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1.
Acta Pharm Sin B ; 12(2): 747-758, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-35256944

RESUMO

Although primary vesical calculi is an ancient disease, the mechanism of calculi formation remains unclear. In this study, we established a novel primary vesical calculi model with d,l-choline tartrate in mice. Compared with commonly used melamine and ethylene glycol models, our model was the only approach that induced vesical calculi without causing kidney injury. Previous studies suggest that proteins in the daily diet are the main contributors to the prevention of vesical calculi, yet the effect of fat is overlooked. To assay the relationship of dietary fat with the formation of primary vesical calculi, d,l-choline tartrate-treated mice were fed a high-fat, low-fat, or normal-fat diet. Genetic changes in the mouse bladder were detected with transcriptome analysis. A high-fat diet remarkably reduced the morbidity of primary vesical calculi. Higher fatty acid levels in serum and urine were observed in the high-fat diet group, and more intact epithelia in bladder were observed in the same group compared with the normal- and low-fat diet groups, suggesting the protective effect of fatty acids on bladder epithelia to maintain its normal histological structure. Transcriptome analysis revealed that the macrophage differentiation-related gene C-X-C motif chemokine ligand 14 (Cxcl14) was upregulated in the bladders of high-fat diet-fed mice compared with those of normal- or low-fat diet-fed mice, which was consistent with histological observations. The expression of CXCL14 significantly increased in the bladder in the high-fat diet group. CXCL14 enhanced the recruitment of macrophages to the crystal nucleus and induced the transformation of M2 macrophages, which led to phagocytosis of budding crystals and prevented accumulation of calculi. In human bladder epithelia (HCV-29) cells, high fatty acid supplementation significantly increased the expression of CXCL14. Dietary fat is essential for the maintenance of physiological functions of the bladder and for the prevention of primary vesical calculi, which provides new ideas for the reduction of morbidity of primary vesical calculi.

2.
Biosci Rep ; 41(2)2021 02 26.
Artigo em Inglês | MEDLINE | ID: mdl-33521822

RESUMO

METHODS: Relevant potential targets for EC were obtained based on Traditional Chinese Medicine System Pharmacology Database (TCMSP), a bioinformatics analysis tool for molecular mechanism of Traditional Chinese Medicine (BATMAN-TCM) and STITCH databases. The Online Mendelian Inheritance in Man (OMIM) and GeneCards databases were utilized to screen the known POI-related targets, while Cytoscape software was used for network construction and visualization. Then, the Gene Ontology (GO) and pathway enrichment analysis were carried out by the Database for Annotation, Visualization and Integrated Discovery (DAVID) database. Furthermore, KGN cells were performed to validate the predicted results in oxidative stress (OS) model, and antioxidant effect was examined. RESULTS: A total of 70 potential common targets for EC in the treatment of POI were obtained through network pharmacology. Metabolic process, response to stimulus and antioxidant activity occupied a leading position of Gene Ontology (GO) enrichment. Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis indicated that PI3K/protein kinase B (AKT), TNF, estrogen, VEGF and MAPK signaling pathways were significantly enriched. In addition, cell experiments showed that EC exhibited antioxidant effects in an H2O2-mediated OS model in ovarian granulosa cells by regulating the expression of PI3K/AKT/nuclear factor erythroid 2-related factor 2 (Nrf2) signaling pathway and multiple downstream antioxidant enzymes. CONCLUSION: EC could regulate multiple signaling pathways and several biological processes (BPs). EC had the ability to down-regulate elevated OS level through the PI3K/AKT/Nrf2 signaling pathway and represented a potential novel treatment for POI.


Assuntos
Catequina/farmacologia , Insuficiência Ovariana Primária/patologia , Antioxidantes/farmacologia , Catequina/química , Bases de Dados Genéticas , Feminino , Ontologia Genética , Humanos , Estereoisomerismo
3.
J Ethnopharmacol ; 269: 113720, 2021 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-33358858

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Jiajian Guishen Formula (JJGSF), which is a prescription of Traditional Chinese Medicine (TCM), has been reported to be useful in the treatment of premature ovarian insufficiency (POI). AIM OF THE STUDY: To investigate the therapeutic effects of JJGSF on the treatment of POI induced by 4-vinylcyclohexene diep-oxide (VCD), an endocrine-disrupting chemical (EDC), and to elucidate the potential mechanism. MATERIALS AND METHODS: Female 8-week-old ICR mice (N = 72) were randomized into six groups, containing the Model group, Control group, three JJGSF groups, and Progynova group which was served as a positive control. After model establishment by VCD, the Progynova group were given a daily intragastric administration of Progynova, and the three JJGSF groups (high dose group, medium dose group and low dose group) received a daily intragastric administration of JJGSF at doses of 9, 4.5 and 2.25 g/kg for four weeks. The general growth of the mice was observed and the estrous cycles were examined. The serum hormone concentrations were measured by enzyme-linked immunosorbent assay (ELISA). To explore the potential mechanism of effect, the protein expressions of H3K9me3, HP1, and HMGA1/HMGA2 related to senescence-associated heterochromatic foci (SAHF), were determined by Immunofluorescence and Western blot analysis, respectively. RESULTS: After treating with JJGSF, the estrous cycles were improved significantly. The level of estrogen (E2) and anti-müllerian hormone (AMH) was increased and the ratio of follicle-stimulating hormone (FSH) to luteinizing hormone (LH) in serum was decreased significantly. Furthermore, a significant down-regulation of HMGA1/HMGA2 on protein level, a reduction distribution of HP1 and H3K9me3 in ovarian, and a lower fraction of SAHF-positive cells were observed after the administration with JJGSF, additionally effects showed a positive correlation with dosages. CONCLUSIONS: JJGSF could treat POI by the mechanism of inhibiting SAHF.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Heterocromatina/efeitos dos fármacos , Insuficiência Ovariana Primária/tratamento farmacológico , Envelhecimento , Animais , Hormônio Antimülleriano/metabolismo , Senescência Celular/efeitos dos fármacos , Homólogo 5 da Proteína Cromobox , Proteínas Cromossômicas não Histona/metabolismo , Cicloexenos/toxicidade , Citocinas/sangue , Modelos Animais de Doenças , Regulação para Baixo/efeitos dos fármacos , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/uso terapêutico , Disruptores Endócrinos/toxicidade , Estradiol/farmacologia , Estradiol/uso terapêutico , Estrogênios/metabolismo , Ciclo Estral/efeitos dos fármacos , Feminino , Hormônio Foliculoestimulante/sangue , Proteína HMGA1a/genética , Proteína HMGA1a/metabolismo , Proteína HMGA2/genética , Proteína HMGA2/metabolismo , Histonas/metabolismo , Hormônio Luteinizante/sangue , Medicina Tradicional Chinesa , Camundongos Endogâmicos ICR , Ovário/efeitos dos fármacos , Ovário/metabolismo , Ovário/patologia , Insuficiência Ovariana Primária/induzido quimicamente , Insuficiência Ovariana Primária/genética , Insuficiência Ovariana Primária/metabolismo , Compostos de Vinila/toxicidade
4.
Nutrients ; 11(4)2019 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-30995790

RESUMO

Major depressive disorder (MDD) is a chronic mental disorder characterized by mixed symptoms and complex pathogenesis. With long history of practical application, traditional Chinese medicine (TCM) offers many herbs for the treatment and rehabilitation of chronic disease. In this study, we developed a modified Chinese herbal formula using Panax ginseng, Angelica Sinensis, Polygala tenuifolia Willd, and Ziziphi spinosae Semen (PAPZ), based on an ancient TCM prescription. The antidepressant effects of PAPZ were investigated with a corticosterone (CORT) model of depression in mice. Our results showed that administration of PAPZ ameliorated depression-like phenotypes in the CORT model. An anatomic study showed that chronic PAPZ administration upregulated the protein expression of brain-derived neurotrophic factor (BDNF) in hippocampal tissue. The enzyme activity of superoxide dismutase was enhanced in hippocampal tissue, in line with a decreased malondialdehyde level. Taken together, these findings suggested that PAPZ has therapeutic effects in a mice depression model through increasing protein expression of BDNF and improving the anti-oxidation ability of the brain.


Assuntos
Antioxidantes/uso terapêutico , Comportamento Animal/efeitos dos fármacos , Depressão/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Hipocampo/efeitos dos fármacos , Magnoliopsida , Fitoterapia , Angelica sinensis , Animais , Antidepressivos/farmacologia , Antidepressivos/uso terapêutico , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Corticosterona , Depressão/metabolismo , Transtorno Depressivo Maior/tratamento farmacológico , Transtorno Depressivo Maior/metabolismo , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas/farmacologia , Hipocampo/metabolismo , Masculino , Malondialdeído/metabolismo , Camundongos Endogâmicos C57BL , Panax , Polygala , Superóxido Dismutase/metabolismo , Ziziphus
5.
Int J Antimicrob Agents ; 53(2): 128-136, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30063999

RESUMO

Human enterovirus 71 (EV-A71) infections cause a wide array of diseases ranging from diarrhoea and rashes to hand-foot-and-mouth disease and, in rare cases, severe neurological disorders. No specific antiviral drug therapy is currently available. Extracts from 75 Chinese medicinal plants selected for antiviral activity based on the Chinese pharmacopeia and advice from traditional Chinese medicine clinicians were tested for activity against EV-A71. The aqueous extract of the rhizome of Cimicifuga heracleifolia (Sheng Ma) and Arnebia euchroma (Zi Cao) showed potent antiviral activity. The active fractions were isolated by bioassay-guided purification, and identified by a combination of high-resolution mass spectrometry and nuclear magnetic resonance. Fukinolic acid and cimicifugic acid A and J, were identified as active anti-EV-A71 compounds for C. heracleifolia, whereas for A. euchroma, two caffeic acid derivatives were tentatively deduced. Commercially available fukinolic acid analogues such as L-chicoric acid and D-chicoric also showed in vitro micromolar activity against EV-A71 lab-strain and clinical isolates.


Assuntos
Antivirais/farmacologia , Boraginaceae/química , Ácidos Cafeicos/farmacologia , Cimicifuga/química , Enterovirus Humano A/efeitos dos fármacos , Fenilacetatos/farmacologia , Extratos Vegetais/farmacologia , Succinatos/farmacologia , Proteases Virais 3C , Cisteína Endopeptidases , Enterovirus Humano A/isolamento & purificação , Infecções por Enterovirus/tratamento farmacológico , Infecções por Enterovirus/virologia , Humanos , Espectrometria de Massas , Medicina Tradicional Chinesa , Testes de Sensibilidade Microbiana , Ressonância Magnética Nuclear Biomolecular , Proteínas Virais/antagonistas & inibidores , Replicação Viral/efeitos dos fármacos
6.
Front Pharmacol ; 9: 1472, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30618762

RESUMO

Qing-Luo-Yin (QLY) is a traditional Chinese medicine (TCM) formula used to treat Hot Syndrome-related rheumatoid arthritis (RA). Previously, we uncovered partial mechanisms involved in the therapeutic actions of QLY on RA. In this study, we further elucidated its anti-rheumatic mechanisms and investigated its possible interactions with methotrexate (MTX) in vivo using an integrating strategy coupled with network pharmacology and metabolomics techniques. Chemical composition of QLY was characterized by HPLC analysis. Collagen induced arthritis (CIA) was developed in male SD rats. The CIA rats were then assigned into different groups, and received QLY, MTX or QLY+MTX treatments according to the pre-arrangement. Therapeutic effects of QLY and its possible interactions with MTX in vivo were evaluated by clinical parameters, digital radiography assessment, histological/immunohistochemical examination, and serological biomarkers. Mechanisms underlying these actions were deciphered with network pharmacology methods, and further validated by metabolomics clues based on UPLC-Q-TOF/MS analysis of urines. Experimental evidences demonstrated that QLY notably alleviated the severity of CIA and protected joints from destruction. Re-balanced levels of hemoglobin and alanine transaminase in serum indicated reduced MTX-induced hepatic injury and myelosuppression under the co-treatment of QLY. Network-based target prediction found dozens of RA related proteins as potential targets of QLY. Upon the further biological function enrichment analysis, we found that a large amount of them were involved in nucleotide metabolism and immune functions. Metabolomics analysis showed that QLY restored amino acids, fatty acids, and energy metabolisms in CIA rats, which solidly supported its therapeutic effects on CIA. Consistently to findings from network pharmacology analysis, metabolomics study also found altered purine, pyrimidine, and pentose phosphate metabolisms in CIA rats receiving QLY treatment. All these clues suggested that inhibition on nucleic acid synthesis was essential to the immunosuppressive activity of QLY in vivo, and could contribute great importance to its therapeutic effects on CIA. Additionally, QLY induced significant antifolate resistance in rats, which would prevent folate from depletion during long-term MTX treatment, and should account for reduced side effects in combination regimen with MTX and QLY.

7.
Biogerontology ; 17(4): 771-82, 2016 08.
Artigo em Inglês | MEDLINE | ID: mdl-27040825

RESUMO

Human longevity continues to increase world-wide, often accompanied by decreasing birth rates. As a larger fraction of the population thus gets older, the number of people suffering from disease or disability increases dramatically, presenting a major societal challenge. Healthy ageing has therefore been selected by EU policy makers as an important priority ( http://www.healthyageing.eu/european-policies-and-initiatives ); it benefits not only the elderly but also their direct environment and broader society, as well as the economy. The theme of healthy ageing figures prominently in the Horizon 2020 programme ( https://ec.europa.eu/programmes/horizon2020/en/h2020-section/health-demographic-change-and-wellbeing ), which has launched several research and innovation actions (RIA), like "Understanding health, ageing and disease: determinants, risk factors and pathways" in the work programme on "Personalising healthcare" ( https://ec.europa.eu/research/participants/portal/desktop/en/opportunities/h2020/topics/693-phc-01-2014.html ). Here we present our research proposal entitled "ageing with elegans" (AwE) ( http://www.h2020awe.eu/ ), funded by this RIA, which aims for better understanding of the factors causing health and disease in ageing, and to develop evidence-based prevention, diagnostic, therapeutic and other strategies. The aim of this article, authored by the principal investigators of the 17 collaborating teams, is to describe briefly the rationale, aims, strategies and work packages of AwE for the purposes of sharing our ideas and plans with the biogerontological community in order to invite scientific feedback, suggestions, and criticism.


Assuntos
Envelhecimento/fisiologia , Proteínas de Caenorhabditis elegans/metabolismo , Caenorhabditis elegans/fisiologia , Estilo de Vida Saudável/fisiologia , Longevidade/fisiologia , Modelos Animais , Animais
8.
Biomed Chromatogr ; 29(2): 167-75, 2015 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-24935437

RESUMO

A high-performance liquid chromatography coupled to time-of-flight mass spectrometry (HPLC-TOF MS) method was successfully developed and validated for the identification and determination of seven ginsenosides, Re , Rf , Rb1 , Rc , Rb2 , Ro and Rd , in a Chinese herbal preparation, Shenfu injection, and rat plasma. Based on the method, the pharmacokinetic profiles of the seven ginsenosides were investigated following intravenous administration of single dose of Shenfu injection to six rats. The established method had high linearity, selectivity, sensitivity, accuracy and precision. The pharmacokinetic results showed that Rb1 , Rc and Rb2 had similar pharmacokinetic profiles and relatively long half-life values (19.29 ± 6.36, 29.54 ± 22.91 and 35.60 ± 30.66 h). The half-lives of Rf and Rd were 4.21 ± 3.68 and 8.49 ± 5.20 h, respectively, indicating that they could be metabolized more rapidly than Rb1 , Rc and Rb2 .


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/farmacocinética , Ginsenosídeos/sangue , Espectrometria de Massas em Tandem/métodos , Administração Intravenosa , Animais , Medicamentos de Ervas Chinesas/administração & dosagem , Masculino , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes
9.
J Ethnopharmacol ; 143(3): 772-8, 2012 Oct 11.
Artigo em Inglês | MEDLINE | ID: mdl-22867635

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: From over 100 Chinese clinical trial publications, we retrieved 22 commercial preparations and 17 clinical prescriptions used as Traditional Chinese Medicine (TCM) for treating mycotic vaginitis, typically caused by Candida albicans. The 8 most frequently used plants as well as another 7 TCM and 18 folk medicinal plants used in the South of China for antifungal therapy were investigated for in vitro antifungal activity. MATERIALS AND METHODS: For each plant we tested 4 extracts prepared with different solvents (water, ethanol, acetone, and n-hexane) for inhibition of Candida albicans and Saccharomyces cerevisiae growth in liquid culture. RESULTS: Some plants have quite strong antifungal activity, such as Tujinpi (Pseudolarix kaempferi Gord.), of which each extract could significantly inhibit the growth of both tested fungi. In addition, the acetone extract of Kushen (Sophora flavescens Ait.), the ethanol, acetone, and hexane extracts of Guanghuoxiang (Pogostemon cablin (Blanco) Benth.) and Gaoliangjiang (Alpinia officinarum Hance), the hexane extract of Dingxiang (Eugenia caryophyllata Thunb.), and the ethanol and acetone extracts of Kulianpi (Melia toosendan Sieb. et Zucc.) and Laliao (Polygonum hydropiper L.), all inhibited Candida albicans growth by more than 50%. In some cases growth inhibition was even comparable to that by the clinically used antifungal miconazole, which we used as our positive control. CONCLUSIONS: The majority of plants, whose clinical use for antifungal treatment is well supported within TCM or Chinese folk medicine, show in vitro antifungal activity against Candida albicans. Since Candida species represent the most common fungal pathogen of humans, these results provide more scientific evidence supporting the clinical application of these plants, and can serve as a starting point for new drug discovery from TCM and Chinese folk medicine.


Assuntos
Antifúngicos/farmacologia , Medicina Tradicional , Extratos Vegetais/farmacologia , Plantas Medicinais , Candida albicans/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Saccharomyces cerevisiae/efeitos dos fármacos
10.
Drug Dev Ind Pharm ; 38(6): 752-61, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-22014311

RESUMO

The aim of the present study was to construct an innovative microemulsion-based patch for simultaneously transdermal delivery of huperzine A (HA) and ligustrazine phosphate (LP). The pseudo-ternary phase diagrams for microemulsion region were developed using oleic acid as oil, Cremophor RH40 as a surfactant, and ethanol as a cosurfactant. 1,8-cineole was added to the microemulsion as a penetration enhancer. The microemulsion-based transdermal patches were prepared by the lamination technique. The permeation studies were performed in vitro to evaluate the abilities of various microemulsions and transdermal patches to deliver HA and LP across the rat abdominal skin, showing that microemulsions increased the permeation rates of HA and LP compared with the control, and the penetration kinetics of the transdermal patch was in a zero order process. The results of the pharmacodynamic studies indicated that the transdermal combination therapy of HA and LP showed more benefits for fighting against amnesia in comparison with monotherapy. The anti-amnesic effects were also confirmed in scopolamine-induced amnesia rats after transdermal administration at multiple doses for 9 consecutive days, and the efficacy exhibited a dose-dependent manner. As a conclusion, the microemulsion-based transdermal patch containing HA and LP might provide a feasible strategy for the prevention of Alzheimer's disease.


Assuntos
Alcaloides/administração & dosagem , Doença de Alzheimer/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Fármacos Neuroprotetores/administração & dosagem , Pirazinas/administração & dosagem , Sesquiterpenos/administração & dosagem , Adesivo Transdérmico , Vasodilatadores/administração & dosagem , Administração Cutânea , Alcaloides/farmacocinética , Doença de Alzheimer/metabolismo , Animais , Relação Dose-Resposta a Droga , Quimioterapia Combinada , Emulsões/química , Masculino , Fármacos Neuroprotetores/farmacocinética , Pirazinas/farmacocinética , Ratos , Ratos Sprague-Dawley , Sesquiterpenos/farmacocinética , Absorção Cutânea , Fatores de Tempo , Vasodilatadores/farmacocinética
11.
Pharmacol Biochem Behav ; 96(4): 449-53, 2010 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-20624417

RESUMO

In the present study, whether coadministration of huperzine A (HA) and ligustrazine phosphate (LP) could effectively improve the memory deficits in association with ameliorating cholinergic impairment and oxidative stress in the scopolamine-induced amnesia rats was assessed. The effects of treatment with Coa [HA (0.14 mg/kg, i.g.) and LP (110 mg/kg, i.g.)] on amnesia were investigated in Morris water maze. Furthermore, the effects on the activities of acetylcholinesterase (AChE) and antioxidant enzymes within the cerebral cortex and hippocampus were evaluated, and the lipid peroxidation product malondialdehyde (MDA) was also analyzed. As a result, coadministration of HA and LP for 10 consecutive days could markedly reverse the scopolamine-induced learning and memory impairment determined by the Morris water maze test. Moreover, AChE activity was significantly inhibited, and superoxide dismutases (SOD) and glutathione peroxidase (GSH-Px) activities were significantly increased with a remarkable reduction in the level of MDA. In conclusion, coadministration of HA and LP effectively prevented cholinergic impairment and oxidative damage, thereby resulting in improvement of spatial learning memory in rats induced by scopolamine. The results suggested that coadministration of HA and LP might offer a novel poly-therapeutic drug regimen for preventing Alzheimer's disease (AD).


Assuntos
Amnésia/tratamento farmacológico , Pirazinas/uso terapêutico , Escopolamina/toxicidade , Sesquiterpenos/uso terapêutico , Acetilcolinesterase/metabolismo , Alcaloides , Amnésia/induzido quimicamente , Animais , Córtex Cerebral/enzimologia , Córtex Cerebral/metabolismo , Glutationa Peroxidase/metabolismo , Hipocampo/enzimologia , Hipocampo/metabolismo , Peroxidação de Lipídeos , Masculino , Pirazinas/administração & dosagem , Ratos , Ratos Sprague-Dawley , Sesquiterpenos/administração & dosagem , Superóxido Dismutase/metabolismo
12.
Eur J Med Chem ; 45(5): 1731-8, 2010 May.
Artigo em Inglês | MEDLINE | ID: mdl-20117861

RESUMO

Fifteen PEG-scutellarin prodrugs were synthesized by modifying carboxyl and phenolic hydroxyl groups of scutellarin with mPEG of different molecular weight (400-3000). The water solubility of prodrugs increased remarkably and reached the maximum value of 783.88 mg/mL (scutellarin, 0.02 mg/mL). The anti-infarct effects of four PEG prodrugs with high water solubility were evaluated by Cerebral Ischemia/Reperfusion in the Middle Cerebral Artery Occlusion (MCAO) model. The results showed that the prodrug 7e could significantly reduce the infarct area from 27.2% to 12.2% (33.3% for the control) and decrease the neurological deficit score from 2.77 to 1.32 (2.85 for the control). The half-life (18.62 min) of the prodrug 7e was significantly longer than that of scutellarin (3.03 min).


Assuntos
Apigenina/farmacologia , Glucuronatos/farmacologia , Infarto da Artéria Cerebral Média/prevenção & controle , Polietilenoglicóis/farmacologia , Pró-Fármacos/farmacologia , Traumatismo por Reperfusão/prevenção & controle , Água/química , Animais , Apigenina/síntese química , Apigenina/química , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos , Glucuronatos/síntese química , Glucuronatos/química , Estrutura Molecular , Peso Molecular , Polietilenoglicóis/síntese química , Polietilenoglicóis/química , Pró-Fármacos/síntese química , Pró-Fármacos/química , Ratos , Ratos Sprague-Dawley , Solubilidade , Estereoisomerismo
13.
J Chromatogr Sci ; 47(8): 728-32, 2009 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-19772754

RESUMO

A sensitive, selective, and reproducible reversed-phase high-performance liquid chromatography method coupled with electrospray ionization-ion trap mass spectrometry (LC-ESI-ITMS) was developed for the simultaneous quantification of pennogenin diglycoside (PD) in a small volume (100 microL) of rat plasma. PD was extracted from rat plasma samples using liquid-liquid extraction with methanol, digoxin as internal standard. The chromatographic separation was performed on a reversed-phase Agilent C(18) (250 mm x 4.6 mm i.d., 5 mum particle size) analytical column using a mobile phase of 0.1% formic acid solution-acetonitrile (75:25, v/v) at a flow-rate of 1.0 mL/min. The mass spectrometer was operated in the negative ion mode at the deprotonated-molecular ions [M-H]- of parent drug. Calibration curve in spiked plasma was linear (correlation coefficient r = 0.999) from 0.5 to 50.0 mg/mL. For the different samples with concentration of 0.50, 5.00, and 50.0 microg/mL, recoveries of PD were (86.45 +/- 4.39)%, (91.40 +/- 4.40)%, and (93.79 +/- 3.29)%, respectively (n = 3). The intra-day assay relative standard deviation at 0.50, 5.00, and 50.0 mg/mL of PD were 4.29%, 5.66%, and 4.03% (n = 3), respectively. The inter-day assay %RSD at the previously mentioned concentrations were 5.53%, 4.99%, and 4.31% (n = 3), respectively. The method was successfully applied to the pharmacokinetic study of PD in rats following either intravenous administration of PD solution or oral administration of the extract in Gongxuening capsules, a famous patent Chinese botanic drug.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/química , Glicosídeos/sangue , Saponinas/sangue , Espectrometria de Massas por Ionização por Electrospray/métodos , Animais , Medicamentos de Ervas Chinesas/análise , Feminino , Glicosídeos/química , Estrutura Molecular , Ratos , Ratos Wistar , Saponinas/química
14.
Zhongguo Zhong Yao Za Zhi ; 34(3): 275-8, 2009 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-19445147

RESUMO

OBJECTIVE: To optimize the formulation and preparation process of sinomenine liposomes. METHOD: Method of aether injection and mixture uniform design were adopted to determine the formulation of sinomenine liposomes is the proportion of phospholipids, cholesterol and Vitamin E with the index of entrapment efficiency. And the single-factor test was used to study the preparation process of the liposomes, including the volume of buffer solution, the preparation temperature and the ultrasonic time. RESULT: The optimized formulation was that the ratio of sinomenine : phospholipids : cholesterol : vitamin E mass ratio was 8.92 : 60.35 : 28.81 : 1.91. The volume of buffer solution was 50 mL x g(-1) membrane, the preparation temperature was 50 degrees C, and the ultrasonic time was 20 min. CONCLUSION: Satisfactory shape and entrapment efficiency of the liposomes can be obtained by the optimized formulation and preparation process.


Assuntos
Química Farmacêutica , Morfinanos/farmacocinética , Tamanho da Partícula , Colesterol , Formas de Dosagem , Portadores de Fármacos , Composição de Medicamentos/economia , Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos , Estabilidade de Medicamentos , Lipossomos , Fosfolipídeos , Tecnologia Farmacêutica
15.
Zhongguo Zhong Yao Za Zhi ; 34(2): 143-7, 2009 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-19385171

RESUMO

OBJECTIVE: To establish a method to evaluate the in vitro release of Chinese medicinal compound sustained release preparations using multi-index chromatographic fingerprint. METHOD: With the Chinese medicinal compound Jiangya sustained tablets as model preparation, the in vitro cumulative release of the main component flavones and fingerprint were determined by HPLC fingerprint. Aacacetin, rutin, luteolin, fingerprint were determined simultaneously and used to calculate the in vitro cumulative release of the tablets. RESULT: Aacacetin, rutin, luteolin, and the fingerprint had different cumulative release. CONCLUSION: Multi-index chromatographic fingerprint can reflect different content of multi components of preparations and can be used in the evaluation on in vitro release of the sustained release preparations of Chinese medicinal compound. The method is simple, rapid, and of multi information.


Assuntos
Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/metabolismo , Cromatografia , Preparações de Ação Retardada , Medicamentos de Ervas Chinesas/administração & dosagem , Fatores de Tempo
16.
Arch Pharm Res ; 31(4): 547-54, 2008 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-18449515

RESUMO

The objective of this study is to investigate the pharmacokinetics and biodistribution of free breviscapine (BVP) and coated BVP-loaded poly (D, L-lactic acid) nanoparticles (BVP-PLA-NPs) in rats after i.v. administration. Coated BVP-PLA-NPs were prepared by the spontaneous emulsification solvent diffusion method and characterized. The BVP content in the NPs, the biological samples and in vitro release was measured by the high-performance liquid chromatography (HPLC). The mean sizes of coated BVP-PLA-NPs were 177 and 319 nm with a narrow distribution and smooth sphere shapes, entrapment efficiency of 86.9% and 93.1%, respectively. Drug release profiles in phosphate buffer and plasma exhibited a biphasic release phenomenon. After i.v. administration of free BVP and NPs suspensions in rats, area under plasma concentration-time curve and elimination t(1/2) were increased 9.3-fold and 10.9-fold for 177 nm of NPs, and 4.4-fold and 17.1-fold for 319 nm of NPs compared with that of free BVP, respectively. NPs were mainly distributed in liver, spleen, heart and brain. In addition, NPs could penetrate blood brain barrier (BBB) and the particle size had some effect on pharmacokinetics and biodistribution. Coated BVP-PLA-NPs could effectively avoid the capture by the reticuloendothelial system and prolong the half-life of BVP. Moreover, these NPs could penetrate BBB and enhance the accumulation of BVP in brain.


Assuntos
Portadores de Fármacos , Medicamentos de Ervas Chinesas/farmacocinética , Flavonoides/farmacocinética , Ácido Láctico/química , Nanopartículas , Polímeros/química , Animais , Barreira Hematoencefálica/metabolismo , Química Farmacêutica , Cromatografia Líquida de Alta Pressão , Composição de Medicamentos , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/química , Flavonoides/administração & dosagem , Flavonoides/química , Injeções Intravenosas , Masculino , Microscopia Eletrônica de Transmissão , Sistema Fagocitário Mononuclear/metabolismo , Tamanho da Partícula , Permeabilidade , Poliésteres , Ratos , Ratos Sprague-Dawley , Solubilidade , Análise Espectral , Tecnologia Farmacêutica/métodos , Distribuição Tecidual
17.
Zhongguo Zhong Yao Za Zhi ; 31(9): 731-4, 2006 May.
Artigo em Chinês | MEDLINE | ID: mdl-17048678

RESUMO

OBJECTIVE: To establish an HPLC method for the determination of entrapment efficiency of sinomenine liposomes. METHOD: The liposomes and dissociated drugs were separated by sephadex filtration, mini-column centrifugation and dialysis. The methodology study and the optimization of determining condition were carried out at the same time. RESULT: Sephadex filtration could effectively separate the sinomenine liposomes from dissociated sinomenine. The column recovery was 98.8%, the average entrapment efficiency of three tests was64.9%, RSD 2.67%. CONCLUSION: The method was simple, exact, and had a good reappearance. It can be used to examine the entrapment efficiency of sinomenine liposomes.


Assuntos
Filtração , Morfinanos/análise , Sinomenium , Dextranos , Portadores de Fármacos , Sistemas de Liberação de Medicamentos , Filtração/métodos , Lipossomos , Morfinanos/administração & dosagem , Morfinanos/isolamento & purificação , Sinomenium/química , Tecnologia Farmacêutica/métodos
18.
Zhong Yao Cai ; 28(10): 913-6, 2005 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-16479930

RESUMO

OBJECTIVE: To study pharmacokinetics of breviscapine in dogs and rabbits after iv. single dose. METHODS: Lc/Lc extract was used to prepare test samples and HPLC was used to determine breviscapine. RESULTS: Breviscaplin was fitted to double-department model in dogs and rabbits after iv. single dose. The main parameters in dogs were: A = 56.93 +/- 23.14, B = 1.61 +/- 1.11, alpha = 0.2328 +/- 0.1321 min, beta = 0.0255 +/- 0.0187 min(-1), t(1/2alpha) = 2.98 +/- 1.42 min, t(1/2beta) = 27.14 +/- 14.35 min, K21 = 0.10312 +/- 0.0112 min(-1), K10 = 0.1904 +/- 0.1319 min(-1), K12 = 0.0367 +/- 0.0306 min(-1), CL = 39.41 +/- 20.44 ml x min(-1), AUC = 3074 +/- 1055 mg x min x L(-1), respectively. The main parameters in rabbits were:A = 2.64 +/- 1.12, B = 0.28 +/- 0.12, alpha = 0.1439 +/- 0.0681 min(-1), beta = 0.0162 +/- 0.0456 min(-1), t1/2alpha = 4.82 +/- 1.65 min, th1/2beta = 42.66 +/- 18.77 min, K21 = 0.0285 +/- 0.0147 min(-1), K10 = 0.0820 +/- 0.00378 min(-1), K12 = 0.0496 +/- 0.0241 min, CL = 337.05 +/- 156.48ml x min(-1), AUC = 356 +/- 114 mg x min x L(-1), respectively. CONCLUSION: Breviscapine has short half-life after intravenous administration to dogs and rabbits,which show breviscapine is eliminated rapidly and has short action time.


Assuntos
Medicamentos de Ervas Chinesas/farmacocinética , Erigeron/química , Flavonoides/farmacocinética , Plantas Medicinais/química , Animais , Área Sob a Curva , Cromatografia Líquida de Alta Pressão/métodos , Cães , Estabilidade de Medicamentos , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/isolamento & purificação , Feminino , Flavonoides/administração & dosagem , Meia-Vida , Injeções Intravenosas , Masculino , Metanol
19.
Zhong Yao Cai ; 27(1): 19-20, 2004 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-15179783

RESUMO

OBJECTIVE: To determine the different lactone content of 10 batches of TLG raw material. METHODS: RP-HPLC-ELSD were used to determine ginkgolide A, B, C(GA, GB, GC). RESULTS: Content of GA, GB and GC were different but TLG very high (all > 90%). CONCLUSION: The quality of TLG could be affected by habitat, season and the preparation method.


Assuntos
Diterpenos/análise , Ginkgo biloba/química , Lactonas/análise , Plantas Medicinais/química , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/química , Ginkgolídeos , Farmacognosia , Folhas de Planta/química
20.
Zhong Yao Cai ; 25(12): 868-71, 2002 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-12685344

RESUMO

By the combinative method of fingerprint spectrums, the ultraviolet spectrum group draft of EGB761 was depicted. The established method is characteristic and reproducible and can be used in the identification and quality control of the medical materials, extracts and preparations. The ultraviolet spectrum group draft of EGB761 was tentatively depicted as: lambda max (nm): H2O solution (C = 0.02 mg/ml) 265.00 +/- 1.00, 201.00 +/- 1.00; EtOH solution (C = 0.02 mg/ml) 267.00 +/- 1.00, 210.00 +/- 1.00; CHCl3 solution (C = 0.4 mg/ml) 241.00 +/- 1.00; petroleum benzine solution (C = 0.4 mg/ml) 211.00 +/- 1.00.


Assuntos
Ginkgo biloba/química , Extratos Vegetais/isolamento & purificação , Etanol , Folhas de Planta/química , Controle de Qualidade , Sensibilidade e Especificidade , Espectrofotometria Ultravioleta/métodos
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