Screening of Carbonic Anhydrase, Acetylcholinesterase, Butyrylcholinesterase, and α-Glycosidase Enzyme Inhibition Effects and Antioxidant Activity of Coumestrol

Abstract

Coumestrol (3,9-dihydroxy-6-benzofuran [3,2-c] chromenone) as a phytoestrogen and polyphenolic compound is a member of the Coumestans family and is quite common in plants. In this study, antiglaucoma, antidiabetic, anticholinergic, and antioxidant effects of Coumestrol were evaluated and compared with standards. To determine the antioxidant activity of coumestrol, several methods—namely N,N-dimethyl-p-phenylenediamine dihydrochloride radical (DMPD•+)-scavenging activity, 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulphonate) radical (ABTS•+)-scavenging activity, 1,1-diphenyl-2-picrylhydrazyl radical (DPPH•)-scavenging activity, potassium ferric cyanide reduction ability, and cupric ion (Cu2+)-reducing activity—were performed. Butylated hydroxyanisole (BHA), Trolox, α-Tocopherol, and butylated hydroxytoluene (BHT) were used as the reference antioxidants for comparison. Coumestrol scavenged the DPPH radical with an IC50 value of 25.95 μg/mL (r2: 0.9005) while BHA, BHT, Trolox, and α-Tocopherol demonstrated IC50 values of 10.10, 25.95, 7.059, and 11.31 μg/mL, respectively. Evaluating these results, Coumestrol had a similar DPPH•-scavenging effect to BHA and Trolox, better than BHT and α-Tocopherol. In addition, the inhibition effects of Coumestrol were tested against the metabolic enzymes acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase II (CA II), and α-glycosidase, which are associated with some global diseases such as Alzheimer’s disease (AD), glaucoma, and diabetes. Coumestrol exhibited Ki values of 10.25 ± 1.94, 5.99 ± 1.79, 25.41 ± 1.10, and 30.56 ± 3.36 nM towards these enzymes, respectively.

The palladium-based complexes bearing 1,3-dibenzylbenzimidazolium with morpholine, triphenylphosphine, and pyridine derivate ligands: synthesis, characterization, structure and enzyme inhibitions

“…Recently, many compounds associated with enzyme inhibition have been evaluated to improve human health and demonstrate the health importance of inhibitors [ 75 , 76 , 77 ]. The synthesized benzimidazolium salt 1 and a series of novel the Palladium-based complexes bearing 1,3-dibenzylbenzimidazolium with morpholine, triphenylphosphine, and pyridine derivate ligands, ( 2 – 6 ), were tested towards cytosolic isoforms hCA I, hCA II and AChE.…”

The combined treatments of brassinolide and zeaxanthin better alleviate oxidative damage and improve hypocotyl length, biomass, and the quality of radish sprouts stored at low temperature

“…The antioxidant capacities included the ferric reducing antioxidant power (FRAP, g kg −1 on a dry weight basis), diphenylpicrylhydrazyl (DPPH, %), and 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS, g kg −1 on a dry weight basis), they were determined with a spectrophotometer at 593 nm, 734 nm, 517 nm, respectively, based on the description of Balaydin et al, 2010 , Durmaz et al, 2022 , and Polat Kose and Gulcin (2021) .…”

Heterocyclic compounds as a magic bullet for diabetes mellitus: a review

“…Also obtained were very effective K i values for chalcone 5c, with a K i value of 8.30 AE 3.80 nM. 204 a-Glycosidase inhibitory action of new chalcone derivatives (5)(6)(7)(8)(9)(10)(11)(12)…”

“…7 DM is linked with dysfunction of the eyes, 8 kidneys, 9 and heart. 10 In broad terms, 11 DM is classified into type-I DM, which is due to the impairment of pancreatic β cells, 11 and type-II DM, 12 due to insulin resistance 13 or by destruction of secreted insulin. 14 Type-II, also known as non-insulin-dependent diabetes mellitus 15 is the most commonly occurring diabetes in 80% of the total affected patients around the world.…”