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1.
Food Chem ; 311: 125948, 2020 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-31877545

RESUMO

The increasing incidence of metabolic syndrome requires more functional food products with low cost and excellent effects to assist treatment. The crude extract of Moringa oleifera Lam. showed excellent hypoglycemic activity. The current study was designed to investigate the effects and mechanism of niazirin, a bioactive component from Moringa oleifera Lam. seed, on diabetic metabolic syndrome. C57BL/6J mice were treated daily with 5 mL/kg/body weight (BW) of saline, while db/db mice were similarly treated with 5 mL/kg/BW of saline, 10 and 20 mg/kg/BW of niazirin, respectively. Results indicated that niazirin could significantly reduce body weight, water and food intake, improve hyperglycemia, insulin resistance, inflammation, carbohydrate and lipid metabolism, non-alcoholic fatty liver. Furthermore, niazirin improved the hepatic energy metabolism via AMPK signaling pathway. Our study provides an evidence of an edible plant product, niazirin, may help in the treatment of metabolic syndrome.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Diabetes Mellitus/tratamento farmacológico , Glicosídeos/administração & dosagem , Hipoglicemiantes/administração & dosagem , Metabolismo dos Lipídeos/efeitos dos fármacos , Moringa oleifera/química , Fenóis/administração & dosagem , Extratos Vegetais/administração & dosagem , Proteínas Quinases Ativadas por AMP/genética , Animais , Diabetes Mellitus/genética , Diabetes Mellitus/metabolismo , Humanos , Resistência à Insulina , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Sementes/química
2.
Medicine (Baltimore) ; 98(47): e17976, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31764805

RESUMO

BACKGROUND: According to the centers for disease control and prevention, 14% of American adults have diabetes - 10% know it, and more than 4% go undiagnosed. Sotagliflozin is a new type of diabetes drug This study is to compare the efficacy of Sotagliflozin therapy for Diabetes Mellitus (DM) between week 24 with week 52. METHODS AND ANALYSIS: Through to October 2019, Web of Science, PubMed Database, Cochrane Library, EMBASE, Clinical Trials and CNKI will be searched to identify randomized controlled trials (RCTs) exploring SOTA therapy for DM. Strict screening and quality evaluation will be performed on the obtained literature independently by 2 researchers; outcome indexes will be extracted. The bias risk of the included studies will be evaluated based on Cochrane assessment tool. Meta-analysis will be performed on the data using Revman 5.3 software. We will provide practical and targeted results assessing the lost efficacy of SOTA therapy for DM from week 24 to week 52, to provide reference for clinicians. ETHICS AND DISSEMINATION: The stronger evidence about the lost efficacy of SOTA for DM from week 24 to week 52 will be provided for clinicians. TRIAL REGISTRATION NUMBER: PROSPERO CRD42019133027. STRENGTHS AND LIMITATIONS OF THIS STUDY: Whether the efficacy of SOTA could last for a long time is still inconclusive, high quality research is still lacking, and this study attempts to explore this issue; The efficacy of SOTA at different times will be compared by direct comparisons and indirect comparisons, this can lead to more accurate and reliable results; The quality of the included literatures are uneven, and some data might be estimated by calculation, which may affect the quality of this study.


Assuntos
Diabetes Mellitus/tratamento farmacológico , Glicosídeos/administração & dosagem , Metanálise como Assunto , Metanálise em Rede , Projetos de Pesquisa , Inibidores do Transportador 2 de Sódio-Glicose/administração & dosagem , Esquema de Medicação , Humanos , Ensaios Clínicos Controlados Aleatórios como Assunto , Fatores de Tempo , Resultado do Tratamento
3.
Zhongguo Zhong Yao Za Zhi ; 44(16): 3502-3511, 2019 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-31602915

RESUMO

The aim of this paper was to compare the properties of Tripterygium Glycosides Tablets and Tripterygium wilfordii Tablets from dose-effect-toxicity on type Ⅱ collagen-induced arthritis( CIA) in rats. SD rats were randomly divided into eight groups,including normal group,model group,Tripterygium Glycosides Tablets groups( 1 times equivalent dose 0.009 g·kg-1,4 times equivalent dose 0.036 g·kg-1,16 times equivalent dose 0.144 g·kg-1),Tripterygium wilfordii Tablets groups( 1 times equivalent dose 0.007 5 mg·kg-1,4 times equivalent dose 0.030 mg·kg-1,16 times equivalent dose 0.120 mg·kg-1). Beginning on the first immunization,Tripterygium Glycosides Tablets and Tripterygium wilfordii Tablets administered intraperitoneally once a day. After the second immunization,the symptoms such as redness and swelling of joints were observed,and the clinical score and incidence of arthritis were evaluated. HE and Masson staining were used to examine the histopathological changes of joints. The expression level of anti-type Ⅱ collagen antibody Ig G in serum was detected by ELISA,routine testing of blood components,the concentration of ALP( alkaline phosphatase),ALT( alanine aminotransferase),AST( aspartate aminotransferase),GGT( gamma-glutamyltransferase),TBi L( total bilirubin),CRE( creatinine) and UREA( urea) in serum were detected by enzymatic assay. The rate of sperm deformity in the epididymis was evaluated under light microscope. The extent of damage to the testis and ovarian tissue was assessed by HE staining. Tripterygium Glycosides Tablets and Tripterygium wilfordii Tablets attenuated the inflammation,redness,swelling and deformity of joints and reduced the clinical score and incidence of arthritis in CIA rats. Meanwhile,it also exhibited obvious reduction in all pathological features such as joint synovitis,pannus,cartilage erosion and bone destruction. Tripterygium Glycosides Tablets and Tripterygium wilfordii Tablets reduced Ig G in a dose-dependent manner,and Tripterygium Glycosides Tablets is better than Tripterygium wilfordii Tablets( P<0.05 or P<0.01). The high doses of Tripterygium Glycosides Tablets and Tripterygium wilfordii Tablets could significantly increase the organ coefficient of liver and spleen and reduced RBC and HGB in CIA rats( P<0.01),and severity leading to death. Gastric mucosal injury and morphological changes of liver and kidney were not observed in CIA rats of Tripterygium Glycosides Tablets and Tripterygium wilfordii Tablets treatment group. The 4 and 16 times doses of Tripterygium Glycosides Tablets and Tripterygium wilfordii Tablets could significantly increase serum ALT,GGT and decrease CRE( P<0.05 or P<0.01). Tripterygium Glycosides Tablets and Tripterygium wilfordii Tablets could increase the sperm deformity rate and damage the testicular seminiferous tubules of CIA male rats. Severity increased with dose and time increasing. The effect of Tripterygium Glycosides Tablets( 16 times) is more significant than Tripterygium wilfordii Tablets( 16 times). Tripterygium Glycosides Tablets and Tripterygium wilfordii Tablets significantly delayed onset of arthritis and inhibited the paw edema and arthritic score. Tripterygium Glycosides Tablets and Tripterygium wilfordii Tablets also caused male reproductive damage,high dose affected hematopoiesis,and maximum dose leading to death. Tripterygium Glycosides Tablets and Tripterygium wilfordii Tablets all depended on dose-effect-toxicity manner. Anti-arthritis effect of Tripterygium Glycosides Tablets is better than Tripterygium wilfordii Tablets,but the toxicity of Tripterygium Glycosides Tablets maximum dose is more obvious. The relevant conclusions of our study will provide experimental references for clinical rational use of drugs,and further clinical studies are needed to confirm our conclusions.


Assuntos
Artrite Experimental/tratamento farmacológico , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/toxicidade , Glicosídeos/administração & dosagem , Glicosídeos/toxicidade , Tripterygium/toxicidade , Animais , Relação Dose-Resposta a Droga , Masculino , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Comprimidos
4.
Molecules ; 24(18)2019 Sep 13.
Artigo em Inglês | MEDLINE | ID: mdl-31540332

RESUMO

Linarin, a flavone glycoside, is considered to be a promising natural product due to its diverse pharmacological activities. Recently, it has been brought into focus for its potential to treat liver failure. In this study, a rapid and sensitive liquid chromatography electrospray-ionization tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of linarin and its three metabolites (acacetin, apigenin, and p-hydroxy benzaldehyde) in plasma and liver tissue samples of normal rats and rats with d-galactosamine (d-GalN)-induced liver injury. After liquid-liquid extraction (LLE) with ethyl acetate, chromatographic separation of the four analytes was achieved using an ACQUITY UPLC BEH-C18 (1.7 µm, 2.1 × 50 mm) with a mobile phase of 0.01% formic acid in methanol and 0.01% formic acid at a flow rate of 0.3 mL/min. The detection was accomplished on a tandem mass spectrometer via an electrospray ionization (ESI) source by multiple reaction monitoring (MRM) in the negative ionization mode. The method had a good linearity over the concentration range of 1.00-200 ng/mL for linarin and its metabolites. The validated method was successfully applied to the pharmacokinetic and liver tissue distribution study of linarin and its metabolites after a single oral administration of linarin (90 mg/kg) to rats.


Assuntos
Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Galactosamina/efeitos adversos , Glicosídeos/farmacocinética , Fígado/química , Plasma/química , Administração Oral , Animais , Cromatografia Líquida , Modelos Animais de Doenças , Glicosídeos/administração & dosagem , Glicosídeos/isolamento & purificação , Masculino , Ratos , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em Tandem , Distribuição Tecidual
5.
Medicine (Baltimore) ; 98(33): e16850, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31415414

RESUMO

BACKGROUND: Type 1 Diabetes Mellitus (T1DM) has long required insulin treatment. Sotagliflflozin (SOTA), as a dual SGLT-1/2 inhibitor, has the potential to be the first oral antidiabetic drug (OAD) to be approved for T1DM in the US market. It is important to evaluate the effectiveness of SOTA for T1DM. METHODS: Web of Science, PubMed datebase, Cochrane Library, Embase, Clinical Trials, and CNKI will be searched to identify randomized controlled trials (RCTs) exploring SOTA adjuvant therapy for T1DM. Strict screening and quality evaluation will be performed on the obtained literature independently by 2 researchers; outcome indexes will be extracted. The bias risk of the included studies will be evaluated based on Cochrane assessment tool. Meta-analysis will be performed on the data using Revman 5.3 software. RESULT: We will provide practical and targeted results assessing the efficacy and safety of SOTA for T1DM patients, to provide reference for clinical use of SOTA. CONCLUSION: The stronger evidence about the efficacy and safety of SOTA for T1DM patients will be provided for clinicians. TRIAL REGISTRATION NUMBER: PROSPERO CRD42019133099.


Assuntos
Diabetes Mellitus Tipo 1/tratamento farmacológico , Glicosídeos/administração & dosagem , Inibidores do Transportador 2 de Sódio-Glicose/administração & dosagem , Administração Oral , Terapia Combinada , Hemoglobina A Glicada/efeitos dos fármacos , Humanos , Metanálise como Assunto , Ensaios Clínicos Controlados Aleatórios como Assunto , Revisões Sistemáticas como Assunto
6.
Life Sci ; 233: 116749, 2019 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-31412264

RESUMO

AIMS: Functional dyspepsia (FD) is very common worldwide with a high prevalence of 10%-30%, and it becomes a heavy burden to patients because of its hard to be cured. In our previous study, phenylethanoid glycosides were found to exist in Houpo, a traditional Chinese medicine commonly used for the treatment of abdominal distention, pain and dyspepsia. In the present study, the effect of magnoloside A (MA), a main phenylethanoid glycoside in Houpo, on FD was firstly evaluated and its potential mechanism was concluded. MATERIALS AND METHODS: MA was orally administered consequently for 3 weeks, and its effect on a FD rat model established through transient neonatal gastric irritation and mature alternate-day fasting was tested. Levels of brain-gut peptides and inflammatory factors in blood or tissues were determined by ELISA methods. Meanwhile, the gut microbiota was analyzed by 16S rRNA gene sequencing and short chain fat acids were determined by GC/MS. KEY FINDINGS: MA exhibited anti-FD activities by fastening the delayed gut emptying rate of FD rat and increasing the levels of gastrin, motilin, and calcitonin gene related protein; and decreasing the levels of 5-hydroxytryptamine, nitric oxide synthase, and vasoactive intestinal peptide. On the other hand, MA can modulate the composition of gut microbiota, resulting in the variation of the short chain fat acids. SIGNIFICANCE: MA ameliorated FD rats by modulating of the secretion of related brain-gut peptides and altering the composition of intestinal microbiota.


Assuntos
Encéfalo/metabolismo , Dispepsia/tratamento farmacológico , Microbioma Gastrointestinal , Trato Gastrointestinal/metabolismo , Glicosídeos/administração & dosagem , Fragmentos de Peptídeos/metabolismo , Administração Oral , Animais , Animais Recém-Nascidos , Dispepsia/metabolismo , Dispepsia/microbiologia , Esvaziamento Gástrico/efeitos dos fármacos , Glicosídeos/química , Magnolia/química , Masculino , Álcool Feniletílico/química , Ratos , Ratos Sprague-Dawley
7.
Acta Pharm ; 69(2): 287-296, 2019 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-31259727

RESUMO

Morroniside is one of the most important iridoid glycosides from Cornus officinalis Sieb. et Zucc. In the present study, the pharmacokinetics and bioavailability studies of morroniside were conducted on Sprague-Dawley (SD) rats. A rat in situ intestinal perfusion model was used to characterize the absorption of morroniside. Caco-2 cells were used to examine the transport mechanisms of morroniside. The pharmacokinetic study of morroniside exhibited linear dose-proportional pharmacokinetic characteristics and low bioavailability (4.3 %) in SD rats. Its average Peff value for transport across the small intestinal segments changed from (3.09 ± 2.03) × 10-6 to (4.53 ± 0.94) × 10-6 cm s-1. In Caco-2 cells, the Papp values ranged from (1.61 ± 0.53) × 10-9 to (1.19 ± 0.22) × 10-7 cm s-1 for the apical to basolateral side and the Pratio values at three concentrations were all lower than 1.2. Morroniside showed poor absorption and it might not be a specific substrate of P-glycoprotein (P-gp).


Assuntos
Cornus/química , Glicosídeos/administração & dosagem , Absorção Intestinal , Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo , Animais , Disponibilidade Biológica , Transporte Biológico , Células CACO-2 , Relação Dose-Resposta a Droga , Glicosídeos/isolamento & purificação , Glicosídeos/farmacocinética , Humanos , Masculino , Ratos , Ratos Sprague-Dawley
8.
J Microencapsul ; 36(6): 523-534, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31190589

RESUMO

Aim: To reduce the toxic effects and achieve efficiency of Tripterygium glycosides, an oral microemulsion was designed. Method: After estimating its stability and characterisation, an animal experiment was held to evaluate its toxicity in vivo, using male and female Sprague Dawley rats. Result: The maximum loading amount of microemulsion to Tripterygium glycosides was 18.87 mg/ml. And comparing to control, the Tripterygium glycoside microemulsion can maintain a normal level of the number of sperms, the weight of testicle, testosterone (∼2.5 ng/mL) and BUN (∼5 mmol/L) to male rats. For female rats, it can prevent the ovary to be atrophy and keep FSH to be stable (>2100 ng/L). The weaker injury induced by drug-loaded microemulsion to rats also could be observed in histological sections to kidney and reproductive organs. Conclusions: Although the blank microemulsion had slight toxicity, it mitigated the toxicity of Tripterygium glycosides to kidney and reproductive system.


Assuntos
Glicosídeos/administração & dosagem , Tripterygium/química , Administração Oral , Animais , Emulsões/efeitos adversos , Emulsões/química , Feminino , Glicosídeos/efeitos adversos , Glicosídeos/química , Glicosídeos/farmacologia , Rim/efeitos dos fármacos , Masculino , Ovário/efeitos dos fármacos , Veículos Farmacêuticos/química , Ratos Sprague-Dawley , Solubilidade , Testículo/efeitos dos fármacos
9.
Indian J Ophthalmol ; 67(6): 801-805, 2019 06.
Artigo em Inglês | MEDLINE | ID: mdl-31124490

RESUMO

Purpose: To evaluate the effect of cyanidin-3-glucoside (C3G) in oxygen-induced retinopathy (OIR) mouse model. Methods: In this experimental study, 10 C57BL / 6J type mice exposed to room air comprised two control groups (n = 5 each; a negative control and a group receiving intravitreal sterile dimethyl sulfoxide [IVS DMSO]). Thirty C57BL / 6J type mice exposed to 75% ± 2% oxygen from postnatal day 7 to postnatal day 12 comprised the OIR groups. On postnatal day 12, these mice were randomized into six groups (n = 5 each): two OIR control groups (negative control and IVS DMSO), two intravitreal C3G groups (300 and 600 ng/µL), and two intraperitoneal C3G groups (0.05 and 0.1 mg/kg). We quantified neovascularization by counting endothelial cell proliferation on the vitreal side of the inner limiting membrane of the retina and examined histological and ultrastructural changes via light and electron microscopy and apoptosis by terminal deoxynucleotidyl transferase deoxy-UTP-nick end labeling. Results: The intravitreal C3G groups yielded lower endothelial cell counts compared with the intravitreal DMSO group. The intraperitoneal high-dose group had lower cell counts compared with the OIR control groups. Electron microscopy revealed significantly less mitochondrial dysmorphology in intravitreal groups and the high-dose intraperitoneal mice. We noted no difference in apoptotic cell count between the controls, low-dose intravitreal, and both intraperitoneal groups. However, apoptotic cell count was significantly higher in the high-dose intravitreal group. Conclusion: C3G suppresses endothelial cell proliferation in an OIR mouse model, leads to a reduced hyperoxia-induced mitochondrial dysmorphology, but increases apoptotic cell death in high concentrations.


Assuntos
Antocianinas/administração & dosagem , Glicosídeos/administração & dosagem , Retina/patologia , Doenças Retinianas/tratamento farmacológico , Animais , Animais Recém-Nascidos , Apoptose , Proliferação de Células , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Injeções Intraperitoneais , Injeções Intravítreas , Camundongos , Camundongos Endogâmicos C57BL , Microscopia Eletrônica , Oxigênio/toxicidade , Retina/efeitos dos fármacos , Doenças Retinianas/induzido quimicamente , Doenças Retinianas/patologia
10.
Food Chem Toxicol ; 131: 110531, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31136780

RESUMO

1-O-(4-hydroxymethylphenyl)-α-L-rhamnopyranoside (MPG) is a phenolic glycoside that exists in Moringa oleifera seeds with various health benefits, whereas its hepatoprotective effect is lacking clarification. Herein, MPG was isolated from Moringa oleifera seeds, and its hepatoprotection against CCl4-induced hepatotoxicity in L02 cells and ICR mice was investigated. Toxicity studies showed that MPG did not induce significant changes in organ coefficients and histological analysis, as well as exhibited no cytotoxicity. In vitro studies indicated that MPG substantially increased cell viability and intracellular SOD activities, and significantly inhibited LDH leakage in CCl4-treated cells. In vivo studies demonstrated that MPG significantly alleviated CCl4-induced hepatotoxicity in mice, as indicated by diagnostic indicators of hepatic injury, as well as the histopathological analysis. Moreover, MPG reduced the lipid peroxidation levels and regulated the inflammatory cytokines. Notably, MPG substantially suppressed the significant elevation of ROS production in hepatocytes of mice intoxicated with CCl4. Moreover, TUNEL assay demonstrated that MPG obviously inhibited hepatic apoptosis induced by CCl4. Altogether, these results suggested that MPG has excellent liver-protecting effects against hepatocytotoxicity induced by CCl4 in mice and L02 cells, which can be further developed as a valuable functional food additive or drug for the treatment of hepatic injury.


Assuntos
Antioxidantes/farmacologia , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Glicosídeos/farmacologia , Moringa oleifera/química , Sementes/química , Administração Oral , Animais , Antioxidantes/administração & dosagem , Antioxidantes/isolamento & purificação , Antioxidantes/toxicidade , Tetracloreto de Carbono/toxicidade , Linhagem Celular , Citocinas/metabolismo , Feminino , Glicosídeos/administração & dosagem , Glicosídeos/isolamento & purificação , Glicosídeos/toxicidade , Fígado/patologia , Masculino , Camundongos Endogâmicos ICR , Estresse Oxidativo/efeitos dos fármacos
11.
BMJ ; 365: l1328, 2019 Apr 09.
Artigo em Inglês | MEDLINE | ID: mdl-30967375

RESUMO

OBJECTIVE: To assess the efficacy and safety of dual sodium glucose cotransporter (SGLT) 1/2 inhibitor sotagliflozin in type 1 diabetes mellitus. DESIGN: Meta-analysis of randomised controlled trials. DATA SOURCES: Medline; Cochrane Library; Embase; international meeting abstracts; international and national clinical trial registries; and websites of US, European, and Japanese regulatory authorities, up to 10 January 2019. ELIGIBILITY CRITERIA FOR SELECTING STUDIES: Randomised controlled trials evaluating the effect of sotagliflozin versus active comparators or placebo on glycaemic and non-glycaemic outcomes and on adverse events in type 1 diabetes in participants older than 18. Three reviewers extracted data for study characteristics, outcomes of interest, and risk of bias and summarised strength of evidence using the grading of recommendations assessment, development, and evaluation approach. Main outcomes were pooled using random effects models. RESULTS: Of 739 records identified, six randomised placebo controlled trials (n=3238, duration 4-52 weeks) were included. Sotagliflozin reduced levels of glycated haemoglobin (HbA1c; weighted mean difference -0.34% (95% confidence interval -0.41% to -0.27%), P<0.001); fasting plasma glucose (-16.98 mg/dL, -22.1 to -11.9; 1 mg/dL=0.0555 mmol/L) and two hour-postprandial plasma glucose (-39.2 mg/dL, -50.4 to -28.1); and daily total, basal, and bolus insulin dose (-8.99%, -10.93% to -7.05%; -8.03%, -10.14% to -5.93%; -9.14%, -12.17% to -6.12%; respectively). Sotagliflozin improved time in range (weighted mean difference 9.73%, 6.66% to 12.81%) and other continuous glucose monitoring parameters, and reduced body weight (-3.54%, -3.98% to -3.09%), systolic blood pressure (-3.85 mm Hg, -4.76 to -2.93), and albuminuria (albumin:creatinine ratio -14.57 mg/g, -26.87 to -2.28). Sotagliflozin reduced hypoglycaemia (weighted mean difference -9.09 events per patient year, -13.82 to -4.36) and severe hypoglycaemia (relative risk 0.69, 0.49 to 0.98). However, the drug increased the risk of ketoacidosis (relative risk 3.93, 1.94 to 7.96), genital tract infections (3.12, 2.14 to 4.54), diarrhoea (1.50, 1.08 to 2.10), and volume depletion events (2.19, 1.10 to 4.36). Initial HbA1c and basal insulin dose adjustment were associated with the risk of diabetic ketoacidosis. A sotagliflozin dose of 400 mg/day was associated with a greater improvement in most glycaemic and non-glycaemic outcomes than the 200 mg/day dose, without increasing the risk of adverse events. The quality of evidence was high to moderate for most outcomes, but low for major adverse cardiovascular events and all cause death. The relatively short duration of trials prevented assessment of long term outcomes. CONCLUSIONS: In type 1 diabetes, sotagliflozin improves glycaemic and non-glycaemic outcomes and reduces hypoglycaemia rate and severe hypoglycaemia. The risk of diabetic ketoacidosis could be minimised by appropriate patient selection and down-titration of the basal insulin dose.


Assuntos
Diabetes Mellitus Tipo 1/tratamento farmacológico , Glicosídeos/uso terapêutico , Hipoglicemia/prevenção & controle , Inibidores do Transportador 2 de Sódio-Glicose/uso terapêutico , Glicemia/análise , Automonitorização da Glicemia/métodos , Diabetes Mellitus Tipo 1/epidemiologia , Cetoacidose Diabética/induzido quimicamente , Cetoacidose Diabética/epidemiologia , Relação Dose-Resposta a Droga , Hemoglobina A Glicada/efeitos dos fármacos , Glicosídeos/administração & dosagem , Glicosídeos/efeitos adversos , Humanos , Ensaios Clínicos Controlados Aleatórios como Assunto , Risco , Inibidores do Transportador 2 de Sódio-Glicose/administração & dosagem , Inibidores do Transportador 2 de Sódio-Glicose/efeitos adversos
12.
Neurochem Res ; 44(7): 1582-1592, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30911982

RESUMO

Hypoxic-ischemic brain damage (HIBD) is a leading cause of death and disability in neonatal or perinatal all over the world, seriously affecting children, families and society. Unfortunately, only few satisfactory therapeutic strategies have been developed. It has been demonstrated that Echinacoside (ECH), the major active component of Cistanches Herba, exerts many beneficial effects, including antioxidative, anti-apoptosis, and neuroprotective in the traditional medical practice in China. Previous research has demonstrated that ECH plays a protective effect on ischemic brain injury. This study aimed to investigate whether ECH provides neuroprotection against HIBD in neonatal rats. We subjected 120 seven-day-old Sprague-Dawley rats to cerebral hypoxia-ischemia (HI) and randomly divided into the following groups: sham group, HI group and ECH (40, 80 and 160 mg/kg, intraperitoneal) post-administration group. After 48 h of HI, 2,3,5-Triphenyltetrazolium chloride, Hematoxylin-Eosin and Nissl staining were conducted to evaluate the extent of brain damage. Superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), and catalase (CAT) activities, total antioxidant capacity (T-AOC), and malondialdehyde (MDA) production were assessed to determine the antioxidant capacity of ECH. TUNEL staining and Western blot analysis was performed to respectively estimate the extent of brain cell apoptosis and the expression level of the apoptosis-related proteins caspase-3, Bax, and Bcl-2. Results showed that ECH remarkably reduced the brain infarct volume and ameliorated the histopathological damage to neurons. ECH post-administration helped recovering the antioxidant enzyme activities and decreasing the MDA production. Furthermore, ECH treatment suppressed neuronal apoptosis in the rats with HIBD was by reduced TUNEL-positive neurons, the caspase-3 levels and increased the Bcl-2/Bax ratio. These results suggested that ECH treatment was beneficial to reducing neuronal damage by attenuating oxidative stress and apoptosis in the brain under HIBD.


Assuntos
Apoptose/efeitos dos fármacos , Glicosídeos/uso terapêutico , Hipóxia-Isquemia Encefálica/tratamento farmacológico , Fármacos Neuroprotetores/uso terapêutico , Estresse Oxidativo/efeitos dos fármacos , Animais , Animais Recém-Nascidos , Encéfalo/patologia , Caspase 3/metabolismo , Catalase/metabolismo , Relação Dose-Resposta a Droga , Feminino , Glutationa Peroxidase/metabolismo , Glicosídeos/administração & dosagem , Hipóxia-Isquemia Encefálica/patologia , Masculino , Malondialdeído/metabolismo , Fármacos Neuroprotetores/administração & dosagem , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Ratos Sprague-Dawley , Superóxido Dismutase/metabolismo , Proteína X Associada a bcl-2/metabolismo
13.
Am J Chin Med ; 47(2): 457-476, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30834778

RESUMO

Ligustroflavone is one major compound contained in active fraction from Fructus Ligustri Lucidi (the fruit of Ligustrum lucidum), which could regulate parathyroid hormone (PTH) levels and improve calcium balance by acting on calcium-sensing receptors (CaSR). This study aimed to explore the potency of ligustroflavone as a CaSR antagonist and its protective effects against diabetic osteoporosis in mice. LF interacted well with the allosteric site of CaSR shown by molecular docking analysis, increased PTH release of primary parathyroid gland cells and suppressed extracellular calcium influx in HEK-293 cells. The serum level of PTH attained peak value at 2 h and maintained high during the period of 1 h and 3 h than that before treatment in mice after a single dose of LF. Treatment of diabetic mice with LF inhibited the decrease in calcium level of serum and bone and the enhancement in urinary calcium excretion as well as elevated circulating PTH levels. Trabecular bone mineral density and micro-architecture were markedly improved in diabetic mice upon to LF treatment for 8 weeks. LF reduced CaSR mRNA and protein expression in the kidneys of diabetic mice. Taken together, ligustroflavone could transiently increase PTH level and regulate calcium metabolism as well as prevent osteoporosis in diabetic mice, suggesting that ligustroflavone might be an effective antagonist on CaSR.


Assuntos
Apigenina/farmacologia , Complicações do Diabetes/complicações , Glicosídeos/farmacologia , Ligustrum/química , Osteoporose/etiologia , Osteoporose/prevenção & controle , Receptores de Detecção de Cálcio/antagonistas & inibidores , Animais , Apigenina/administração & dosagem , Apigenina/isolamento & purificação , Densidade Óssea/efeitos dos fármacos , Cálcio/metabolismo , Osso Esponjoso/metabolismo , Células Cultivadas , Expressão Gênica/efeitos dos fármacos , Glicosídeos/administração & dosagem , Glicosídeos/isolamento & purificação , Células HEK293 , Humanos , Rim/metabolismo , Masculino , Camundongos Endogâmicos C57BL , Glândulas Paratireoides/citologia , Glândulas Paratireoides/metabolismo , Hormônio Paratireóideo/metabolismo , Receptores de Detecção de Cálcio/genética , Receptores de Detecção de Cálcio/metabolismo , Fatores de Tempo
14.
Diabetes Care ; 42(5): 919-930, 2019 05.
Artigo em Inglês | MEDLINE | ID: mdl-30833371

RESUMO

OBJECTIVE: To evaluate effects of the dual sodium-glucose cotransporter (SGLT) 1 and SGLT2 inhibitor sotagliflozin in combination with insulin on glucose time in range (TIR) and glucose excursions, postprandial glucose (PPG), and other glycemic metrics in adults with type 1 diabetes using masked continuous glucose monitoring (CGM). RESEARCH DESIGN AND METHODS: Data sets from the inTandem1 (clinical trial reg. no. NCT02384941) and inTandem2 (clinical trial reg. no. NCT02421510) double-blind randomized trials evaluating sotagliflozin versus placebo in adults with type 1 diabetes treated with optimized insulin were pooled for analyses of masked CGM data from a subset of participants in each trial. The pooled cohort included patients randomized to receive placebo (n = 93), sotagliflozin 200 mg (n = 89), or sotagliflozin 400 mg (n = 96). The primary outcome was change from baseline to week 24 in glucose TIR (3.9-10.0 mmol/L [70-180 mg/dL]). Secondary end points included time below and above the target range and 2-h PPG level assessed after a standardized mixed meal. RESULTS: Mean percentage of glucose TIR/percentage time spent at <3.9 mmol/L (<70 mg/dL) during week 24 was 51.6%/5.9%, 57.8%/5.5%, and 64.2%/5.5% with placebo, sotagliflozin 200 mg, and sotagliflozin 400 mg, respectively, which corresponded to a placebo-adjusted change from a baseline of +5.4%/-0.3% (P = 0.026; +1.3/-0.1 h/day) for sotagliflozin 200 mg and +11.7%/-0.1% (P < 0.001; +2.8/-0.02 h/day) for sotagliflozin 400 mg. Placebo-adjusted PPG reductions were 1.9 ± 0.7 mmol/L (35 ± 13 mg/dL; P = 0.004) and 2.8 ± 0.7 mmol/L (50 ± 13 mg/dL; P < 0.001) with sotagliflozin 200 and 400 mg, respectively. CONCLUSIONS: Combined with optimized insulin in type 1 diabetes, sotagliflozin significantly increased glucose TIR without increasing time spent at <3.9 mmol/L and reduced PPG, thereby improving glycemic control.


Assuntos
Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Diabetes Mellitus Tipo 1/sangue , Diabetes Mellitus Tipo 1/tratamento farmacológico , Glicosídeos/administração & dosagem , Insulina/administração & dosagem , Adulto , Idoso , Automonitorização da Glicemia/métodos , Diabetes Mellitus Tipo 1/epidemiologia , Método Duplo-Cego , Quimioterapia Combinada , Feminino , Glicosídeos/efeitos adversos , Humanos , Hipoglicemiantes/administração & dosagem , Hipoglicemiantes/efeitos adversos , Insulina/efeitos adversos , Estudos Longitudinais , Masculino , Pessoa de Meia-Idade , Estudos Multicêntricos como Assunto/estatística & dados numéricos , Período Pós-Prandial/efeitos dos fármacos , Ensaios Clínicos Controlados Aleatórios como Assunto/estatística & dados numéricos , Estudos Retrospectivos , Fatores de Tempo
15.
Biomed Res Int ; 2019: 4379639, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30834264

RESUMO

Objective: To study the protective effect of Echinacoside for 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) induced dopaminergic (DA) neurons injury in the subacute mouse model of Parkinson's disease (PD) and to explore its mechanism of action. Methods: We chose 10 weeks of healthy wild type C57BL/6 male mice, hypodermic MPTP 30 mg/kg/day, five days, to prepare PD subacute mouse model. Behavior indexes of open field test and pole test were applied to examine the function of ECH to PD subacute mice model of PD sample action. The effects of ECH on dopaminergic neurons and astrocyte were examined using Immunohistochemistry including tyrosine hydroxylase (TH) and glial fibrillary acidic protein (GFAP) expression. The total numbers of TH-positive neurons and GFAP-positive cells in the substantia nigra pars compacts (SNpc) and ventral tegmental area (VTA) were obtained stereologically using the optical fractionator method. Enzyme-linked immunosorbent assay (ELISA) method was used to detect the inflammatory cytokines in the serum, including TNF-α (Ttumor necrosis factor alpha) and IFN-γ (interferon gamma). Protein expressions of ionized calcium binding adaptor molecule 1 (IBA-1), TNF-α, Cleaved caspase-3, glial derived neurotrophic factor (GDNF), and phosphorylated and total extracellular signal-regulated kinase (p-ERK and ERK) in the anatomical region of substantia nigra (SN) were tested by protein immunoblot method (i.e., Western blotting). Results: ECH reversed the reduction of total distance in open field test in MPTP-induced PD model mice (P < 0.01), shortened the return time and total time of PD subacute model mice in pole test (P < 0.01, P < 0.05), significantly reversed the reduction of TH positive neurons induced by MPTP (P < 0.05), and reduced the activation of astrocytes (P < 0.05). Meanwhile, ECH significantly inhibited the expression of IBA-1, Cleaved caspase-3, and TNF-α in midbrain of MPTP model mice (P < 0.05, P < 0.05, and P < 0.05) and upregulated the expression of GDNF (P < 0.05). And ECH lowered the level of TNF-α and IFN-γ in serum (P < 0.05, P < 0.05). Conclusion: ECH has protective effects on the MPTP subacute model mice, its mechanism may be through inhibiting activation of microglia and astrocytes, reducing inflammatory reaction and promoting the secretion of neurotrophic factors, and eventually resulting in the reduction of the DA neurons apoptosis.


Assuntos
Glicosídeos/administração & dosagem , Intoxicação por MPTP/tratamento farmacológico , Fármacos Neuroprotetores/administração & dosagem , Doença de Parkinson/tratamento farmacológico , Animais , Proteínas de Ligação ao Cálcio/genética , Caspase 3/genética , Corpo Estriado/efeitos dos fármacos , Corpo Estriado/patologia , Modelos Animais de Doenças , Neurônios Dopaminérgicos/efeitos dos fármacos , Neurônios Dopaminérgicos/patologia , Regulação da Expressão Gênica/efeitos dos fármacos , Proteína Glial Fibrilar Ácida/genética , Humanos , Imuno-Histoquímica , Intoxicação por MPTP/genética , Intoxicação por MPTP/patologia , Camundongos , Proteínas dos Microfilamentos/genética , Microglia/efeitos dos fármacos , Microglia/patologia , Doença de Parkinson/genética , Doença de Parkinson/patologia , Substância Negra/efeitos dos fármacos , Substância Negra/patologia , Fator de Necrose Tumoral alfa/genética , Tirosina 3-Mono-Oxigenase/genética
16.
Molecules ; 24(3)2019 Feb 11.
Artigo em Inglês | MEDLINE | ID: mdl-30754654

RESUMO

In Traditional Chinese Medicine (TCM), Mori ramulus (Chin.Ph.)-the dried twigs of Morus alba L.-is extensively used as an antirheumatic agent and also finds additional use in asthma therapy. As a pathological high xanthine oxidase (XO, EC 1.1.3.22) activity is strongly correlated to hyperuricemy and gout, standard anti-hyperuremic therapy typically involves XO inhibitors like allopurinol, which often cause adverse effects by inhibiting other enzymes involved in purine metabolism. Mori ramulus may therefore be a promissing source for the development of new antirheumatic therapeutics with less side effects. Coumarins, one of the dominant groups of bioactive constituents of M. alba, have been demonstrated to possess anti-inflammatory, antiplatelet aggregation, antitumor, and acetylcholinesterase (AChE) inhibitory activities. The combination of HPLC (DAD) and Q-TOF technique could give excellent separating and good structural characterization abilities which make it suitable to analyze complex multi-herbal extracts in TCM. The aim of this study was to develop a HPLC (DAD)/ESI-Q-TOF-MS/MS method for the identification and profiling of pharmacologically active coumarin glycosides in Mori ramulus refined extracts for used in TCM. This HPLC (DAD)/ESI-Q-TOF-MS/MS method provided a rapid and accurate method for identification of coumarin glycosides-including new natural products described here for the first time-in the crude extract of M. alba L. In the course of this project, two novel natural products moriramulosid A (umbelliferone-6-ß-d-apiofuranosyl-(1→6)-ß-d-glucopyranoside) and moriramulosid B (6-[[6-O-(6-deoxy-α-l-mannopyranosyl)-ß-d-glucopyranosyl]oxy]-2H-1-benzopyran-1-one) were newly discovered and the known natural product Scopolin was identified in M. alba L. for the first time.


Assuntos
Glicosídeos/administração & dosagem , Glicosídeos/química , Hiperuricemia/tratamento farmacológico , Morus/química , Ácido Oxônico/efeitos adversos , Ácido Úrico/sangue , Alopurinol/administração & dosagem , Animais , Cromatografia Líquida de Alta Pressão , Cumarínicos/química , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas/química , Etanol/química , Glicosídeos/farmacologia , Hiperuricemia/induzido quimicamente , Hiperuricemia/metabolismo , Masculino , Camundongos , Estrutura Molecular , Extratos Vegetais/química , Distribuição Aleatória , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em Tandem
17.
Phytomedicine ; 53: 274-285, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30668407

RESUMO

BACKGROUND: Renal fibrosis is the most common pathway leading to end-stage renal disease. It is characterized by excess extracellular matrix (ECM) accumulation and renal tissue damage, subsequently leading to kidney failure. Asperulosidic acid (ASPA), a bioactive iridoid glycoside, exerts anti-tumor, anti-oxidant, and anti-inflammatory activities, but its effects on renal fibrosis induced by unilateral ureteral obstruction (UUO) have not yet been investigated. PURPOSE: This study aimed to investigate the protective effect of ASPA on renal fibrosis induced by UUO, and to explore its pharmacological mechanism. METHODS: Thirty-six Sprague-Dawley (SD) rats were randomly divided into six groups: sham group, UUO model group, three ASPA treatment groups (10, 20, and 40 mg/kg), and captopril group (20 mg/kg). Rats were administered vehicle, ASPA or captopril intraperitoneally once a day for 14 consecutive days. Urea nitrogen (BUN), uric acid (UA) and inflammatory factors in serum samples were evaluated on the 7th, 10th, and 14th day after renal fibrosis induction. In addition, the 12 h urine was collected to test the content of urinary protein (upro) on the 14th day. The obstructive renal tissues were collected for pathological analysis (hematoxylin and eosion (H&E) staining and Masson's Trichrome staining) and immunohistochemical analysis on the 14th day after renal fibrosis induction. The mRNA expression of related factors and the protein levels of smad2, smad3, and smad4 were measured in UUO-induced rats by real time PCR and Western blot, respectively. RESULTS: The levels of BUN, UA, and upro were elevated in UUO-induced rats, but ASPA treatment improved renal function by reducing the levels of BUN, UA, and upro. The protein levels of tumor necrosis factor-α (TNF-α), interleukin-1ß (IL-1ß) and IL-6, as well as the mRNA levels of TNF-α, IL-1ß, IL-6, monocyte chemoattractant protein-1 (MCP-1) and interferon-γ (IFN-γ), were decreased after ASPA administration (10, 20 and 40 mg/kg) in a dose-dependent manner. The ASPA exerted an alleviation effect on the inflammatory response through inhibition of nuclear factor-kappa B (NF-κB) pathway. In addition, reductions in α-smooth muscle actin (α-SMA), collagen III, and fibronectin expression were observed after ASPA administration at doses of 20 and 40 mg/kg. Furthermore, the renal expression of transforming growth factor-ß1 (TGF-ß1), smad2, smad3, and smad4 was down-regulated by ASPA treatment at doses of 20 and 40 mg/kg. CONCLUSION: ASPA possessed protective effects on renal interstitial fibrosis in UUO-induced rats. These effects may be through inhibition of the activation of NF-κB and TGF-ß1/smad2/smad3 signaling pathways.


Assuntos
Fibrose/tratamento farmacológico , Glicosídeos/farmacologia , Rim/efeitos dos fármacos , Rim/metabolismo , Obstrução Ureteral/tratamento farmacológico , Animais , Citocinas/genética , Citocinas/metabolismo , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Fibrose/metabolismo , Fibrose/patologia , Glicosídeos/administração & dosagem , Rim/patologia , Nefropatias/tratamento farmacológico , Masculino , NF-kappa B/metabolismo , Substâncias Protetoras/farmacologia , Ratos Sprague-Dawley , Transdução de Sinais/efeitos dos fármacos , Proteína Smad2/metabolismo , Proteína Smad3/metabolismo , Fator de Crescimento Transformador beta1/metabolismo , Obstrução Ureteral/metabolismo
18.
Molecules ; 23(12)2018 Dec 10.
Artigo em Inglês | MEDLINE | ID: mdl-30544700

RESUMO

As a folk medicine, Moringa oleifera L. is used effectively to treat inflammatory conditions and skin diseases. However, its mechanism of action is not well understood, limiting its medical use. We isolated and identified three compounds, namely niazirin, marumoside A and sitosterol-3-O-ß-d-glucoside, from the seeds of Moringa oleifera, and studied their effects on the expression of Th17-relevant cytokines (IL-12/IL-23 p40, IL-17A, IL-22 and IL-23 p19) using lipopolysaccharide-stimulated THP-1 cells. Additionally, as Th17 plays a critical role in the pathogenesis of psoriasis, we used a 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced psoriasis-like skin lesion mouse model to study their potential therapeutic application in vivo. The compounds suppressed the expression of IL-12/IL-23 p40, IL-17A, IL-22 and IL-23 p19 in vitro, and in vivo they ameliorated psoriasis-like skin lesions, decreased IL-17A mRNA expression, and increased the expression of keratinocyte differentiation markers. To our knowledge, this is the first report regarding the mechanism and therapeutic application of Moringa oleifera seeds to treat psoriasis-like lesions in vivo.


Assuntos
Citocinas/genética , Moringa oleifera/química , Extratos Vegetais/administração & dosagem , Psoríase/tratamento farmacológico , Acetato de Tetradecanoilforbol/efeitos adversos , Células Th17/imunologia , Animais , Modelos Animais de Doenças , Regulação da Expressão Gênica/efeitos dos fármacos , Glicosídeos/administração & dosagem , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Humanos , Lipopolissacarídeos/efeitos adversos , Camundongos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Psoríase/induzido quimicamente , Psoríase/genética , Pirróis/administração & dosagem , Pirróis/isolamento & purificação , Pirróis/farmacologia , Sementes/química , Sitosteroides/administração & dosagem , Sitosteroides/isolamento & purificação , Sitosteroides/farmacologia , Células Th17/efeitos dos fármacos
19.
Parasit Vectors ; 11(1): 614, 2018 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-30501613

RESUMO

BACKGROUND: The sand fly Lutzomyia longipalpis is the main vector of American visceral leishmaniasis, a disease caused by parasites of the genus Leishmania. Adults of this insect feed on blood (females only) or sugar from plant sources, but their digestion of carbohydrates is poorly studied. Beta-glycosides as esculin and amygdalin are plant compounds and release toxic compounds as esculetin and mandelonitrile when hydrolyzed. Beta-glucosidase and trehalase are essential enzymes in sand fly metabolism and participate in sugar digestion. It is therefore possible that the toxic portions of these glycosides, released during digestion, affect sand fly physiology and the development of Leishmania. RESULTS: We tested the oral administration to sand flies of amygdalin, esculin, mandelonitrile, and esculetin in the sugar meal. These compounds significantly decreased the longevity of Lutzomyia longipalpis females and males. Lutzomyia longipalpis adults have significant hydrolytic activities against esculin and feeding on this compound cause changes in trehalase and ß-glucosidase activities. Female trehalase activity is inhibited in vitro by esculin. Esculin is naturally fluorescent, so its ingestion may be detected and quantified in whole insects or tissue samples stored in methanol. Mandelonitrile neither affected the amount of sugar ingested by sand flies nor showed repellent activity. Our results show that mandelonitrile significantly reduces the viability of L. amazonensis, L. braziliensis, L. infantum and L. mexicana, in a concentration-dependent manner. Esculetin caused a similar effect, reducing the number of L. infantum and L. mexicana. Female L. longipalpis fed on mandelonitrile had a reduction in the number of parasites and prevalence of infection after seven days of infection with L. mexicana, either by counting in a Neubauer chamber or by qPCR assays. CONCLUSIONS: Glycosides have significant effects on L. longipalpis longevity and metabolism and also affect the development of parasites in culture and inside the insect. These observations might help to conceptualize new vector control strategies using transmission blocking sugar baits.


Assuntos
Glicosídeos/toxicidade , Controle de Insetos/métodos , Insetos Vetores/enzimologia , Insetos Vetores/parasitologia , Leishmania/crescimento & desenvolvimento , Psychodidae/enzimologia , Psychodidae/parasitologia , Acetonitrilos/toxicidade , Amigdalina/toxicidade , Animais , Esculina/toxicidade , Feminino , Glicosídeos/administração & dosagem , Leishmaniose/prevenção & controle , Leishmaniose/transmissão , Masculino , Trealase/efeitos dos fármacos , Umbeliferonas/administração & dosagem , Umbeliferonas/toxicidade , beta-Glucosidase/efeitos dos fármacos
20.
Chin J Nat Med ; 16(11): 871-880, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30502769

RESUMO

Poliumoside is representative of phenylethanoid glycosides, which are widely found in many plants. Poliumoside is also regarded as the main active component of Callicarpa kwangtungensis Chun (CK), though its oral bioavailability in rat is extremely low (0.69%) and its in vivo and in vitro metabolism has not yet been systematically investigated. In the present study, an ultra performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS) method was employed to identify the metabolites and investigate the metabolic pathways of poliumoside in rat after oral administration 1.5 g·kg-1 of poliumoside. As a result, a total of 34 metabolites (30 from urine, 17 from plasma, and 4 from bile) and 9 possible metabolic pathways (rearrangment, reduction, hydration, hydrolyzation, dehydration, methylation, hydroxylation, acetylation, and sulfation) were proposed in vivo. The main metabolite, acteoside, was quantified after incubated with rat intestinal bacteria in vitro. In conclusion, the present study systematically explored the metabolites of poliumoside in vivo and in vitro, proposing metabolic pathways that may be significant for further metabolic studies of poliumoside.


Assuntos
Bactérias/metabolismo , Bile/química , Ácidos Cafeicos/química , Callicarpa/química , Medicamentos de Ervas Chinesas/química , Glicosídeos/química , Intestinos/microbiologia , Plasma/química , Urina/química , Administração Oral , Animais , Ácidos Cafeicos/administração & dosagem , Ácidos Cafeicos/sangue , Ácidos Cafeicos/urina , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/metabolismo , Glicosídeos/administração & dosagem , Glicosídeos/sangue , Glicosídeos/urina , Masculino , Espectrometria de Massas/métodos , Estrutura Molecular , Ratos , Ratos Sprague-Dawley
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