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Alpha-Glucosidase- and Lipase-Inhibitory Phenalenones from a New Species of Originating from Thailand.
Macabeo, Allan Patrick G Pilapil, Luis Agustin E Garcia, Katherine Yasmin M Quimque, Mark Tristan J Phukhamsakda, Chayanard Cruz, Allaine Jean C Hyde, Kevin D Stadler, Marc
Macabeo, Allan Patrick G
Pilapil, Luis Agustin E
Garcia, Katherine Yasmin M
Quimque, Mark Tristan J
Phukhamsakda, Chayanard
Cruz, Allaine Jean C
Hyde, Kevin D
Stadler, Marc
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2020-02-20
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Abstract
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.
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Molecules. 2020 Feb 20;25(4). pii: molecules25040965. doi: 10.3390/molecules25040965.
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1420-3049
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Attribution-NonCommercial-ShareAlike 4.0 International