Phytochemical analysis and anticholinesterase activity of aril of Myristica fragrans Houtt
Arezoo Rastegari, Azadeh Manayi, Mahdi Rezakazemi, Mahdieh Eftekhari, Mahnaz Khanavi, Tahmineh Akbarzadeh, Mina Saeedi
Abstract
Abstract In this study, the ethyl acetate fraction of Myristica fragrans Houtt. was investigated for its in vitro anticholinesterase activity as well as neuroprotectivity against H 2 O 2 -induced cell death in PC12 neuronal cells and the ability to chelate bio-metals (Zn 2+ , Fe 2+ , and Cu 2+ ). The fraction was inactive toward acetylcholinesterase (AChE); however, it inhibited the butyrylcholinesterase (BChE) with IC 50 value of 68.16 µg/mL, compared with donepezil as the reference drug (IC 50 = 1.97 µg/mL) via Ellman’s method. It also showed good percentage of neuroprotection (86.28% at 100 µg/mL) against H 2 O 2 -induced neurotoxicity and moderate metal chelating ability toward Zn 2+ , Fe 2+ , and Cu 2+ . The phytochemical study led to isolation and identification of malabaricone A ( 1 ), malabaricone C ( 2 ), 4-(4-(3,4-dimethoxyphenyl)-2,3-dimethylbutyl)benzene-1,2-diol ( 3 ), nectandrin B ( 4 ), macelignan ( 5 ), and 4-(4-(benzo[ d ][1,3]dioxol-5-yl)-1-methoxy-2,3-dimethylbutyl)-2-methoxyphenol ( 6 ) which were assayed for their cholinesterase (ChE) inhibitory activity. Compounds 1 and 3 were not previously reported for M. fragrans . Among isolated compounds, compound 2 showed the best activity toward both AChE and BChE with IC 50 values of 25.02 and 22.36 μM, respectively, compared with donepezil (0.07 and 4.73 μM, respectively).