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


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, 2,20 -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 hydrox yanisole (BHA), Trolox, ?-Tocopherol, and butylated hydroxytoluene (BHT) were used as the refer ence 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 ?-Tocopherol demonstrated IC50 values of 10.10, 25.95, 7.059, and 11.31 µg/mL, respectively. When these results evaluated, Coumestrol had simi lar DPPH• -scavenging effect to BHT and lower better than Trolox, BHA and ?-tocopherol. In addition, the inhibition effects of Coumestrol were tested against the metabolic enzymes acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase II (CA II), and ?-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.


Anahtar Kelimeler

Coumestrol, Carbonic anhydrase, α-glycosidase, Acetylcholinesterase, Antioxidant activity, Butyrylcholinesterase, Phenolic compound


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