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1.
Bioresour Technol ; 302: 122845, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32000129

RESUMO

Plasticizer dibutyl phthalate (DBP) pollution has received more and more attention. In this study, a DBP degrading bacteria Enterobacter sp. DNB-S2 was found to suffer membrane damage and oxidative stress during DBP degradation. Physiological and transcriptome analysis showed that 100 µmol L-1 anthraquinone-2,6-disulfonate (AQDS) could enhance the ability of strain DNB-S2 for biodegradation of DBP. AQDS adjusted the cell surface structure, including increase levels of hydrophobic and unsaturated fatty acids. These changes increased the chemotactic ability of the strain DNB-S2 to the hydrophobic pollutant DBP and the fluidity of the cell membrane. The expression of methyl chemotactic protein and genes associated with cell membrane-fixed components were up-regulated. AQDS also improved the scavenging ability of ·OH and H2O2 of DNB-S2 by promoting expression genes related to glutathione metabolism, thereby reducing oxidative stress. These results will provide new insights into the biodegradation of DBP.


Assuntos
Dibutilftalato , Peróxido de Hidrogênio , Antraquinonas , Biodegradação Ambiental , Estresse Oxidativo
2.
Braz Oral Res ; 33: e117, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31939498

RESUMO

The aim of this study was to evaluate the effect of mineral trioxide aggregate (MTA) and Brazilian propolis on the cell viability, mineralization, anti-inflammatory ability, and migration of human dental pulp cells (hDPCs). The cell viability was evaluated with CCK-8 kit after 1, 5, 7, and 9 days. The deposition of calcified matrix and the expression of osteogenesis-related genes were evaluated by Alizarin Red staining and real-time PCR after incubation in osteogenic medium for 21 days. The expression of inflammation-related genes in cells was determined after exposure to 1 µg/mL LPS for 3 h. Finally, the numbers of cells that migrated through the permeable membranes were compared during 15 h. Propolis and MTA significantly increased the viability of hDPCscompared to the control group on days 7 and 9. In the propolis group, significant enhancement of osteogenic potential and suppressed expression of IL-1ß and IL-6 was observed after LPS exposure compared to the MTA and control groups. The number of migration cells in the propolis group was similar to that of the control group, while MTA significantly promoted cell migration. Propolis showed comparable cell viability to that of MTA and exhibited significantly higher anti-inflammatory and mineralization promotion effects on hDPCs.


Assuntos
Compostos de Alumínio/farmacologia , Anti-Inflamatórios/farmacologia , Compostos de Cálcio/farmacologia , Polpa Dentária/citologia , Polpa Dentária/efeitos dos fármacos , Óxidos/farmacologia , Própole/farmacologia , Silicatos/farmacologia , Antraquinonas , Brasil , Movimento Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Combinação de Medicamentos , Humanos , Interleucina-1beta/análise , Interleucina-6/análise , Odontoblastos/efeitos dos fármacos , Reação em Cadeia da Polimerase em Tempo Real , Reprodutibilidade dos Testes , Estatísticas não Paramétricas , Fator de Necrose Tumoral alfa/análise
3.
Chemosphere ; 238: 124539, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31470310

RESUMO

The performance and microbial community structure of anaerobic dynamic membrane bioreactor (AnDMBR) treating textile wastewater was investigated. The reactor showed excellent soluble COD and color removal of 98.5% and >97.5%, respectively. Dynamic membrane layer grown over the 3D printed dynamic membrane support showed decent rejection for high molecular weight compounds (>20 kDa); and the total suspended solid rejection by the dynamic layer was >98.8%. Gel permeation chromatography analysis of extracellular polymeric substance (EPS) and effluent samples revealed EPS accounted for more than 76.7% of low molecular weight fractions (<20 kDa) that end up in the effluent. Higher applied flux facilitated the rapid formation dynamic layer which enabled a satisfactory effluent quality. Microbial community analysis revealed that during the operation the archaeal community was relatively stable while obvious changes took place in the bacterial community. Introduction of dye Remazol Brilliant Blue R (RBBR) to the AnDMBR increased the abundances of phyla of Proteobacteria and Spirochaetae whereas fractions of Firmicutes and Euryarchaeota decreased obviously. Furthermore, relative stable abundances of phyla Aminicenantes, Bacteroidetes, Thermotogae and Chloroflexi among the top six phyla detected in the system ensured a healthy anaerobic degradation environment for RBBR wastewater treatment.


Assuntos
Antraquinonas/isolamento & purificação , Antraquinonas/metabolismo , Reatores Biológicos/microbiologia , Membranas Artificiais , Têxteis , Águas Residuárias/química , Anaerobiose , Corantes/isolamento & purificação , Corantes/metabolismo , Matriz Extracelular de Substâncias Poliméricas/microbiologia , Proteobactérias/metabolismo , Spirochaeta/metabolismo , Poluentes Químicos da Água/isolamento & purificação , Poluentes Químicos da Água/metabolismo
4.
Chemosphere ; 239: 124779, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31521934

RESUMO

Laccase mediator system (LMS), a very attractive candidate for refractory organics biodegradation, harbors tremendous potential on industry application. However, the performance of LMS usually varies with the discrepancy of mediators and substrates in their chemical structures. Here, we adopt electrochemical analysis that is able to assess the degradation performance of various LMS on three different dyes by quantitative analysis of reaction outcome. Two mechanisms were suggested to explain the grafting of three mediators (1-Hydroxybenzotriazole, Violuric Acid and Acetosyringone), involving the transformation of proton or electron to produce active moieties, which subsequently react with target substrates. A thorough electrochemical insight into the redox features of mediators and its change in the presence of laccase and substrates were carried out using electrochemical analysis. The effectiveness of each kind of LMS on substrates was preliminarily evaluated by analyzing the change of the peak current and potential of mediators. The actual conversion rate of dyes was used to verify the analysis results, which confirms the important role of the stability of the oxidized form as well as their redox potential of the mediators in determining the mechanism of substrate oxidation. The application of electrochemical analysis in efficiency evaluation of LMS shed new light on effective selection of suitable mediators for degradation of refractory organics. It was therefore possible to prejudge the efficacy of LMS by analyzing the electrochemical parameters of target substances and mediators, which undoubtedly has broad further application prospects of LMS.


Assuntos
Corantes/química , Lacase/química , Poluentes Químicos da Água/química , Acetofenonas/química , Antraquinonas/química , Barbitúricos/química , Biodegradação Ambiental , Cor , Vermelho Congo/química , Técnicas Eletroquímicas , Lacase/metabolismo , Oxirredução , Corantes de Rosanilina/química , Trametes/enzimologia , Triazóis/química
5.
Artigo em Inglês | MEDLINE | ID: mdl-31877432

RESUMO

Gandou Decoction (GDD), a well-known traditional Chinese medicine prescription, has been widely used for decades in clinical practice to treat Wilson's disease (WD) in China. However, due to lack of in vivo metabolism research, the absorbed components and metabolites of GDD have not been fully elucidated. In this study, a rapid and high-throughput ultra-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF-MSE) was applied to rapidly identify prototypes and metabolites after oral administration of GDD. On this basis, the possible metabolic pathways of the main prototypes were proposed between normal and copper-laden rats. As a result, a total of 89 GDD-related xenobiotics were detected in normal dosed rats, including 83 (36 prototypes and 47 metabolites) in plasma and 52 (21 prototypes and 31 metabolites) in liver; a total of 77 GDD-related xenobiotics were detected in copper-laden dosed rats, including 68 (31 prototypes and 37 metabolites) in plasma and 42 (19 prototypes and 23 metabolites) in liver. Our findings showed that anthraquinones, alkaloids and protostane triterpenoids as well as a few saponins, flavonoids, tannins and curcuminoids were the main absorbed chemical components of GDD in rat plasma; anthraquinones, protostane triterpenoids and curcuminoids were the major components in rat liver. Glucuronidation and sulfation were deduced to be the predominant metabolic pathways of GDD. Methylation, acetylation, reduction, hydroxylation, demethylation and deglycosylation were often occurred in the metabolic process. Furthermore, the holistic metabolic profile of GDD revealed that copper-laden rats and normal rats had certain differences in drug absorption and metabolism. This study offered a solid basis for ascertaining bioactive components and action mechanism of GDD.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas , Fígado , Espectrometria de Massas em Tandem/métodos , Alcaloides/análise , Alcaloides/farmacocinética , Animais , Antraquinonas/análise , Antraquinonas/farmacocinética , Cobre/administração & dosagem , Cobre/efeitos adversos , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/farmacocinética , Medicamentos de Ervas Chinesas/farmacologia , Fígado/efeitos dos fármacos , Fígado/metabolismo , Metaboloma/efeitos dos fármacos , Metabolômica , Ratos , Triterpenos/análise , Triterpenos/farmacocinética
6.
Chem Commun (Camb) ; 55(100): 15129-15132, 2019 Dec 12.
Artigo em Inglês | MEDLINE | ID: mdl-31788680

RESUMO

Here, a reaction-based indicator displacement hydrogel assay (RIA) was developed for the detection of hydrogen peroxide (H2O2) via the oxidative release of the optical reporter Alizarin Red S (ARS). In the presence of H2O2, the RIA system displayed potent biofilm inhibition for Methicillin-resistant Staphylococcus aureus (MRSA), as shown through an in vitro assay quantifying antimicrobial efficacy. This work demonstrated the potential of H2O2-responsive hydrogels containing a covalently bound diol-based drug for controlled drug release.


Assuntos
Antraquinonas/química , Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Peróxido de Hidrogênio/química , Staphylococcus aureus Resistente à Meticilina/fisiologia , Antraquinonas/farmacologia , Antibacterianos/química , Escherichia coli/efeitos dos fármacos , Hidrogéis/química , Hidrogéis/farmacologia , Testes de Sensibilidade Microbiana , Pseudomonas aeruginosa/efeitos dos fármacos , Solubilidade
7.
BMC Complement Altern Med ; 19(1): 364, 2019 Dec 11.
Artigo em Inglês | MEDLINE | ID: mdl-31829180

RESUMO

BACKGROUND: The body responds to overnutrition by converting stem cells to adipocytes. In vitro and in vivo studies have shown polyphenols and other natural compounds to be anti-adipogenic, presumably due in part to their antioxidant properties. Purpurin is a highly antioxidative anthraquinone and previous studies on anthraquinones have reported numerous biological activities in cells and animals. Anthraquinones have also been used to stimulate osteoblast differentiation, an inversely-related process to that of adipocyte differentiation. We propose that due to its high antioxidative properties, purpurin administration might attenuate adipogenesis in cells and in mice. METHODS: Our study will test the effect purpurin has on adipogenesis using both in vitro and in vivo models. The in vitro model consists of tracking with various biomarkers, the differentiation of pre-adipocyte to adipocytes in cell culture. The compound will then be tested in mice fed a high-fat diet. Murine 3T3-L1 preadipocyte cells were stimulated to differentiate in the presence or absence of purpurin. The following cellular parameters were measured: intracellular reactive oxygen species (ROS), membrane potential of the mitochondria, ATP production, activation of AMPK (adenosine 5'-monophosphate-activated protein kinase), insulin-induced lipid accumulation, triglyceride accumulation, and expression of PPARγ (peroxisome proliferator activated receptor-γ) and C/EBPα (CCAAT enhancer binding protein α). In vivo, mice were fed high fat diets supplemented with various levels of purpurin. Data collected from the animals included anthropometric data, glucose tolerance test results, and postmortem plasma glucose, lipid levels, and organ examinations. RESULTS: The administration of purpurin at 50 and 100 µM in 3T3-L1 cells, and at 40 and 80 mg/kg in mice proved to be a sensitive range: the lower concentrations affected several measured parameters, whereas at the higher doses purpurin consistently mitigated biomarkers associated with adipogenesis, and weight gain in mice. Purpurin appears to be an effective antiadipogenic compound. CONCLUSION: The anthraquinone purpurin has potent in vitro anti-adipogenic effects in cells and in vivo anti-obesity effects in mice consuming a high-fat diet. Differentiation of 3T3-L1 cells was dose-dependently inhibited by purpurin, apparently by AMPK activation. Mice on a high-fat diet experienced a dose-dependent reduction in induced weight gain of up to 55%.


Assuntos
Adipogenia/efeitos dos fármacos , Antraquinonas/farmacologia , Fármacos Antiobesidade/farmacologia , Dieta Hiperlipídica , Células 3T3-L1 , Tecido Adiposo/efeitos dos fármacos , Animais , Antioxidantes/farmacologia , Peso Corporal/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/metabolismo
8.
Sichuan Da Xue Xue Bao Yi Xue Ban ; 50(6): 840-846, 2019 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-31880115

RESUMO

OBJECTIVE: To investigate the regulatory effect and its mechanism of chrysophanol (CP) on renal injury and immune response in immunoglobin A (IgA) nephropathy rats. METHODS: IgA nephropathy rat model was established by the method of lipopolysaccharide + bovine serum protein + carbon tetrachloride. Then the rats were randomly divided into 5 groups: control group, IgA group, IgA+low, medium and high dose of CP groups(2.5, 5 and 10 mg/kg for each group respectively). IgA+CP groups were intraperitoneally injected with different doses of chrysophanol once a day for 4 weeks, and the control group and IgA group were given isovolumetric saline. Urine protein content, serum creatinine and urea nitrogen were detected at 24 h after the administration of drugs. Kidney histopathological damage and apoptosis were measured by HE and TUNEL staining. The expression levels of Caspase-3 and Caspase-9 were detected by RT-PCR and Western blot; The contents of malondialdehyde (MDA), superoxide dismutase (SOD) and (glutathione peroxidase, Gpx) were detected by enzyme-linked immunosorbent assay (ELISA). The expression of interleukin-1ß, -6 (IL-1ß, IL-6) and tumor necrosis factor (TNF-α) in serum and kidney tissue were measured by ELISA and Western blot, respectively. The mRNA and protein expression levels of toll-like receptro 4 (TLR4), nuclear factor-κB P65 (NF-κB P65) were also detected by RT-PCR and Western blot, and vascular cell adherin molecule (VCAM-1) protein level was deteted by Western blot. RESULTS: In IgA nephropathy rats, the administration of CP reduced proteinuria, serum creatinine and urea nitrogen in a dose-dependent manner (P < 0.01). It also improved the pathological damage of kidney tissue, reduced the apoptosis rate (P < 0.01), and decreased the mRNA and protein expression levels of apoptosis-related proteins Caspase-3 and Caspase-9 (P < 0.01). CP inhibited MDA production while increased the activities of antioxidant enzymes Gpx and SOD (P < 0.01), and decreased the levels of serum and protein expression of IL-1ß, IL-6 and TNF-α (P < 0.01), as well as the expression levels of TLR4, NF-κB P65 and VCAM-1 (P < 0.01). CONCLUSION: Chrysophanol could play a protective role in IgA nephropathy rats, and its mechanism may be related to alleviating kidney injury and regulating immune response.


Assuntos
Glomerulonefrite por IGA , Animais , Antraquinonas , Bovinos , Rim , NF-kappa B , Ratos , Receptor 4 Toll-Like , Fator de Necrose Tumoral alfa
9.
J Agric Food Chem ; 67(50): 13998-14004, 2019 Dec 18.
Artigo em Inglês | MEDLINE | ID: mdl-31747274

RESUMO

The contents of anthraquinone (ATQ) and polycyclic aromatic hydrocarbons (anthracene (ANT) and PAH4) in smoked Frankfurter-style sausages were investigated depending on various smoking conditions. During smoking, the smoke generator, the smoking duration, the type of wood, and some more plant-specific parameters were tested. The sausages were also barbecued on a charcoal grill. The lowest mean contents of all analytes were observed when friction smoke was used (ATQ < limit of quantification (LOQ); ANT < LOQ; PAH4 < limit of detection (LOD)) and the highest when the settings of ventilations flaps were changed (ANT 36.3 µg/kg; PAH4 2.2 µg/kg) or at an intensive smoke density (ATQ 3.2 µg/kg). The contents increased with the smoking time, but irregularities were detected after 10 min. The use of different types of wood had no influence on the ATQ content but affected the PAH content. In barbecued samples, ATQ and ANT contents were detected at the level of friction smoke and maximum PAH4 contents were found above the exposure during smoking. Due to the varying influence of the smoking parameters on the two analytes, there was no direct correlation between the contents of ATQ and ANT in all smoking experiments.


Assuntos
Antraquinonas/química , Culinária/métodos , Produtos da Carne/análise , Hidrocarbonetos Policíclicos Aromáticos/química , Animais , Carvão Vegetal/química , Culinária/instrumentação , Contaminação de Alimentos/análise , Temperatura Alta , Fumaça/análise , Suínos , Madeira/química
10.
Planta Med ; 85(14-15): 1143-1149, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31559608

RESUMO

Rhein, an anthraquinone extracted from rhubarb, is used in traditional Chinese medicine for diuresis, diarrhoea, inflammation, and immune regulation. Atezolizumab, a programmed cell death ligand 1 monoclonal antibody, is mainly used to treat bladder cancer and non-small cell lung cancer unresponsive to chemotherapy. We explored the effects of rhein and atezolizumab in combination on breast cancer. Mice with established 4T1 breast cancer xenografts were administered rhein (10 mg/kg) and atezolizumab (10 mg/kg), alone and in combination, and the effects on tumour growth were evaluated. The proportion of CD8+ T cells in the spleen and tumour tissue, the levels of TNF-α, and interleukin-6 in serum as well as the mRNA levels of apoptotic factors (caspase-3, caspase-8, caspase-9, and Bax/Bcl-2) were also evaluated. All of the treatment groups had inhibitory effects on the xenograft tumour growth, with results that were significantly different from those in the control group. In addition, the proportion of CD8+ T cells in the spleen and tumour was significantly increased in the combination therapy group and was significantly different from the other treatment groups. The serum levels of TNF-α and IL-6 were significantly increased in the rhein and combination therapy groups. Finally, the levels of various apoptotic factors in tumour tissues were significantly higher in the combination treatment group than those in the other groups. Administration of rhein, atezolizumab, or their combination all had therapeutic effects on 4T1 breast cancer xenografts in mice, with the combination treatment having stronger effects.


Assuntos
Antraquinonas/administração & dosagem , Anticorpos Monoclonais Humanizados/administração & dosagem , Neoplasias da Mama/tratamento farmacológico , Inibidores de Caspase/administração & dosagem , Caspases/efeitos dos fármacos , Inibidores Enzimáticos/administração & dosagem , Rheum/química , Animais , Antraquinonas/química , Inibidores de Caspase/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Quimioterapia Combinada , Inibidores Enzimáticos/química , Feminino , Xenoenxertos , Humanos , Medicina Tradicional Chinesa , Camundongos , Camundongos Endogâmicos BALB C
11.
Org Biomol Chem ; 17(38): 8711-8715, 2019 10 14.
Artigo em Inglês | MEDLINE | ID: mdl-31549123

RESUMO

A chemoenzymatic reduction of citreorosein by the NADPH-dependent polyhydroxyanthracene reductase from Cochliobolus lunatus or MdpC from Aspergillus nidulans in the presence of Na2S2O4 gave access to putative biosynthetic intermediates, (R)-3,8,9,10-tetrahydroxy-6-(hydroxymethyl)-3,4-dihydroanthracene-1(2H)-one and its oxidized form, (R)-3,4-dihydrocitreorosein. Herein, we discuss the implications of these results towards the (bio)synthesis of aloe-emodin and (+)-rugulosin C in fungi.


Assuntos
Antraquinonas/metabolismo , Proteínas Fúngicas/metabolismo , Oxirredutases atuantes sobre Doadores de Grupo CH-CH/metabolismo , Antraquinonas/química , Ascomicetos/enzimologia , Proteínas Fúngicas/química , Estrutura Molecular , Oxirredução , Oxirredutases atuantes sobre Doadores de Grupo CH-CH/química
12.
Bioresour Technol ; 293: 122100, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31518817

RESUMO

Alizarin Red S (ARS) has been extensively used in the dyeing industry. In order to effectively remove the ARS form dyeing wastewater, polyethyleneimine (PEI)-functionalized magnetic carbon nanotubes (PEI@MCNTs) adsorbent was successfully prepared and its adsorption performances were also investigated in detail. The PEI@MCNTs could efficiently remove the ARS from acidic aqueous solution (pH ≤ 6.0) within 40 min under room temperature. Benefiting from a large number of adsorption sites and multiple interactions, PEI@MCNTs possessed high selectivity towards ARS with spontaneous adsorption process. The maximum adsorption capacity of PEI@MCNTs for ARS was 196.08 mg g-1 obtained from Langmuir isotherm, higher than that of available conventional adsorbents. Moreover, the PEI@MCNTs could be easily collected by an external magnet, and then effectively regenerated through 10 mM NaOH solution. The prepared PEI@MCNTs could be considered as the promising adsorbent for the removal of anthraquinone dyes in large-scale wastewater treatment.


Assuntos
Nanotubos de Carbono , Poluentes Químicos da Água , Adsorção , Antraquinonas , Cinética , Polietilenoimina
13.
J Biosci ; 44(4)2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31502566

RESUMO

4,5-Dihydroxyanthraquinone-2-carboxylic acid (Rhein) has been shown to have various physiological and pharmacological properties including anticancer activity and modulatory effects on bioenergetics. In this study, we explored the impact of rhein on protein profiling of undifferentiated (UC) and differentiated (DC) SH-SY5Y cells. Besides that, the cellular morphology and expression of differentiation markers were investigated to determine the effect of rhein on retinoic acidinduced neuronal cell differentiation. Using two-dimensional gel electrophoresis and matrix-assisted laser desorption/ ionization-time-of-flight mass spectrometry we evaluated the changes in the proteome of both UC and DC SH-SY5Y cells after 24 h treatment with rhein. Validation of selected differentially expressed proteins and the assessment of neuronal differentiation markers were performed by western blotting. Proteomic analysis revealed significant changes in the abundance of 15 proteins linked to specific cellular processes such as cytoskeleton structure and regulation, mitochondrial function, energy metabolism, protein synthesis and neuronal plasticity. We also observed that the addition of rhein to the cultured cells during differentiation resulted in a significantly reduced neurite outgrowth and decreased expression of neuronal markers. These results indicate that rhein may strongly interfere with the differentiation process of SH-SY5Y neuroblastoma cells and is capable of inducing marked proteomic changes in these cells.


Assuntos
Antraquinonas/farmacologia , Diferenciação Celular/efeitos dos fármacos , Neuroblastoma/tratamento farmacológico , Proteômica , Linhagem Celular Tumoral , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Células-Tronco Neurais/efeitos dos fármacos , Neuritos/efeitos dos fármacos , Neuritos/patologia , Neuroblastoma/genética , Neuroblastoma/patologia , Crescimento Neuronal/efeitos dos fármacos , Neurônios/efeitos dos fármacos
14.
Biol Res ; 52(1): 50, 2019 Sep 06.
Artigo em Inglês | MEDLINE | ID: mdl-31492196

RESUMO

BACKGROUND: Ureteral obstruction causes injury of the renal tissues and can irreversibly progress to renal fibrosis, with atrophy and apoptosis of tubular cells. The goal of the current study was to examine the effects of rhein on the apoptosis o renal tubular cells as well as renal fibrosis using a rodent model of unilateral ureteral obstruction (UUO). METHODS: UUO was induced through ureteral ligation, then animals received treatments with rhein or vehicle. The control rats only received sham operation. The renal tissue was harvested 1 week after surgery for assessment of kidney fibrosis. RESULTS: The expressions of collagen I and α-smooth muscle actin (α-SMA), as well as the severity of renal tubular apoptosis and fibrosis were time-dependently increased following UUO. Treatments with rhein partially inhibited such responses. Renal interstitial fibrosis was associated with STAT3 (signal transducer and activator of transcription 3) phosphorylation as well as altered expressions of Bax and Bcl2, both apoptosis-related proteins. Treatment with rhein also partly blocked these responses. CONCLUSION: These findings demonstrated that rhein mitigated apoptosis of renal tubular cell as well as renal fibrosis in a UUO rodent model. This curative effect is likely mediated via suppression of STAT3 phosphorylation.


Assuntos
Antraquinonas/administração & dosagem , Apoptose/efeitos dos fármacos , Rim/patologia , Obstrução Ureteral/prevenção & controle , Animais , Modelos Animais de Doenças , Progressão da Doença , Fibrose/metabolismo , Fibrose/patologia , Fibrose/prevenção & controle , Masculino , Fosforilação , Ratos , Ratos Sprague-Dawley , Fator de Transcrição STAT3/metabolismo , Obstrução Ureteral/metabolismo , Obstrução Ureteral/patologia
15.
Phytother Res ; 33(11): 2960-2970, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31410907

RESUMO

Although the approved hepatitis B virus (HBV)-polymerase inhibitors (e.g., lamivudine) often lead to drug-resistance, several natural products have shown promising efficacies. Though Aloe vera (AV) gel and its constituents are shown inhibitors of many viruses, their anti-HBV activity still remains elusive. We therefore, tested the anti-HBV potential of AV extract and its anthraquinones in hepatoma cells, including molecular docking, high-performance thin layer chromatography (HPTLC), and cytochrome P450 (CYP3A4) activation analyses. Our anti-HBV assays (HBsAg/HBeAg Elisa) showed maximal inhibition of viral antigens production by aloe-emodin (~83%) > chrysophanol (~62%) > aloin B (~61%) > AV extract (~37%) in HepG2.2.15 cells. Interestingly, the effect of aloe-emodin was comparable with lamivudine (~86%). Moreover, sequential treatment with lamivudine (pulse) followed by aloe-emodin (chase) enhanced the efficacy of monotherapy by ~12%. Docking (AutoDock Vina) of the anthraquinones indicated strong interactions with HBV-polymerase residues that formed stable complexes with high Gibbs's free energy. Further, identification of aloe-emodin and aloin B by validated HPTLC in AV extract strongly endorsed its anti-HBV potential. In addition, our luciferase-reporter gene assay of transfected HepG2 cells showed moderate induction of CYP3A4 by aloe-emodin. In conclusion, this is the first report on anti-HBV potential of AV-derived anthraquinones, possibly via HBV-polymerase inhibition. Of these, although aloin B exhibits novel antiviral effect, aloe-emodin appears as the most promising anti-HBV natural drug with CYP3A4 activating property towards its enhanced therapeutic efficacy.


Assuntos
Aloe/química , Antraquinonas/uso terapêutico , Vírus da Hepatite B/efeitos dos fármacos , Hepatite B/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Antraquinonas/farmacologia , Antivirais/farmacologia , Antivirais/uso terapêutico , Linhagem Celular , Emodina/análogos & derivados , Emodina/farmacologia , Emodina/uso terapêutico , Células Hep G2 , Humanos , Fitoterapia/métodos , Extratos Vegetais/farmacologia
16.
Nat Commun ; 10(1): 3443, 2019 08 01.
Artigo em Inglês | MEDLINE | ID: mdl-31371724

RESUMO

Self-assembly of twelve pentatopic tectons, which have complementary edges or can be linked using either digonal or trigonal connectors, represents the optimal synthetic strategy to achieve spherical objects, such as chemical capsids. This process requires conditions that secure uninterrupted equilibria of binding and self-correction en route to the global energy minimum. Here we report the synthesis of a highly soluble, deca-heterosubstituted corannulene that bears five terpyridine ligands. Spontaneous self-assembly of twelve such tectons with 30 cadmium(II) cations produces a giant icosahedral capsid as a thermodynamically stable single product in high yield. Nuclear magnetic resonance (NMR) methods, mass spectrometry analyses, small-angle X-ray scattering, transmission electron microscopy, and atomic force microscopy indicate that this spherical capsid has an external diameter of nearly 6 nm and shell thickness of 1 nm, in agreement with molecular modeling. NMR and liquid chromatography evidences imply that chiral self-sorting complexation generates a racemic mixture of homochiral capsids.


Assuntos
Proteínas do Capsídeo/metabolismo , Capsídeo/química , Hidrocarbonetos Policíclicos Aromáticos/metabolismo , Montagem de Vírus/fisiologia , Antraquinonas , Cádmio/metabolismo , Modelos Moleculares , Termodinâmica
17.
Anal Chim Acta ; 1081: 131-137, 2019 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-31446950

RESUMO

In the absence of adequate reference material, a problem often encountered in natural product chemistry, we investigated the use of surrogate standards in two-dimensional qNMR for the quantification of anthraquinones in the bark of alder buckthorn (Frangula alnus). Using the integrals of cross signals in the HSQC spectrum obtained from commercial standards rutin and duroquinone and adapting the delays for the 1JCH coupling, we quantified the total amount of anthraquinones and anthraquinone glucosides, as well as the content of the value-determining glucofrangulins and frangulins. Thereby, duroquinone was used as an external standard to establish the calibration curve for the methylated anthraquinone scaffold, whereas calibration curves for the glycosides were obtained using the anomeric proton signals of the rutinose disaccharide. The method was validated for accuracy, precision, specificity, linearity and limit of quantitation and shows clear advantages over the method of the European Pharmacopeia, especially in terms of specificity and meaningfulness of the results. Apart from being a useful alternative in the quality control of alder buckthorn, the presented approach demonstrates, moreover, the versatility of sophisticated 2D measurements in quantitative NMR.


Assuntos
Antraquinonas/análise , Glicosídeos/análise , Rhamnus/química , Benzoquinonas/normas , Espectroscopia de Ressonância Magnética/métodos , Espectroscopia de Ressonância Magnética/normas , Padrões de Referência , Rutina/normas
18.
J Microbiol Biotechnol ; 29(9): 1383-1390, 2019 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-31434174

RESUMO

In this study, we expressed cotA laccase from Bacillus subtilis on the surface of B. subtilis spores for efficient decolorization of synthetic dyes. The cotE, cotG, and cotY genes were used as anchoring motifs for efficient spore surface display of cotA laccase. Moreover, a His6 tag was inserted at the C-terminal end of cotA for the immunological detection of the expressed fusion protein. Appropriate expression of the CotE-CotA (74 kDa), CotG-CotA (76 kDa), and CotY-CotA (73 kDa) fusion proteins was confirmed by western blot. We verified the surface expression of each fusion protein on B. subtilis spore by flow cytometry. The decoloration rates of Acid Green 25 (anthraquinone dye) for the recombinant DB104 (pSDJH-EA), DB104 (pSDJH-GA), DB104 (pSDJH-YA), and the control DB104 spores were 48.75%, 16.12%, 21.10%, and 9.96%, respectively. DB104 (pSDJH-EA) showed the highest decolorization of Acid Green 25 and was subsequently tested on other synthetic dyes with different structures. The decolorization rates of the DB104 (pSDJH-EA) spore for Acid Red 18 (azo dye) and indigo carmine (indigo dye) were 18.58% and 43.20%, respectively. The optimum temperature for the decolorization of Acid Green 25 by the DB104 (pSDJH-EA) spore was found to be 50°C. Upon treatment with known laccase inhibitors, including EDTA, SDS, and NaN3, the decolorization rate of Acid Green 25 by the DB104 (pSDJH-EA) spore decreased by 23%, 80%, and 36%, respectively.


Assuntos
Antraquinonas/metabolismo , Bacillus subtilis/enzimologia , Corantes/metabolismo , Lacase/metabolismo , Bacillus subtilis/genética , Bacillus subtilis/metabolismo , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismo , Biodegradação Ambiental , Inibidores Enzimáticos/química , Expressão Gênica , Cinética , Lacase/antagonistas & inibidores , Lacase/genética , Proteínas Recombinantes de Fusão/genética , Proteínas Recombinantes de Fusão/metabolismo , Esporos Bacterianos/enzimologia , Esporos Bacterianos/genética , Esporos Bacterianos/metabolismo , Temperatura Ambiente
19.
Molecules ; 24(16)2019 Aug 20.
Artigo em Inglês | MEDLINE | ID: mdl-31434258

RESUMO

Herein, a direct strategy to synthesize 3-(2-hydroxybenzoyl)-1-aza-anthraquinones with excellent efficiency, mild conditions, and benign functional group compatibility was reported. A variety of 3-formylchromone compounds were employed as compatible substrates and this protocol gave the 3-(2-hydroxybenzoyl)-1-aza-anthraquinone derivatives in good to excellent yields without inert gas and expensive transition metal catalysts. Some compounds displayed good anti-proliferative activities.


Assuntos
Antraquinonas/síntese química , Antineoplásicos/síntese química , Antraquinonas/química , Antraquinonas/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Proliferação de Células , Técnicas de Química Sintética , Ensaios de Seleção de Medicamentos Antitumorais , Células HT29 , Células HeLa , Humanos , Metais , Estrutura Molecular
20.
Environ Toxicol ; 34(12): 1292-1302, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31436023

RESUMO

Rhein (4,5-dihydroxyanthraquinone-2-carboxylic acid) is a major component of many medicinal herbs such as Rheum palmatum L. and Polygonum multiflorum. Despite being widely used, intoxication cases associated with rhein-containing herbs are often reported. Currently, there are no available reports addressing the effects of rhein on apoptosis in human liver L02 cells. Thus, the aim of this study is to determine the cytotoxic effects and the underlying mechanism of rhein on human normal liver L02 cells. In the present study, the methyl thiazolyl tetrazolium assay demonstrated that rhein decreased the viability of L02 cells in dose-dependent and time-dependent ways. Rhein was found to trigger apoptosis in L02 cells as shown by Annexin V-fluoresceine isothiocyanate (FITC) apoptosis detection kit and cell mitochondrial membrane potential (MMP) assay, with nuclear morphological changes demonstrated by Hoechst 33258 staining. Detection of intracellular superoxide dismutase activity, lipid oxidation (malondialdehyde) content, and reactive oxygen species (ROS) levels showed that apoptosis was associated with oxidative stress. Moreover, it was observed that the mechanism implicated in rhein-induced apoptosis was presumably via the death receptor pathway and the mitochondrial pathway, as illustrated by upregulation of TNF-α, TNFR1, TRADD, and cleaved caspase-3, and downregulation of procaspase-8, and it is suggested that rhein may increase hepatocyte apoptosis by activating the increase of TNF-α level. Meanwhile, rhein upregulates the expression of Bax and downregulates the expression of procaspase-9 and -3, and it is suggested that the mitochondrial pathway is activated and rhein-induced apoptosis may be involved. In addition, we also want to explore whether rhein-induced apoptosis is related to the autophagic changes induced by rhein. The results showed that rhein treatment increased P62 and decreased LC3-II and beclin-1, which means that autophagy was weakened. The results of our studies indicated that rhein induced caspase-dependent apoptosis via both the Fas death pathway and the mitochondrial pathway by generating ROS, and meanwhile the autophagy tended to weaken.


Assuntos
Antraquinonas/toxicidade , Apoptose/efeitos dos fármacos , Autofagia/efeitos dos fármacos , Proteínas Adaptadoras de Sinalização de Receptores de Domínio de Morte/metabolismo , Mitocôndrias/efeitos dos fármacos , Caspase 3/metabolismo , Células Cultivadas , Regulação da Expressão Gênica/efeitos dos fármacos , Hepatócitos/citologia , Hepatócitos/metabolismo , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Rheum/química , Rheum/metabolismo , Superóxido Dismutase/metabolismo
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