RESUMO
A sensitive analytical method for the determination of a new active steroid, butane acid-(5-androsten-17-one-3beta-ol)-diester (A1998), was developed by high performance liquid chromatography with laser-induced fluorescence detection following the pre-column derivatization with dansylhydrazine. The calibration curve for A1998 derivatization was found linear in the dynamic range from 0.025 to 5.0 microg/ml, with the precision less than 6% (CV) and the mean extraction efficiency greater than 92%. In 200 microl of plasma samples the limit of quantitation was as low as 0.025 microg/ml with a signal-to-noise ratio of 10. This assaying was further applied to the determination of the pharmacokinetic parameters of A1998 in rats with an intravenous injection of A1998. Values for clearance for elimination, volume of distribution at steady state and terminal half life in the above case were determined as 50.3+/-1.1 ml/min kg, 1329.0+/-111.0 ml/kg and 44.0+/-2.7 min, respectively.
Assuntos
Antiarrítmicos/sangue , Cromatografia Líquida de Alta Pressão , Desidroepiandrosterona/sangue , Avaliação Pré-Clínica de Medicamentos/métodos , Lasers , Espectrometria de Fluorescência , Animais , Antiarrítmicos/administração & dosagem , Antiarrítmicos/química , Antiarrítmicos/farmacocinética , Disponibilidade Biológica , Calibragem , Catálise , Compostos de Dansil/química , Desidroepiandrosterona/administração & dosagem , Desidroepiandrosterona/análogos & derivados , Desidroepiandrosterona/química , Desidroepiandrosterona/farmacocinética , Avaliação Pré-Clínica de Medicamentos/normas , Feminino , Corantes Fluorescentes/química , Meia-Vida , Hidrazinas/química , Injeções Intravenosas , Taxa de Depuração Metabólica , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes , Temperatura , Fatores de Tempo , Ácido Trifluoracético/químicaRESUMO
AIM: To investigate the pharmacological effects of rice flavone (5,4'-dihydroxy-3',5'-dimethoxy-7-O-beta-D-glucopyranosyloxy-flavone, RF) separated from panicle-differentiating to flowing rice on rat experimental hepatic injury. METHODS: Models of rat acute hepatic injury induced by carbon tetrachloride (CCl(4)) administration, rat hepatic fibrosis induced by thioacetamide, injury of primary cultured rat hepatocytes induced by CCl(4), respectively, were established. After treated with RF, content of serum alanine transaminase (ALT), aspartate aminotransferase (AST) and albumin (Alb), hyaluronic acid (HA), the activity of glutathione peroxidase (GSH-Px), superoxide dismutase (SOD), and hydroxyproline (Hyp) were measured and liver tissue was observed pathologically by hematoxylin-eosin (HE) staining. Effects of RF on pathological changes, function index, enzyme of scavenging free radicals and blood rheology were evaluated. RESULTS: In model of rat acute hepatic injury induced by CCl(4), RF can significantly decrease the contents of serum ALT, AST, increase the content of Alb, improve the dropsy and fat denaturalization of hepatocytes. In model of rat hepatic fibrosis induced by thioacetamide, RF can inhibit the increase of HA, Hyp and whole blood viscosity, and improve the activities of GSH-Px and SOD, and inauricular microcirculation. CONCLUSION: RF has apparent protective effects on hepatic injury by increasing activity of GSH-Px and SOD, scavenging free radicals produced by CCl(4), reducing blood viscosity, and improving microcirculation and blood supply.
Assuntos
Flavonas/farmacologia , Cirrose Hepática/tratamento farmacológico , Oryza/química , Fitoterapia , Extratos Vegetais/farmacologia , Doença Aguda , Animais , Tetracloreto de Carbono , Células Cultivadas , Modelos Animais de Doenças , Hepatócitos/efeitos dos fármacos , Hepatócitos/patologia , Cirrose Hepática/induzido quimicamente , Cirrose Hepática/patologia , Masculino , Ratos , Ratos Sprague-Dawley , TioacetamidaRESUMO
OBJECTIVE: To study the protective effects of polysaccharide of Spirulina platensis and Sargassum thunbeergii on vascular of alloxan (ALX) induced diabetic rats. METHOD: With the doses of polysaccharide of Spirulina platensis (PSP) and Sargassum thunbeergii (PST) compound (1:1) 12.261, 36.783, 110.349 mg x kg(-1) by i.g. administration to alloxan induced diabetic rats respectively for 6 weeks. Then the blood glucose and the TC, HDL-C, TG, NO, ET in serum were detected. The contraction and relaxation response to NE and ACh in aortic rings of the alloxan induced diabetic rats has been studied. RESULT: The results showed the compound of PSP and PST could decrease the blood glucose and the TC, TG, NO, ET in serum and increase HDL-C than in the alloxan induced diabetic rats. The contraction responses to NE in aortic rings of the alloxan induced diabetic rats were significantly elevated in the normal rats, and the responses to ACh were significantly lower. PSP and PST compound could significantly lower the responses to NE and significantly elevate the responses to ACh in aortic rings of the alloxan induced diabetic rats. CONCLUSION: PSP and PST compound could decrease blood glucose and could protect the vascular of alloxan induced diabetic rats.
