刘磊,孙璐,黄海华,杨田英,钟大放
LIU Lei 1, SUN Lu 2, HUANG Hai hua 1, YANG Tian ying 3, ZHONG Da fang 2 (1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China; 2. Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharma

• 1:沈阳药科大学制药工程学院
• 2:沈阳药科大学药物代谢与药物动力学实验室
• 3:沈阳药科大学制药工程学院
• 4:大连美罗大药房连锁有限公司

摘要(Abstract)：

目的研究微生物对萘普生的转化能力。方法以雅致小克银汉霉菌AS 3 1 5 6为转化菌株 ,并对转化条件进行优化 ,利用液相色谱 质谱联用法检测转化液中萘普生的代谢产物。结果根据液相色谱和质谱数据推测 ,主要转化产物为O 去甲基萘普生。对影响O 去甲基萘普生形成因素的考察发现 ,以pH 6 0 ,底物浓度 0 0 2 5 % ,转化反应持续 72h等条件较为适宜 ,其产率大于 95 %。结论雅致小克银汉霉菌AS 3 1 5 6能够高度专一性地对萘普生进行O 去甲基转化反应 ,可以作为药物代谢研究新的体外模型。
Objective To study the microbial transformation of naproxen. Methods Cunninghamella elegans AS 3 156 and LC/MS n analysis were used.Results The observed product was O demethyl naproxen by LC/MS n data. Influential factors of the O demethylation were investigated, and the optimized conditions were pH 6 0, 0 025% of substrate concentration, and 72 h of incubation, and the yield of the metabolite was >95%. Conclusions C.elegans AS 3 156 has the ability to catalyze the O demethylation of naproxen specifically, and it can be used as a new in vitro model of the mammalian drug metabolism.

关键词(KeyWords)： 萘普生;微生物转化;雅致小克银汉霉菌;去甲基化;液相色谱质谱分析
naproxen; microbial transformation; Cunninghamella elegans ; O demethylation; LC/MS n

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金资助项目 (3 993 0 1 80 )

作者(Authors): 刘磊,孙璐,黄海华,杨田英,钟大放
LIU Lei 1, SUN Lu 2, HUANG Hai hua 1, YANG Tian ying 3, ZHONG Da fang 2 (1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China; 2. Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharma

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