Alpha-Glucosidase- and Lipase-Inhibitory Phenalenones from a New Species of Pseudolophiostoma Originating from Thailand
The alpha-glucosidase- and lipase-inhibitory activities of three phenalenones ( - ) and one phenylpropanoid ( ) from the ethyl acetate extracts of a sp. are described. They represent the first secondary metabolites reported from the genus . Scleroderolide ( ) and sclerodione ( ) exhibited potent α-g...
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Veröffentlicht in: | Molecules (Basel, Switzerland) Switzerland), 2020-02, Vol.25 (4), p.965 |
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Hauptverfasser: | , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | The alpha-glucosidase- and lipase-inhibitory activities of three phenalenones (
-
) and one phenylpropanoid (
) from the ethyl acetate extracts of a
sp. are described. They represent the first secondary metabolites reported from the genus
. Scleroderolide (
) and sclerodione (
) exhibited potent α-glucosidase- and porcine-lipase-inhibitory activity during primary screening, with better IC
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
and
. 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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ISSN: | 1420-3049 1420-3049 |
DOI: | 10.3390/molecules25040965 |