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作 者:陈为烤[1] 居文政[2] 许黎君[1] 谈恒山[3]
机构地区:[1]南京中医药大学药学院,南京210029 [2]南京中医药大学附属医院,南京210029 [3]南京军区总医院,南京210002
出 处:《药学与临床研究》2008年第5期351-354,共4页Pharmaceutical and Clinical Research
基 金:科技部"十一五"支撑计划课题--药物临床研究关键技术研究与应用(No:2006BAI14B07)
摘 要:目的:通过测定细胞色素P450(CYP450)含量和甲醛生成率,考察脉络宁注射液对小鼠总CYP450以及红霉素-N-脱甲基酶(CYP3A)和氨基比林-N-脱甲基酶(CYP2E1)活性的影响。方法:采用紫外分光光度法和体外温孵反应,测定并比较了给药组和对照组小鼠在肝脏系数、微粒体蛋白含量、CYP450含量及甲醛生成速率方面的差异。结果:两种剂量脉络宁对小鼠肝脏系数和CYP450含量影响都不显著,但均能提高微粒体蛋白含量;两种剂量脉络宁均可抑制CYP2E1的活性,临床等效用量时对CYP3A活性影响不显著,高剂量时可能抑制CYP3A活性。结论:脉络宁注射液对CYP3A和CYP2E1亚型活性有影响。Objective: To investigate the effects of Mailuoning Injection on mouse's overall CYP450s, erythromycin-N-demethylase(CYP3A) and aminopyrine-N-demethylase (CYP2EI)activities via determining overall CYP450 content and formaldehyde formation rate. Method: UV-Visible spectrophotometery and in vitro microsomal incubations were performed to determine and compare the differences between groups of Mailuoning-treated mice and controls in terms of liver coefficiency, microsomal protein content, CYP450 content and formaldehyde formation rate. Result: Two doses of Mailuoning Injection had insignificant impact on mouse liver coefficiency and CYP450 content, but could increase microsomal protein contents. Meanwhile, both doses might inhibit CYP2E1 activity, and high dose might inhibit CYP3A activity, but clinically equivalent dose failed. Conclusion: Mailuoning Injection could affect CYP3A and CYP2E1 activities.
关 键 词:脉络宁注射液 CYP450 氨基比林-N-脱甲基酶 红霉素-N-脱甲基酶
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