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学科主题: 物理化学
题名: The UDP-glucuronosyltransferase 1A6 isozyme is responsible for protocatechuic aldehyde glucuronidation in human live
作者: Liu HX(刘慧鑫) ;  Zou HF(邹汉法) ;  Yang L(杨凌)
会议名称: 2nd ASIAN PACIFIC REGIONAL ISSX MEETING
会议日期: 2008-5-11
出版日期: 2008-05-11
会议地点: 中国
通讯作者: 杨凌
部门归属: 十八室
主办者: DRUG METABOLISM REVIEWS
摘要: Glucuronidation is an important pathway in the metabolism of protocatechuic aldehyde (3,4-dihydroxybenzaldehyde, PAL). However, the metabolites and primary UDP-glucuronosyltransferase (UGT) isozymes responsible for PAL glucuronidation remain to be determined in human. Here, we characterized PAL glucuronidation by human liver micorsomes (HLMs), human intestine microsomes (HIMs) and 12 recombinant UGT isozymes to identify what kinds of metabolites are and which human UGT isozymes involved. Two metabolites (M-1 and M-2) were detected in reactions catalyzed by HLMs, HIMs, recombinant UGT1A6 and recombinant UGT1A9 and identified as mono-glucuronides by LC-MS. The PAL glucuronidation activity was significantly correlated with UGT1A6 activity rather than UGT1A9 activity from 15 individual HLMs. A kinetic study showed that PAL glucuronidation by recombinant UGT1A6, rcombinant UGT1A9, HIMs, and HLMs followed Michaelis-Menten. The Km values of HLMs, HIMs, recombinant UGT1A6 and recombinant UGT1A9 for PAL glucuronidation were as follows: 432.7 ± 24.5, 626.9 ± 49.2, 367.5 ± 25.1 and 379.9 ± 42.5 μM for M-1; 336.7 ± 15.3, 494.3 ± 48.7, 211.4 ± 13.4, and 238.5 ± 26.2 μM for M-2, respectively. A chemical inhibition showed that the IC50 for phenylbutazone inhibition of PAL glucuronidation was similar in HLMs (61.9 ± 7.9 μM) compared with recombinant UGT1A6 (45.3 ± 7.7 μM). In contrast, androsterone inhibited recombinant UGT1A9-catalyzed PAL glucuronidation with IC50 value of 27.1 ± 3.8 μM, but the IC50 value of androsterone in HLMs was > 500 μM . In combination, we identified UGT1A6 was the major isozyme responsible for PAL glucuronidation in HLMs.
语种: 中文
内容类型: 会议论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/113474
Appears in Collections:中国科学院大连化学物理研究所_会议论文

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Recommended Citation:
Liu HX,Zou HF,Yang L. The UDP-glucuronosyltransferase 1A6 isozyme is responsible for protocatechuic aldehyde glucuronidation in human live[C]. 见:2nd ASIAN PACIFIC REGIONAL ISSX MEETING. 中国. 2008-5-11.
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