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1.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 37(4): 480-484, 2017 04.
Artigo em Chinês | MEDLINE | ID: mdl-30650510

RESUMO

Objective To observe the effect of clopidogrel on plasma protein binding rates of gin- senoside Rg1. Methods Concentrations of ginsenoside Rg1 were measured in fetal bovine serum and phosphate buffered solution (PBS). Samples were randomly divided into ginsenoside Rg1 groups (low: 0.4; middle: 1. 0; high 5. 0 mg/L, respectively) and clopidogrel combined ginsenoside Rg1 groups (low: 0. 4 mg/L +2. 0 mg/L clopidogrel; middle: 1. 0 mg/L +2. 0 mg/L clopidogrel; high: 5. 0 mg/L +2. 0 mg/L clo- pidogrel). The effect of clopidogrel on plasma protein binding rates of ginsenoside Rgl was observed u- sing equilibrium dialysis. Then 3-dimensional structure of bovine serum albumin (BSA) was constructed using homology modeling. On this basis, binding effect of small compounds (ginsenoside Rg1 and clopi- dogrel) and BSA was observed using molecular docking method. Results The serum protein binding rate was 11. 2% ±2. 1% in the low dose ginsenoside Rg1 group, 13. 4% ±2. 2% in the middle dose ginsenoside Rgl group, and 14. 6% ±1. 4% in the high dose ginsenoside Rg1 group, respectively. It was 6. 5% ±2. 3% in the clopidogrel combined low dose ginsenoside Rg1 group, 9. 2% ±1. 5% in the clopi- dogrel combined middle dose ginsenoside Rg1 group, 12.1% ± 1. 7% in the clopidogrel combined high dose ginsenoside Rg1 group, respectively. They were lower in clopidogrel combined ginsenoside Rg1 groups than in ginsenoside Rg1 groups with statistical difference (P <0. 05). Results of molecular doc- king showed that competitive binding effect existed between compounds (ginsenoside Rg1 and clopi- dogrel) and BSA. Conclusion Results of equilibrium dialysis and molecular docking comprehensively in- dicated clopidogrel had effect on plasma protein binding rate of ginsenoside Rg1.


Assuntos
Clopidogrel , Ginsenosídeos , Inibidores da Agregação Plaquetária , Ligação Proteica , Proteínas Sanguíneas , Clopidogrel/farmacologia , Ginsenosídeos/metabolismo , Simulação de Acoplamento Molecular , Inibidores da Agregação Plaquetária/farmacologia , Ligação Proteica/efeitos dos fármacos
2.
Yao Xue Xue Bao ; 50(3): 319-25, 2015 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-26118111

RESUMO

This study aimed to explore the impact of depression caused by chronic unpredictable mild stress (CUMS) on in vivo activity of six kinds of CYP450 isoforms in rats. According to 'Katz' method, the model of CUMS was established. Tolbutamide, chlorzoxazone, theophylline, midazolam, omeprazole and dextromethorphan were chosen as probe substrates of CYP2C6, CYP2E1, CYP1A2, CYP3A2, CYP2D1 and CYP2D2 of rats. Plasma concentration of six kinds of CYP450 in control group and model group were determined by LC-MS/MS and computed pharmacokinetic parameters. Consequently, metabolism of theophylline and chlorzoxazone accelerated significantly (P < 0.01), but tolbutamide, dextromethorphan, omeprazole and midazolam had no significant difference. The present study proved that depression caused by CUMS had strong induction to CYP1A2 and medium induction to CYP2E1.


Assuntos
Sistema Enzimático do Citocromo P-450/metabolismo , Fígado/enzimologia , Estresse Fisiológico , Animais , Clorzoxazona/metabolismo , Cromatografia Líquida , Depressão , Dextrometorfano/metabolismo , Midazolam/metabolismo , Omeprazol/metabolismo , Ratos , Espectrometria de Massas em Tandem , Teofilina/metabolismo , Tolbutamida/metabolismo
3.
Nan Fang Yi Ke Da Xue Xue Bao ; 35(1): 109-12, 2015 Jan 20.
Artigo em Chinês | MEDLINE | ID: mdl-25758663

RESUMO

OBJECTIVE: To investigate the effect of clopidogrel on the binding rate of ginsenosides with rat serum proteins (RSA). METHODS: Equilibrium dialysis and liquid chromatography-mass spectrometry were employed to quantify the concentration of ginsenoside Rg1 and Rb1. The protein-binding rates of Rg1 and Rb1 in the presence or absence of clopidogrel (1.0 mg/L) were determined. A molecular simulation model (consisting of homology modeling and molecular docking interaction) was used to reveal the target protein-compound interactions. RESULTS: The binding rates of ginsenosides Rg1 (0.4, 1.0, and 2.0 mg/L) with RSA were (30.16∓2.82)%, (33.42∓4.21)%, and (34.61∓3.42)%, and those of and Rb1 were (50.13∓2.34)%, (51.23∓3.23)%, and (53.11∓3.26)%, respectively. In the presence of clopidogrel, the binding rates of Rg1 decreased to (22.13∓2.72)%, (21.42∓3.22)%, and (25.45∓3.52)%, and those of Rb1 to (40.13∓3.24)%, (41.25∓4.15)%, and (43.11∓3.31)%, receptively. The molecular docking suggested that these compounds competed to bind with RSA. CONCLUSION: Clopidogrel can competitively bind to RSA with ginsenosides to lower the plasma protein binding rates of ginsenosides.

4.
Zhong Yao Cai ; 37(10): 1820-5, 2014 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-25895391

RESUMO

OBJECTIVE: To study the synergistic action of Compound Danshen Dripping Pill (CDDP) on Clopidogrel Bisulfate (CPG) counteracting platelet aggregation. METHODS: 40 Sprague-Dawley (SD) rats were randomized into four groups: normal control group (CMC-Na), CPG alone group (30 mg/kg), CDDP alone group (324 mg/kg), co-administration group (CPG 30 mg/kg and CDDP 324 mg/kg). The rats received gastric infusion of corresponding drugs for 21 continuous days. Blood sample of SD rats were collected by puncture of the abdominal artery for the determination of coagulation parameters such as prothrombin time (PT), activated partial thromboplastin time (APTT), fibrinogen (FIB) concentration and thrombin time (TT) in each group. Another 40 SD rats were used for the observation of inhibitory effect on the thrombosis in arteriovenous shunt. Finally, homology modeling and molecular docking were employed to simulate their interaction between the P2Y purinoceptor 12 (P2Y12) target and bioactive compounds contained in CDDP. RESULTS: The bleeding time of coagulation parameters was prolonged, the thrombosis in arteriovenous shunt was inhibited in the medication group. The above effect was much better in the combination group. The molecular docking showed that bioactive compounds contained in CDDP was able to inhibit target P2Y12. CONCLUSION: CDDP can enhance the effect of CPG on inhibiting platelet aggregation.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Agregação Plaquetária/efeitos dos fármacos , Salvia miltiorrhiza/química , Ticlopidina/análogos & derivados , Animais , Tempo de Sangramento , Coagulação Sanguínea , Testes de Coagulação Sanguínea , Clopidogrel , Hemostáticos , Tempo de Tromboplastina Parcial , Inibidores da Agregação Plaquetária , Tempo de Protrombina , Antagonistas do Receptor Purinérgico P2Y/farmacologia , Ratos , Ratos Sprague-Dawley , Tempo de Trombina , Trombose , Ticlopidina/farmacologia
5.
Zhong Yao Cai ; 37(12): 2240-3, 2014 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-26080512

RESUMO

OBJECTIVE: To investigate the effect of clopidogrel on the pharmacokinetic of Fufang Danshen Dripping Pill (FDDP); METHODS: 20 SD rats were randomly divided into two group,which were intrinsically administrated FDDP(324 mg/kg) alone and combination of FDDP(324 mg/kg) and clopidogrel(30 mg/kg) respectively for 21 days. The ginsenoside Rg, from FDDP was determined by HPLC and its pharmacokinetic parameter were finally compared. RESULTS: The value of Cmax and AUC0-∞ of ginsenoside Rg, were increased from 1.97 ± 0.44 mg/L and 8.44 ± 2.64 mg/L · h to 2.48 ± 0.63 mg/L and 14.38 ± 5.72 mg/L · h respectively. CONCLUSION: Long term with clopidogrel has effect on the pharmacokinetic character of Rg, from FDDP, this research may provides theoretical support for the FDDP-clopidogrel combination treatment in clinical.


Assuntos
Medicamentos de Ervas Chinesas/farmacocinética , Ginsenosídeos/farmacocinética , Ticlopidina/análogos & derivados , Animais , Cromatografia Líquida de Alta Pressão , Clopidogrel , Sinergismo Farmacológico , Ratos , Ratos Sprague-Dawley , Ticlopidina/farmacologia
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