Transport of 3-bromopyruvate across the human erythrocyte membrane

摘要: 3-Bromopyruvic acid (3-BP) is a promising anticancer compound because it 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 therapy with 3-BP side effects due to its interaction cells, erythrocytes. Transport into critical for have intracellular effects. aim our study was the kinetic characterization transport human uptake by erythrocytes linear within first 3 min and pH-dependent. rate decreased increasing pH in range 6.0–8.0. Km Vm values were 0.89 mM 0.94 mmol/(l x min), respectively. inhibited competitively pyruvate significantly DIDS, SITS, 1-cyano-4-hydroxycinnamic acid. Flavonoids also transport: most potent inhibition found luteolin quercetin.