Multiple ABC Transporters Efflux Baicalin

Bernadett Kalapos-Kovács, Balázs Magda, Márton Jani, Zsolt Fekete, P. Szabó, I. Antal, Péter Krajcsi, I. Klebovich

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

Baicalein, the aglycone formed by hydrolysis of baicalin in the intestine, is well absorbed by passive diffusion but subjected to extensive intestinal glucuronidation. Efflux of baicalin, the low passive permeability glucuronide of baicalein from enterocytes, likely depends on a carrier-mediated transport. The present study was designed to explore potential drug-herb interaction by investigating the inhibitory effect of baicalin on the transport of reporter substrates by transporters and to identify the transporters responsible for the efflux of baicalin from enterocytes and hepatocytes. The interaction of baicalin with specific ABC transporters was studied using membranes from cells overexpressing human BCRP, MDR1, MRP2, MRP3 and MRP4. Baicalin was tested for its potential to inhibit vesicular transport by these transporters. The transport of baicalin by the selected transporters was also investigated. Transport by BCRP, MRP3 and MRP4 was inhibited by baicalin with an IC50 of 3.41 ± 1.83 μM, 14.01 ± 2.51 μM and 14.39 ± 5.69 μM respectively. Inhibition of MDR1 (IC50 = 94.84 ± 31.10 μM) and MRP2 (IC50 = 210.13 ± 110.49 μM) was less potent. MRP2 and BCRP are the apical transporters of baicalin that may mediate luminal efflux in enterocytes and biliary efflux in hepatocytes. The basolateral efflux of baicalin is likely mediated by MRP3 and MRP4 both in enterocytes and hepatocytes. Via inhibition of transport by ABC transporters, baicalin could interfere with the absorption and disposition of drugs.

Original languageEnglish
Pages (from-to)1987-1990
Number of pages4
JournalPhytotherapy Research
Volume29
Issue number12
DOIs
Publication statusPublished - Dec 1 2015

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ATP-Binding Cassette Transporters
Enterocytes
Inhibitory Concentration 50
Hepatocytes
baicalin
Herb-Drug Interactions
Glucuronides
Intestines
Permeability
Hydrolysis
Cell Membrane

Keywords

  • ABC transporters
  • baicalin
  • BCRP
  • MDR1
  • MRP

ASJC Scopus subject areas

  • Pharmacology

Cite this

Multiple ABC Transporters Efflux Baicalin. / Kalapos-Kovács, Bernadett; Magda, Balázs; Jani, Márton; Fekete, Zsolt; Szabó, P.; Antal, I.; Krajcsi, Péter; Klebovich, I.

In: Phytotherapy Research, Vol. 29, No. 12, 01.12.2015, p. 1987-1990.

Research output: Contribution to journalArticle

Kalapos-Kovács, B, Magda, B, Jani, M, Fekete, Z, Szabó, P, Antal, I, Krajcsi, P & Klebovich, I 2015, 'Multiple ABC Transporters Efflux Baicalin', Phytotherapy Research, vol. 29, no. 12, pp. 1987-1990. https://doi.org/10.1002/ptr.5477
Kalapos-Kovács B, Magda B, Jani M, Fekete Z, Szabó P, Antal I et al. Multiple ABC Transporters Efflux Baicalin. Phytotherapy Research. 2015 Dec 1;29(12):1987-1990. https://doi.org/10.1002/ptr.5477
Kalapos-Kovács, Bernadett ; Magda, Balázs ; Jani, Márton ; Fekete, Zsolt ; Szabó, P. ; Antal, I. ; Krajcsi, Péter ; Klebovich, I. / Multiple ABC Transporters Efflux Baicalin. In: Phytotherapy Research. 2015 ; Vol. 29, No. 12. pp. 1987-1990.
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