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

WOS: 000314531000027PubMed ID: 22299585A 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.FP7 EU grant (Metoxia)European Union (EU)This study was financed by an FP7 EU grant (Metoxia) to CTS