In vitro inhibition of human carbonic anhydrase I and II isozymes with natural phenolic compounds

Senturk M., GÜLÇİN İ., BEYDEMİR Ş., KÜFREVİOĞLU Ö. İ., Supuran C. T.

Chemical Biology and Drug Design, cilt.77, sa.6, ss.494-499, 2011 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 77 Sayı: 6
  • Basım Tarihi: 2011
  • Doi Numarası: 10.1111/j.1747-0285.2011.01104.x
  • Dergi Adı: Chemical Biology and Drug Design
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.494-499
  • Anahtar Kelimeler: Carbonic anhydrase, Enzyme inhibitor, HCA i, HCA ii, Natural phenol
  • Bilecik Şeyh Edebali Üniversitesi Adresli: Evet

Özet

Inhibition of two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I and II with some natural phenolic derivatives was investigated using the esterase assay with 4-nitrophenyl acetate as substrate. Resveratrol, catechin, silymarin, dobutamin, and curcumin showed KI values in the range of 4.47-9.47mm for hCA I and of 2.86-7.44μm against hCA II, respectively. These natural product phenols were generally competitive inhibitors with 4-nitrophenylacetate as substrate. Some natural phenols investigated here showed effective hCA II inhibitory effects, in the same range as the clinically used sulfonamide acetazolamide, and might be used as leads for generating enzyme inhibitors possibly targeting other CA isoforms that have not been yet assayed for their interactions with such agents. © 2011 John Wiley & Sons A/S.