Analysis of saponins and phenolic compounds as inhibitors of ?-carbonic anhydrase isoenzymes
Küçük Resim Yok
Tarih
2014
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Informa Healthcare
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 ?-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 KI-s ranging between 0.1 and 4 µM, whereas a few derivatives were ineffective (KI-s > 100 µM). The results were remarkable which might lead to design of novel CAIs with a diverse inhibition mechanism compared to sulfonamide/sulfamate inhibitors. © 2013 Informa UK, Ltd.
Açıklama
Anahtar Kelimeler
Carbonic anhydrase, Inhibition, Natural phenolics, Saponins
Kaynak
Journal of Enzyme Inhibition and Medicinal Chemistry
WoS Q Değeri
Scopus Q Değeri
Q1
Cilt
28
Sayı
2
