Multiple studies have been recorded on the synthesis and design of multi‐aim anti‐Alzheimer molecules. Using dual butyrylcholinesterase/acetylcholinesterase inhibitor molecules has attracted more interest in the therapy for Alzheimer’s disease. In this study, a tannic acid compound showed excellent inhibitory effects against acetylcholine esterase (AChE), α‐glycosidase, α‐amylase, and butyrylcholinesterase (BChE). IC50 values of tannic acid obtained 11.9 nM against α‐glycosidase and 3.3 nM against α‐amylase, respectively. In contrast, Ki values were found of 50.96 ± 2.18 μM against AChE and 53.17 ± 4.47 μM against BChE. α‐Glycosidase inhibitor compounds can be utilized as a novel group of antidiabetic drugs. By competitively decreasing glycosidase activity, these inhibitor molecules help to hamper the fast breakdown of sugar molecules and thereby control the blood sugar level.
dc.contributor.author | Kaya, Ruya | |
dc.contributor.author | Taslimi, Parham | |
dc.contributor.author | Naldan, Muhammet Emin | |
dc.contributor.author | Gulçin, İlhami | |
dc.date.accessioned | 2019-04-30T06:44:36Z | |
dc.date.available | 2019-04-30T06:44:36Z | |
dc.date.issued | 2019 | |
dc.identifier.issn | 1875-628X | |
dc.identifier.uri | http://hdl.handle.net/11772/1135 | |
dc.description.abstract | Background: The present paper focuses on the in vitro inhibition of some sedative drugs such as Midazolam, Propofol, Hipnodex, Ketamine, and Pental sodium on acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), and α-glycosidase (α-Gly) enzymes. Methods: These drugs were tested in diverse concentrations, which showed positive effects in vitro AChE, BChE, and α-Gly activities. Ki values were 20.14, 94.93, 636.78, 416.42, and 953.75 µM for AChE, 17.52, 32.03, 88.02, 93.48, and 91.84 µM for BChE, and 10.87, 156.68, 48.21, 37.88, 151.01 µM for α-glycosidase, respectively. Results: An enhancing number of experiential observations show potentially harmful effects of sedative drugs on the extension of brain. Conclusion: Midazolam exhibited effective inhibitory activity compared with the other drugs for these enzymes. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | Bentham Science | en_US |
dc.relation.isversionof | 10.2174/1570180815666180924110023 | en_US |
dc.rights | info:eu-repo/semantics/restrictedAccess | en_US |
dc.subject | Sedative drugs | en_US |
dc.subject | α-glycosidase | en_US |
dc.subject | Acetylcholinesterase | en_US |
dc.subject | Butyrylcholinesterase | en_US |
dc.subject | Enzyme inhibition | en_US |
dc.subject | Propofol | en_US |
dc.subject | Midazolam | en_US |
dc.title | Multiple studies have been recorded on the synthesis and design of multi‐aim anti‐Alzheimer molecules. Using dual butyrylcholinesterase/acetylcholinesterase inhibitor molecules has attracted more interest in the therapy for Alzheimer’s disease. In this study, a tannic acid compound showed excellent inhibitory effects against acetylcholine esterase (AChE), α‐glycosidase, α‐amylase, and butyrylcholinesterase (BChE). IC50 values of tannic acid obtained 11.9 nM against α‐glycosidase and 3.3 nM against α‐amylase, respectively. In contrast, Ki values were found of 50.96 ± 2.18 μM against AChE and 53.17 ± 4.47 μM against BChE. α‐Glycosidase inhibitor compounds can be utilized as a novel group of antidiabetic drugs. By competitively decreasing glycosidase activity, these inhibitor molecules help to hamper the fast breakdown of sugar molecules and thereby control the blood sugar level. | en_US |
dc.type | article | en_US |
dc.relation.journal | Letters in Drug Design & Discovery | en_US |
dc.contributor.department | Bartın Üniversitesi, Fen Fakültesi, Biyoteknoloji Bölümü | en_US |
dc.identifier.volume | 16 | en_US |
dc.identifier.startpage | 592 | en_US |
dc.identifier.endpage | 596 | en_US |
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