Inhibition of mammalian carbonic anhydrase isoforms I, II and VI with thiamine and thiamine-like molecules

Abstract

Here we determined the in vitro inhibitory effects of 5-(2-hydroxyethyl)-3,4-dimethylthiazolium iodide (1), 3-Benzyl-5-(2-hydroxyethyl)-4-methylthiazolium chloride (2) and thiamine (3) on human erythrocyte carbonic anhydrase I, II isozymes (hCA I and hCA II) and secreted isoenzyme CA VI. K_I values ranged from 0.38 to 2.27 µM for hCA I, 0.085 to 0.784 µM for hCA II and 0.062 to 0.593 µM for hCA VI, respectively. The compounds displayed relatively strong actions on hCA II, in the same range as the clinically used sulfonamidesethoxzolamide, zonisamide and acetazolamide.

Keywords::

• Carbonic anhydrase
• thiamine
• inhibition

Acknowledgement

The authors thank to Prof. Claudiu T. supuran for several helpful publications on CA inhibitors.

Declaration of interest

The authors report no conflicts of interest.