萘普生的微生物转化

Studies of microbial transformation of naproxen

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.