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In Vitro Effects of Some Flavones on Human Pyruvate Kinase Isoenzyme M2
Author(s) -
Aslan Erdem,
Adem Sevki
Publication year - 2015
Publication title -
journal of biochemical and molecular toxicology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.526
H-Index - 58
eISSN - 1099-0461
pISSN - 1095-6670
DOI - 10.1002/jbt.21673
Subject(s) - baicalein , flavones , apigenin , chemistry , pkm2 , luteolin , scutellarin , biochemistry , pharmacology , pyruvate kinase , flavanone , in vitro , enzyme , wogonin , scutellaria baicalensis , flavonoid , medicine , glycolysis , alternative medicine , chromatography , traditional chinese medicine , pathology , antioxidant
PKM2 is an important target for designing anticancer drug. Inhibitors and activators of this enzyme are suitable molecules for use in treating cancer. The aim of the present study was to investigate the effect of certain flavones on PKM2. Apigenin, wogonin, flavone, 3‐hydroxyflavone, 5‐hydroxyflavone, 6‐hydroxyflavone, and 7‐hydroxyflavone effectively inhibited PKM2, with IC 50 in the range of 0.99–2.120 μM. The kinetic study indicated that these compounds acted as noncompetitive with K i values of 3.53–5.67 μM toward phosphoenolpyruvate. Scutellarin and tangeritin demonstrated strong activation effect with AC 50 values < 2 μM. Diosmetin, baicalin, baicalein, and luteolin showed an intermediate‐level activator effect. These results demonstrate that flavone and their analogs could serve as leading compounds to develop new potent and selective inhibitor and activator for PKM2.