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

2020; Multidisciplinary Digital Publishing Institute; Volume: 25; Issue: 4 Linguagem: Inglês

10.3390/molecules25040965

1433-1373

Allan Patrick G. Macabeo, Luis Agustin E. Pilapil, Katherine Yasmin M. Garcia, Mark Tristan J. Quimque, Chayanard Phukhamsakda, Allaine Jean C. Cruz, Kevin D. Hyde, Marc Stadler,

Essential Oils and Antimicrobial Activity

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.