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題 名 | Metabolism of Flutamide in Diet Control Fischer 344 and Brown Norway×F 344 Rats, and Its Hydroxylation and Conjugation by Human CYP450s and UDP-Glucuronosyltransferases=食量控制對Flutamide在大白鼠體內代謝的影響,並人體細胞色素及尿甘二磷酸葡萄糖醛酸轉化酵素對其羥基化及接合之研究 |
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作 者 | 張淳文; | 書刊名 | 藥物食品分析 |
卷 期 | 8:3 2000.09[民89.09] |
頁 次 | 頁166-173 |
分類號 | 418.1 |
關鍵詞 | 食量控制; 不限食量; 羥基化; 接合作用; 細胞色素; 細胞微體; 尿甘二磷酸葡萄糖醛酸轉化酵素; Flutamide; Diet restricted; Non limited-fed; Hydroxylation; Glucuronidation; CYP450; UDP-glucuronosyltransferase; |
語 文 | 英文(English) |
英文摘要 | In our current report, flutamide (2-methyl-N-[4-nitro-3-(trifluoromethyl)- phenyl] propanamide) treated diet control and non limited-fed Fischer 344 (F344) and Brown Norway (BN) ’ F344 rats showed that diet control reduces spontaneous and flutamide-induced hyperplasia(1). In this continued study, we found that serum concentrations of active metabolite of flutamide, 2-hydroxyflutamide (OH-flu), were 181 ± 26.6 ng/mL and 68 ± 8.0 ng/mL (p<0.05), in non-limited fed and diet control F344 rats. In BN ’ F344 rats, the serum concentrations of 2-OH-flutamide were 232± 57 ng/mL and 52±6 ng/mL (p<0.05) in non-limited fed and diet control animals. In diet control groups, liver microsomes from flutamide-treated F344 rats showed high 7-ethoxyresorufin O-deethylase (EROD) activity, while 7-Benzoxyresorufin O- dealkylase (BROD) activity was not affected significantly. Both rat and human liver microsomes showed flutamide oxidation activity. Human liver microsomes showed 10 times higher activity than rat liver microsomes (0.673±0.04 vs 0.063 ± 0.008 nmol OH-flu/min/mg protein). Microsomes from human tissues such as colon, colon cancer, kidney, bladder, pancreas, prostate, prostate cancer, or ovarian cancer, showed no or non-detectable activity for flutamide hydroxylation. CYP450 1A1, 1A2, 1B1 and 2C19 from human lymphoblastoid cell lines, oxidized flutamide to OH-flu in vitro with activities from 0.118 ±0.005 to 0.275 ±0.010 nmol/min/mg protein. Microsomes isolated from human kidney, colon, and liver showed UDP-glucuronosyltransferase (UGT) activity for glucuronidation of OH-flu. Human kidney showed the highest activity. Several human recombinant UGTs (1A1, 1A4, 1A6, 1A7, 1A9, and 1A10) also showed glucuronidation activity for OH-flu. It was found that UGT1A6 was more active than other human UGTs. |
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