This study is the first to analyse the methanolic root extract of Athamanta sicula L., an endemic Mediterranean plant, leading to the isolation of two phenylpropanoids: apiol and myristicin. The extract and isolated compounds were evaluated for their inhibitory potential against α-amylase, α-glucosidase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) using in vitro assays, molecular docking, and ADME predictions. The crude extract demonstrated superior inhibition of α-amylase and α-glucosidase compared to acarbose. Among the isolated compounds, apiol showed more activity than myristicin, particularly against α-glucosidase. Both compounds inhibited BChE, with apiol (IC50 = 330.07 µM; MolDock score = −89.89) outperforming myristicin (IC50 = 385.08 µM; MolDock score = −87.86). Favourable ADME properties, including high gastrointestinal absorption and blood-brain barrier penetration, were also predicted. These findings suggest that apiol and myristicin are key contributors to the plant’s bioactivity, making them promising multi-target lead compounds for developing new treatments for diabetes and Alzheimer’s disease.
Athamanta sicula L. Root extract: in vitro and in silico evaluation of anti-diabetic and anti-Alzheimer’s activities of apiol and myristicin
Pollastro, Federica;Salamone, Stefano
2026-01-01
Abstract
This study is the first to analyse the methanolic root extract of Athamanta sicula L., an endemic Mediterranean plant, leading to the isolation of two phenylpropanoids: apiol and myristicin. The extract and isolated compounds were evaluated for their inhibitory potential against α-amylase, α-glucosidase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) using in vitro assays, molecular docking, and ADME predictions. The crude extract demonstrated superior inhibition of α-amylase and α-glucosidase compared to acarbose. Among the isolated compounds, apiol showed more activity than myristicin, particularly against α-glucosidase. Both compounds inhibited BChE, with apiol (IC50 = 330.07 µM; MolDock score = −89.89) outperforming myristicin (IC50 = 385.08 µM; MolDock score = −87.86). Favourable ADME properties, including high gastrointestinal absorption and blood-brain barrier penetration, were also predicted. These findings suggest that apiol and myristicin are key contributors to the plant’s bioactivity, making them promising multi-target lead compounds for developing new treatments for diabetes and Alzheimer’s disease.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.


