The fungus Pestalotiopsis guepini as a model for biotransformation of ciprofloxacin and norfloxacin

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• 作者：I. A. Parshikov ; T. M. Heinze ; J. D. Moody ; J. P. Freeman ; A. J. Williams and J. B. Sutherland
• 刊名：Applied Microbiology and Biotechnology
• 出版年：2001
• 出版时间：August 2001
• 年：2001
• 卷：56
• 期：3-4
• 页码：474-477
• 全文大小：51 KB

文摘

The metabolism of the fluoroquinolone drugs ciprofloxacin and norfloxacin by Pestalotiopsis guepini strain P-8 was investigated. Cultures were grown at 28 °C in sucrose/peptone broth for 18 days after dosing with ciprofloxacin (300 µM) or norfloxacin (313 µM). Four major metabolites were produced from each drug; and these were purified by high-performance liquid chromatography and identified by mass spectrometry and proton nuclear magnetic resonance spectroscopy. Ciprofloxacin metabolites included N-acetylciprofloxacin (52.0 % ), desethylene-N-acetylciprofloxacin (9.2 % ), N-formylciprofloxacin (4.2 % ), and 7-amino-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (2.3 % ). Norfloxacin metabolites included N-acetylnorfloxacin (55.4 % ), desethylene-N-acetylnorfloxacin (8.8 % ), N-formylnorfloxacin (3.6 % ), and 7-amino-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (2.1 % ). N-Formylciprofloxacin and the four transformation products from norfloxacin are all known to be mammalian metabolites.