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1.
Huan Jing Ke Xue ; 42(3): 1433-1442, 2021 Mar 08.
Artigo em Chinês | MEDLINE | ID: mdl-33742940

RESUMO

The loss of nitrogen (N) and phosphorus (P) from aquaculture has caused eutrophication of freshwater systems. Here, surface flow constructed wetland (SFCW) planted with Myriophyllum elatinoides were used to treat swine wastewater from a medium-sized hoggery in subtropical Central China. Inflow concentrations of NH4+-N, TN, TP, and COD ranged from 535.4 to 591.09, 682.09 to 766.96, 57.73 to 82.29, and 918.4 to 1940.43 mg·L-1, respectively. The mean removal efficiencies of NH4+-N, TN, TP, and COD were 97.4%, 97.1%, 91.0%, and 90.2%, respectively, and CW1 had the largest contributions of 37.3%, 38.4%, 43.3%, and 27.4%, respectively. Plant N and P uptake ranged 23.87-79.96 g·m-2 and 5.34-18.98 g·m-2, accounting for 19.1% and 20.2% of removal, respectively. Sediment N and P accumulation ranged 19.17-56.62 g·m-2 and 10.59-26.62 g·m-2, accounting for 19.8% and 61.7% of removal, respectively. Multiple linear regression showed that environmental factors explained 79.9% of the N removal and 70.1% of the P removal; DO was the main factor affecting N removal, and sediment adsorption was the key process in P removal. These results show that M. elatinoides constructed wetland can efficiently treat swine wastewater, thereby reduce the discharge of pollutants downstream.


Assuntos
Águas Residuárias , Áreas Alagadas , Animais , China , Nitrogênio/análise , Fósforo , Suínos , Eliminação de Resíduos Líquidos
2.
Math Biosci Eng ; 17(3): 2616-2635, 2020 03 04.
Artigo em Inglês | MEDLINE | ID: mdl-32233557

RESUMO

In this paper, we propose a predator-prey model with genetic differentiation both in the predator and prey. First, we analyze two special cases: a model without the predators and a model with one genotype in both the predator and prey, and for each model show that the positive equilibria are always globally stable when they exist, while the boundary equilibria are always unstable. Then, for the newly proposed model, we give the results that the positive equilibrium is always local stable when it exists, the boundary equilibrium at the origin is always unstable, and the stability of another boundary equilibrium is determined by the existence of the positive equilibrium. Moreover, our discussions show the existence of local center manifolds near the equilibria. Finally, we give some examples to illustrate our results.


Assuntos
Modelos Biológicos , Comportamento Predatório , Animais , Dinâmica Populacional
3.
Fitoterapia ; 141: 104450, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31837410

RESUMO

Cajaninstilbene acid (CSA), a bioactive constituent isolated from pigeon pea leaves, exhibited neuroprotective activities in previous studies. The present study aims to evaluate the antidepressant effects of CSA by using behavioral despair models of tail suspension test (TST) and forced swimming test (FST), and a chronic unpredictable mild stress (CUMS) model. CSA (30 or 60 mg/kg), intragastrically administrated for 7 days, could significantly reduce the immobility time of mice in TST and FST. CSA treatment (15 or 30 mg/kg) significantly reversed the depressive-like behavioral changes of mice induced by 3 or 6 weeks CUMS that caused the decrease of sucrose preference, the increase of latency to feed in the novelty-suppressed feeding test, and the increase of immobility time in TST of mice. Furthermore, the related mechanisms of the effect were explored by accessing the metabolite levels of kynurenine pathway of tryptophan metabolism and the expression of some related proteins in cerebral cortex of CUMS mice. Our results showed that the kynurenine pathway was upregulated after CUMS, while the alteration could be significantly reversed by CSA. CSA also reversed the CUMS-induced decrease in the levels of BDNF, PSD-95, p-Akt/Akt and p-mTOR/mTOR. Therefore, the antidepressant-like effects of CSA might be achieved through regulating tryptophan metabolism, promoting BDNF and PSD-95 expression, and activating Akt/mTOR pathway in the cerebral cortex.


Assuntos
Antidepressivos/farmacologia , Cajanus/química , Salicilatos/farmacologia , Estilbenos/farmacologia , Animais , Antidepressivos/química , Fator Neurotrófico Derivado do Encéfalo/genética , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Regulação da Expressão Gênica/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Estrutura Molecular , Folhas de Planta/química
4.
Front Pharmacol ; 10: 1084, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31680939

RESUMO

Amyloid-ß1-42 (Aß1-42) oligomers play an important role at the early stage of Alzheimer's disease (AD) and have been a vital target in the development of therapeutic drugs for AD. Cajaninstilbene acid (CSA), a major bioactive stilbene isolated from pigeon pea (Cajanus cajan) leaves, exerted the neuroprotective property in our previous studies. The present study utilized a validated mouse model of early-stage AD induced by bilateral injection of Aß1-42 oligomers into hippocampal CA1 regions (100 pmol/mouse) to investigate the cognitive enhancing effects of CSA and the underlying mechanism, by a combination of animal behavioral tests, immunohistochemistry, liquid chromatography-tandem mass spectrometry analysis, and Western blot methods. Intragastric administration of CSA (7.5, 15, and 30 mg/kg) attenuated the impairment of learning and memory induced by Aß1-42 oligomers. CSA stimulated Aß clearance and prevented microglial activation and astrocyte reactivity in the hippocampus of model mice. It also decreased the high levels of Glu but increased the low levels of GABA. In addition, CSA inhibited excessive expression of GluN2B-containing NMDARs and upregulated the downstream PKA/CREB/BDNF/TrkB signaling pathway. These results suggest that CSA could be a potential therapeutic agent at the early stage of AD.

5.
Life Sci ; 234: 116751, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31415771

RESUMO

AIMS: The present study aims to investigate the impacts of olfactory bulbectomy (OBX) on urinary metabolic profile and tryptophan metabolites in prefrontal cortex (PFC) of rats, and to explore the regulation effects of fluoxetine. MAIN METHODS: OBX model was developed by aspiration of olfactory bulbs. After fluoxetine treatment (10 mg/kg) for 14 days, urine samples were collected and behavior tests were applied. Tryptophan (TRP) metabolites and neurotransmitters in PFC were determined by prominence ultrafast liquid chromatography-QTRAP-mass spectrometry, and tryptophan hydroxylase 2 (TPH2) and indoleamine-2,3-dioxygenase 1 (IDO1) were evaluated by western blot. Urinary metabolites were analyzed by ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry-based metabonomics strategy. KEY FINDING: OBX rats showed hyperlocomotion in open field, hyperactivity in open arm and despair status, and fluoxetine reserved these behavioral abnormalities. The levels of TRP, 5-HIAA, 5-HIAA/5-HT ratio and DA increased, while kynurenine and 5-HT decreased in PFC of OBX rats. The activities of TPH2 and IDO1were inhibited after OBX. Twenty-six altered metabolites were identified as potential biomarkers in OBX rats involved in tryptophan metabolism, gut microbiota metabolism, energy metabolism, purine metabolism, ascorbate and aldarate metabolism, and tyrosine metabolism. Among them, 15 abnormal metabolites were corrected by fluoxetine to some extent. SIGNIFICANCE: Our results revealed that urinary metabolic profile changed greatly in OBX rats, and identified biomarkers might be helpful for the diagnosis of agitated depression. The regulation effects of fluoxetine on urinary metabolic profile and tryptophan metabolites in PFC might contribute to its antidepressant action in OBX rats.


Assuntos
Antidepressivos de Segunda Geração/uso terapêutico , Depressão/tratamento farmacológico , Depressão/metabolismo , Fluoxetina/uso terapêutico , Metaboloma/efeitos dos fármacos , Animais , Antidepressivos de Segunda Geração/farmacologia , Depressão/urina , Modelos Animais de Doenças , Fluoxetina/farmacologia , Masculino , Bulbo Olfatório/cirurgia , Córtex Pré-Frontal/efeitos dos fármacos , Córtex Pré-Frontal/metabolismo , Ratos Sprague-Dawley , Triptofano/metabolismo
6.
Int J Ophthalmol ; 12(8): 1323-1329, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31456924

RESUMO

AIM: To investigate the behavioral and psychological disorders and the prevalence of parent ratings of attention deficit hyperactivity disorder (ADHD) symptoms among children with bilateral congenital cataracts (CCs). METHODS: This cross-sectional study investigated children with bilateral CC aged 3-8y (CC group) using Conners' Parent Rating Scale-48 (CPRS-48) from July to December 2016. The abnormal rates of psychological symptoms in CC children and normal vision (NV) children were compared using the Chi-square test. The scores of CC children were compared with those of NV children and the Chinese urban norm using the independent samples t-test and one-sample t-test, respectively. RESULTS: A total of 262 valid questionnaires were collected. The ratio of CC children to NV children was 119:143. The overall rate of psychological symptoms in CC children was 2.28 times higher than that in NV children (46.22% vs 20.28%, Pearson's χ 2=20.062; P<0.001). CC children showed higher scores for conduct problems, learning problems, impulsiveness/hyperactivity, anxiety, and hyperactivity index than NV children and the Chinese urban norm, particularly between the ages of 3 and 5y. Furthermore, male children aged between 6 and 8y showed a higher impulsive/hyperactive score than females of the same age (t=6.083, P<0.001). CONCLUSION: Children with bilateral CCs have a higher rate of ADHD symptoms than children with NV. This study provides clinical evidence that screening for psychological symptoms and particularly for ADHD symptoms in children with bilateral CC are recommended for an early diagnosis and timely treatment.

7.
Artigo em Inglês | MEDLINE | ID: mdl-30836315

RESUMO

l-Tryptophan (Trp) metabolites and related neurotransmitters play crucial roles in physiological functions, and their imbalances are implicated in the pathology of depression, Alzheimer's disease and other diseases. Measurement of Trp metabolites and related neurotransmitters possesses a great potential to elucidate the disease mechanisms and evaluate the outcomes of therapeutic interventions. A simple, rapid, sensitive and specific liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for simultaneous determination of Trp, l-kynurenine (Kyn), kynurenic acid (Kyna), 3-hydroxykynurenine (3-HK), 5-hydroxytryptamine (5-HT), 5-hydroxyindoleacetic acid (5-HIAA), norepinephrine (NE), l-glutamic acid (Glu), γ-aminobutyric acid (GABA) and acetylcholine (ACh) in mice serum and the brain tissues in a single chromatographic run. Samples were spiked with the internal standard, mixed with trifluoroacetic acid to precipitate protein and analyzed by LC-MS/MS. Chromatographic separation was achieved using a Restek Ultra Aqueous C18 column in combination with a gradient elution within 8 min. Mass spectrometric detection was performed using multiple reaction monitoring with electrospray ionization source in positive mode. The method exhibited good selectivity and correlation coefficient values for the calibration curves of each analyte were >0.99. The limit of detection and quantification ranged from 0.96 to 24.48 nmol/L and 3.42 to 244.82 nmol/L, respectively. The intra- and inter-day precision were ≤13.92%. All analytes were stable in prepared samples at room temperature in the autosampler for 24 h. This method was successfully applied to the analysis of biological samples from control and chronic mild stress (CMS) induced depression mice. It was found that Kyn and 3-HK pathways were enhanced by CMS, while the levels of Trp, Kyna, 5-HIAA, Glu, GABA and ACh were significantly reduced. The changes in 5-HT and NE levels were not uniform in the periphery and the brain. This method can therefore be applied to analyze Trp metabolites and related neurotransmitters levels to monitor disease states, study the mechanisms and outcomes of therapeutic interventions.


Assuntos
Química Encefálica/fisiologia , Cromatografia Líquida/métodos , Neurotransmissores/análise , Espectrometria de Massas em Tandem/métodos , Triptofano/análise , Animais , Limite de Detecção , Modelos Lineares , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Neurotransmissores/sangue , Neurotransmissores/metabolismo , Reprodutibilidade dos Testes , Triptofano/sangue , Triptofano/metabolismo
8.
Front Pharmacol ; 9: 902, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30210336

RESUMO

The leaf of the lotus (Nelumbo nucifera) is a natural plant resource used as both food and herbal medicine (He-Ye) in China. Alkaloids are considered the major bioactive compound of the herb and exhibit various biological activities, including anti-hyperlipidemia, anti-obesity, anti-inflammatory, and anti-hyperuricemic effects. Nuciferine (NF) and N-nuciferine (N-NF) are two major alkaloids found in the herb. In the present work, the plasma and brain pharmacokinetics of the two compounds were investigated after oral and intravenous (i.v.) administration of a lotus leaf alkaloid fraction to SD rats via ultra-performance liquid chromatography coupled with photodiode array detection and brain microdialysis. After oral administration (50 mg/kg), the two compounds NF and N-NF were rapidly absorbed into the blood and reached a mean maximum concentration (Cmax) of 1.71 µg/mL at 0.9 h and 0.57 µg/mL at 1.65 h, respectively. After i.v. administration (10 mg/kg), NF and N-NF were found to have a relatively wide volume of distribution (Vd, λz, 9.48 and 15.17 L/kg, respectively) and slow elimination half-life (t1/2, λz, 2.09 and 3.84 h, respectively). The oral bioavailability of NF and N-NF was estimated as 58.13% and 79.91%, respectively. After i.v. dosing (20 mg/kg), the two compounds rapidly crossed the blood-brain barrier and reached their Cmax (in unbound form): 0.32 and 0.16 µg/mL at 0.89 and 1.22 h, respectively. Both alkaloids had widespread distribution in the brain, with Vd, λz/F-values of 19.78 L/kg and 16.17 L/kg, respectively. The mean t1/2, λz values of NF and N-NF in the brain were 1.24 and 1.39 h, respectively. These results can help us to better understand the characteristics and neuro-pharmacological effects of the lotus alkaloid fraction.

9.
Biomed Chromatogr ; 32(8): e4250, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29578591

RESUMO

Danhong Injection (DHI) as a Chinese patent medicine is mainly used to treat ischemic encephalopathy and coronary heart disease in combination with other chemotherapy. However, the information on DHI's potential drug interactions is limited. The goal of this work was to examine the potential P450-mediated metabolism drug interaction arising from DHI and its active components. The results showed that DHI inhibited CYP2C19, CYP2D6, CYP3A4, CYP2E1 and CYP2C9 with IC50 values of 1.26, 1.42, 1.63, 1.10 and 1.67% (v/v), respectively. Danshensu and rosmarinic acid inhibited CYP2E1 and CYP2C9 with IC50 values of 36.63 and 75.76 µm, and 34.42 and 76.89 µm, respectively. Salvianolic acid A and B inhibited CYP2D6, CYP2E1 and CYP2C9 with IC50 values of 33.79, 21.64 and 31.94 µm, and 45.47, 13.52 and 24.15 µm, respectively. The study provides some useful information for safe and effective use of DHI in clinical practice.


Assuntos
Inibidores das Enzimas do Citocromo P-450/farmacologia , Sistema Enzimático do Citocromo P-450/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Cromatografia Líquida de Alta Pressão , Humanos , Medicina Tradicional Chinesa , Espectrometria de Massas em Tandem
10.
J Agric Food Chem ; 65(20): 4066-4073, 2017 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-28485147

RESUMO

As a major active stilbene from the leaves of pigeon pea (Cajanus cajan), cajaninstilbene acid (CSA) exerts various pharmacological activities. The present study aimed to investigate the pharmacokinetics of CSA and one of its main metabolites (M1) to explore their fate in the body and provide a pharmacokinetic foundation for their in vivo biological activities and functional food or complementary medicine application. M1 was characterized as CSA-3-O-glucuronide using the multiple reaction monitoring-information-dependent acquisition-enhanced product ion technique. After oral and intravenous administration, plasma, urine, and bile were collected and analyzed to estimate pharmacokinetic properties of CSA and M1 and to explore the main excretion route. The oral bioavailability of CSA was estimated to be 44.36%. This study first reported that CSA is mainly metabolized to CSA-3-O-glucuronide via the first-pass effect to limit its oral bioavailability and excreted predominantly through the biliary route, while the enterohepatic circulation, extravascular distribution, and renal reabsorption characteristics of CSA might delay its elimination.


Assuntos
Cajanus/química , Glucuronídeos/farmacocinética , Extratos Vegetais/farmacocinética , Salicilatos/farmacocinética , Estilbenos/farmacocinética , Animais , Disponibilidade Biológica , Glucuronídeos/química , Glucuronídeos/metabolismo , Masculino , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Ratos , Ratos Sprague-Dawley , Salicilatos/química , Salicilatos/metabolismo , Estilbenos/química , Estilbenos/metabolismo , Distribuição Tecidual
11.
Front Pharmacol ; 8: 101, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28326038

RESUMO

Ganoderic acid A (GAA), a representative active triterpenoid from Ganoderma lucidum, has been reported to exhibit antinociceptive, antioxidative, cytotoxic, hepatoprotective and anticancer activities. The present study aims (1) to identify GAA metabolites, in vivo by analyzing the bile, plasma and urine after intravenous administration to rats (20 mg/kg), and in vitro by incubating with rat liver microsomes (RLMs) and human liver microsomes (HLMs); (2) to investigate the metabolic kinetics of main GAA metabolites. Using HPLC-DAD-MS/MS techniques, a total of 37 metabolites were tentatively characterized from in vivo samples based on their fragmentation behaviors. The metabolites detected in in vitro samples were similar to those found in vivo. GAA underwent extensive phase I and II metabolism. The main metabolic soft spots of GAA were 3, 7, 11, 15, 23-carbonyl groups (or hydroxyl groups) and 12, 20, 28 (29)-carbon atoms. Ganoderic acid C2 (GAC2) and 7ß,15-dihydroxy-3,11,23-trioxo-lanost-26-oic acid were two main reduction metabolites of GAA, and their kinetics followed classical hyperbolic kinetics. The specific isoenzyme responsible for the biotransformation of the two metabolites in RLMs and HLMs was CYP3A. This is the first report on the comprehensive metabolism of GAA, as well as the metabolic kinetics of its main metabolites.

12.
Artigo em Inglês | MEDLINE | ID: mdl-28346885

RESUMO

Ganoderic acid A (GAA), an active triterpenoid of the traditional Chinese herbal medicine Lingzhi, has been reported to exhibit antinociceptive, antioxidative, and anti-cancer activities. The present study aims to establish a sensitive and rapid UPLC-MS/MS method for studying the plasma and brain pharmacokinetics of GAA in rats. The analytes were separated on a C18 column eluted with a gradient mobile phase consisting of acetonitrile and 0.1% aqueous formic acid at 0.3mL/min. The eluate was monitored by a mass detector using an MRM (m/z, 515.3-285.1) model in negative electrospray ionization. The calibration curve showed good linearity (r2>0.99), with limits of detection and quantification of 0.25 and 2.00 nmol/L, respectively. The intra- and inter-day precision and accuracy were less than 9.99% and ranged from 97.45% to 114.62%, respectively. The extraction recovery from plasma was between 92.89% and 98.87%. GAA was found to be stable in treated samples at room temperature (22°C) for 12h and in plasma at -20°C for 7d. The developed method was successfully applied to a pharmacokinetic study of GAA in rats. GAA could be rapidly absorbed into the circulation (Tmax, 0.15h) and eliminated relatively slowly (t1/2, 2.46h) after orally dosing, and could also be detected in the brain lateral ventricle (Tmax, 0.25h and t1/2, 1.40h) after intravenously dosing. The absolute oral bioavailability and brain permeability of GAA were estimated to be 8.68% and 2.96%, respectively.


Assuntos
Encéfalo/metabolismo , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/farmacocinética , Ácidos Heptanoicos/sangue , Ácidos Heptanoicos/líquido cefalorraquidiano , Lanosterol/análogos & derivados , Espectrometria de Massas em Tandem/métodos , Analgésicos/sangue , Analgésicos/líquido cefalorraquidiano , Animais , Antineoplásicos Fitogênicos/sangue , Antineoplásicos Fitogênicos/líquido cefalorraquidiano , Antioxidantes/farmacocinética , Lanosterol/sangue , Lanosterol/líquido cefalorraquidiano , Limite de Detecção , Masculino , Microdiálise/métodos , Ratos Sprague-Dawley
13.
Huan Jing Ke Xue ; 38(5): 2012-2020, 2017 May 08.
Artigo em Chinês | MEDLINE | ID: mdl-29965108

RESUMO

In order to investigate the effect of temperature on the cellulose-degrading bacteria and denitrifying bacteria, the denitrification and phosphorus removal of solid carbon source of cellulose corncob+sulfur/sponge iron nitrogen and phosphorus removal composite system, abbreviated as SCSC-S/Fe, was analyzed under different temperature conditions, and the surface structure and microbial properties of corncob before and after reaction were analyzed by scanning electron microscope (SEM) and MiSeq high-throughput sequencing technologies. The results indicated that when temperature increased from 15, 20, 25 to 30℃, the average TN removal rate of the system increased from 78.88% to 92.70%, the average removal rate of TP increased from 82.58% to 89.15%;microbial properties showed that the surface reaction after corncob was dominated by spherical and rod-shaped microorganisms; the proportion of cellulose-degrading bacteria was 11.01% higher at 30℃ than 20℃, and the proportion of denitrifying bacteria decreased by 21.26%. It can be seen that the cellulose -degrading bacteria were more sensitive to the temperature than the denitrification bacteria, and more obviously affected by the temperature.


Assuntos
Reatores Biológicos/microbiologia , Celulose/metabolismo , Nitrogênio/isolamento & purificação , Fósforo/isolamento & purificação , Desnitrificação , Ferro , Temperatura
14.
Huan Jing Ke Xue ; 38(10): 4309-4315, 2017 Oct 08.
Artigo em Chinês | MEDLINE | ID: mdl-29965216

RESUMO

In order to improve the ability of denitrification and phosphorus removal from reclaimed water, a novel composite filler was prepared using sulfur powder and sponge iron powder, and a comparative experiment was constructed at different HRT(hydraulic retention time) and C/N(carbon-nitrogen ratio) conditions between the novel filler and the composite filler. The results showed that the efficiency of nitrogen and phosphorus removal on the novel filler was higher than that on the grain filler (more than 30% higher at HRT=4 h and C/N=1). Moreover, based on the 16S rRNA gene clone library, the denitrification system in the two reactors included sulfur autotrophic denitrification bacteria and heterotrophic denitrification bacteria, while the proportion of sulfur autotrophic denitrification bacteria in the novel filler system was higher. The dominant bacteria in the novel filler and composite filler were Sulfurimonas and Acinetobacter, respectively.


Assuntos
Reatores Biológicos/microbiologia , Desnitrificação , Nitrogênio/isolamento & purificação , Fósforo/isolamento & purificação , Purificação da Água , Processos Autotróficos , Bactérias/classificação , Ferro , Nitratos , RNA Ribossômico 16S , Enxofre
15.
J Ethnopharmacol ; 194: 913-917, 2016 Dec 24.
Artigo em Inglês | MEDLINE | ID: mdl-27771456

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The Chinese herbal medicine He-Ye, the leaves of the lotus (Nelumbo nucifera) plant, is traditionally used in China for the treatment of sunstroke, thirst, diarrhea, and fever. Currently, the leaf is used not only as an herbal tea to reduce lipid level and control body weight, but also as a major ingredient in some lipid-lowering Chinese patented medicines. Our previous study demonstrated that the alkaloid fraction (AF) of the herb has a strong inhibitory effect on CYP2D6 isoenzyme activity in vitro. The present study aims to further verify this activity using the in vivo rat model and to explore the inhibitory mechanism on CYP2D6 using human liver microsomes (HLMs). MATERIALS AND METHODS: After a continuous 7-d oral dose of AF (50mg/kg) or a vehicle, Sprague Dawley rats received a single intravenous dose of dextromethorphan or metoprolol. Blood samples were collected at various time points, and the plasma concentrations of the relevant metabolites dextrorphan and hydroxymetoprolol were assayed by LC-MS/MS for evaluating the effect of AF on their pharmacokinetics and CYP2D6 activity. Dextromethorphan as a probe at different concentrations was incubated with HLMs in an incubation buffer system, in the presence or absence of AF at different concentrations. After incubation, the produced metabolite was assayed. RESULTS: After being pretreated with AF in rats, the plasma concentrations of dextrorphan and hydroxymetoprolol significantly decreased, with Cmax going from 79.44 to 29.96 and 151.18 to 83.39hng/mL (P<0.05), AUCall from 167.27 to 62.25 and 347.68 to 223.24hng/mL (P<0.05), and AUCinf from 183.39 to 84.76 and 350.59 to 234.57hng/mL (P<0.05), respectively, in comparison with those of untreated rats. The t1/2 of hydroxymetoprolol significantly increased from 1.14 to 1.99h (P<0.05). The in vitro incubation test showed that AF competitively inhibited the CYP2D6, with apparent Ki value of 0.64µg/mL. CONCLUSIONS: AF can strongly inhibit the activity of CYP2D6 enzyme, as confirmed by in vivo and in vitro models. Possible drug interactions may occur between AF and other medications metabolized by CYP2D6. Thus, caution should be paid when the lotus leaf and its preparations are concurrently administered with conventional medicines.


Assuntos
Alcaloides/farmacologia , Inibidores do Citocromo P-450 CYP2D6/farmacologia , Citocromo P-450 CYP2D6/metabolismo , Isoenzimas/antagonistas & inibidores , Nelumbo/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Alcaloides/química , Animais , Dextrometorfano/farmacologia , Dextrorfano/farmacologia , Interações Medicamentosas , Masculino , Metoprolol/farmacologia , Microssomos Hepáticos/efeitos dos fármacos , Microssomos Hepáticos/metabolismo , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley
16.
Huan Jing Ke Xue ; 37(2): 558-64, 2016 Feb 15.
Artigo em Chinês | MEDLINE | ID: mdl-27363144

RESUMO

Kinetic curves and isotherms were investigated to study the sorption mechanism of phosphorus onto the sediments of Sanggou Bay, together with the surface charge properties of sediments and the forms of phosphorus studied. The results showed that the sorption including a fast process and a slow one, and could be described by a two-compartment first order equation. The thermodynamic isotherms were well fitted with a modified Langmuir equation. The maximum adsorption capacity was larger in summer than in spring, and the smaller particle size was favorable to the sorption. The maximum adsorption capacities (Qm) were 0.0471-0.1230 mg x g(-1), and the zero equilibrium phosphorus concentration (EPC0) of the sediments ranged from 0.0596 mg x L(-1) to 0.1927 mg x L(-1), which indicated that the sediments from Sanggou Bay were sources of phosphorus. Inorganic phosphorus (IP) was the main form of total phosphorus (TP). The contents of exchangeable or loosely absorbed P and Fe-bound P increased significantly in the samples after sorption. The sorption process involved physical sorption and chemical sorption, with the former being the predominant.


Assuntos
Baías , Monitoramento Ambiental , Sedimentos Geológicos/química , Fósforo/análise , Poluentes Químicos da Água/análise , Adsorção , China , Estações do Ano , Propriedades de Superfície
17.
J Ethnopharmacol ; 188: 39-47, 2016 Jul 21.
Artigo em Inglês | MEDLINE | ID: mdl-27109340

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Ginseng, the roots and rhizomes of Panax ginseng C.A. Mey. (Araliaceae), is used as a tonic herb for thousands of years in Asian countries. Saponins are recognized as its major active ingredients and reportedly can ease disorders caused by various adverse stimuli. Nevertheless, it is unclear whether ginseng saponins have beneficial effects on stress caused by microgravity. AIM OF THE STUDY: This study aimed to assess the anti-stress effects and corresponding mechanisms of ginseng total saponins (GTSs) on simulated microgravity (SM) hindlimb-unloaded rats using a metabolomics method. MATERIALS AND METHODS: The stressed rats were induced by hindlimb unloading for 7 continuous days. Levels of plasma corticosterone (CORT) and weights of immune organs including the thymuses, spleens, and adrenal glands were determined. Urinary metabolic profiles of the rats under the simulated microgravity condition with and without GTSs intervention were compared using an ultra-performance liquid chromatography quadrupole time of flight mass spectrometry (UPLC-QTOF-MS) based metabolomics method. Multivariate statistical analysis including Principal Component Analysis (PCA) and Partial Least Squares project to latent structures-Discriminant Analysis (PLS-DA) were performed. RESULTS: Compared with control (66.22±10.40ng/mL), the plasma CORT level of the SM rats (82.67±13.64ng/mL) were significantly (p<0.05) elevated, and GTSs could restore this elevation to a lower level (77.75±14.35ng/mL). GTSs could also significantly alleviate the atrophy of the thymuses and the spleens, as well as the hypertrophy of the adrenal glands of the SM rats. Urinary metabolic profiling showed comprehensive metabolic variation among the three groups. A series of metabolic pathways including taurine and hypotaurine, purine and pyridine, and amino acid were affected. Eleven potential biomarkers such as taurine, adenine, and valine were identified. GTSs could correct the disturbed metabolic pathways and restore the variation of these potential markers. CONCLUSION: GTSs can exert anti-stress effects by reducing the secretion of plasma CORT, enhancing the immune function, and restoring an array of disturbed metabolic pathways and metabolites. The findings of this study provide crucial evidence of a link between metabolic imbalance and microgravity, and reveal a molecular basis for the anti-stress benefits of GTSs in the management of microgravity-related disorders.


Assuntos
Aminoácidos/urina , Elevação dos Membros Posteriores , Metabolômica , Panax/química , Extratos Vegetais/farmacologia , Saponinas/farmacologia , Estresse Fisiológico/efeitos dos fármacos , Glândulas Suprarrenais/efeitos dos fármacos , Glândulas Suprarrenais/metabolismo , Glândulas Suprarrenais/patologia , Animais , Comportamento Animal/efeitos dos fármacos , Biomarcadores/sangue , Biomarcadores/urina , Cromatografia Líquida de Alta Pressão , Biologia Computacional , Corticosterona/sangue , Hipertrofia , Análise dos Mínimos Quadrados , Masculino , Metabolômica/métodos , Análise Multivariada , Reconhecimento Automatizado de Padrão , Fitoterapia , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Análise de Componente Principal , Ratos Sprague-Dawley , Saponinas/isolamento & purificação , Espectrometria de Massas por Ionização por Electrospray , Baço/efeitos dos fármacos , Baço/metabolismo , Baço/patologia , Timo/efeitos dos fármacos , Timo/metabolismo , Timo/patologia , Fatores de Tempo , Urinálise , Simulação de Ausência de Peso
18.
J Pharm Biomed Anal ; 125: 329-38, 2016 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-27100700

RESUMO

Microgravity-induced memory deficiency seriously affects learning and memory ability of the astronaut during spaceflight, with few effective countermeasures. Panax ginseng C. A. Mey. has been used as a nootropic herb for thousands of years in Asian countries. Saponins are recognized as its major active components. Previous studies have shown that ginseng saponins offer protection against memory deficits caused by various factors. Nevertheless, the underlying mechanisms of their nootropic effects are still largely unknown. In this study, we evaluated the memory-improving effects of ginseng total saponins (GTS) on simulated microgravity hindlimb-unloaded rats using a metabolomics approach. After being exposed to a 7-days hindlimb unloading (HU), variations of plasmatic and hippocampal metabolic profiles of rats with and without GTS intervention were examined by a liquid chromatography-mass spectrometry (LC-MS) based untargeted metabolomics method. Subsequently, 8 hippocampal neurotransmitters were determined using a LC-MS/MS method. Finally, a LC-MS/MS based targeted metabolomics was performed to validate biomarkers found in the untargeted analysis. Besides, to support the metabolomics results, passive avoidance (PA) test, Nissl staining, and plasmatic corticosterone (CORT) levels determination were performed. The results showed that HU could lead to variations of 7 neurotransmitters and significantly different plasmatic and hippocampal metabolic profiles. GTS could restore most of the imbalanced neurotransmitters, especially glutamic acid and acetylcholine, and correct the levels of various disturbed learning and memory relevant biomarkers such as asparagine, phenylalanine, tyrosine, tryptophan, and choline. In addition, GTS could markedly ameliorate HU-induced memory deficiency, protect hippocampal neurons from damage, and down-regulate elevated CORT levels. In conclusion, GTS exhibits memory-improving effects mainly through regulating the metabolism of amino acids, neurotransmitters, choline, kynurenine, and sphingolipids. The findings of this study not only can deepen our understanding of the underlying molecular mechanisms of MG-induced memory disorders, but also provide scientific evidence for choosing ginseng as a countermeasure against MG-induced memory deficiency.


Assuntos
Cromatografia Líquida/métodos , Espectrometria de Massas/métodos , Transtornos da Memória/tratamento farmacológico , Metabolômica , Panax/metabolismo , Saponinas/uso terapêutico , Ausência de Peso/efeitos adversos , Animais , Masculino , Transtornos da Memória/etiologia , Ratos , Ratos Sprague-Dawley
19.
ACS Appl Mater Interfaces ; 7(15): 8284-92, 2015 Apr 22.
Artigo em Inglês | MEDLINE | ID: mdl-25825954

RESUMO

A series of phenolphthalein-based poly(arylene ether sulfone nitrile)s (PESN) multiblock copolymers containing 1-methylimidazole groups (ImPESN) were synthesized to prepare anion exchange membranes (AEMs) for alkaline fuel cells. The ion groups were introduced selectively and densely on the unit of phenolphthalein as the hydrophilic segments, allowing for the formation of ion clusters. Strong polar nitrile groups were introduced into the hydrophobic segments with the intention of improving the dimensional stability of the AEMs. A well-controlled multiblock structure was responsible for the well-defined hydrophobic/hydrophilic phase separation and interconnected ion-transport channels, as confirmed by atomic force microscopy and small angle X-ray scattering. The ImPESN membranes with low swelling showed a relatively high water uptake, high hydroxide ion conductivity together with good mechanical, thermal and alkaline stability. The ionic conductivity of the membranes was in the range of 3.85-14.67×10(-2) S·cm(-1) from 30 to 80 °C. Moreover, a single H2/O2 fuel cell with the ImPESN membrane showed an open circuit voltage of 0.92 V and a maximum power density of 66.4 mW cm(-2) at 60 °C.

20.
Zhongguo Gu Shang ; 27(1): 17-20, 2014 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-24754138

RESUMO

OBJECTIVE: To study soft tissue changes observed through musculoskeletal ultrasound (MSUS) in the treatment of knee osteoarthritis with needle-knife, so as to provide MSUS basis for needle-knife in the treatment of knee osteoarthritis. METHODS: Forty patients with knee osteoarthritis treated in the Third Affiliated Hospital of Beijing University of Chinese Medicine from December 2011 to December 2012 were selected according to inclusion and exclusion criteria. All the patients were treated with needle-knife release method. The VAS scores and knee joint circumference were recorded before treatment and 2 weeks after treatment. The changes of knee joint hydrops articuli and joint synovial thickness were measured through MSUS. RESULTS: The knee pain index was 6.850 +/- 1.417 before treatment and 2.790 +/- 1.299 after treatment;the index after treatment was lower than that of before treatment. The knee joint circumference was 407.320 +/- 45.151 mm before treatment and 391.240 +/- 41.129 mm after treatment; the knee joint circumference decreased after treatment. The amount of hydrops articuli observed by musculoskeletal ultrasound showed that 47 knees were cured, 19 knees improved and 2 knees failed. The synovial membrane thickness: 43 knees cured, 17 knees improved and 8 knees failed. CONCLUSION: The hydrops articuli and synovial thickness of knee joint of patients with knee osteoarthritis observed under the MSUS is consistent with the main symptoms and signs, which suggests that MSUS observation on soft tissue changes before and after needle knife in the treatment of knee osteoarthritis with high reliability.


Assuntos
Articulação do Joelho/diagnóstico por imagem , Articulação do Joelho/patologia , Agulhas , Osteoartrite do Joelho/patologia , Osteoartrite do Joelho/cirurgia , Adulto , Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Osteoartrite do Joelho/complicações , Osteoartrite do Joelho/diagnóstico por imagem , Dor/complicações , Membrana Sinovial/patologia , Resultado do Tratamento , Ultrassonografia
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