秀丽小克银汉霉对组胺拮抗剂氮他定的真菌生物转化作用
Fungal biotransformation of the antihistamine azatadine by Cunninghamella elegans.
作者信息
Zhang D, Hansen E B, Deck J, Heinze T M, Sutherland J B, Cerniglia C E
机构信息
Division of Microbiology, Food and Drug Administration, Jefferson, Arkansas 72079, USA.
出版信息
Appl Environ Microbiol. 1996 Sep;62(9):3477-9. doi: 10.1128/aem.62.9.3477-3479.1996.
The metabolism of the antihistamine azatadine by the zygomycete fungus Cunninghamella elegans ATCC 9245 was investigated. Within 72 h from the addition of the drug to 48-h-old cultures grown in Sabouraud dextrose broth, 95% of azatadine was biotransformed. Two major metabolites, 7-hydroxyazatadine (25%) and 8-hydroxyazatadine (50%), and two minor metabolites, N-desmethylazatadine and 9-hydroxyazatadine, were isolated by high-performance liquid chromatography and characterized by mass spectrometric and proton nuclear magnetic resonance spectroscopic analyses.
研究了接合菌真菌雅致小克银汉霉ATCC 9245对抗组胺药氮他定的代谢情况。在将药物添加到在沙氏葡萄糖肉汤中培养48小时的培养物后的72小时内，95%的氮他定发生了生物转化。通过高效液相色谱法分离出两种主要代谢产物，7-羟基氮他定（25%）和8-羟基氮他定（50%），以及两种次要代谢产物，N-去甲基氮他定和9-羟基氮他定，并通过质谱和质子核磁共振光谱分析对其进行了表征。
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