Synthesis and Biological Evaluation of Flavonoids as Antiacetyl- cholinesterase Agent

Saleh Nazifi Ibrahim, Farediah Ahmad
2014 Jurnal Teknologi  
A series of chalcones, a flavone and one flavanone were synthesized and elucidated structurally by IR and 1 H NMR spectroscopies. The synthetic compounds were then screened for acetylcholinesterase inhibitory activity using thin layer chromatography (TLC) and microplate assays. In the TLC assay, only 2′-hydroxy-4-methoxychalcone and 2′-hydroxy-4′-O-prenyl-2,6-dichlorochalcone were found to show moderate and weak activity respectively against acetylcholinesterase (AchE) at 0.1 mM concentration
more » ... mpared to the control galanthamine. 4′-Hydroxy-2,6-dichlorochalcone, 2′-hydroxy-4-nitrochalcone, 2′-hydroxy-4-(dimethyl)aminochalcone and 2′-hydroxy-4-methoxychalcone showed moderate AchE inhibitory activity with percentage inhibition of 54.24, 46.14 and 49.32 % respectively in the microplate assay. Abstrak Satu siri kalkon, satu flavon dan flavanon telah disintesis dan strukturnya dikenal pasti melalui spektroskopi IR dan 1 H NMR. Semua sebatian yang telah disintesis disaring untuk cerakin rencatan asetilkolinesterase menggunakan kromatografi lapisan nipis (TLC) dan plat mikro. Dalam cerakin TLC, hanya 2′-hidroksi-4metoksikalkon dan 2′-hidroksi-4′-O-prenil-2,6-diklorokalkon masing-masing mempamerkan aktiviti sederhana dan lemah terhadap asetilkolinesterase (AchE) pada kepekatan 0.1 mM berbanding kawalan galantamina. 4′-Hidroksi-2,6-diklorokalkon, 2′-hidroksi-4-nitrokalkon, 2′-hidroksi-4-(dimetil)aminokalkon dan 2′-hidroksi-4-metoksikalkon menunjukkan rencatan AchE sederhana masingmasing dengan peratus rencatan 54.24, 46.14 dan 49.32% dalam cerakin plat mikro.
doi:10.11113/jt.v69.2588 fatcat:ussqcnu4sfe3ti6pc44odx2hym