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The alpha-glucosidase- and lipase-inhibitory activities of three phenalenones (<b>1</b>&#8722;<b>3</b>) and one phenylpropanoid (<b>4</b>) from the ethyl acetate extracts of a <i>Pseudolophiosptoma</i> sp. are described. They represent the first secondary metabolites reported from the genus <i>Pseudolophiostoma</i>. Scleroderolide (<b>1</b>) and sclerodione (<b>2</b>) exhibited potent &#945;-glucosidase- and porcine-lipase-inhibitory activity during primary screening, with better IC₅₀ values 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 <b>1</b> and <b>2</b>. Both compounds exhibited strong binding affinities to both alpha-glucosidase and porcine lipase through H-bonding and &#960;&#8722;&#960; interactions. Interestingly, favorable in silico ADME (absorption, distribution, metabolism, and excretion) properties such as gastrointestinal absorption were also predicted using software.