کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8993186 | 1113471 | 2005 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Repeated Glucuronidation at One Hydroxyl Group Leads to Structurally Novel Diglucuronides of Steroid Sex Hormones
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Repeated Glucuronidation at One Hydroxyl Group Leads to Structurally Novel Diglucuronides of Steroid Sex Hormones Repeated Glucuronidation at One Hydroxyl Group Leads to Structurally Novel Diglucuronides of Steroid Sex Hormones](/preview/png/8993186.png)
چکیده انگلیسی
Androgens (androsterone, dihydrotestosterone and testosterone) and estrogens (estradiol, estriol and estrone) were incubated with liver microsomes from rats, dogs, monkeys and humans in the presence of uridine diphosphoglucuronic acid (UDPGA), and the glucuronides produced were structurally characterized by liquid chromatography-tandem mass spectrometry. After 2-h incubation with dog liver microsomes, all substrates tested were converted (approximately 2-10%) to structurally novel diglucuronides, where two glucuronosyl groups are bound to a single hydroxyl group in tandem. Two-dimensional nuclear magnetic resonance spectroscopy unambiguously elucidated the chemical structures of the 3-O-diglucuronide of estrone and the 17-O-diglucuronide of testosterone isolated from the incubation mixture. Monkey and human liver microsomes were also found to have the activity to form this type of diglucuronide, albeit more slowly than the dog liver microsomes, but rat liver microsomes produced no detectable diglucuronides. The rate of formation of estrone 3-O-diglucuronide from the corresponding monoglucuronide in dog liver microsomes followed classical Michaelis-Menten kinetics at substrate concentrations from 50 to 1000 μM, with a Km value of 127.1 μM and a Vmax value of 47.0 pmol/min/mg protein.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Drug Metabolism and Pharmacokinetics - Volume 20, Issue 4, 2005, Pages 282-293
Journal: Drug Metabolism and Pharmacokinetics - Volume 20, Issue 4, 2005, Pages 282-293
نویسندگان
Takahiro Murai, Haruo Iwabuchi, Toshihiko Ikeda,