-Glucosidase and Lipase Inhibitory Phenalenones from a New Species of Pseudolophiostoma Originating from Thailand (original) (raw)

-Glucosidase and Lipase Inhibitory Phenalenones from a New Species of Pseudolophiostoma Originating from Thailand

The -glucosidase and lipase inhibitory activities of three phenalenones (1–3) and one phenylpropanoid (4) from the ethyl acetate extracts of a Pseudolophiosptoma sp. are described. They represent the first reported secondary metabolites from the genus Pseudolophiostoma. Scleroderolide (1) and sclerodione (2) exhibited potent -glucosidase and porcine lipase inhibitory activity during primary screening, with better IC50s compared to the positive controls, N-deoxynojirimycin and orlistat. In silico techniques were employed to validate the probable biological targets and elucidate the mechanism of actions of phenalenones 1 and 2. Both compounds exhibited strong binding affinities to both -glucosidase and porcine lipase through H-bonding and - interactions. Interestingly, favorable in silico ADME properties such as gastrointestinal absorption were also predicted using computational programmes.