Analysis of saponins and phenolic compounds as inhibitors of alpha-carbonic anhydrase isoenzymes

Koz O., EKİNCİ D., Perrone A., Piacente S., Alankus-Caliskan O., BEDİR E., ...Daha Fazla

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.28, sa.2, ss.412-417, 2013 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 28 Sayı: 2
  • Basım Tarihi: 2013
  • Doi Numarası: 10.3109/14756366.2011.651464
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.412-417
  • Anahtar Kelimeler: Carbonic anhydrase, inhibition, natural phenolics, saponins, ISOZYME-II, THERAPEUTIC APPLICATIONS, IN-VITRO, PURIFICATION, ENZYME, ANTIOXIDANT, BINDING, METALS, DESIGN, EMATE
  • Ondokuz Mayıs Üniversitesi Adresli: Evet

Özet

A series of phenolic and saponin type natural products such as quercetin, rutin, catechin, epicatechin, silymarin, trojanoside H, astragaloside IV, astragaloside VIII and astrasieversianin X, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). We here report inhibitory effects of these compounds against five alpha-CA isozymes (hCA I, hCA II, bCA III, hCA IV and hCA VI). Most of the phenolic and saponin type compounds inhibited the isoenzymes quite effectively at low micromolar K-i-s ranging between 0.1 and 4 mu M, whereas a few derivatives were ineffective (K-i-s > 100 mu M). The results were remarkable which might lead to design of novel CAIs with a diverse inhibition mechanism compared to sulfonamide/sulfamate inhibitors.