학술논문

Alpha-Glucosidase- and Lipase-Inhibitory Phenalenones from a New Species of Pseudolophiostoma Originating from Thailand.
Document Type
Article
Source
Molecules. Feb2020, Vol. 25 Issue 4, p965. 1p. 2 Diagrams, 4 Charts, 1 Graph.
Subject
*ALPHA-glucosidases
*GLUCOSIDASES
*METABOLITES
*ETHYL acetate
*BIOCHEMICAL mechanism of action
*LIPASES
*SPECIES
Language
ISSN
1420-3049
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. [ABSTRACT FROM AUTHOR]