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1.
Bioorg Chem ; 78: 427-435, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29698893

RESUMO

Three new norditerpenoids alkaloids, 1ß-hydroxy,14ß-acetyl condelphine (1), jadwarine-A (2), jadwarine-B (3) along with two known alkaloids isotalatizidine hydrate (4) and dihydropentagynine (5) were isolated from medicinal plant Delphinium denudatum. The structures of natural products 1-5 were established on the basis of HR-EIMS, 1H and 13C NMR (1D & 2D) spectroscopic data as well as by comparison from literature data. The structures of compound 1 and 4 were also confirmed by single crystal X-ray diffraction studies. In-vitro AChE and BChE enzyme inhibitory activities of compounds 1-5 and molecular docking studies were performed to investigate the possible molecular inhibitory mechanism of the isolated natural products. Compound 2, 4 and 5 showed competitive inhibitory effects by inhibiting AChE and BChE, respectively, while 1 and 3 showed non-competitive inhibition. This work is the first report that provides a supporting evidence about the use of constituents of Delphinium denudatum in cerebral dementia and Alzheimer diseases.


Assuntos
Acetilcolinesterase/metabolismo , Alcaloides/farmacologia , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/farmacologia , Delphinium/química , Diterpenos/farmacologia , Alcaloides/química , Alcaloides/isolamento & purificação , Animais , Inibidores da Colinesterase/química , Inibidores da Colinesterase/isolamento & purificação , Diterpenos/química , Diterpenos/isolamento & purificação , Relação Dose-Resposta a Droga , Electrophorus , Cavalos , Conformação Molecular , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade
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