Assessment of Anticholinergic and Antidiabetic Properties of Some Natural and Synthetic Molecules: An In Vitro and In Silico Approach

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Özet

Introduction: This study aimed to determine the in vitro and in silico effects of some natural and synthetic molecules on acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and α-glucosidase enzymes. Background: Alzheimer's disease (AD) and Type II diabetes mellitus (T2DM) are considered the most important diseases of today’s world. However, the side effects of therapeutic agents used in both diseases limit their use. Therefore, developing drugs with high therapeutic efficacy and better pharmacological profile is important. Objectives: This study sets out to determine the related enzyme inhibitors used in treating AD and T2DM, considered amongst the most important diseases of today’s world. Methods: In the current study, the in vitro and in silico effects of dienestrol, hesperetin, L-thyroxine, 3,3',5-Triiodo-L-thyronine (T3) and dobutamine molecules on AChE, BChE and α-glycosidase enzyme activities were investigated. Results: All the molecules showed an inhibitory effect on the enzymes. The IC50 and Ki values of the L-Thyroxine molecule, which showed the strongest inhibition effect for the AChE enzyme, were determined as 1.71 µM and 0.83 ± 0.195 µM, respectively. In addition, dienestrol, T3, and dobutamine molecules showed a more substantial inhibition effect than tacrine. The dobutamine molecule showed the most substantial inhibition effect for the BChE enzyme, and IC50 and Ki values were determined as 1.83 µM and 0.845 ± 0.143 µM, respectively. The IC50 and Ki values for the hesperetin molecule, which showed the strongest inhibition for the α-glycosidase enzyme, were determined as 13.57 µM and 12.33 ± 2.57 µM, respectively. Conclusion: According to the results obtained, the molecules used in the study may be considered potential inhibitor candidates for AChE, BChE and α-glycosidase.

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AlanDeğerDil
dc.contributor.authorÇomaklı, Veysel
dc.contributor.authorAygül, İmdat
dc.contributor.authorSağlamtaş, Rüya
dc.contributor.authorKuzu, Müslüm
dc.contributor.authorDemirdağ, Ramazan
dc.contributor.authorAkincioğlu, Hülya
dc.contributor.authorAdem, Şevki
dc.contributor.authorGülçin, İlhami
dc.date.accessioned2026-10-22T10:20:31.055041226Z
dc.date.available2026-10-22T10:20:31.055041226Z
dc.date.issued2024
dc.description.abstractIntroduction: This study aimed to determine the in vitro and in silico effects of some natural and synthetic molecules on acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and α-glucosidase enzymes. Background: Alzheimer's disease (AD) and Type II diabetes mellitus (T2DM) are considered the most important diseases of today’s world. However, the side effects of therapeutic agents used in both diseases limit their use. Therefore, developing drugs with high therapeutic efficacy and better pharmacological profile is important. Objectives: This study sets out to determine the related enzyme inhibitors used in treating AD and T2DM, considered amongst the most important diseases of today’s world. Methods: In the current study, the in vitro and in silico effects of dienestrol, hesperetin, L-thyroxine, 3,3',5-Triiodo-L-thyronine (T3) and dobutamine molecules on AChE, BChE and α-glycosidase enzyme activities were investigated. Results: All the molecules showed an inhibitory effect on the enzymes. The IC50 and Ki values of the L-Thyroxine molecule, which showed the strongest inhibition effect for the AChE enzyme, were determined as 1.71 µM and 0.83 ± 0.195 µM, respectively. In addition, dienestrol, T3, and dobutamine molecules showed a more substantial inhibition effect than tacrine. The dobutamine molecule showed the most substantial inhibition effect for the BChE enzyme, and IC50 and Ki values were determined as 1.83 µM and 0.845 ± 0.143 µM, respectively. The IC50 and Ki values for the hesperetin molecule, which showed the strongest inhibition for the α-glycosidase enzyme, were determined as 13.57 µM and 12.33 ± 2.57 µM, respectively. Conclusion: According to the results obtained, the molecules used in the study may be considered potential inhibitor candidates for AChE, BChE and α-glycosidase.
dc.identifier.doi10.2174/1573409919666230518151414
dc.identifier.eissn1875-6697
dc.identifier.endpage451
dc.identifier.issn1573-4099
dc.identifier.issue5
dc.identifier.pmid37202895
dc.identifier.scopus2-s2.0-85188289755
dc.identifier.startpage441
dc.identifier.urihttps://rdlopen.rawdatalibrary.net/r/gumushane/12764
dc.identifier.volume20
dc.identifier.wosWOS:001208305200002
dc.language.isoen
dc.publisherBentham Science Publishers
dc.relation.ispartofCurrent Computer-Aided Drug Design
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectacetylcholinesterase
dc.subjectAlzheimer's disease
dc.subjectbutyrylcholin-esterase
dc.subjectinhibition
dc.subjectMolecular modelling
dc.subjecttype II diabetes mellitus
dc.subjectα-glycosidase
dc.subject.classificationChemistry, Medicinal
dc.subject.classificationComputer Science, Interdisciplinary Applications
dc.subject.classificationPharmacology & Pharmacy
dc.subject.classificationComputer Science
dc.subject.otherAcetylcholinesterase
dc.subject.otheralpha-Glucosidases
dc.subject.otherAlzheimer Disease
dc.subject.otherButyrylcholinesterase
dc.subject.otherCholinergic Antagonists
dc.subject.otherCholinesterase Inhibitors
dc.subject.otherComputer Simulation
dc.subject.otherDiabetes Mellitus, Type 2
dc.subject.otherGlycoside Hydrolase Inhibitors
dc.subject.otherHumans
dc.subject.otherHypoglycemic Agents
dc.subject.otherMolecular Docking Simulation
dc.subject.otherDrug interactions
dc.subject.otherEnzyme inhibition
dc.subject.otherFlavonoids
dc.subject.otherNeurodegenerative diseases
dc.subject.otheralpha glucosidase enzyme
dc.subject.othercholinesterase
dc.subject.otherdienestrol
dc.subject.otherdiethylstilbestrol
dc.subject.otherdobutamine
dc.subject.otheresterase
dc.subject.otherglucosidase
dc.subject.otherglycosidase
dc.subject.otherhesperetin
dc.subject.otherliothyronine
dc.subject.othernatural product
dc.subject.otherphytochemical
dc.subject.otherthiocholine
dc.subject.otherthyroxine
dc.subject.otherunclassified drug
dc.subject.otheralpha glucosidase
dc.subject.otherantidiabetic agent
dc.subject.othercholinergic receptor blocking agent
dc.subject.othercholinesterase inhibitor
dc.subject.otherglycosidase inhibitor
dc.subject.otherAlzheimers disease
dc.subject.otherButyrylcholin-esterase
dc.subject.otherDiabetes mellitus
dc.subject.otherGlycosidases
dc.subject.otherInhibition
dc.subject.otherType II
dc.subject.otherType II diabetes mellitu
dc.subject.otherΑ-glycosidase
dc.subject.otheranticholinergic effect
dc.subject.otherantidiabetic activity
dc.subject.otherArticle
dc.subject.otherbiological activity
dc.subject.othercardiovascular disease
dc.subject.othercomputer model
dc.subject.othercrystal structure
dc.subject.otherenzyme activity
dc.subject.otherfood industry
dc.subject.otherhuman
dc.subject.otherIC50
dc.subject.otherin vitro study
dc.subject.otherinsulin release
dc.subject.otherinsulin resistance
dc.subject.othermolecular docking
dc.subject.othermolecule
dc.subject.othernon insulin dependent diabetes mellitus
dc.subject.otherpathogenesis
dc.subject.otherprevalence
dc.subject.otherspectrophotometry
dc.subject.othersynthetic molecule
dc.subject.othertherapy effect
dc.subject.otherchemistry
dc.subject.otherdrug effect
dc.subject.otherdrug therapy
dc.subject.othermetabolism
dc.subject.otherMolecules
dc.titleAssessment of Anticholinergic and Antidiabetic Properties of Some Natural and Synthetic Molecules: An In Vitro and In Silico Approach
dc.typeArticle
dspace.entity.typePublication
rdl.citation.openalex8
rdl.citation.scopus8
rdl.citation.wos7
rdl.departmentDepartment of Nutrition and Dietetics, Gümüşhane University, Gümüşhane, Türkiye
rdl.oa.statusclosed
rdl.sdgSDG03
rdl.source.indexSCOPUS
rdl.source.indexWOS
rdl.source.indexPUBMED
rdl.wos.indexScience Citation Index Expanded (SCI-EXPANDED)