Open Access

Transport of 3-bromopyruvate across the human erythrocyte membrane

  • Izabela Sadowska-Bartosz1, 5Email author,
  • Mirosław Soszyński2,
  • Stanisław Ułaszewski3,
  • Young Ko4 and
  • Grzegorz Bartosz1, 2
Cellular & Molecular Biology LettersAn International Journal201419:189

https://doi.org/10.2478/s11658-014-0189-1

Received: 5 October 2013

Accepted: 10 March 2014

Published: 9 April 2014

Abstract

3-Bromopyruvic acid (3-BP) is a promising anticancer compound because it is a strong inhibitor of glycolytic enzymes, especially glyceraldehyde 3-phosphate dehydrogenase. The Warburg effect means that malignant cells are much more dependent on glycolysis than normal cells. Potential complications of anticancer therapy with 3-BP are side effects due to its interaction with normal cells, especially erythrocytes. Transport into cells is critical for 3-BP to have intracellular effects. The aim of our study was the kinetic characterization of 3-BP transport into human erythrocytes. 3-BP uptake by erythrocytes was linear within the first 3 min and pH-dependent. The transport rate decreased with increasing pH in the range of 6.0–8.0. The Km and Vm values for 3-BP transport were 0.89 mM and 0.94 mmol/(l cells x min), respectively. The transport was inhibited competitively by pyruvate and significantly inhibited by DIDS, SITS, and 1-cyano-4-hydroxycinnamic acid. Flavonoids also inhibited 3-BP transport: the most potent inhibition was found for luteolin and quercetin.

Keywords

3-Bromopyruvic acid Erythrocytes Polyphenols Flavonoids Transport Monocarboxylate transporter 1-Cyano-4-hydroxycinnamic acid Luteolin Quercetin

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