Comparison of Inhibition Capability of Scutellarein and Scutellarin Towards Important Liver UDP‐Glucuronosyltransferase (UGT) Isoforms

• DOI: 10.1002/ptr.4990
• Publication Date: 2013-04-26T05:28:53Z
• Authors: Guang‐You Ma; Yun‐Feng Cao; Cui‐Min Hu; Zhong‐Ze Fang; Xiao‐Yu Sun; Mo Hong; Zhi‐Tu Zhu
• Keywords: Scutellarin; Flavones

Scutellarin is an important bioactive flavonoid extracted from Erigeron breviscapus (Vant.) Hand‐Mazz, and scutellarein the corresponding aglycone of scutellarin. The present study aims to compare inhibition potential scutellarin towards several UDP‐glucuronosyltransferase (UGT) isoforms, including UGT1A1, UGT1A6, UGT1A9 UGT2B7. It was demonstrated that exerted stronger tested UGT isoforms than Furthermore, kinetic type parameters (K i ) were determined for scutellarein's these isoforms. Competitive all demonstrated, K values calculated be 0.02, 5.0, 5.8 35.9 μM 1A6, 1A9 2B7, respectively. Using in vivo maximum plasma concentration rat, vitro–in extrapolation performed predict situation, indicating most possible adverse effects due UGT1A1. All results remind us monitor utilization scutellarein, herbs containing two components. Copyright © 2013 John Wiley & Sons, Ltd.