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...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Molecules (Basel, Switzerland) Switzerland), 2020-02, Vol.25 (4), p.965
Hauptverfasser: 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
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules25040965