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Poor oral bioavailability of a promising anticancer agent andrographolide is due to extensive metabolism and efflux by P-glycoprotein.
TLDR
AP has poor oral bioavailability because of its rapid biotransformation and efflux by P-gp, and how intestinal disposition affects its bioavailability is determined. Expand
Natural polyphenol disposition via coupled metabolic pathways
  • Zhongqiu Liu, M. Hu
  • Biology, Medicine
  • Expert opinion on drug metabolism & toxicology
  • 31 May 2007
TLDR
More research is needed to determine if the metabolites of polyphenols in plasma are active or reactive, which will help explain their mechanism of actions, and how these coupled processes enable a duo recycling scheme of enteric and enterohepatic recycling. Expand
Involvement of CYP3A4/5 and CYP2D6 in the metabolism of aconitine using human liver microsomes and recombinant CYP450 enzymes.
TLDR
Aconitine can be transformed into at least six CYP-mediated metabolites in HLMs, and CYP 3A4/5 and 2D6 were the most important CYP isoforms responsible for the de-methylation, N-deethylation, dehydrogenation, and hydroxylation of aconitine. Expand
Structure and concentration changes affect characterization of UGT isoform-specific metabolism of isoflavones.
TLDR
It is proposed that a newly discovered UGT3A1 isoform capable of metabolizing phenols and estrogens might be responsible for the metabolism of isoflavones such as formononetin in humans. Expand
Pharmacokinetics of aconitine as the targeted marker of Fuzi (Aconitum carmichaeli) following single and multiple oral administrations of Fuzi extracts in rat by UPLC/MS/MS.
TLDR
The pharmacokinetic behaviour of processed Fuzi was determined and it was found that multiple dose might increase the bioavailability of aconitine, which may result in its toxicity. Expand
A gene catalogue of the Sprague-Dawley rat gut metagenome
TLDR
Ninety-seven percent of the functional pathways in the human catalog were present in the rat catalogue, underscoring the potential use of rats for biomedical research. Expand
Controlled release of optimized electroporation enhances the transdermal efficiency of sinomenine hydrochloride for treating arthritis in vitro and in clinic
TLDR
Electroporation may be an effective complementary method for transdermal permeation of Sinomenine hydrochloride and the controlled release of electroporation May be a promising clinical method fortransdermal drug administration. Expand
Coupling of UDP-glucuronosyltransferases and multidrug resistance-associated proteins is responsible for the intestinal disposition and poor bioavailability of emodin.
TLDR
UGT is a main metabolic pathway for emodin in the intestine, and the MRP family is composed of major efflux transporters responsible for the excretion of emodIn glucuronide in the intestines. Expand
Use of Isoform-Specific UGT Metabolism to Determine and Describe Rates and Profiles of Glucuronidation of Wogonin and Oroxylin A by Human Liver and Intestinal Microsomes
TLDR
Correlation studies clearly showed that UGT isoform-specific metabolism could describe their metabolism rates and profiles in human liver and intestinal microsomes, and suggested UGT1A9 is likely the main isoform responsible for liver metabolism. Expand
Determination of ginsenosides Rb1, Rb2, and Rb3 in rat plasma by a rapid and sensitive liquid chromatography tandem mass spectrometry method: Application in a pharmacokinetic study.
TLDR
The value of R b(1) is higher than that of Rb(2) or Rb (3), indicating that ginsenosides with hexose and hydroxyl groups (Rb(1)) could present better pharmacokinetic behaviors than those with pentose groups in the same glycosylation site by oral administration. Expand
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