UPSI Digital Repository (UDRep)
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UPSI Digital Repository (UDRep)
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| Abstract : Universiti Pendidikan Sultan Idris |
| Intensive investigation of phytochemicals from edible Melicope glabra leaves provided a series of O-alkylated quercetins (1?13). The quercetin 1 bearing prenyl and methyl motif showed potent inhibition to human acetylcholinesterase (hAChE) with mixed type I mode, while quercetin was inactive. The position of methyl group was also a critical factor to hAChE inhibition: 1 (4?-O-methyl, IC50 = 12.7 ?M) vs 2 (3?-O-methyl, IC50 = 119 ?M). Inhibitory potency was doubly confirmed with the binding affinity (KSV) based on fluorescence quenching. O-Methyl groups on quercetin were observed to influence ?-secretase (BACE1) inhibition. Thus, O-methylated quercetins (4?6) displayed potential inhibitions against BACE1 with IC50 values of 1.3, 4.1, and 14.1 ?M, respectively. All compounds (3?6) have noncompetitive mode to BACE1. Additionally, all quercetin derivatives (1?13) had antioxidant potentials against different radical sources (ABTS, ORAC and FRAP). The UPLC-ESI-Q-TOF/MS indicated that the leaves part had promising metabolites towards hAChE and BACE1 inhibitions, which are the most predominant phytochemicals. ? 2021 The Authors |
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