Abstract:
:Acetylcholinesterase (AChE) inhibitors increase the availability of acetylcholine in central cholinergic synapses and are the most promising drugs currently available for the treatment of Alzheimer's disease (AD). Our screening study indicated that the water fraction of the methanolic extract of Lycopodiella cernua (L.) Pic. Serm. significantly inhibited AChE in vitro. Bioassay-guided fractionation led to the isolation of a new lignan glycoside, lycocernuaside A (12), and fourteen known compounds (1-11 and 13-15). Compound 7 exhibited the most potent AChE inhibitory activity with an IC50 value of 0.23 μM. Compound 15 had the most potent inhibitory activity against BChE and BACE1 with IC50 values of 0.62 and 2.16 μM, respectively. Compounds 4 and 7 showed mixed- and competitive-type AChE inhibition. Compound 7 noncompetitively inhibited BChE whereas 15 showed competitive and 8, 13, and 14 showed mixed-type inhibition. The docking results for complexes with AChE or BChE revealed that inhibitors 4, 7, and 15 stably positioned themselves in several pocket/catalytic domains of the AChE and BChE residues.
journal_name
Chem Biol Interactjournal_title
Chemico-biological interactionsauthors
Hung TM,Lee JS,Chuong NN,Kim JA,Oh SH,Woo MH,Choi JS,Min BSdoi
10.1016/j.cbi.2015.07.008subject
Has Abstractpub_date
2015-10-05 00:00:00pages
74-82eissn
0009-2797issn
1872-7786pii
S0009-2797(15)30022-3journal_volume
240pub_type
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