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Gancao (Glycyrrhizae Radix) provides the main contribution to Shaoyao-Gancao decoction on enhancements of CYP3A4 and MDR1 expression via pregnane X receptor pathway in vitro.
- Source :
- BMC Complementary & Alternative Medicine; 12/29/2018, Vol. 18 Issue 1, p1-12, 12p, 3 Diagrams, 1 Chart, 3 Graphs
- Publication Year :
- 2018
-
Abstract
- Background: Chinese herbal formula Shaoyao Gancao decoction (SGD) is often used as an adjuvant with chemotherapeutic agents to treat cancer. Due to the herb-drug interactions, the alternations of drug metabolic enzyme and drug transporters induced by SGD deserve to be explored. We aimed to investigate the effect of SGD on the pregnane X receptor (PXR)-mediated transcriptional regulation of cytochrome P450 3A4 (CYP3A4) and drug transporter multidrug resistance protein 1 (MDR1) in vitro. Besides, we assessed the contribution of constituent herbs to SGD on the regulation of CYP3A4 and MDR1. Methods: The dual luciferase reporter gene system containing the hPXR expression plasmid and the reporter gene plasmid of CYP3A4 or MDR1 was co-transfected to HepG2 and Caco2 cells. Luciferase activities were determined using a Dual-luciferase reporter assay kit. The gene expression of CYP3A4 and MDR1 in the hPXR-transfected LS174T cells were assessed by real-time qPCR. Finally, the contribution of constituent herbs from SGD was evaluated. Results: SGD, Shaoyao and Gancao concentration-dependently increased promoter activities of CYP3A4 and MDR1 in vitro. Moreover, SGD, Shaoyao and Gancao up-regulated CYP3A4 and MDR1 mRNA in hPXR-transfected LS174T cells. As the herbal constituent of SGD, Gancao possesses significantly higher levels of metabolic enzyme and drug transporters compared with Shaoyao. Conclusion: SGD tends to enhance CYP3A4 and MDR1 expression via PXR pathway, especially Gancao provides the main contribution. This study highlights a potential in vitro mechanism for SGD on the regulation of drug metabolic enzymes and drug transporters. [ABSTRACT FROM AUTHOR]
- Subjects :
- BIOCHEMISTRY
CELL lines
CELLULAR signal transduction
COMBINED modality therapy
DRUG resistance
GENE expression
GLYCOPROTEINS
PHENOMENOLOGY
DRUG-herb interactions
CHINESE medicine
MESSENGER RNA
OXIDOREDUCTASES
POLYMERASE chain reaction
STEROID receptors
TUMORS
PLANT extracts
REVERSE transcriptase polymerase chain reaction
IN vitro studies
MEMBRANE transport proteins
CYTOCHROME P-450
Subjects
Details
- Language :
- English
- ISSN :
- 14726882
- Volume :
- 18
- Issue :
- 1
- Database :
- Complementary Index
- Journal :
- BMC Complementary & Alternative Medicine
- Publication Type :
- Academic Journal
- Accession number :
- 133780114
- Full Text :
- https://doi.org/10.1186/s12906-018-2402-7