(3,4-Dihydroxyphenyl)(2,3,4-trihydroxyphenyl)methanone and its derivatives as carbonic anhydrase isoenzymes inhibitors

Rosmarinic acid inhibits some metabolic enzymes including glutathioneS-transferase, lactoperoxidase, acetylcholinesterase, butyrylcholinesterase and carbonic anhydrase isoenzymes

“…The hydrolysis of both substrates was monitored spectrophotometrically by formation of the yellow 5-thio-2-nitrobenzoate anion as the result of the reaction of DTNB with thiocholine, released by enzymatic hydrolysis of AChI/BChI, with absorption maximum at a wavelength of 412 nm 19 . CNBr-activated-sepharose 4B was used for the purification of LPO from bovine milk 20 . LPO purity was checked by sodium dodecyl sulphate polyacrylamide gel electrophoresis (SDS-PAGE) 21 .…”

Synthesis of N-alkyl (aril)-tetra pyrimidine thiones and investigation of their human carbonic anhydrase I and II inhibitory effects

“…A single band was observed for each hCA isoenzyme. Both CA isoenzymes activities were determined in accordance with the method of Verpoorte et al 77 described previously 47,49 . The increasing absorbance at 348 nm of p-nitrophenylacetate (NPA) to p-nitrophenolate (NP) was recorded during a short period (3 minutes) at 25 C using a spectrophotometer (Shimadzu, UV-VIS Spectrophotometer, UVmini-1240).…”

“…Two cytosolic human CA isoforms (hCA I, and II) are widespread throughout the human body and are drug targets for clinically used diuretics, anticonvulsants and antiglaucoma drugs [38][39][40][41][42] . Five of the vertebrate CA isoforms are cytosolic (CA I, II, III, VII and XIII), some others (CA IV, IX, XII, XIV and XV) are membrane bound, two isoenzymes (CA VA and VB) are mitochondrial, and one isoform (CA VI) is secreted in saliva [43][44][45][46][47][48] . It was recently reported that CA XV isoform is not expressed in humans or in living primates.…”

“…Sepharose-4B-L tyrosine-sulphanilamide affinity gel was prepared and used according to the previous studies 47,63 . At the outset, the pH of the homogenate was adjusted to 8.7 using solid Tris(hydroxymethyl)aminomethane.…”

Synthesis and inhibitory properties of some carbamates on carbonic anhydrase and acetylcholine esterase

“…Human CAs (hCAs) all belongs to the a-family and so far 16 different CA isoforms discovered in this class [32][33][34] . In humans, CAs are dispersed in different tissues including the reproductive tract, the gastrointestinal tract, kidneys, the nervous system, skin, eyes, lungs, and among some others [35][36][37][38] . Carbonic anhydrase isoenzymes contain a zinc ion (Zn 2+ ) in their active site, coordinated by three His residues and a H 2 O molecule/hydroxide ion (ÀOH) in the a-and g-CAs or by two Cys and one His residues (in the b class), with the fourth ligand being a H 2 O molecule/ÀOH ion acting as nucleophile in the catalyzed reactions [39][40][41][42][43] .…”