Phytochemical analysis and anticholinesterase activity of aril of Myristica fragrans Houtt

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 H₂O₂-induced cell death in PC12 neuronal cells and the ability to chelate bio-metals (Zn²⁺, Fe²⁺, and Cu²⁺). The fraction was inactive toward acetylcholinesterase (AChE); however, it inhibited the butyrylcholinesterase (BChE) with IC₅₀ value of 68.16 µg/mL, compared with donepezil as the reference drug (IC₅₀ = 1.97 µg/mL) via Ellman’s method. It also showed good percentage of neuroprotection (86.28% at 100 µg/mL) against H₂O₂-induced neurotoxicity and moderate metal chelating ability toward Zn²⁺, Fe²⁺, and Cu²⁺. 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 IC₅₀ values of 25.02 and 22.36 μM, respectively, compared with donepezil (0.07 and 4.73 μM, respectively).