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学科主题物理化学
The UDP-glucuronosyltransferase 1A6 isozyme is responsible for protocatechuic aldehyde glucuronidation in human live
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
2008-05-11
会议地点中国
页码29/1
部门归属十八室
主办者DRUG METABOLISM REVIEWS
英文摘要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
文献类型会议论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/113474
专题中国科学院大连化学物理研究所
通讯作者Yang L(杨凌)
推荐引用方式
GB/T 7714
Liu HX,Zou HF,Yang L. The UDP-glucuronosyltransferase 1A6 isozyme is responsible for protocatechuic aldehyde glucuronidation in human live[C],2008:29/1.
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