A. Macabeo, L. A. E. Pilapil, K. Y. M. Garcia, M. T. Quimque, C. Phukhamsakda, A. J. C. Cruz, K. Hyde, M. Stadler
Molecules, 2020
The alpha-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 secondary metabolites reported from the genus Pseudolophiostoma. Scleroderolide (1) and sclerodione (2) exhibited potent α-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 1 and 2. Both compounds exhibited strong binding affinities to both alpha-glucosidase and porcine lipase through H-bonding and π–π interactions. Interestingly, favorable in silico ADME (absorption, distribution, metabolism, and excretion) properties such as gastrointestinal absorption were also predicted using software.
Cited by 4 publications.
Field of study: Chemistry