Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV

Innocenti A., Gulcin I., Scozzafava A., SUPURAN C. T.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, cilt.20, sa.17, ss.5050-5053, 2010 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 20 Sayı: 17
  • Basım Tarihi: 2010
  • Doi Numarası: 10.1016/j.bmcl.2010.07.038
  • Dergi Adı: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.5050-5053
  • Anahtar Kelimeler: Carbonic anhydrase, Polyphenol, Resveratrol, Curcumin, Catechin, Dobutamine, Silymarine, Enzyme inhibitor, Isozymes I-XV, ERYTHROCYTE ISOZYMES I, VITRO ANTIOXIDANT, SALICYLIC-ACID, ACTIVE-SITE, ACTIVATORS, PHENOLS, SERIES, XIV, DERIVATIVES, COUMARINS
  • Atatürk Üniversitesi Adresli: Evet

Özet

A series of polyphenolic derivatives, including resveratrol, dobutamine, curcumin, catechin and silymarine were investigated for the inhibition of all the catalytically active mammalian isozymes of the metalloprotein carbonic anhydrase (CA, EC 4.2.1.1), that is, CA I-CA XV. These polyphenols effectively inhibited CAs, with K(I)s in the range of 380 nM-12.02 mu M. The various isozymes showed quite diverse inhibition profiles with these compounds, which possess scaffolds not present in other investigated CA inhibitors (CAIs). These data may lead to drug design campaigns of effective CAIs possessing a diverse inhibition mechanism compared to sulfonamide/sulfamate inhibitors, based on such less investigated scaffolds. (C) 2010 Elsevier Ltd. All rights reserved.