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Article Abstract
In our search for bioactive natural products from the lichen species in Vietnam, Usnea aciculifera Vain (Parmeliaceae) in particular, two new depsides (1 and 2), one new monocyclic phenolic (3), and seven known (4-10) were isolated. The α-glucosidase inhibitory ability of 1-10 was assessed in vitro and further analyzed by molecular docking. Besides, the two new depsides were also assayed for their cytotoxicity against three human cancer cell lines (KB, MCF-7, and HepG2) and a normal human lung fibroblast (WI-38). As a result, 1-10 exhibited similar or superior α-glucosidase inhibition activity (IC values ranging from 18.60 to 93.19 µM) than the positive standard, acarbose (IC = 100.02 µM). Furthermore, molecular docking evaluation suggested that effective α-glucosidase inhibition can be achieved by firmly blocking Site 1 while extending the structure toward Site 2 enhances the bioactivity if done correctly. As for the cytotoxicity of compounds 1 and 2, they both exhibited moderate activity against the three cancer cell lines (IC values ranging from 18.11 to 30.28 µM).
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