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Open AccessArticle

Two Approaches for Evaluating the Effects of Galangin on the Activities and mRNA Expression of Seven CYP450

1
Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, Shijiazhuang 050017, China
2
National Clinical Drug Monitoring Center, Department of Pharmacy, Hebei Province General Center, Shijiazhuang 050051, China
*
Author to whom correspondence should be addressed.
Academic Editors: In-Soo Yoon and Hyun-Jong Cho
Molecules 2019, 24(6), 1171; https://doi.org/10.3390/molecules24061171
Received: 1 March 2019 / Revised: 21 March 2019 / Accepted: 22 March 2019 / Published: 25 March 2019
(This article belongs to the Special Issue Method Development and Validation in Food and Pharmaceutical Analysis)
Galangin is a marker compound of honey and Alpinia officinarum Hance that exhibits great potential for anti-microbial, anti-diabetic, anti-obesity, anti-tumour and anti-inflammatory applications. Galangin is frequently consumed in combination with common clinical drugs. Here, we evaluated the effects of galangin on cytochrome P450 (CYP)-mediated metabolism, using two different approaches, to predict drug–drug interactions. Male Sprague Dawley rats were administered galangin daily for 8 weeks. A “cocktail-probes” approach was employed to evaluate the activities of different CYP450 enzymes. Blood samples of seven probe drugs were analysed using liquid chromatography-tandem mass spectrometry in positive and negative electrospray-ionisation modes. Pharmacokinetic parameters were calculated to identify statistical differences. CYP mRNA-expression levels were investigated in real-time quantitative polymerase chain reaction experiments. The galangin-treated group showed significantly decreased AUC0–∞ and Cmax values for CYP1A2, and CYP2B3. The galangin-treated group showed significantly increased AUC0–∞ and Cmax values for CYP2C13 and CYP3A1. No significant influences were observed in the pharmacokinetic profiles of CYP2C11, CYP2D4 and CYP2E1. The mRNA-expression results were consistent with the pharmacokinetic results. Thus, CYP450 enzyme activities may be altered by long-term galangin administration, suggesting galangin to be a promising candidate molecule for enhancing oral drug bioavailability and chemoprevention and reversing multidrug resistance. View Full-Text
Keywords: CYP450 enzyme; cocktail probe drug; RT-PCR; LC-MS/MS; galangin CYP450 enzyme; cocktail probe drug; RT-PCR; LC-MS/MS; galangin
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MDPI and ACS Style

Ma, Y.-L.; Zhao, F.; Yin, J.-T.; Liang, C.-J.; Niu, X.-L.; Qiu, Z.-H.; Zhang, L.-T. Two Approaches for Evaluating the Effects of Galangin on the Activities and mRNA Expression of Seven CYP450. Molecules 2019, 24, 1171.

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