and inflammatory cell infiltration are obvious. Additionally, in TP model group, serum ALT, AST and MDA levels were significantly increased, SOD and GSH levels were decreased, IL-6 and IL-17 levels were increased, IL-10 levels were decreased, and TLR4 protein levels were increased (P < 0.05). Compared with the TP model group, liver tissue injury and inflammatory cell infiltration were reduced in the QE group, and serum levels of ALT, AST, MDA, IL-6 and IL-17 were all decreased. TLR4 expression was down-regulated (P < 0.05) in both QE groups, and the decease levle was more significant in the high-dose QE group (P < 0.05, compared with the low-dose QE group). CONCLUSION: Quercetin can reduce TP-induced liver injury by reducing oxidative damage, promoting antioxidant and regulating cytokine secretion.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Quercetina/farmacología , Animales , Antioxidantes/metabolismo , Citocinas/metabolismo , Diterpenos , Compuestos Epoxi , Hígado/efectos de los fármacos , Hígado/patología , Ratones , Ratones Endogámicos C57BL , Estrés Oxidativo , Fenantrenos , Distribución Aleatoria
10.
BMC Complement Altern Med ; 19(1): 333, 2019 Nov 26.
Artículo en Inglés | MEDLINE | ID: mdl-31771569

RESUMEN

BACKGROUND: Monotropein, astragalin, and spiraeoside (MAS) are active compounds extracted from medicinal herbs; monotropein from Morinda officinalis How (Rubiaceae), astragalin (kaempferol 3-O-glucoside) from Cuscuta chinensis Lamark (Convolvulaceae) and spiraeoside from the outer scales of Allium cepa L. (Liliceae) in a ratio of 6.69:0.41:3.61. Monotropein, astragalin, and spiraeoside are well-known antioxidants, anti-inflammatory, and antinociceptive agents. The current investigation aims to study the molecular mechanism of varicocele-induced male infertility and the underlying pharmacological mechanisms of MAS. METHODS: Four groups were included: control (CTR), MAS 200 group (MAS 200 mg/kg), varicocele group (VC), and VC + MAS 200 group (MAS 200 mg/kg). Sprague-Dawley (SD) rats were treated with 200 mg/kg MAS or vehicle once daily for 28 days. The possible signaling mechanism and effects of MAS were measured via histological staining, immunohistochemistry, western blot, and biochemical assays. RESULTS: Parameters such as sperm motility and count, Johnsen's scores, spermatogenic cell density, serum testosterone, testicular superoxide dismutase (SOD), catalase, glutathione peroxidase (GPx) and expression of the steroidogenic acute regulatory protein (StAR) improved significantly in the VC + MAS 200 group compared with the VC group. MAS treatment of varicocele-induced group significantly decreased the levels of serum luteinizing hormone (LH) and follicle-stimulating hormone (FSH), as well as testicular interleukin-6 (IL6), tumor necrosis factor-α (TNF-α), ROS/RNS, and malondialdehyde (MDA). It also decreased the apoptotic index and reduced the expression of endoplasmic reticulum (ER) protein levels (Grp78, p-IRE1α, and p-JNK) and apoptotic markers such as cleaved caspase-3 and Bax/Bcl2 ratio. CONCLUSION: This study suggests that the crosstalk between oxidative stress, ER stress, and mitochondrial pathway mediates varicocele-induced testicular germ cell apoptosis. MAS promotes spermatogenesis in varicocele-induced SD rat, probably by decreasing cytokines (IL-6, TNF-α) levels, regulating abnormal sex hormones, and decreasing oxidative stress, ER stress, and apoptosis.


Asunto(s)
Iridoides/farmacología , Quempferoles/farmacología , Estrés Oxidativo/efectos de los fármacos , Quercetina/análogos & derivados , Varicocele/metabolismo , Animales , Antioxidantes/farmacología , Peso Corporal/efectos de los fármacos , Modelos Animales de Enfermedad , Estrés del Retículo Endoplásmico/efectos de los fármacos , Masculino , Mitocondrias/efectos de los fármacos , Tamaño de los Órganos/efectos de los fármacos , Quercetina/farmacología , Ratas , Ratas Sprague-Dawley , Transducción de Señal/efectos de los fármacos , Testículo/química , Testículo/efectos de los fármacos , Testículo/patología , Varicocele/patología
11.
Int J Nanomedicine ; 14: 6813-6830, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31692568

RESUMEN

Background: We recently showed that quercetin-conjugated iron oxide nanoparticles (QNPs) promoted the bioavailability of quercetin (Qu) in the brain of rats and improved the learning and memory of diabetic rats. In this study, we characterized the modifications in the antitoxic effects of Qu after conjugation. Materials and methods: We conjugated Qu to dextran-coated iron oxide nanoparticles (DNPs) and characterized DNPs and QNPs using FTIR, XRD, DLS, Fe-SEM, and EDX analyzes. The antiradical properties of Qu, DNPs, and QNPs were compared by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity assay. Catalase-like activities of DNPs and QNPs were estimated using catalase activity assay kit, and the antitoxic effects of Qu and QNPs were evaluated with spectrophotometry, MTT assay, flow cytometry, and real-time q-PCR. Results: Qu had a stronger anti-radical activity than DNPs and its activity decreased after being conjugated to DNPs. The catalase-like activity of DNPs remained intact after conjugation. DNPs had less toxicity on PC12 cells viabilities as compared to free Qu, and the conjugation of Qu with DNPs attenuated its cytotoxicity. Furthermore, MTT assay results indicated 24 h pretreatment with Qu had more protective effects than QNPs against H2O2-induced cytotoxicity, while Qu and QNPs had the same effects for 48 and 72 h incubation. Although the total antioxidant capacity of Qu was attenuated after conjugation, the results of flow cytometry and real-time q-PCR confirmed that 24 h pretreatment with the low concentrations of Qu and QNPs had the similar antioxidant, anti-inflammatory, and anti-apoptotic effects against the cytotoxicity of H2O2. Conclusion: Qu and QNPs showed the similar protective activities against H2O2-induced toxicity in PC12 cells. Given the fact that QNPs have magnetic properties, they may serve as suitable carriers to be used in neural research and treatment.


Asunto(s)
Antioxidantes/farmacología , Compuestos Férricos/química , Peróxido de Hidrógeno/toxicidad , Nanopartículas del Metal/uso terapéutico , Quercetina/farmacología , Animales , Antioxidantes/química , Antioxidantes/farmacocinética , Catalasa/farmacología , Dextranos/química , Liberación de Fármacos , Compuestos Férricos/farmacología , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/farmacología , Nanopartículas del Metal/química , Células PC12 , Quercetina/química , Quercetina/farmacocinética , Ratas , Espectroscopía Infrarroja por Transformada de Fourier , Difracción de Rayos X
12.
Life Sci ; 238: 116938, 2019 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-31593704

RESUMEN

AIMS: To investigate the effect of 7-O-geranylquercetin (GQ), a derivative of quercetin (Q), on reversing drug resistance in breast cancer MCF-7/ADR cells and reveal the mechanisms related to P-glycoprotein (P-gp). MAIN METHODS: Cell viability was determined by MTT assay. Accumulation of adriamycin (ADR) in cells was determined by confocal fluorescence microscope and microplate reader while that of rhodamine (Rh) was measured by flow cytometry. Expression levels of P-gp and MDR1 gene in cells were detected by western blot and Real-Time PCR, respectively. Molecular docking of GQ and Q with P-gp was conducted using AutoDock program. Xenograft model was established by inoculating MCF-7/ADR cells in BALB/c-nude mice. Tumor bearing mice were administered with ADR via tail vein injection and/or GQ (Q) by gavage. Expression levels of P-gp in tissues were detected by western blot and immunohistochemistry. KEY FINDINGS: GQ could reverse drug resistance of MCF-7/ADR cells to ADR. GQ inhibited the efflux of ADR by down-regulating the expression of P-gp protein and its encoding gene MDR1 in MCF-7/ADR cells. Molecular modeling showed that GQ matched with P-gp better than Q. GQ enhanced the antitumor effects of ADR and decreased the expression of P-gp in mice and its activities were higher than that of Q. GQ could reverse drug resistance of MCF-7/ADR cells by down-regulating the expression of P-gp in vitro and in vivo. SIGNIFICANCES: The reversal effect of GQ on P-gp-mediated drug resistance indicates its potential as a reversal agent for drug resistance in cancer chemotherapy.


Asunto(s)
Apoptosis/efectos de los fármacos , Neoplasias de la Mama/tratamiento farmacológico , Doxorrubicina/farmacología , Resistencia a Múltiples Medicamentos/efectos de los fármacos , Resistencia a Antineoplásicos/efectos de los fármacos , Quercetina/análogos & derivados , Subfamilia B de Transportador de Casetes de Unión a ATP/genética , Subfamilia B de Transportador de Casetes de Unión a ATP/metabolismo , Animales , Antibióticos Antineoplásicos/farmacología , Neoplasias de la Mama/metabolismo , Neoplasias de la Mama/patología , Proliferación Celular/efectos de los fármacos , Femenino , Humanos , Ratones , Ratones Endogámicos BALB C , Ratones Desnudos , Quercetina/farmacología , Células Tumorales Cultivadas , Ensayos Antitumor por Modelo de Xenoinjerto
13.
Life Sci ; 236: 116939, 2019 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-31593705

RESUMEN

Taxifolin (TAX) reportedly exerts protective and therapeutic effects in liver. Herein, the effects of TAX against acetaminophen (APAP)-induced hepatotoxicity were investigated. Pharmacodynamics, pharmacology and metabolomics analyses of TAX were assessed on C57 mice and L-02 cells. TAX was administered for 7 days, and APAP was given on the last day to establish an acute liver injury model. ALT and AST levels were determined, and liver ROS, MDA, GST, GSH and GPX1 were analysed. The expression and protein abundance of GPX1, GPS-Pi, GCLC and GCLM were assessed by PCR and western blotting, and metabolic changes in cells and serum were investigated by UPLC-Q-Orbitrap-MS. Serum ALT and AST, and liver ROS, MDA, GST, GSH and GPX1 levels confirmed the protective effects of TAX. Besides, we found Only treating with TAX decreased the expression of CYP2E1 in mice liver tissue. TAX reversed the APAP-induced decrease in cell viability in L-02 cells, and reduced cellular ROS levels. Furthermore, TAX reversed the APAP-induced decrease in antioxidant enzymes at both mRNA and protein levels. Metabolomics analysis identified metabolites mainly related to glutathione metabolism (36 in vivo and 23 in vitro). The concentration of glutathione, oxidized glutathione, carnitine, succinic acid, pyroglutamic acid, citrulline, taurine, palmitoleic acid, phytoshingosine-1-P and sphingosine-1-P were close to normal levels after treating with TAX. These results indicate that TAX prevents APAP-induced liver injury by inhibiting APAP metabolic activation mediated by CYP450 enzymes, modulating glutathione metabolism, and expression of related antioxidative signals. These properties could be harnessed to prevent or treat hepatotoxicity.


Asunto(s)
Acetaminofén/toxicidad , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Glutatión/metabolismo , Metaboloma , Sustancias Protectoras/farmacología , Quercetina/análogos & derivados , Analgésicos no Narcóticos/toxicidad , Animales , Antiinflamatorios no Esteroideos/farmacología , Enfermedad Hepática Inducida por Sustancias y Drogas/etiología , Enfermedad Hepática Inducida por Sustancias y Drogas/metabolismo , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Ratones , Ratones Endogámicos C57BL , Estrés Oxidativo/efectos de los fármacos , Quercetina/farmacología , Especies Reactivas de Oxígeno/metabolismo
14.
Drug Des Devel Ther ; 13: 3321-3329, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31571833

RESUMEN

Objective: This study aimed to evaluate the effect of quercetin and/or sitagliptin on testicular damage induced by doxorubicin (DOX). Methodology: Twenty-five male Wistar rats, weighing 240±20 g, were randomly divided into five groups as follows: a negative control group; that was treated with 1 mL of 0.9% sodium chloride; a DOX-treated group received Intraperitoneal (I.P.) DOX injection (3 mg/kg); a group treated with quercetin 80 mg/kg + sitagliptin 10 mg/kg + DOX; a group treated with quercetin 80 mg/kg + DOX; and a group treated with sitagliptin 10 mg/kg+ DOX. All treatment were given orally daily for 21 days with I.P. DOX 3 mg/kg injection for the treatment groups at days 8, 10, 12, 15, 17, and 19. On day 22, blood was collected for analysis of testosterone, luteinizing hormone (LH), follicle-stimulating hormone (FSH), alkaline phosphatase (ALP), lactate dehydrogenase (LDH), glutathione peroxidase (GPx), and total antioxidant capacity (TAOC). The testes were also removed and sent for histopathological examination. Results: The study revealed that the combination of quercetin with sitagliptin produced a significant increase in testosterone and FSH levels with a non-significant increase in LH level. This combination also non-significantly decreased the level of ALP and LDH and restored the GPx level with enhancing TAOC. Conclusion: The results suggest quercetin/sitagliptin combination as a promising therapeutic modality for attenuation of DOX-induced testicular toxicity in rats, and the main mechanism involved in such effect could be due to the antioxidant and anti-inflammatory properties of both agents.


Asunto(s)
Antibióticos Antineoplásicos/toxicidad , Doxorrubicina/toxicidad , Quercetina/farmacología , Fosfato de Sitagliptina/farmacología , Testículo/efectos de los fármacos , Fosfatasa Alcalina/sangre , Animales , Antioxidantes/metabolismo , Hormona Folículo Estimulante/sangre , Glutatión Peroxidasa/sangre , L-Lactato Deshidrogenasa/sangre , Hormona Luteinizante/sangre , Masculino , Estrés Oxidativo/efectos de los fármacos , Ratas , Ratas Wistar , Testículo/patología , Testosterona/sangre
15.
Sichuan Da Xue Xue Bao Yi Xue Ban ; 50(4): 533-539, 2019 Jul.
Artículo en Chino | MEDLINE | ID: mdl-31642231

RESUMEN

OBJECTIVE: To investigate the protective effect of (2R, 3R)-dihydroquercetin 7-O-ß-D-glucopyranose (C1) extracted from Coreopsis tinctoria Nutt. in a mouse model of alcoholic acute pancreatitis (FAEE-AP) induced byfatty acid ethyl ester (FAEE). METHODS: The 30 healthy SPF mice were randomly divided into control group, model group, low dose group, middle dose group and high dose group, 6 in each group. Alcoholic pancreatitis was induced by ethanol and palmitoleic acid administration (1.75 g/kg ethanol, 200 mg/kg palmitoleic acid, 2 times peritoneal injections). The three treatment groups were given C1 (0 h, 4 h, 8 h) at the dose of 12.5, 25 and 50 mg/kg, respectively. After 24 h of molding, the serum amylase, lipase and IL-6 levels were detected. The trypsin level in pancreatic tissue and myeloperoxidase (MPO) level in pancreatic and lung tissue were detected. Hematoxylin-eosin (HE) staining was used to observe the pathological changes of pancreatic tissue and immunohistochemical (IHC) staining was used to detect the expression of nuclear factor-erythroid 2 related factor 2 (Nrf2) in pancreatic tissue. RESULTS: The pancreatic histopathological scores, serum amylase and lipase activity, trypsin level in pancreatic tissue, serum IL-6 level, MPO level of pancreas and lung were significantly higher in the model group than in the control group (P < 0.01). Compared with the model group, the pancreatic histopathologies of the low dose group was significantly improved (P < 0.05), as well as the serum amylase and lipase activity, trypsin level of pancreas, serum IL-6 level, the pancreas andthe lung's MPO level decreased significantly (P < 0.05), and up-regulate that expression of Nrf2 in pancreatic tissue. CONCLUSION: 12.5 mg/kg of (2R, 3R) -dihydroquercetin 7-O-ß-D-glucopyranose (C1) improved the expression of Nrf2, reduced the expression of inflammatory factor IL-6, and protected acute pancreatitis caused by FAEE.


Asunto(s)
Coreopsis/química , Glicósidos/farmacología , Pancreatitis Alcohólica/tratamiento farmacológico , Quercetina/farmacología , Enfermedad Aguda , Animales , Modelos Animales de Enfermedad , Interleucina-6/metabolismo , Ratones , Factor 2 Relacionado con NF-E2/metabolismo , Páncreas , Quercetina/análogos & derivados , Distribución Aleatoria
16.
Life Sci ; 236: 116933, 2019 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-31614146

RESUMEN

AIMS: Hepatocellular carcinoma (HCC) pathogenesis involves the interplay of multiple signalling pathways. Notch and Hedgehog (Hh) are two major developmental pathways that act in concert to regulate adult cell repair. CK2α -serine-threonine kinase-down-regulation enhanced apoptotic activity and was proven beneficial for HCC patients. Quercetin is a bioactive flavonoid and has been shown to protect against HCC through its antioxidant activity. This study was carried out to elucidate the antineoplastic effect of quercetin through regulating both Notch and Hh pathways, apoptosis, cell proliferation and CK2α activity. MAIN METHODS: Hepatocellular carcinoma was induced in male Sprague Dawley rats by thioacetamide. Quercetin was administered in both protective and curative doses. Parameters of liver function and oxidative stress were assessed. CK2α, Notch and Hh pathways were evaluated using RT-PCR and ELISA. Apoptosis was investigated by detecting caspase-3, caspase-8 and p53. Proliferative and cell cycle markers as cyclin D1 and Ki-67 were detected immunohistochemically. KEY FINDINGS: Quercetin inhibited CK2α and downregulated mRNA and protein expression of Notch1 and Gli2. Quercetin also suppressed caspase-3 expression but not caspase-8. Quercetin elevated p53 expression whereas proliferative and cell cycle markers cyclin D1 and Ki-67 were downregulated. Markers of hepatic cellular integrity such as AST, ALT, ALP, GGT, albumin and bilirubin were significantly ameliorated. This was confirmed by histological examination. Quercetin also alleviated oxidative stress as shown by SOD, GSH, MDA and NO levels. SIGNIFICANCE: We can conclude that in addition to its antioxidant power, quercetin blocked Notch, Hedgehog, regulated the apoptotic and proliferative pathways and inhibited CK2α in HCC.


Asunto(s)
Antioxidantes/farmacología , Carcinoma Hepatocelular/metabolismo , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Neoplasias Hepáticas/metabolismo , Quercetina/farmacología , Transducción de Señal/efectos de los fármacos , Animales , Apoptosis/efectos de los fármacos , Carcinoma Hepatocelular/tratamiento farmacológico , Carcinoma Hepatocelular/patología , Quinasa de la Caseína II/antagonistas & inhibidores , Quinasa de la Caseína II/metabolismo , Proliferación Celular/efectos de los fármacos , Proteínas Hedgehog/antagonistas & inhibidores , Proteínas Hedgehog/metabolismo , Neoplasias Hepáticas/tratamiento farmacológico , Neoplasias Hepáticas/patología , Masculino , Estrés Oxidativo , Ratas , Ratas Sprague-Dawley , Receptores Notch/antagonistas & inhibidores , Receptores Notch/metabolismo
17.
Int J Nanomedicine ; 14: 6575-6585, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31616144

RESUMEN

Background and purpose: In a past study, we developed and optimized a novel cationic PEGylated niosome containing anticancer drugs (doxorubicin or quercetin) and siRNA. This study intended to evaluate the anti-tumor effects of the combination therapy to target both the proteins and genes responsible for the development of gastric cancer. CDC20, known as an oncogene, is a good potential therapeutic candidate for gastric cancer. Methods: In order to increase the loading capacity of siRNA and achieve appropriate physical properties, we optimized the cationic PEGylated niosome in terms of the amount of the cationic lipids. Drugs (doxorubicin and quercetin) and CDC20siRNA were loaded into the co-delivery system, and physical characteristics, thermosensitive controlled-release, gene silencing efficiency, and apoptosis rate were determined. Results: The results showed that the designed co-delivery system for the drugs and gene silencer had an appropriate size and a high positive charge for loading siRNA, and also showed a thermosensitive drug release behavior, which successfully silenced the CDC20 expression when compared with the single delivery of siRNA or the drug. Moreover, the co-delivery of drugs and CDC20siRNA exhibited a highly inhibitory property for the cell growth of gastric cancer cells. Conclusion: It seems that the novel cationic PEGylated niosomes co-loaded with anticancer drug and CDC20siRNA has a promising application for the treatment of gastric cancer.


Asunto(s)
Proteínas Cdc20/metabolismo , Doxorrubicina/uso terapéutico , Polietilenglicoles/química , Quercetina/uso terapéutico , ARN Interferente Pequeño/metabolismo , Neoplasias Gástricas/tratamiento farmacológico , Neoplasias Gástricas/metabolismo , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico , Apoptosis/efectos de los fármacos , Cationes , Proteínas Cdc20/genética , Línea Celular Tumoral , Doxorrubicina/farmacología , Liberación de Fármacos , Endocitosis , Ácidos Grasos Monoinsaturados/química , Silenciador del Gen/efectos de los fármacos , Humanos , Liposomas , Tamaño de la Partícula , Compuestos de Amonio Cuaternario/química , Quercetina/farmacología , ARN Interferente Pequeño/genética , Electricidad Estática , Temperatura Ambiental
18.
Int J Mol Sci ; 20(19)2019 Oct 08.
Artículo en Inglés | MEDLINE | ID: mdl-31597315

RESUMEN

Iodinated contrast media (CM) are the leading cause of acute renal failure of toxic origin. Between 21% and 50% of patients that receive them develop contrast-induced nephropathy (CIN). All prophylactic measures used so far have failed to provide effective prevention. Since oxidative stress is involved in the damage, a possible preventive strategy could be the administration of antioxidant substances, such as quercetin. This compound has shown renoprotective effects in experimental studies. The aim of this study was to evaluate whether quercetin may be helpful in preventing CIN in patients undergoing coronary catheterization. A clinical phase II study was conducted. Patients were distributed in two groups, namely, CM (patients who only received contrast media) and CM+Q (patients who were pretreated with quercetin orally for 3-5 days). Results showed less incidence of CIN in the CM+Q group, possibly due to glomerular protection, evidenced by a lower increase in serum creatinine and albuminuria; and a lower decrease in the glomerular filtration rate (GFR). Furthermore, in this group, the relative risk of developing CIN observed in patients that received a high dose of contrast media was inferior. In conclusion, this is the first study that demonstrates that quercetin is a promising safe candidate in preventing CIN.


Asunto(s)
Medios de Contraste/efectos adversos , Enfermedades Renales/etiología , Enfermedades Renales/prevención & control , Sustancias Protectoras/farmacología , Quercetina/farmacología , Anciano , Biomarcadores , Medios de Contraste/administración & dosificación , Medios de Contraste/clasificación , Creatinina/metabolismo , Femenino , Tasa de Filtración Glomerular/efectos de los fármacos , Humanos , Enfermedades Renales/diagnóstico , Enfermedades Renales/metabolismo , Masculino , Sustancias Protectoras/uso terapéutico , Quercetina/uso terapéutico
19.
BMC Complement Altern Med ; 19(1): 266, 2019 Oct 11.
Artículo en Inglés | MEDLINE | ID: mdl-31601198

RESUMEN

BACKGROUND: Propolis is a natural bee product with a wide range of biological activities that are related to its chemical composition. The present study investigated the quantification of quercetin (Q) in Ardabil ethanol extract of propolis (AEEP), and then compared its anti-bacterial, anti- biofilm and cytotoxic effects on cancer and normal cell lines. METHOD: In the present study, the chemical composition of AEEP was determined through the high-performance liquid chromatography (HPLC). The AEEP and its main component, quercetin (Q), were evaluated in vitro against 57 oral streptococci by a broth micro-dilution method. The biofilm formation was assessed through the crystal violet staining and MTT assays. The impact of AEEP and Q anti-proliferative effect were evaluated on the fibroblast as normal and cancer cell lines (KB and A431). RESULTS: The Q concentration in the composition of AEEP was 6.9% of all its components. The findings indicated that the AEEP and Q were efficient against the cariogenic bacteria and were able to inhibit the S.mutans biofilm adherence at a sub-MIC concentration. Moreover, electron micrographs indicated the inhibition of biofilms compared to control biofilms. In addition, the AEEP and Q indicated a dose-dependent cytotoxic effect on A431 and KB cell lines. On the contrary, they had no cytotoxic effect on fibroblast cells. CONCLUSION: The results indicated that the synergistic impact of main components of AEEP was related to the inhibition of the cancer cell proliferation, cariogenic bacteria and oral biofilm formation. It may play a promising role in the complementary medicine and, it is suggested to be used as food additives.


Asunto(s)
Antibacterianos/farmacología , Antineoplásicos/farmacología , Neoplasias/fisiopatología , Própolis/química , Streptococcus/efectos de los fármacos , Animales , Antibacterianos/análisis , Antineoplásicos/análisis , Abejas , Biopelículas/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Humanos , Irán , Pruebas de Sensibilidad Microbiana , Boca/microbiología , Neoplasias/tratamiento farmacológico , Quercetina/análisis , Quercetina/farmacología , Streptococcus/crecimiento & desarrollo
20.
Zhongguo Zhong Yao Za Zhi ; 44(17): 3786-3791, 2019 Sep.
Artículo en Chino | MEDLINE | ID: mdl-31602954

RESUMEN

It is reported that energy metabolism is the core feature of tumor cells. This study is aimed to investigate the regulatory effect of two flavonoids( glabridin and quercetin) on energy supply and glycolysis of breast cancer cells,and provide reference for developing some anticancer herbal drugs with the function of regulating tumor energy metabolism. Based on the characteristics of each pathway during energy metabolism,in the present study,the triple negative breast cancer tumor cells( MDA-MB-231) were selected to investigate the effects of glabridin and quercetin on the energy metabolism of breast cancer cells and discuss the possible mechanisms from the following five potential targets: glucose uptake,protein expression of glucose transporter 1( GLUT1),adenosine triphosphate( ATP) level,lactate dehydrogenase( LDH) activity,and lactic acid( LD) concentration. The results showed that both quercetin and glabridin could decrease the glucose uptake capacity of breast cancer cells by down-regulating the protein expression of GLUT1. Quercetin had no significant effect on LDH activity and LD concentration; it did not affect the glycolysis process,but increased the intracellular ATP level. Glabridin decreased the activity of LDH and reduced LD concentration,thereby inhibiting the glycolysis metabolism of breast cancer cells. Therefore,both quercetin and glabridin can regulate the energy metabolism of breast cancer cells and can be used as potential anticancer agents or anti-cancer adjuvants.


Asunto(s)
Neoplasias de la Mama/metabolismo , Metabolismo Energético , Isoflavonas/farmacología , Fenoles/farmacología , Quercetina/farmacología , Línea Celular Tumoral , Glucosa/metabolismo , Transportador de Glucosa de Tipo 1/metabolismo , Humanos
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