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Anticholinesterase potential of flavonols from paper mulberry (Broussonetia papyrifera) and their kinetic studies |
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| Authors: | Hyung Won RyuMarcus J. Curtis-Long Sunin JungIl Yun Jeong Dong Sub KimKyu Young Kang Ki Hun Park |
| Affiliation: | a Division of Applied Life Science (BK21 Program), IALS, GyeongSang National University, Jinju 660-701, Republic of Korea b Graduate Program in Biochemistry and Biophysics, Brandeis University, 415 South Street, Waltham, MA 02453, USA c Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeonbuk 580-185, Republic of Korea |
| Abstract: | It is necessary to develop food additives to help treat chronic disorders like neurodegenerative diseases from medicinal plants. Ethanol extracts of paper mulberry were found to display significant inhibition against cholinesterases, enzymes that are strongly linked with Alzheimer’s disease (AD). The active components were identified as prenylated flavonols (2-4) that inhibited two related human cholinesterases in a dose-dependent manner, with IC50’s ranging between 0.8 and 3.1 μM and between 0.5 and 24.7 μM against human acetylcholinesterase (hAChE) and butylcholinesterase (BChE), respectively. Prenyl groups within these flavonols were found to play a critical role for inhibition because the parent compound 1, quercetin, was inactive (IC50 > 500 μM) towards the target enzymes. Flavonols (2-4) showed mixed inhibition kinetics as well as slow and time-dependent reversible inhibition toward hAChE. The affinity between protein and inhibitors was investigated using fluorescence quenching. The affinity constants (KSA) of inhibitors increased in proportion to their inhibitory potencies. |
| Keywords: | Human acetylcholinesterase Butylcholinesterase Time-dependent inhibitor Fluorescence quenching Broussonetia papyrifera |
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