Hydrolyzable Tannins Are Iron Chelators That Inhibit DNA Repair Enzyme ALKBH2
Date of Original Version
Hydrolyzable tannins are a class of polyphenolic compounds commonly found in natural products. In this work, we studied the in vitro inhibitory mechanism of six molecules in this class on ALKBH2, an Fe(II)/α-ketoglutarate-dependent DNA repair enzyme in the AlkB family. We determined the IC50 values of these compounds on the repair of 3-methylcytosine and 1-methyladenine, the prototypical substrates of ALKBH2. A structure-activity relationship was also observed between the strength of inhibition and the number of galloyl moieties in a molecule. In addition, we found that the inhibition by this class of polyphenolic compounds on ALKBH2 is through an iron-chelating mechanism.
Chemical Research in Toxicology
Chen, Fangyi, Qi Tang, Hang Ma, Ke Bian, Navindra P. Seeram, and Deyu Li. "Hydrolyzable Tannins Are Iron Chelators That Inhibit DNA Repair Enzyme ALKBH2." Chemical Research in Toxicology 32, 6 (2019): 1082-1086. doi:10.1021/acs.chemrestox.8b00398.