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1.
J Fish Dis ; 46(9): 977-986, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37294673

RESUMO

Streptococcosis disease caused by Streptococcus agalactiae (Group B Streptococcus, GBS) results in a huge economic loss of tilapia culture. It is urgent to find new antimicrobial agents against streptococcosis. In this study, 20 medicinal plants were evaluated in vitro and in vivo to obtain medicinal plants and potential bioactive compounds against GBS infection. The results showed that the ethanol extracts of 20 medicinal plants had low or no antibacterial properties in vitro, with a minimal inhibitory concentration ≥256 mg/L. Interestingly, in vivo tests showed that 7 medicinal plants could significantly inhibit GBS infection in tilapia, and Sophora flavescens (SF) had the strongest anti-GBS activity in tilapia, reaching 92.68%. SF could significantly reduce the bacterial loads of GBS in different tissues (liver, spleen and brain) of tilapia after treated with different tested concentrations (12.5, 25.0, 50.0 and 100.0 mg/kg) for 24 h. Moreover, 50 mg/kg SF could significantly improve the survival rate of GBS-infected tilapia by inhibiting GBS replication. Furthermore, the expression of antioxidant gene cat, immune-related gene c-type lysozyme and anti-inflammatory cytokine il-10 in liver tissue of GBS-infected tilapia significantly increased after treated with SF for 24 h. Meanwhile, SF significantly reduced the expression of immune-related gene myd88 and pro-inflammatory cytokines il-8 and il-1ß in liver tissue of GBS-infected tilapia. The negative and positive models of UPLC-QE-MS, respectively, identified 27 and 57 components of SF. The major components of SF extract in the negative model were α, α-trehalose, DL-malic acid, D- (-)-fructose and xanthohumol, while in the positive model were oxymatrine, formononetin, (-)-maackiain and xanthohumol. Interestingly, oxymatrine and xanthohumol could significantly inhibit GBS infection in tilapia. Taken together, these results suggest that SF can inhibit GBS infection in tilapia, and it has potential for the development of anti-GBS agents.


Assuntos
Ciclídeos , Doenças dos Peixes , Plantas Medicinais , Infecções Estreptocócicas , Tilápia , Animais , Sophora flavescens , Streptococcus agalactiae/genética , Doenças dos Peixes/tratamento farmacológico , Doenças dos Peixes/microbiologia , Infecções Estreptocócicas/tratamento farmacológico , Infecções Estreptocócicas/veterinária , Infecções Estreptocócicas/microbiologia , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Tilápia/microbiologia , Citocinas , Ciclídeos/microbiologia
2.
Zhongguo Zhong Yao Za Zhi ; 48(1): 82-95, 2023 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-36725261

RESUMO

With the approach of untargeted metabolomics and correlation analysis, this study aimed to explore the mechanism of Aurantii Fructus from Lingnan region in alleviating dryness by analyzing the different effects of raw Aurantii Fructus(RAF) and processed Aurantii Fructus(PAF) on fecal endogenous metabolism in normal rats. Eighteen Sprague-Dawley(SD) rats were randomly divided into a control group(C), an RAF group(10 g·kg~(-1)), and a PAF group(10 g·kg~(-1)). After seven days of administration, the effects of RAF and PAF on dryness-related indexes were compared, including water intake, fecal water content, salivary secretion, the expression of AQP5, VIP, and 5-HT in the submandibular gland, as well as the expression of AQP3, VIP, and 5-HT in the colon. The fecal samples in each group were determined by LC-MS. Multivariate statistical analysis and Pearson correlation coefficient were used for screening the differential metabolites and metabolic pathways in alleviating dryness of RAF. The results indicated that both RAF and PAF showed certain dryness, and the dryness of RAF was more significant. Moreover, PAF could alleviate dryness of RAF to a certain extent by reducing the water intake, fecal water content, and the expression of AQP3, VIP, and 5-HT in the colon and increasing the salivary secretion and the levels of AQP5, VIP, and 5-HT in the submandibular gland. According to the analysis of fecal metabolomics, 99 and 58 metabolites related to dryness were found in RAF and PAF respectively, where 16 of them played an important role in alleviating dryness of RAF. Pathway analysis revealed that the mechanism of PAF in alleviating dryness of RAF was presumably related to the regulation of riboflavin metabolism, purine metabolism, arginine biosynthesis, pyrimidine metabolism, alanine metabolism, aspartate metabolism, glutamate metabolism, and retinol metabolism pathways. This study suggested that PAF might alleviate dryness of RAF by affecting the metabolic levels of the body, which provides a new basis for further clarifying the processing mechanism of PAF.


Assuntos
Medicamentos de Ervas Chinesas , Ratos , Animais , Medicamentos de Ervas Chinesas/farmacologia , Ratos Sprague-Dawley , Serotonina , Metabolômica , Água
3.
J Food Sci ; 87(8): 3355-3365, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35822303

RESUMO

Drying is the key process through which the aroma of tencha forms. However, the effects of drying method on volatiles are unknown. We compared tencha-ro drying with regular drying. Volatiles in tencha infusions were extracted using headspace solid-phase microextraction and solvent-assisted flavor evaporation combined with gas chromatography-mass spectrometry. Partial least squares (PLS), odor activity value (OAV), and heat map analyses were performed to identify the optimal drying method for creating a seaweed-like aroma. Changes in the key volatile compounds of the samples were investigated. The tencha infusions contained 125 volatiles with nine chemical structures. According to the sensory evaluation, tencha-ro drying was the optimal method for producing high-quality tencha with an intense and consistent seaweed-like aroma. The PLS model accurately distinguished among the types of tencha. By combining OAVs with screening through multivariate statistical analysis, six volatile compounds were revealed to contribute substantially to tencha's seaweed-like aroma: 2-ethyl-3,5-dimethylpyrazine, 2-ethyl-6-methylpyrazine, 2-ethyl-5-methylpyrazine, dimethyl sulfide, ß-ionone, and 2-formyl-1-methylpyrrole. The findings provide a theoretical basis and technical guidance for the processing of high-quality tencha with a strong seaweed-like aroma. PRACTICAL APPLICATION: This study demonstrated that tencha-ro drying contributes to the formation of a seaweed-like aroma in tencha and provides theoretical guidance for tea factories to use the appropriate drying methods for high-quality tencha.


Assuntos
Camellia sinensis , Compostos Orgânicos Voláteis , Camellia sinensis/química , Cromatografia Gasosa-Espectrometria de Massas/métodos , Odorantes/análise , Microextração em Fase Sólida , Verduras , Compostos Orgânicos Voláteis/análise
4.
Pharm Biol ; 60(1): 810-824, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-35587996

RESUMO

CONTEXT: Moringa oleifera Lam. (Moringaceae) (MO) is an important food plant that has high nutritional and medical value. However, there is limited information on whether its seeds can improve sleep. OBJECTIVE: This study investigated the effects of MO seed ethanol extracts (EEMOS) on sleep activity improvement and examined the underlying mechanisms. MATERIALS AND METHODS: Male ICR mice were placed into six groups (n = 12) and treated as follows: Control (sodium carboxymethyl cellulose, 20 mL/kg), estazolam tablets (2 mg/kg), EEMOS (1, 2 g/kg) and kaempferol (1, 2 mg/kg). These samples were successively given intragastric for 14 d. Locomotor activity assay, pentobarbital-induced sleeping and pentetrazol-induced seizures tests were utilized to examine the sedative-hypnotic effects (SHE) of EEMOS. RESULTS: Compared with the control group, the results revealed that EEMOS (2 g/kg) and KA (2 mg/kg) possessed good SHE and could significantly elevate the levels of γ-aminobutyric acid and reduce the levels of glutamic acid in the mouse hypothalamus (p < 0.05). Moreover, SHE was blocked by picrotoxin, flumazenil and bicuculline (p < 0.05). EEMOS (2 g/kg) and KA (2 mg/kg) significantly upregulated the protein expression levels of glutamic acid decarboxylase-65 (GAD65) and α1-subunit of GABAA receptors in the hypothalamus of mice (p < 0.05), not affecting glutamic acid decarboxylase-67 (GAD67) and γ2-subunit expression levels (p > 0.05). Additionally, they cause a significant increase in Cl- influx in human cerebellar granule cells at a concentration of 8 µg/mL (p < 0.05). DISCUSSION AND CONCLUSIONS: These findings demonstrated that EEMOS could improve sleep by regulating GABAA-ergic systems, and encourage further clinical trials to treat insomnia.


Assuntos
Moringa oleifera , Pentobarbital , Animais , Etanol/farmacologia , Glutamato Descarboxilase/metabolismo , Hipnóticos e Sedativos/farmacologia , Quempferóis/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos ICR , Pentobarbital/farmacologia , Extratos Vegetais/farmacologia , Receptores de GABA-A/metabolismo , Sementes , Sono , Ácido gama-Aminobutírico/metabolismo , Ácido gama-Aminobutírico/farmacologia
5.
J Fish Dis ; 45(6): 815-823, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35315084

RESUMO

Streptococcus agalactiae, also known as Group B Streptococcus (GBS), can infect humans, terrestrial animals and fish. The emergence of bacterial resistance of S. agalactiae to antibiotics leads to an urgent need of exploration of new antimicrobial agents. In the study, the antibacterial activity of natural component plumbagin (PLB) against S. agalactiae was investigated in vitro and in vivo. The results showed that the minimal inhibitory concentration (MIC) of PLB against S. agalactiae was 8 mg/L. The growth curve assay revealed that PLB could inhibit the growth of S. agalactiae. In addition, the time-killing curve showed that S. agalactiae was killed almost completely by 2-fold MIC of PLB within 12 h. Transmission electron microscopy results showed obvious severe morphological destruction and abnormal cells of S. agalactiae after treated with PLB. The pathogenicity of S. agalactiae to zebrafish was significantly decreased after preincubation with PLB for 2 h in vitro, further indicating the bactericidal activity of PLB. Interestingly, PLB could kill S. agalactiae without inducing resistance development. Furthermore, pretreatment and post-treatment assays suggested that PLB also exhibited the antibacterial activity against S. agalactiae infection in vivo by effectively reducing the bacterial load and improving the survival rate of S. agalactiae-infected zebrafish. In summary, PLB had potent antibacterial activity against S. agalactiae in vitro and in vivo, and it could be an excellent antimicrobial candidate to prevent and control S. agalactiae infection.


Assuntos
Doenças dos Peixes , Infecções Estreptocócicas , Animais , Antibacterianos/farmacologia , Doenças dos Peixes/microbiologia , Naftoquinonas , Infecções Estreptocócicas/tratamento farmacológico , Infecções Estreptocócicas/microbiologia , Infecções Estreptocócicas/veterinária , Streptococcus agalactiae , Peixe-Zebra
6.
Food Chem ; 359: 129950, 2021 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-33945989

RESUMO

The black tea could be stored for a long time, and subsequently affects the flavor characteristics. In the present study, the effects of storage years (1, 2, 3, 4, 5, 10, 17 and 20 years) on the chemical profiling and taste quality of keemun black tea (KBT) were compared by metabolomics and quantitative sensory evaluation. The main polyphenols were degraded during the storing, especially 10-year storage, but caffeine and theobromine were stable. The intensity of bitterness, astringency, umami was negatively correlated to storage years, with correlation coefficient at -0.95, -0.91 and -0.83 respectively, whereas sweetness had positive correlation coefficient at 0.74. Quinic acid, galloylated catechins, linolenic acid, linoleic acid, malic acid, palamitic acid, and theaflavin-3́-gallate were marker compounds which were responsible for distinguishing short and long time preserved KBT. The contents of fatty acids were positively correlated to storage time and sweet intensity.


Assuntos
Metabolômica , Chá/química , Adstringentes/análise , Biflavonoides , Cafeína/análise , Catequina , Ácido Gálico/análogos & derivados , Polifenóis/análise , Ácido Quínico/análise , Paladar
7.
Int Immunopharmacol ; 86: 106727, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32593158

RESUMO

Luteolin, a natural flavonoid exists in various medicinal plants, has strong anti-inflammatory effect. However, anti-inflammatory mechanism of luteolin has not been fully explored. Hence, we systematically investigated druggability and anti-inflammatory mechanism of luteolin based on network pharmacology and in vitro experiments. The absorption, distribution, metabolism and excretion of luteolin were evaluated by TCMSP server. Targets associated with luteolin and inflammation were collected from public databases, and the overlapping targets between luteolin and inflammation were analyzed by Draw Venn diagram. Then the protein-protein interaction network of luteolin against inflammation was constructed. Further, gene function and pathway enrichment analysis were performed. Finally, in vitro experiments were carried out to estimate the accuracy of predicted target genes. ADME results indicated that luteolin has great potential to be developed into a drug. 226 overlapping targets were screened by matching 280 targets of luteolin with 9015 targets of inflammation. 9 core targets of luteolin against inflammation were identified, including MMP9, MAPK1, HSP90AA1, CASP3, ALB, EGFR, SRC, HRAS and ESR1. Gene function were mainly involved in metabolism, energy pathways and signal transduction. Metabolic pathways, pathways in cancer, PI3K-AKT signaling pathway, Ras signaling pathway and so on might be the critical pathways of luteolin against inflammation. RT-qPCR and ELISA results indicated that luteolin decreased the expression of most of core genes at protein and mRNA levels (MMP9, MAPK1, HSP90AA1, EGFR, SRC and HRAS). Luteolin is expounded to have great potential to be developed into a drug and target various genes and pathways to perform anti-inflammatory effect.


Assuntos
Anti-Inflamatórios/farmacologia , Luteolina/farmacologia , Proteoma/efeitos dos fármacos , Transcriptoma/efeitos dos fármacos , Animais , Anti-Inflamatórios/farmacocinética , Anti-Inflamatórios/uso terapêutico , Caspase 3/metabolismo , Biologia Computacional , Bases de Dados Genéticas , Bases de Dados de Produtos Farmacêuticos , Receptores ErbB/metabolismo , Receptor alfa de Estrogênio/metabolismo , Proteínas de Choque Térmico HSP90/metabolismo , Inflamação/tratamento farmacológico , Inflamação/genética , Luteolina/farmacocinética , Luteolina/uso terapêutico , Metaloproteinase 9 da Matriz/metabolismo , Camundongos , Proteína Quinase 1 Ativada por Mitógeno/metabolismo , Mapas de Interação de Proteínas , Proteínas Proto-Oncogênicas p21(ras)/metabolismo , Proteínas Proto-Oncogênicas pp60(c-src)/metabolismo , Células RAW 264.7 , Albumina Sérica/metabolismo , Transdução de Sinais/efeitos dos fármacos
8.
J Agric Food Chem ; 68(10): 3149-3162, 2020 Mar 11.
Artigo em Inglês | MEDLINE | ID: mdl-32062961

RESUMO

Moringa oleifera Lam. (MO), which is widely consumed as both food and herbal medicine in tropical and subtropical regions, has a wide spectrum of health benefits. Yet, whether the oil obtained from MO seeds could affect (improve) the sleep activity remains unclear. Herein, we used the locomotor activity, pentobarbital-induced sleeping, and pentetrazol-induced convulsions test to examine sedative-hypnotic effects (SHE) of MO oil (MOO) and explored the underlying mechanisms. Besides, the main components of MOO like oleic acid, ß-Sitosterol, and Stigmasterol were also evaluated. The results showed that they possessed good SHE. Except for oleic acid and Stigmasterol, they could significantly elevate γ-amino butyric acid (GABA) and reduce glutamic acid (Glu) levels in the hypothalamus of mice. Moreover, SHE was blocked by picrotoxin, flumazenil, and bicuculline, except for oleic acid, which could not be antagonized by picrotoxin. Molecular mechanisms showed that MOO and ß-Sitosterol significantly upregulated the amount of protein-level expression of Glu decarboxylase-65 (GAD65) and α1-subunit of GABAA receptors in the hypothalamus of mice, not affecting GAD67, γ2 subunits. These data indicated that MOO modulates sleep architectures via activation of the GABAA-ergic systems.


Assuntos
Hipnóticos e Sedativos/administração & dosagem , Moringa oleifera/química , Pentobarbital/administração & dosagem , Extratos Vegetais/administração & dosagem , Óleos de Plantas/administração & dosagem , Receptores de GABA-A/metabolismo , Sono/efeitos dos fármacos , Ácido gama-Aminobutírico/metabolismo , Animais , Humanos , Hipotálamo/efeitos dos fármacos , Hipotálamo/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos ICR , Receptores de GABA-A/genética , Sementes/química , Ácido gama-Aminobutírico/genética
9.
Hepatology ; 68(4): 1260-1276, 2018 10.
Artigo em Inglês | MEDLINE | ID: mdl-29624717

RESUMO

Hepatitis B virus (HBV) infection remains a major health problem worldwide. Maintenance of the covalently closed circular DNA (cccDNA), which serves as a template for HBV RNA transcription, is responsible for the failure of eradicating chronic HBV during current antiviral therapy. cccDNA is assembled with cellular histone proteins into chromatin, but little is known about the regulation of HBV chromatin by histone posttranslational modifications. In this study, we identified silent mating type information regulation 2 homolog 3 (SIRT3) as a host factor restricting HBV transcription and replication by screening seven members of the sirtuin family, which is the class III histone deacetylase. Ectopic SIRT3 expression significantly reduced total HBV RNAs, 3.5-kb RNA, as well as replicative intermediate DNA in HBV-infected HepG2-Na+ /taurocholate cotransporting polypeptide cells and primary human hepatocytes. In contrast, gene silencing of SIRT3 promoted HBV transcription and replication. A mechanistic study found that nuclear SIRT3 was recruited to the HBV cccDNA, where it deacetylated histone 3 lysine 9. Importantly, occupancy of SIRT3 on cccDNA could increase the recruitment of histone methyltransferase suppressor of variegation 3-9 homolog 1 to cccDNA and decrease recruitment of SET domain containing 1A, leading to a marked increase of trimethyl-histone H3 (Lys9) and a decrease of trimethyl-histone H3 (Lys4) on cccDNA. Moreover, SIRT3-mediated HBV cccDNA transcriptional repression involved decreased binding of host RNA polymerase II and transcription factor Yin Yang 1 to cccDNA. Finally, hepatitis B viral X protein could relieve SIRT3-mediated cccDNA transcriptional repression by inhibiting both SIRT3 expression and its recruitment to cccDNA. CONCLUSION: SIRT3 is a host factor epigenetically restricting HBV cccDNA transcription by acting cooperatively with histone methyltransferase; these data provide a rationale for the use of SIRT3 activators in the prevention or treatment of HBV infection. (Hepatology 2018).


Assuntos
DNA Viral/genética , Epigênese Genética/genética , Hepatite B/genética , Domínios PR-SET/genética , Sirtuína 3/genética , Replicação Viral/genética , DNA Complementar/genética , Hepatite B/fisiopatologia , Vírus da Hepatite B/genética , Histona Metiltransferases/metabolismo , Humanos , Reação em Cadeia da Polimerase em Tempo Real/métodos , Sensibilidade e Especificidade
10.
J Food Drug Anal ; 25(4): 854-861, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28987362

RESUMO

This study aimed to investigate the direct and immune-stimulated antiproliferative activities of jelly fig achenes fractions including pectinesterase inhibitors, crude polyphenols extract, and purified polyphenols extract (PP). Beside the measurement of cell viability of U937, the quantity of cytokines in conditioned medium and morphologic changes in leukemia were observed. After surveying all fractions in jelly fig, the obtained fractions of polyphenol exhibited the highest stimulating effects and directly cytotoxic effects against leukemia with the lowest effect found in protein fractions. The leukemia treated by our PP fraction showed dose-dependent response between the concentration and G2/M cell numbers of the U937 cells. The PP fraction had more pronounced effect on immune-stimulated than direct antiproliferative activities. The finding was also supported by morphological analysis by showing the formation of apoptotic bodies and differentiation from immature U937 cells into mature monocytes/macrophages on cells cultured with PP-conditioned medium. In conclusion, polyphenol fraction of pectinesterase inhibitors from jelly fig showed the immune-stimulated antiproliferative activities against U937 cell.


Assuntos
Proliferação de Células/efeitos dos fármacos , Ficus/química , Inibidores do Crescimento/farmacologia , Leucemia/fisiopatologia , Extratos Vegetais/farmacologia , Proteínas de Plantas/farmacologia , Polifenóis/farmacologia , Humanos , Leucemia/tratamento farmacológico , Células U937
11.
Fitoterapia ; 121: 212-222, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28774689

RESUMO

A flavonoid hesperetin is reported to have a variety of biological activities, including anticancer, antiviral, antioxidant, neuroprotective and anti-inflammatory properties. Thirty-one novel hesperetin derivatives were designed, synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells and CCl4-induced acute liver injury model. Among these compounds, 5b displayed the excellent anti-inflammatory activity on decreasing NO, IL-6 and TNF-α both in vitro and vivo. In addition, 5b could also reduce the release of NO, IL-6 and TNF-α production by LPS stimulated RAW 264.7 cell through MAPK and NF-κB signaling pathway in a concentration dependent manner. From in vivo study, it was also observed that 5b attenuated liver histopathologic changes in mouse models.


Assuntos
Anti-Inflamatórios/farmacologia , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Hesperidina/farmacologia , Animais , Anti-Inflamatórios/síntese química , Hesperidina/síntese química , Interleucina-6/metabolismo , Fígado/efeitos dos fármacos , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos C57BL , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Células RAW 264.7 , Fator de Necrose Tumoral alfa/metabolismo
12.
ACS Appl Mater Interfaces ; 9(31): 25755-25766, 2017 Aug 09.
Artigo em Inglês | MEDLINE | ID: mdl-28714303

RESUMO

The design of biocompatible and efficacious anticancer biomaterials to achieve relatively low tumor recurrence rates is the main pursuit of cancer photothermal therapy (PTT). RADA16-I is a synthetic amphiphilic peptide with the sequence RADARADARADARADA that can self-assemble into a peptide nanofiber hydrogel. In this study, we synthesized a novel melittin-RADA32-indocyanine green (ICG) hydrogel ("MRI hydrogel"), which contains melittin in the peptide hydrogel backbone and ICG in the hydrogel matrix, for enhanced PTT of glioblastomas. The MRI hydrogel exhibited physiologic characteristics similar to those of the RADA16 hydrogel, while displaying concentration-dependent cytotoxicity to C6 glioma cells and photothermal effects. The in vivo biodistribution of the MRI hydrogel was visualized by near-infrared fluorescence and photoacoustic imaging. More importantly, in vivo PTT provided by the MRI hydrogel significantly reduced the tumor size and the tumor recurrence rate compared with the RADR16-ICG hydrogel and other controls, suggesting a synergistic effect of MRI hydrogel-carried melittin and ICG-based PTT treatment. Thus, MRI provides an alternative tool for the safe and efficient PTT treatment of tumors.


Assuntos
Meliteno/química , Glioblastoma , Humanos , Hidrogéis , Fototerapia , Distribuição Tecidual
13.
Curr Drug Deliv ; 14(5): 650-657, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28201965

RESUMO

PURPOSE: This study aimed to develop a synchronized and sustained-release silymarin dropping pill, and to evaluate its pharmacokinetic characteristics. METHOD: Polyoxyethylene stearate, glyceryl monostearate, and stearic acid were used to prepare the dropping pills. X-ray powder diffraction, differential scanning calorimetry, and release were used to evaluate its physicochemical properties. The plasma concentration of silybin in beagle dogs after oral administration of silymarin dropping pills and silymarin capsule was determined by RP-HPLC. RESULTS: Synchronized release was achieved with high similarity factor f2 values between every set of two of the five components. Mean plasma concentration-time curves of silymarin after oral administration of dropping pills in beagle dogs were in accordance with first-order absorption and open twocompartment model. The Tmax, Cmax, and AUC0-∞ of dropping pills in beagle dogs were 0.8750±0.13 h, 0.8183±0.07 µg·ml-1, and 2.274±0.90 µg·h·ml-1, respectively. Silymarin dropping pills prolonged in vivo exposure and reduced maximum in vivo concentration, achieving a stable level in the serum. CONCLUSION: The combination of solid dispersion technique and dropping pill formulation allowed synchronized release of multiple components in herbal medicine, and has potential application in the development of sustained release in herbal medicine.


Assuntos
Preparações de Ação Retardada , Medicamentos de Ervas Chinesas/administração & dosagem , Silimarina/administração & dosagem , Administração Oral , Animais , Disponibilidade Biológica , Cães , Medicamentos de Ervas Chinesas/farmacocinética , Silimarina/farmacocinética , Solubilidade
14.
Drug Des Devel Ther ; 10: 519-31, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26889080

RESUMO

The pharmacological activity of herbal medicine is an overall action of each component in accordance with their original proportion. An efficient, sustained, and controlled-release drug delivery system of herbal medicine should ensure the synchronized drug release of each active component during the entire release procedure. In this study, silymarin (SM), a poorly soluble herbal medicine, was selected as a model drug to develop a synchronized-release drug delivery system: an SM microporous osmotic pump (MPOP) tablet. The SM was conjugated with phospholipid (SM phytosome complex, SM-PC) to improve the solubility, and the difference in the apparent octanol-water partition coefficient between the two components was significantly reduced. The dissolution rate of SM-PC was significantly higher than SM active pharmaceutical ingredients and was the same as that of the commercial SM capsule. The SM-PC was used to generate the MPOP tablet. SM was mixed with poly(ethylene) oxide and sodium chloride (an osmotic agent) to form the MPOP core, followed by coating with cellulose acetate and poly(ethylene) oxide to generate the SM MPOP. The results demonstrated that SM MPOP could synchronically and sustainably release the five active components within 12 hours (the similar coefficient f 2 between two components was >65), and the average cumulative release rate was 85%. Fitting of the drug-release curve showed a zero-order release profile for SM MPOP. Our study showed that the phytosome complex technique combined with the MPOP system will achieve synchronized release of the various active components of herbal medicine and have potential applications in developing sustained release preparations in herbal medicine.


Assuntos
Sistemas de Liberação de Medicamentos , Silimarina/administração & dosagem , Varredura Diferencial de Calorimetria , Preparações de Ação Retardada , Osmose , Solubilidade , Espectrofotometria Infravermelho , Comprimidos , Difração de Raios X
15.
Zhongguo Zhen Jiu ; 34(6): 551-4, 2014 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-25112086

RESUMO

OBJECTIVE: To compare the clinical efficacy differences between fire needling technique of filiform needle at high stress points and regular acupuncture on chrondromalacia patellae so as to provide the better therapy for the treatment of this disease. METHODS: Sixty cases of chrondromalacia patellae were randomized into a fire needling group (28 cases) and a routine acupuncture group (32 cases). In the fire needling group, 5 to 6 high stress points were localized according to the symptoms, palpation and imaging condition and were stimulated with fire needling technique of filiform needle. The treatment was given once every two days, 5 treatments made one session. In the routine acupuncture group, the regular acupuncture was applied at Dubi (ST 35), Xiguan (LR 7), Yanglingquan (GB 34), Yinlingquan (SP 9), Zusanli (ST 36), etc. The treatment was given once every day, 5 treatments made one session. Lysholm score, VSA score, patella title angle (PTA) and lateral patella angle (LPA) of the affected knees before and after treatment, as well as the clinical efficacy after treatment were observed in the two groups. RESULTS: After treatment, Lysholm score, VSA score, PTA and LPA were all improved apparently in the two groups (all P < 0.01). After the treatments, the improvements in Lysholm score, VSA score, PTA and LPA in the fire needling group were more obvious than those in the routine acupuncture group (all P < 0.05). The effective rate was 92.9% (26/28) in the fire needling group, better than 87.5% (28/32) in the routine acupuncture group (P < 0.01). CONCLUSION: The fire needling technique of filiform needle at the high stress points relieves the clinical symptoms of chrondromalacia patellae and recovers the biodynamical structure of patellae.


Assuntos
Pontos de Acupuntura , Terapia por Acupuntura , Condromalacia da Patela/terapia , Terapia por Acupuntura/instrumentação , Terapia por Acupuntura/métodos , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Resultado do Tratamento , Adulto Jovem
16.
Cell Biol Int ; 38(5): 639-46, 2014 May.
Artigo em Inglês | MEDLINE | ID: mdl-24446394

RESUMO

Artesunate (ART), derived from a common traditional Chinese medicine, has beeen used an antimalarial for several years. In this study, the effect and mechanism of ART on anti-human cervical cancer cells was examined. The level of prostaglandin E2 (PGE2 ) and the population of CD4+CD25+Foxp3 regulatory T cells (Treg) in peripheral blood were detected by flow cytometry. In vivo antitumor activity was investigated in mice with cervical cancer by the subcutaneous injection of various concentrations of ART. The concentrations of PGE2 in the supernatants of CaSki cells were measured using an ELISA kit. Cyclooxygenase-2 (COX-2) and Foxp3 expression were determined using quantitative polymerase chain reaction (qPCR) and western blot analysis. The effect of ART on the viability of CaSki and Hela cells was evaluated with a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. It was identified that the level of PGE2 and the population of CD4+CD25+Foxp3 Treg cells in the peripheral blood were significantly higher in cervical cancer patients and mice with cervical cancer. ART was capable of inhibiting orthotopic tumor growth, which correlated with a decrease in the level of PGE2 and the percentage of Treg cells in mice with cervical cancer. Furthermore, ART decreased COX-2 expression and the production of PGE2 in CaSki and Hela cells. Notably, the supernatants of CaSki cells treated with ART lowered the expression of Foxp3 in Jurkat T cells, which was capable of being reversed by exogenous PGE2 . Our data revealed that ART may elicit an anti-tumor effect against cervical cancer by inhibition of PGE2 production in CaSki and Hela cells, which resulted in the decrease of Foxp3 expression in T cells. Therefore, ART may be an effective drug for immunotherapy of cervical cancer.


Assuntos
Artemisininas/farmacologia , Dinoprostona/antagonistas & inibidores , Fatores de Transcrição Forkhead/antagonistas & inibidores , Regulação Neoplásica da Expressão Gênica , Tolerância Imunológica/efeitos dos fármacos , Neoplasias do Colo do Útero , Animais , Artesunato , Dinoprostona/biossíntese , Feminino , Fatores de Transcrição Forkhead/biossíntese , Células HeLa , Humanos , Tolerância Imunológica/fisiologia , Células Jurkat , Camundongos , Camundongos Endogâmicos C57BL , Neoplasias do Colo do Útero/metabolismo
17.
Parasitol Res ; 112(12): 4065-72, 2013 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-24005478

RESUMO

With the aim of finding natural anthelmintic agents against Dactylogyrus intermedius (Monogenea) in goldfish (Carassius auratus), 26 plants were screened for antiparasitic properties using in vivo anthelmintic efficacy assay. The results showed that Caesalpinia sappan, Lysima chiachristinae, Cuscuta chinensis, Artemisia argyi, and Eupatorium fortunei were found to have 100% anthelmintic efficacy at 125, 150, 225, 300, and 500 mg L(-1) after 48 h of exposure. Crude extract of the five plants were further partitioned with petroleum ether, chloroform, ethyl acetate, methanol, and water to obtain anthelmintically active fractions with various polarity. Among these fractions tested, the ethyl acetate extract of L. chiachristinae was found to be the most effective with a 50% effective concentration (EC50) value of 5.1 mg/L after 48 h of exposure. This was followed by ethyl acetate extract of C. chinensis (48 h-EC50 = 8.5 mg L(-1)), chloroform extracts of C. sappan (48 h-EC50 = 15.6 mg L(-1)), methanol extract of C. chinensis (48 h-EC50 = 15.9 mg L(-1)), and chloroform and petroleum ether extract of L. chiachristinae (EC50 values of 17.2 and 21.1 mg/L, respectively), suggesting that these plants, as well as the active fractions, provide potential sources of botanic drugs for the control of D. intermedius in aquaculture.


Assuntos
Anti-Helmínticos/farmacologia , Doenças dos Peixes/tratamento farmacológico , Carpa Dourada/parasitologia , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Trematódeos/efeitos dos fármacos , Animais , Anti-Helmínticos/uso terapêutico , Aquicultura , Descoberta de Drogas , Doenças dos Peixes/parasitologia , Extratos Vegetais/uso terapêutico
18.
Mol Genet Metab ; 100(1): 46-50, 2010 May.
Artigo em Inglês | MEDLINE | ID: mdl-20074989

RESUMO

Carnitine uptake defect (CUD) is an autosomal recessive fatty acid oxidation defect caused by a deficiency of the high-affinity carnitine transporter OCTN2. CUD patients may present with hypoketotic hypoglycemia, hepatic encephalopathy or dilated cardiomyopathy. Tandem mass spectrometry screening of newborns can detect CUD, although transplacental transport of free carnitine from the mother may cause a higher free carnitine level and cause false negatives during newborn screening. From Jan 2001 to July 2009, newborns were screened for low free carnitine levels at the National Taiwan University Hospital screening center. Confirmation tests included dried blood spot free acylcarnitine levels and mutation analyses for both babies and their mothers. Sixteen newborns had confirmation tests for persistent low free carnitine levels; four had CUD, six had mothers with CUD, and six cases were false positives. All babies born to mothers with CUD had transient carnitine deficiency. The six mothers with CUD were put on carnitine supplementation (50-100mg/kg/day). One mother had dilated cardiomyopathy at diagnosis and her cardiac function improved after treatment. Analysis of the SLC22A5 gene revealed that p.S467C was the most common mutation in mothers with CUD, while p.R254X was the most common mutation in newborns and children with CUD. Newborn screening allows for the detection of CUD both in newborns and mothers, with an incidence in newborns of one in 67,000 (95% CI: one in 31,600-512,000) and a prevalence in mothers of one in 33,000 (95% CI: one in 18,700-169,000). Detection of CUD in mothers may prevent them from developing dilated cardiomyopathy.


Assuntos
Carnitina/deficiência , Proteínas de Transporte de Cátions Orgânicos/genética , Adulto , Cardiomiopatia Dilatada/etiologia , Carnitina/sangue , Carnitina/metabolismo , Reações Falso-Negativas , Humanos , Recém-Nascido , Erros Inatos do Metabolismo Lipídico/complicações , Erros Inatos do Metabolismo Lipídico/epidemiologia , Erros Inatos do Metabolismo Lipídico/genética , Mães , Mutação , Triagem Neonatal/métodos , Proteínas de Transporte de Cátions Orgânicos/deficiência , Membro 5 da Família 22 de Carreadores de Soluto , Taiwan/epidemiologia , Espectrometria de Massas em Tandem
19.
Int J Ment Health Syst ; 3(1): 1, 2009 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-19121218

RESUMO

BACKGROUND: Yuli Veterans Hospital (YVH) has been the largest mental hospital for the patients with chronic and severe mental illness in Taiwan for the past 50 years. While this hospital used to be a symbol of hopelessness among patients and their families and an unspoken shame among Taiwan psychiatry and mental health circles it now represents an example of how an old, custodial hospital can be transformed into a very different institution. In this case study we will describe the features of this transformation, which, over the past 20 years, has aimed to help extended stay inpatients with severe mental illness to integrate into the local community of Yuli even though it is not their original home. METHODS: Using historical documents and oral narratives from Yuli inhabitants, workers and patients of YVH, we will offer a case study of the Yuli model. RESULTS: There are four main components of the Yuli model: holistic medical support, vocational rehabilitation, case management, and the residential program. The four components help patients recover two essential features of their lives: vocational life and ordinary daily routines. As the process of recovery evolves, patients gradually regain inner stability, dignity, self-confidence, and a sense of control. The four components are critical to rebuild the structure and order of life of the patients and are indispensable and interdependent parts of one service package. They operate simultaneously to benefit the patients to the greatest degree possible. DISCUSSION: There are many challenges to the further development and financial viability of the model of services developed at YVH. There are also important questions concerning the replicability of the Yuli model in other sociocultural and service system contexts. CONCLUSION: This case study reveals the possibility of transforming a custodial mental hospital into a hospital providing high quality care. Hospital and community are not in opposition. They are part of a continuum of care for the patients. We reinterpret and redefine the boundary and function of hospital and community, and thereby create a new service model, the Yuli Model, to help patients to reintegrate into the community. The Yuli model, which particularly focuses on the needs of people with long-standing illness and prolonged hospital stay, illustrates one approach to linking hospital and community in a creative and constructive manner.

20.
Zhongguo Zhen Jiu ; 28(1): 75-7, 2008 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-18257197

RESUMO

OBJECTIVE: To understand the quality of the papers issued in Chinese Acupuncture and Moxibustion in past 7 years, so as to provide reference for its development. METHODS: Analyze information quality of the papers based on the treatises issued in Chinese Acupuncture and Moxibustion between 2000-2006. RESULTS: (1) Most of the authors come from medical schools and their affiliated hospitals (including scientific research units), accounting for 61. 0%; (2) Authors of each paper mainly range between 2-3 persons, accounting for 40.0%; (3) There are 405 papers with support of funds (mainly from provincial and ministerial funds) in the 7 years, accounting for 26. 2% of the total number of the papers; (4) Publication delay shortens annually, averaging 255. 3 days in the past 7 years and 210.5 days in 2006; (5) RCT papers of clinical researches account for 30.4% and show a raising tendency year by year. CONCLUSION: Chinese Acupuncture and Moxibustion has considerable advantages in the above-mentioned four aspects, showing the high quality of "key periodical", but the proportion of RCT papers still needs to be further increased.


Assuntos
Terapia por Acupuntura , Bibliometria , Moxibustão , Publicações Periódicas como Assunto/normas , China , Publicações Periódicas como Assunto/estatística & dados numéricos , Controle de Qualidade
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