Huang Hai-Hua, Ma Gui-Lei, Sun Yu-Ming, Li Qiang, Zhong Da-Fang
Department of Pharmaceutical Microbiology, Shenyang Pharmaceutical University, Shenyang 110016, China.
Acta Pharmacol Sin. 2005 Jul;26(7):893-6. doi: 10.1111/j.1745-7254.2005.00091.x.
To study phase II metabolites of etofesalamide in filamentous fungi.
Seven fungi were screened to transform etofesalamide. The metabolites of etofesalamide were assayed using liquid chromatography coupled to mass spectrometry. The major metabolite was subject to enzymatic hydrolysis to confirm its structure.
Etofesalamide was converted into two phase II metabolites: glucoside and riboside conjugates. Glucoside conjugate was the major product with a yield greater than 90%; no phase I metabolites were detected.
Glucoside and riboside conjugations of etofesalamide in filamentous fungi differ from the phase II metabolism of glucuronidation in mammals.
研究依托法胺在丝状真菌中的Ⅱ相代谢产物。
筛选7种真菌以转化依托法胺。采用液相色谱-质谱联用技术测定依托法胺的代谢产物。对主要代谢产物进行酶水解以确定其结构。
依托法胺转化为两种Ⅱ相代谢产物：葡萄糖苷和核糖苷缀合物。葡萄糖苷缀合物是主要产物，产率大于90%；未检测到Ⅰ相代谢产物。
依托法胺在丝状真菌中的葡萄糖苷和核糖苷缀合与哺乳动物中的葡萄糖醛酸化Ⅱ相代谢不同。
