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2-Arylbenzofurans From Artocarpus Lakoocha and Methyl Ether Analogs With Potent Cholinesterase Inhibitory Activity

2-Arylbenzofurans From Artocarpus Lakoocha and Methyl Ether Analogs With Potent Cholinesterase Inhibitory Activity

Umalee Namdaung, Anan Athipornchai, Thongchai Khammee, Mayuso Kuno, Sunit Suksamrarn

Eur J Med Chem. 2018 Jan 1;143:1301-1311.

PMID: 29126732

Abstract:

In vitro screening for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the Artocarpus lakoocha root-bark extracts revealed interesting results. Bioassay-guided fractionation resulted in the isolation of two new (1 and 2) and six known 2-arylbenzofurans 3-8, along with one stilbenoid 9 and one flavonoid 10. The structures of the isolated compounds were elucidated by UV, IR, 1D- and 2D-NMR and MS spectroscopic data analysis. Compounds 4, 6 and 7 exhibited more potent AChE inhibitory activity (IC50 = 0.87-1.10 μM) than the reference drug, galantamine. Compounds 4, 8 and 9 displayed greater BChE inhibition than the standard drug. The preferential inhibition of BChE over AChE indicated that 4 also showed a promising dual AChE and BChE inhibitor. The synthetic mono-methylated analogs 4a-c and 6a-b were found to be good BChE inhibitors with IC50 values ranging between 0.31 and 1.11 μM. Based on the docking studies, compounds 4 and 6 are well-fitted in the catalytic triad of AChE. Compounds 4 and 6 showed different binding orientations on BChE, and the most potent BChE inhibitor 4 occupied dual binding to both CAS and PAS more efficiently.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP69353215	Galanthamine, Hydrobromide - CAS 69353-21-5		69353-21-5	Price

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