Abstract:
:Naringin, as a component universal existing in the peel of some fruits or medicinal plants, was usually selected as the material to synthesise bioactive derivates since it was easy to gain with low cost. In present investigation, eight new acacetin-7-O-methyl ether Mannich base derivatives (1-8) were synthesised from naringin. The bioactivity evaluation revealed that most of them exhibited moderate or potent acetylcholinesterase (AChE) inhibitory activity. Among them, compound 7 (IC50 for AChE = 0.82 ± 0.08 μmol•L-1, IC50 for BuChE = 46.30 ± 3.26 μmol•L-1) showed a potent activity and high selectivity compared with the positive control Rivastigmine (IC50 for AChE = 10.54 ± 0.86 μmol•L-1, IC50 for BuChE = 0.26 ± 0.08 μmol•L-1). The kinetic study suggested that compound 7 bind to AChE with mix-type inhibitory profile. Molecular docking study revealed that compound 7 could combine both catalytic active site (CAS) and peripheral active site (PAS) of AChE with four points (Trp84, Trp279, Tyr70 and Phe330), while it could bind with BuChE via only His 20.
journal_name
Nat Prod Resjournal_title
Natural product researchauthors
Liu HR,Men X,Gao XH,Liu LB,Fan HQ,Xia XH,Wang QAdoi
10.1080/14786419.2017.1340280subject
Has Abstractpub_date
2018-03-01 00:00:00pages
743-747issue
6eissn
1478-6419issn
1478-6427journal_volume
32pub_type
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