The impact of hydroquinone on acetylcholine esterase and certain human carbonic anhydrase isoenzymes (hCA I, II, IX, and XII)

Abstract

Carbonic anhydrases (CAs) are widespread and the most studied members of a great family of metalloenzymes in higher vertebrates including humans. CAs were investigated for their inhibition of all of the catalytically active mammalian isozymes of the Zn 2+

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

“…CAIs have lately emerged that CAIs could have potential as anticancer, anti-obesity and anti-infective drugs 29 . Phenolic and polyphenolic compounds have a lot of biological activities in fact been evaluated as CAIs by our group earlier, being shown that many such derivatives are potent inhibitors of several physiologically relevant isoforms, such as CA IX and XII 4,6,12,17,29 . They may constitute interesting lead molecules for identifying novel CAIs.…”

“…Carbonic anhydrases (CAs, EC 4.2.1.1) are zinc-containing metalloenzymes that catalyse the reversible hydration of carbon dioxide (CO 2 ) in a two-step reaction, to yield bicarbonate (HCO 3 À ) and protons (H + ) 5 . CO 2 , HCO 3 À and H + are essential molecules or ions in many important physiologic processes in all life kingdoms, throughout the tree of life and for this reason, relatively high amounts of CAs are present in different tissues or cell compartments of most investigated organisms 6 .…”

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

“…Human carbonic anhydrase isoenzymes (hCA I and II) and acetylcholine esterase (AChE) inhibition profile of carbamate derivatives (10)(11)(12)(13)(14)(15)(16) …”

“…The synthesis of methyl 4,6-dimethoxy-2,3-dihydro-1H-indene-2-carboxylate (6) (5) was synthesized according to the literature procedure 13 . Compound 5 (1.0 g, 4.0 mmol) was dissolved in TFA (6.12 mL, 79.92 mmol).…”

“…This conversion reaction is very slow and should be speed up somehow. Carbonic anhydrase (CA, EC 4.2.1.1) catalyzes this reaction with typical catalytic rates of the different forms of this enzyme ranging between 10 4 and 10 6 reactions per second [13][14][15][16][17][18] . Carbonic anhydrases are mainly Zn 2+ containing metalloenzymes that catalyze the reversible interconversion of CO 2 and H 2 O to HCO 3 À and a proton (H + ) for the hydration reaction or consumes one equivalent of H + for the dehydration reaction [15][16][17][18][19][20] .…”