In vitro potential modulation of baicalin and baicalein on P-glycoprotein activity and expression in Caco-2 cells and rat gut sacs

Pharmaceutical Biology
Qing MiaoShuangcheng Ma

Abstract

Context Previous studies have shown that Scutellariae Radix, the dried root of Scutellaria baicalensis Georgi (Labiatae), has a certain inhibitory effect on P-glycoprotein (P-gp), but the effects of its main active constituents on P-gp are still ambiguous. Objectives In vitro studies were performed to investigate the effects of its main active constituents (baicalin and its aglycone, baicalein) on the activity and expression of P-gp in intestine using Caco-2 cells and rat gut sacs. Materials and methods In Caco-2 cell experiments, the effects of baicalin and baicalein on P-gp activity were investigated using a P-gp substrate, rhodamine 123 and non-substrate fluorescein Na, by determining their intracellular fluorescence accumulation, and their effects on P-gp expression were determined using flow cytometry. In addition, rat gut sac model was selected to investigate the effects of baicalin and baicalein on the transport of verapamil, a classical P-gp substrate. The gut sacs of male Sprague-Dawley rats were filled with 0.4 mL the test solution contained verapamil (0.2575 mg/mL) and the drugs [baicalin and baicalein, at concentrations of 1/8 IC50 (59.875, 41.5 μg/mL), 1/4 IC50 (119.75, 83 μg/mL) and 1/2 IC50 (239.5, 166 μg/mL)], a...Continue Reading

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Citations

Mar 16, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Keumhan NohTae Cheon Jeong
Jun 23, 2016·Pharmaceutical Biology·Kaiyou WangJixiao Lang
Jan 22, 2019·The Journal of Pharmacy and Pharmacology·Xin TianXiaojian Zhang
Oct 17, 2020·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Camila Juliana DomínguezAldo Domingo Mottino
Feb 23, 2020·Drug Resistance Updates : Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy·Sabrina DallavalleRoberta Fruttero

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