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Open AccessArticle

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

Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, Shijiazhuang 050017, China
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;
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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