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Inhibition effect of flavonoids on monocarboxylate transporter 1 (MCT1) in Caco-2 cells

Chang-Koo Shim1, Eun-Pa Cheon, Keon Wook Kang

  • 1National Research Laboratory of Transporters Targeted Drug Design, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 151-742, Korea.

The Journal of Pharmacy and Pharmacology
|November 3, 2007
PubMed

Insights

Flavonoids like naringenin and silybin competitively inhibit monocarboxylate transporter 1 (MCT1), impacting benzoic acid uptake in cells. This suggests potential diet-drug interactions involving flavonoids and MCT1 substrates.

Area of Science:

  • Pharmacology
  • Cell Biology
  • Nutraceuticals

Background:

  • Monocarboxylate transporter 1 (MCT1) plays a crucial role in transporting various substrates, including drugs and nutrients.
  • Flavonoids are plant-derived compounds with diverse biological activities, including potential interactions with cellular transporters.

Purpose of the Study:

  • To investigate the inhibitory effects of specific flavonoids on monocarboxylate transporter 1 (MCT1) activity.
  • To examine the impact of flavonoids on benzoic acid cellular uptake in Caco-2 cells.

Main Methods:

  • Caco-2 cell model used to assess cellular uptake of [(14)C]-benzoic acid in the presence of various flavonoids.
  • Enzyme kinetics and RT-PCR were employed to determine inhibition mechanisms and gene expression levels.
  • Western blot analysis was performed to evaluate MCT1 protein expression.

Main Results:

  • Naringenin, morin, silybin, and quercetin significantly inhibited [(14)C]-benzoic acid uptake in Caco-2 cells.
  • Naringenin and silybin demonstrated potent competitive inhibition of MCT1 with low IC50 and Ki values.
  • Flavonoid treatment did not alter MCT1 gene or protein expression levels.

Conclusions:

  • Certain flavonoids act as competitive inhibitors of MCT1, affecting the transport of its substrates.
  • The findings highlight the potential for diet-drug interactions between dietary flavonoids and medications that utilize MCT1 for absorption or distribution.

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