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目的:对药物利培酮进行微生物转化研究,并对主要转化产物进行检识和结构鉴定,预测其微生物转化途径。方法:构建利培酮微生物转化模型,采用LC-MSn方法检测原药及其转化物;通过比较菌液样品和空白样品的正离子色谱图寻找转化产物,根据其多级质谱图,确定转化产物的分子结构,进而预测利培酮微生物转化途径。结果:从不同培养时间利培酮微生物转化液中鉴定出4个转化产物,除产物9-OH利培酮外,其余3个转化产物可能都是新的利培酮代谢产物。结论:利培酮在Cunninghamella blakesleeana AS 3.153中被转化为多种产物,利用LC-MSn可以快速检查和鉴定。
OBJECTIVE: To study the microbial transformation of risperidone, identify and identify the major transformation products, and predict the microbial transformation pathway. Methods: The model of microbial transformation of risperidone was constructed, and the original drug and its transformant were detected by LC-MSn method. The products of transformation were found by comparing the positive ion chromatogram of the bacterial liquid sample and the blank sample. Based on the multi-mass spectra, Molecular structure, and then predict the risperidone microbial transformation pathway. Results: Four transformants were identified from the risperidone microbial transformants at different culture periods. The three transformants except the 9-OH-risperidone product may be the new metabolites of risperidone. Conclusions: Risperidone was converted to various products in Cunninghamella blakesleeana AS 3.153 and was rapidly checked and characterized using LC-MSn.