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Metabolic profiling of corylin in vivo and in vitro
TLDR
Corylin was subjected to massive first‐pass metabolism in liver and intestine, while CYP1A1, 1B1, 2C19 and UGT1A 1 were the main contributors and the proposed metabolic pathway of corylin involed CYP and U GT isoforms were summarized, which could help to understand the metabolic fate of c Corylin in vivo. Expand
Efflux excretion of bisdemethoxycurcumin‐O‐glucuronide in UGT1A1‐overexpressing HeLa cells: Identification of breast cancer resistance protein (BCRP) and multidrug resistance‐associated proteins 1
TLDR
Chemical inhibition and gene silencing results both indicated that generated BDMC-O-glucoside were excreted primarily by the BCRP and MRP1 transporters. Expand
Chemical inhibition and stable knock-down of efflux transporters leads to reduced glucuronidation of wushanicaritin in UGT1A1-overexpressing HeLa cells: the role of breast cancer resistance protein
TLDR
Chemical inhibition and gene silencing results suggested that BCRP, MRP1, MRp3 and MRP4 were significant contributors to excretion of wushanicaritin glucuronides. Expand
The Efflux Mechanism of Fraxetin-O-Glucuronides in UGT1A9-Transfected HeLa Cells: Identification of Multidrug Resistance-Associated Proteins 3 and 4 (MRP3/4) as the Important Contributors
TLDR
The results indicate that MRP3 and MRP4 contribute more to the excretion of fraxetin-O-glucuronides than the other transporters do, while no obvious modifications in theexcretion rates, intracellular levels, and fmet values of glucuronides were observed after short hairpin RNA (shRNA)-mediated silencing of transporter BCRP and MRp1. Expand
In vitrometabolic mapping of neobavaisoflavone in human cytochromes P450 and UDP‐glucuronosyltransferase enzymes by ultra high‐performance liquid chromatography coupled with quadrupole time‐of‐flight
TLDR
It is found that NBIF underwent massive glucuronidation and oxidation by human liver microsomes (HLM) in this study with the intrinsic clearance values of 12.04, 10.01, and 6.99&mgr;L/min/mg for M2, M3, M4, and M5, respectively. Expand
Characterization of human UDP-glucuronosyltransferases responsible for glucuronidation and inhibition of norbakuchinic acid, a primary metabolite of hepatotoxicity and nephrotoxicity component
Norbakuchinic acid (NBKA) is the most abundant metabolite of bakuchiol (a hepatotoxicity and nephrotoxicity component in Psoralea corylifolia L.) in plasma and urine. The present study aimed toExpand
The roles of breast cancer resistance protein (BCRP/ABCG2) and multidrug resistance-associated proteins (MRPs/ABCCs) in the excretion of cycloicaritin-3-O-glucoronide in UGT1A1-overexpressing HeLa
TLDR
BCRP, MRP1 and MRP4 were identified as the most important contributors for CICT-3-G excretion and UGT1A1 stably transfected HeLa cells were a simple and practical tool to study UGT 1A1-mediated glucuronidation and to characterize BCRP and MRPs- mediated glucuronide transport at a cellular level. Expand
Characterization of metabolic activity, isozyme contribution and species differences of bavachin, and identification of efflux transporters for bavachin‐O‐glucuronide in HeLa1A1 cells
  • Y. Li, Chunxia Xu, +6 authors X. Yao
  • Medicine, Chemistry
  • The Journal of pharmacy and pharmacology
  • 9 July 2020
TLDR
Bavachin is a bioactive natural flavonoid with oestrogen‐like activity and its metabolic and disposal fates involving in CYPs, UGTs and efflux transporters are investigated. Expand
Metabolism and disposition of corylifol A from Psoralea corylifolia: metabolite mapping, isozyme contribution, species differences and identification of efflux transporters for corylifol
  • Yang Li, Jinjin Xu, +6 authors X. Yao
  • Medicine, Chemistry
  • Xenobiotica; the fate of foreign compounds in…
  • 2 March 2020
TLDR
CYPs, UGTs, MRP4 and BCRP were important determinants of CA pharmacokinetics, and activity correlation analysis proved CYP2C8,UGT1A1 and 1A9 were the main active hepatic isozymes. Expand
Mechanism of the efflux transport of demethoxycurcumin-O-glucuronides in HeLa cells stably transfected with UDP-glucuronosyltransferase 1A1
TLDR
The BCRP, MRP1 and MRP3 transporters were identified as the most important contributors to the excretion of DMC-O-glucuronides and their transport by breast cancer resistance protein (BCRP) and multidrug resistance-associated proteins (MRPs) in HeLa cells stably transfected with UGT1A1 was investigated. Expand