Subject Area物理化学
Characterization of Human UDP-Glucuronosyltransferase Isoforms Responsible for the in vitro Glucuronidation of Esculetin
Ge GB(葛广波); Liang SC(梁思成); Liu HX(刘慧鑫); Zhang YY(张延延); Yang L(杨凌)
Conference Name16th North American Regional ISSX Meeting
Conference Date2009-10-18
Conference Place美国
Funding OrganizationThe International Society for the Study of Xenobiotics (ISSX)
AbstractEsculetin (6,7-dihydroxycoumarin), is one of coumarin analogs isolated from various plant including Cichorium intybus, Artemisia scoparia and Fraxinus japonica Blume, has been found to exhibit broaden biological effects, such as analgesic, anti-inflammatory, anti-tumor, anti-arrhythmic, and scavenging activity against reactive oxygen species. Esculetin has been widely used in many Asia countries, and a previous study showed that it can be metabolized by recombinant human UDP-glucuronosyltransferase (UGT) 2B15. However, the metabolic pathway of esculetin in human has not been well-characterized. In the present study, the glucuronidation pathway of esculetin was investigated by using human liver microsomes (HLMs) and 12 commercially available recombinant human UGTs. The results showed that only one metabolite (M-1) can be rapidly formed in the presence of UDPGA with HLMs, which was identified as a C-6 mono glucuronidation metabolite by liquid chromatography/mass spectrometry (LC/MS) and nuclear magnetic resonance (NMR), indicating that C-6 phenolic group of esculetin was a preferred glucuronidation site. Recombinant human UGTs study revealed that many UGT isoforms (including UGT1A6, UGT1A1, UGT1A7, UGT1A8 and UGT2B15) involved in C-6 glucuronidation of esculetin, and further study revealed that Km value of M-1 in human liver microsomes was 208 + 31 μM. These results indicated that many UGT isoforms have contributed glucuronidation clearance of esculetin via the selective glucuronidation of C-6 phenolic group.
WOS IDWOS:000280165300274
Citation statistics
Cited Times:1[WOS]   [WOS Record]     [Related Records in WOS]
Document Type会议论文
Corresponding AuthorYang L(杨凌)
Recommended Citation
GB/T 7714
Ge GB,Liang SC,Liu HX,et al. Characterization of Human UDP-Glucuronosyltransferase Isoforms Responsible for the in vitro Glucuronidation of Esculetin[C],2009:287/1.
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