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ASSESSMENTS OF CEANOTHANES TRITERPENES AS CHOLINESTERASE INHIBITORS: AN INVESTIGATION OF POTENTIAL AGENTS WITH NOVEL INSPIRATION FOR DRUG TREATMENT OF NEURODEGENERATIVE DISEASES

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dc.creatorEVELYN DEL PILAR MUÑOZ NÚÑEZ
dc.creatorSOLEDAD MARGARITA QUIROZ CARREÑO
dc.creatorEDGAR RAFAEL PASTENE NAVARRETE
dc.creatorCARLOS LEONARDO ARMANDO CÉSPEDES ACUÑA
dc.creatorJULIO ENRIQUE ILDEFONSO ALARCÓN ENOS
dc.date2022
dc.date.accessioned2025-01-10T15:32:25Z
dc.date.available2025-01-10T15:32:25Z
dc.date.issued2022
dc.description.abstractTHE PURPOSE OF THIS STUDY WAS TO DETERMINE THE INHIBITORY CAPACITY OF CEANOTHANES TRITERPENES ISOLATE FROM CHILEAN RHAMNACEAE ON ACETYLCHOLINESTERASE (ACHE) AND BUTYRYLCHOLINESTERASE (BCHE) ENZYMES. SEVEN CEANOTHANES TRITERPENES WERE ISOLATED FROM AERIAL PARTS OF PLANT MATERIAL BY CLASSICAL PHYTOCHEMICAL METHODS OR PREPARED BY THE HEMISYNTHETIC METHOD. STRUCTURES WERE DETERMINED BY THE SPECTROSCOPIC METHOD (1H-NMR AND 13C NMR) AND MASS SPECTROMETRY (MS). ACHE AND BCHE ACTIVITY WERE DETERMINED BY THE ELLMANN METHOD FOR ALL COMPOUNDS. ALL TESTED COMPOUNDS EXERTED A GREATER AFFINITY TO ACHE THAN TO BCHE, WHERE COMPOUND 3 HAS AN IC50 OF 0.126 UM FOR ACHE AND OF >500 UM TO BCHE. KINETIC STUDIES INDICATED THAT ITS INHIBITION WAS COMPETITIVE AND REVERSIBLE. ACCORDING TO THE MOLECULAR COUPLING AND DISPLACEMENT STUDIES OF THE PROPIDIUM IODIDE TEST, THE INHIBITORY EFFECT OF COMPOUND 3 WOULD BE PRODUCED BY INTERACTION WITH THE PERIPHERAL ANIONIC SITE (PAS) OF ACHE. THE COMPOUNDS TESTED (1?7) SHOWED AN IMPORTANT INHIBITORY ACTIVITY OF ACHE, BINDING TO PAS. THEREFORE, INHIBITORS THAT BIND TO PAS WOULD PREVENT THE FORMATION OF THE ACHE-A? COMPLEX, CONSTITUTING A NEW ALTERNATIVE IN THE TREATMENT OF ALZHEIMER?S DISEASE (AD).
dc.formatapplication/pdf
dc.identifier.doi10.3390/metabo12070668
dc.identifier.issn2218-1989
dc.identifier.urihttps://repositorio.ubiobio.cl/handle/123456789/12495
dc.languagespa
dc.publisherMETABOLITES
dc.relation.uri10.3390/metabo12070668
dc.rightsPUBLICADA
dc.subjectMOLECULAR DOCKING
dc.subjectCEANOTHANE TRITERPENE
dc.subjectACETYLCHOLINESTERASE INHIBITOR
dc.titleASSESSMENTS OF CEANOTHANES TRITERPENES AS CHOLINESTERASE INHIBITORS: AN INVESTIGATION OF POTENTIAL AGENTS WITH NOVEL INSPIRATION FOR DRUG TREATMENT OF NEURODEGENERATIVE DISEASES
dc.typeARTÍCULO
dspace.entity.typePublication
ubb.EstadoPUBLICADA
ubb.Otra ReparticionDEPARTAMENTO DE CIENCIAS BASICAS
ubb.Otra ReparticionDEPARTAMENTO DE CIENCIAS BASICAS
ubb.Otra ReparticionDEPARTAMENTO DE CIENCIAS BASICAS
ubb.Otra ReparticionDEPARTAMENTO DE CIENCIAS BASICAS
ubb.Otra ReparticionDEPARTAMENTO DE CIENCIAS BASICAS
ubb.SedeCHILLÁN
ubb.SedeCHILLÁN
ubb.SedeCHILLÁN
ubb.SedeCHILLÁN
ubb.SedeCHILLÁN
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