- Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV.
Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV.
Bioorganic & medicinal chemistry letters (2010-08-03)
Alessio Innocenti, Ilhami Gülçin, Andrea Scozzafava, Claudiu T Supuran
PMID20674354
ABSTRACT
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 microM. 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.
MATERIALS
Product Number
Brand
Product Description
Sigma-Aldrich
Phenol, puriss., meets analytical specification of Ph. Eur., BP, USP, 99.5-100.5% (GC)
Sigma-Aldrich
Phenol, puriss., ≥99.5% (GC), meets analytical specification of Ph. Eur., BP, USP, crystalline (detached)
Sigma-Aldrich
Phenol, contains hypophosphorous as stabilizer, loose crystals, ACS reagent, ≥99.0%
Sigma-Aldrich
Phenol solution, BioReagent, Saturated with 0.01 M citrate buffer, pH 4.3 ± 0.2, for molecular biology
Sigma-Aldrich
Phenol solution, BioReagent, Equilibrated with 10 mM Tris HCl, pH 8.0, 1 mM EDTA, for molecular biology