Benzydamine N-oxygenation as a measure of flavin-containing monooxygenase activity.
Benzydamine N-oxygenation as a measure of flavin-containing monooxygenase activity.
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苄达明 N-氧化作为含黄素单加氧酶活性的量度。
DOI：
10.1385/1-59259-998-2:157
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发表时间：
2006
影响因子：
--
通讯作者：
A. Rettie
中科院分区：
文献类型：
--
作者：
C. Yeung;A. Rettie
Benzydamine 是一种非甾体类抗炎药，可通过含黄素单加氧酶 (FMO) 依赖性代谢形成稳定的 N-氧化物。通过使用带有荧光检测的简单反相高效液相色谱 (HPLC) 测定，可以以高特异性和灵敏度对该代谢物进行定量。重组 FMO 酶的研究表明，FMOI 和 FMO3 是苯乙胺 N-氧化的主要催化剂，细胞色素 P450 酶的贡献极小。对人肝微粒体进行的研究证实，FMO3 在很大程度上负责该组织中苯达明 N-氧化物的形成。这些特性使苯甲胺成为多种组织和细胞类型中 FMO 活性的有用体外探针。此外，苯甲胺似乎是人肝脏 FMO3 的合适体内探针。本章详细介绍了通过含 FMO 的酶组分测定苯达明 N-氧化物形成速率的实验方案。
Benzydamine is a nonsteroidal anti-inflammatory drug that undergoes flavin-containing monooxygenase (FMO)-dependent metabolism to a stable N-oxide. This metabolite can be quantified with high specificity and sensitivity by using a simple reverse-phase high-performance liquid chromatography (HPLC) assay with fluorescence detection. Studies with recombinant FMO enzymes demonstrate that FMOI and FMO3 are the primary catalysts of benzydamine N-oxygenation, with minimal contributions from cytochrome P450 enzymes. Investigations conducted with human liver microsomes confirm that FMO3, in large part, is responsible for benzydamine N-oxide formation in this tissue. These features render benzydamine a useful in vitro probe for FMO activity in a wide range of tissues and cell types. In addition, benzydamine appears to be a suitable in vivo probe for human liver FMO3. This chapter provides a detailed account of the experimental protocol for determining rates of formation of benzydamine N-oxide by FMO-containing enzyme fractions.
影响因子：
5.8
作者：
Lang, DH;Yeung, CK;Rettie, AE
通讯作者：
Rettie, AE