2. Academic Validation
  3. Alpha-Glucosidase- and Lipase-Inhibitory Phenalenones from a New Species of Pseudolophiostoma Originating from Thailand

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

  • Molecules. 2020 Feb 20;25(4):965. doi: 10.3390/molecules25040965.
Allan Patrick G Macabeo 1 2,  Luis Agustin E Pilapil 1,  Katherine Yasmin M Garcia 1,  Mark Tristan J Quimque 1,  Chayanard Phukhamsakda 3,  Allaine Jean C Cruz 1,  Kevin D Hyde 3,  Marc Stadler 2
Affiliations

Affiliations

  • 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.
PMID: 32093426 DOI: 10.3390/molecules25040965
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.

Keywords

Dothideomycetes; Pseudolophiostoma sp.; anti-lipase; anti-α-glucosidase; molecular docking; phenalenones.

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