NDLI: Gambogic acid suppresses cytochrome P450 3A4 by downregulating pregnane X receptor and up-regulating DEC1 in human hepatoma HepG2 cells

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New approaches for biomonitoring exposure to the human carcinogen aristolochic acid

Towards the development of mechanism-based biomarkers to diagnose drug hypersensitivity

The puzzle of toxicity of gold nanoparticles. The case-study of HeLa cells

In vitro models for neurotoxicology research

Molecular modeling and spectroscopic study of quinone–protein adducts: insight into toxicity, selectivity, and reversibility

CpG site-specific RASSF1a hypermethylation is associated with occupational PAH exposure and genomic instability

Interleukin-6 promotes dietary carcinogen-induced DNA damage in colorectal cancer cells

Dose–response assessment of the dermal toxicity of triclosan in B6C3F1 mice

Behavioral and dopaminergic damage induced by acute iron toxicity in Caenorhabditis elegans

Toxicity mechanism of graphene oxide and nitrogen-doped graphene quantum dots in RBCs revealed by surface-enhanced infrared absorption spectroscopy

Participation of b^0,+ and B^0,+ systems in the transport of mercury bound to cysteine in intestinal cells

Lack of effect of metofluthrin and sodium phenobarbital on replicative DNA synthesis and Ki-67 mRNA expression in cultured human hepatocytes

The Zishen Yutai pill shows no reproductive toxicity on embryo-fetal development in rats and rabbits

Identification and quantification of biomarkers to confirm the poisoning by Ginkgo biloba seeds in a 2-year-old boy

Perfluorooctane sulfonate induces apoptosis of hippocampal neurons in rat offspring associated with calcium overload

Metabolomics reveals disturbed metabolic pathways in human lung epithelial cells exposed to airborne fine particulate matter

Metabolomic profiling of emodin-induced cytotoxicity in human liver cells and mechanistic study

Two generation reproduction and teratogenicity studies of feeding diaveridine in Wistar rats

Toxicological assessment of PEG functionalized f-block rare earth phosphate nanorods

Differential effects of p38 and JNK activation by GSK3 on cadmium-induced autophagy and apoptosis

Exocyclic DNA adducts in sheep with skeletal fluorosis resident in the proximity of the Portoscuso-Portovesme industrial estate on Sardinia Island, Italy

Do poly(epsilon-caprolactone) lipid-core nanocapsules induce oxidative or inflammatory damage after in vivo subchronic treatment?

Neurobehavioral changes induced by di(2-ethylhexyl) phthalate and the protective effects of vitamin E in Kunming mice

Inhibition of the flavonoid extract from silkworm cocoons on DMBA/UVB-induced skin damage and tumor promotion in BALB/c mice

Effects of monoolein-based cubosome formulations on lipid droplets and mitochondria of HeLa cells

Biocompatibility studies on lanthanum oxide nanoparticles

Prenatal nicotine exposure induced GDNF/c-Ret pathway repression-related fetal renal dysplasia and adult glomerulosclerosis in male offspring

Gambogic acid suppresses cytochrome P450 3A4 by downregulating pregnane X receptor and up-regulating DEC1 in human hepatoma HepG2 cells

Umbelliferone β-d-galactopyranoside exerts an anti-inflammatory effect by attenuating COX-1 and COX-2

A new animal model for Polygonum multiflorum Thunb-induced liver injury in rats and its potential mechanisms

Synthesis and analysis of novel analogues of dexrazoxane and its open-ring hydrolysis product for protection against anthracycline cardiotoxicity in vitro and in vivo

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Gambogic acid suppresses cytochrome P450 3A4 by downregulating pregnane X receptor and up-regulating DEC1 in human hepatoma HepG2 cells

Content Provider	Royal Society of Chemistry (RSC)
Author	Liu, Jie Hu, Gang Liu, Wei Chen, Rui-Ni Yang, Jian Wang, Yu-Wen Guo, Qing-Long Hu, Jin-Hua Gui, Hai-Yan Ning, Rui
Copyright Year	2015
Abstract	Gambogic acid (GA) was approved by the Chinese Food and Drug Administration for phase II clinical trials in patients with solid tumors. Recently, combinations of GA and chemotherapeutic agents have represented a promising therapeutic approach for cancer. However, little is known about the effect of GA on drug metabolism enzymes. In this study, we report for the first time that GA is a potent repressor of the cytochrome P450 3A4 (CYP3A4) enzyme, which is responsible for the oxidative metabolism of more than 60% of all pharmaceuticals. After HepG2 cells were treated with GA, the expression of CYP3A4 decreased at both the mRNA and protein levels, and CYP3A4 enzymatic activity was also reduced. Moreover, GA-mediated repression of CYP3A4 occurred after the decrease of PXR. Knockdown of PXR decreased CYP3A4 at the mRNA and protein levels, whereas PXR overexpression increased the CYP3A4 mRNA and protein levels. GA markedly decreased CYP3A4 expression in both normal and PXR overexpressing cells. Meanwhile, differentiated embryonic chondrocyte gene 1 (DEC1) expression rapidly increased in response to GA treatment, and subsequently, CYP3A4 expression continuously decreased. Overexpression of DEC1 decreased CYP3A4 mRNA and protein levels, and knockdown of DEC1 partially abolished the GA-mediated decrease in CYP3A4 expression. Taken together, our data suggest that two transcriptional factors, PXR and DEC1, are involved in the GA-mediated suppression of CYP3A4 in HepG2 cells.
Starting Page	1059
Ending Page	1071
Page Count	13
File Format	HTM / HTML PDF
ISSN	2045452X
Volume Number	4
Issue Number	4
Journal	Toxicology Research
DOI	10.1039/c4tx00239c
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Open
Subject Keyword	DEC1 Messenger RNA Chondrocyte Gene Enzyme Pregnane X receptor Metabolism CYP3A4 Chinese Food and Drug Administration Protein Cancer
Content Type	Text
Resource Type	Article
Subject	Health, Toxicology and Mutagenesis Toxicology

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Gambogic acid suppresses cytochrome P450 3A4 by downregulating pregnane X receptor and up-regulating DEC1 in human hepatoma HepG2 cells

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