The determination of the carbonic anhydrases activators in vitro effect of mixed donor crown ethers

J Biochem Mol Toxicol. 2018 Mar;32(3):e22032. doi: 10.1002/jbt.22032. Epub 2018 Jan 12.

Abstract

Carbonic anhydrases (CAs) play an important function in various physiological and pathological processes. Therefore, many researchers work in this field in order to design and synthesize new drugs. Both inhibitors and activators of CAs, which are associated with the diagnosis and treatment of many diseases, are very important. The emergence of the use of CA activators in the treatment of Alzheimer has led many scholars to work on this issue. In this study, CA activators and inhibitors are determined. The crown ethers compounds (1, 2, 3, 6, 7, 8, and 9) were found to cause activation on enzyme activities of hCA I and II. The AC50 values on hCA I and II of the compounds are in the range of 4.6565-374.979 μM. The 4 (IC50 ; 1.301 and 3.215 μM for hCA I and II) and 5 (IC50 ; 73.96 and 378.5 μM for hCA I and II) compounds were found to cause inhibition on enzyme activities of hCA I and II.

Keywords: activation; carbonic anhydrase; inhibition; mixed donor crown ether.

MeSH terms

  • Carbonic Anhydrase I / chemistry*
  • Carbonic Anhydrase II / chemistry*
  • Enzyme Activators / chemistry*
  • Ethers
  • Humans

Substances

  • Enzyme Activators
  • Ethers
  • Carbonic Anhydrase I
  • Carbonic Anhydrase II