In vivo and mechanistic evidence of nuclear receptor CAR induction by artemisinin

USH Simonsson, M Lindell… - European journal of …, 2006 - Wiley Online Library
Background Artemisinin (a sesquiterpene lactone endoperoxide) has become important in
multi‐drug treatment of malaria. There is evidence that artemisinin induces drug metabolism …

Differential effects of clinically used derivatives and metabolites of artemisinin in the activation of constitutive androstane receptor isoforms

O Burk, R Piedade, L Ghebreghiorghis… - British journal of …, 2012 - Wiley Online Library
BACKGROUND AND PURPOSE Widespread resistance to antimalarial drugs requires
combination therapies with increasing risk of pharmacokinetic drug–drug interactions. Here …

Antimalarial artemisinin drugs induce cytochrome P450 and MDR1 expression by activation of xenosensors pregnane X receptor and constitutive androstane receptor

O Burk, KA Arnold, AK Nussler, E Schaeffeler… - Molecular …, 2005 - ASPET
Artemisinin drugs are of utmost importance in the treatment of malaria, because they
represent the sole class of therapeutically used antimalarial drugs to which malaria …

Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes

J Xing, BJ Kirby, D Whittington, Y Wan… - Drug Metabolism and …, 2012 - ASPET
Artemisinin drugs have become the first-line antimalarials in areas of multidrug resistance.
However, monotherapy with artemisinin drugs results in comparatively high recrudescence …

Effects of artemisinin antimalarials on Cytochrome P450 enzymes in vitro using recombinant enzymes and human liver microsomes: potential implications for …

T Ericsson, J Sundell, A Torkelsson, KJ Hoffmann… - Xenobiotica, 2014 - Taylor & Francis
Cytochrome P450 enzyme system is the most important contributor to oxidative metabolism
of drugs. Modification, and more specifically inhibition, of this system is an important …

Identification of the human cytochrome P450 enzymes involved in the in vitro metabolism of artemisinin

Svensson, Ashton - British journal of clinical pharmacology, 1999 - Wiley Online Library
Aims The study aimed to identify the specific human cytochrome P450 (CYP450) enzymes
involved in the metabolism of artemisinin. Methods Microsomes from human B …

Artemisinin antimalarials moderately affect cytochrome P450 enzyme activity in healthy subjects

S Asimus, D Elsherbiny, TN Hai… - Fundamental & …, 2007 - Wiley Online Library
The aim of this study was to investigate which principal human cytochrome P450 (CYP450)
enzymes are affected by artemisinin and to what degree the artemisinin derivatives differ …

Artemisinin autoinduction is caused by involvement of cytochrome P450 2B6 but not 2C9

USH Simonsson, B Jansson, TN Hai… - Clinical …, 2003 - Wiley Online Library
Aim Our goal was to investigate whether artemisinin autoinduction is caused by an increase
in cytochrome P450 (CYP) 2B6 or CYP2C9 activities, we evaluated the effects of multiple …

Impact of chrysosplenetin on the pharmacokinetics and anti-malarial efficacy of artemisinin against Plasmodium berghei as well as in vitro CYP450 enzymatic …

S Wei, H Ji, B Yang, L Ma, Z Bei, X Li, H Dang, X Yang… - Malaria Journal, 2015 - Springer
Background Artemisinin (ART) is an efficacious and safe anti-malarial drugs but has low oral
bioavailability and auto-induction profiles during multiple dosing. The pharmacokinetic …

Artemisia extracts differ from artemisinin effects on human hepatic CYP450s 2B6 and 3A4 in vitro

NF Kane, BH Kiani, MR Desrosiers, MJ Towler… - Journal of …, 2022 - Elsevier
Abstract Ethnopharmacological relevance The Chinese medicinal herb, Artemisia annua L.,
has been used for> 2,000 yr as traditional tea infusions to treat a variety of infectious …