Analysis of saponins and phenolic compounds as inhibitors of alpha-carbonic anhydrase isoenzymes
Küçük Resim Yok
Tarih
2013
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Taylor & Francis Ltd
Erişim Hakkı
info:eu-repo/semantics/closedAccess
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.
Açıklama
Anahtar Kelimeler
Carbonic anhydrase, inhibition, natural phenolics, saponins
Kaynak
Journal of Enzyme Inhibition and Medicinal Chemistry
WoS Q Değeri
Q3
Scopus Q Değeri
Cilt
28
Sayı
2
