online publication date: November 2023
Katherine Yasmin M. Garcia, Joe Anthony H. Manzano, and Allan Patrick G. Macabeo
ARTICLE DOI: https://doi.org/10.53603/actamanil.71.2023.adzs2369
The previously known cytotoxic cytochalasan, cytochalasin B (1), was isolated and purified from the ethyl acetate extract of the rice fermentation culture of the Alpine asphodel-associated Dothideomycetes fungus, Sparticola triseptata after iterative chromatographic purifications. The structure of 1 was established through extensive 1D and 2D-NMR spectroscopic experiments along with high-resolution electrospray ionization mass spectrometry (HRESIMS) and by comparison of its spectroscopic data with the literature. The potential of cytochalasin B (1) as antidiabetic and anti-obesity compound was screened using microplate, colorimetric enzyme inhibitory assays. Thus, 1 displayed significant in vitro α-glucosidase and porcine pancreatic lipase inhibitory activities with IC50 values of 5.46 µM and 8.43 µM, respectively when compared to the positive drug controls, acarbose and Orlistat®. Molecular simulation experiments using molecular docking showed moderately strong affinity of 1 onto the active sites of α-glucosidase and porcine pancreatic lipase with binding energies (BE) of -8.6 kcal/mol and -7.5 kcal/mol, respectively.
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