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Open AccessFeature PaperArticle

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

1
Laboratory for Organic Reactivity, Discovery and Synthesis (LORDS), Research Center for the Natural and Applied Sciences, University of Santo Tomas, Espana Blvd., Manila 1015, Philippines
2
Department of Microbial Drugs, Helmholtz Centre for Infection Research and German Centre for Infection Research (DZIF), partner site Hannover/Braunschweig, Inhoffenstrasse 7, 38124 Braunschweig, Germany
3
Center of Excellence in Fungal Research, Mae Fah Luang University, Chiang Rai 57100, Thailand
*
Author to whom correspondence should be addressed.
Molecules 2020, 25(4), 965; https://doi.org/10.3390/molecules25040965
Received: 5 February 2020 / Revised: 18 February 2020 / Accepted: 18 February 2020 / Published: 20 February 2020
(This article belongs to the Special Issue Natural Products from Fungi)
The alpha-glucosidase- and lipase-inhibitory activities of three phenalenones (13) 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. View Full-Text
Keywords: Dothideomycetes; Pseudolophiostoma sp.; phenalenones; anti-α-glucosidase; anti-lipase; molecular docking Dothideomycetes; Pseudolophiostoma sp.; phenalenones; anti-α-glucosidase; anti-lipase; molecular docking
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Macabeo, A.P.G.; Pilapil, L.A.E.; Garcia, K.Y.M.; Quimque, M.T.J.; Phukhamsakda, C.; Cruz, A.J.C.; Hyde, K.D.; Stadler, M. Alpha-Glucosidase- and Lipase-Inhibitory Phenalenones from a New Species of Pseudolophiostoma Originating from Thailand. Molecules 2020, 25, 965.

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