The behavior of some chalcones on acetylcholinesterase and carbonic anhydrase activity

被引：65

作者：

Aslan, Hatice Esra ^{[1
]}

Demir, Yeliz ^{[1
]}

ozaslan, Muhammet Serhat ^{[1
]}

Turkan, Fikret ^{[2
]}

Beydemir, Sukru ^{[3
]}

Kufrevioglu, Omer Irfan ^{[1
]}

机构：

[1] Ataturk Univ, Dept Chem, Fac Sci, Erzurum, Turkey

[2] Igdir Univ, Hlth Serv Vocat Sch, Igdir, Turkey

[3] Anadolu Univ, Dept Biochem, Fac Pharm, Eskisehir, Turkey

来源：

DRUG AND CHEMICAL TOXICOLOGY | 2019年 / 42卷 / 06期

关键词：

Acetylcholinesterase; carbonic anhydrase; chalcone; inhibition; purification;

D O I：

10.1080/01480545.2018.1463242

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Carbonic anhydrase (CA) has a key role in respiration, carbon dioxide and bicarbonate transport. Acetylcholinesterase (AChE) is a serine hydrolase and mostly abundant at neuromuscular junctions and cholinergic brain synapses. Inhibitors of these enzymes could aid in illuminating the role in disease processes. In this study, we separately purified CA I and CA II from human erythrocytes. The purity of the enzymes was showed by SDS-PAGE analysis. We also investigated the inhibition of seven chalcones toward hCA I, hCA II, and AChE. The chalcones were effective inhibitors of the cytosolic CA isoforms (hCA I and hCA II) and AChE with K-i values in the range of 1.83-7.05 mu M for hCA I, 0.59-5.50 mu M for hCA II, and 0.61-86.11 mu M for AChE. All compounds were showed competitive inhibition aganist both enzymes. These compounds can be a potent inhibitor of AChE enzyme and both cytosolic CA isoenzymes which are commonly used in the pharmaceutical and medical industries.

引用

页码：634 / 640

页数：7

共 51 条

[1] Akincioglu A., Et al., Discovery of potent carbonic anhydrase and acetylcholine esterase inhibitors: novel sulfamoylcarbamates and sulfamides derived from acetophenones, Bioorganic & Medicinal Chemistry, 23, pp. 3592-3602, (2015)
[2] Aktas A., Et al., Novel NHC precursors: synthesis, characterization, and carbonic anhydrase and acetylcholinesterase inhibitory properties, Archiv Der Pharmazie, 350, 6, (2017)
[3] Aslan H.E., Beydemir S., Phenolic compounds: the inhibition effect on polyol pathway enzymes, Chemico-Biological Interactions, 266, pp. 47-55, (2017)
[4] Balseven H., Et al., Facile synthesis and characterization of novel pyrazole-sulfonamides and their inhibition effects on human carbonic anhydrase isoenzymes, Bioorganic & Medicinal Chemistry, 21, pp. 21-27, (2013)
[5] Bayrak C., Et al., The first synthesis of 4-phenylbutenone derivative bromophenols including natural products and their inhibition profiles for carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase enzymes, Bioorganic Chemistry, 72, pp. 359-366, (2017)
[6] Beydemir S., Demir Y., Antiepileptic drugs: impacts on human serum paraoxonase-1, Journal of Biochemical and Molecular Toxicology, 31, 6, (2016)
[7] Bradford M.M., A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding, Analytical Biochemistry, 72, pp. 248-254, (1976)
[8] Burmaoglu S., Et al., Synthesis and biological evaluation of phloroglucinol derivatives possessing alpha-glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity, Archiv Der Pharmazie, 351, 2, (2018)
[9] Cai C.Y., Et al., Analogues of xanthones–chalcones and bis-chalcones as alpha-glucosidase inhibitors and anti-diabetes candidates, European Journal of Medicinal Chemistry, 130, pp. 51-59, (2017)
[10] Cheng J.H., Et al., Synthesis and cytotoxic, anti-inflammatory, and anti-oxidant activities of 2′,5′-dialkoxylchalcones as cancer chemopreventive agents, Bioorganic & Medicinal Chemistry, 16, pp. 7270-7276, (2008)

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