(E)-2-苄基环酮:第十七部分。环查尔酮类似物(E)-2-[(4'-甲氧基苯基)亚甲基]-苯并亚龙-1-酮微粒体转化反应的LC-MS研究

F. Kenari, S. Molnár, Z. Pintér, Sobhan Bitaraf, P. Perjési
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引用次数: 1

摘要

用大鼠肝微粒体研究了抗增殖(E)-2-[(4 ' -甲氧基苯基)亚甲基]-苯并萘龙-1-one (2c)的生物转化。通过高效液相色谱-质谱法鉴定了一种单氧化(2c+O)和去甲基化(2c- ch2)代谢物。未发现大鼠肝微粒体羰基还原酶的预期产物(E)-2-[(4′-甲氧基苯基)亚甲基]-苯并萘龙-1-醇。微粒体的gst催化反应导致非对映异构体gst偶联物的形成。在本HPLC条件下,非对映异构体加合物被分离成两个色谱峰(2c-GSH-1和2c-GSH-2)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
(E)-2-Benzylidenecyclanones: Part XVII. An LC-MS study of microsomal transformation reactions of (E)-2-[(4'-methoxyphenyl)methylene]-benzosuberon-1-one: A cyclic chalcone analog
Biotransformation of the antiproliferative (E)-2-[(4’-methoxyphenyl)methylene]-benzosuberon-1-one (2c) was studied using rat liver microsomes. As a result of the CYP-catalyzed transformations, one monooxygenated (2c+O) and the demethylated (2c-CH2) metabolites were identified by HPLC-MS. (E)-2-[(4’-methoxyphenyl)methylene]-benzosuberon-1-ol, the expected product of rat liver microsomal carbonyl reductase, was not found in the incubates. Microsomal GST-catalyzed reaction of the compound resulted in formation of diastereomeric GST-conjugates. Under the present HPLC conditions, the diastereomeric adducts were separated into two chromatographic peaks (2c-GSH-1 and 2c-GSH-2).
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