Anti-Inflammatory, Antiallergic and COVID-19 Main Protease (M(pro)) Inhibitory Activities of Butenolides from a Marine-Derived Fungus Aspergillus costaricaensis

来自海洋真菌哥斯达黎加曲霉(Aspergillus costaricaensis)的丁烯内酯的抗炎、抗过敏和 COVID-19 主蛋白酶 (M(pro)) 抑制活性

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Abstract

Amid the current COVID-19 pandemic, the emergence of several variants in a relatively high mutation rate (twice per month) strengthened the importance of finding out a chemical entity that can be potential for developing an effective medicine. In this study, we explored ethyl acetate (EtOAc) extract of a marine-derived fungus Aspergillus cosatricaensis afforded three butenolide derivatives, butyrolactones I, VI and V (1-3), two naphtho-γ-pyrones, TMC-256 A1 (4) and rubrofusarin B (5) and methyl p-hydroxyphenyl acetate (6). Structure identification was unambiguously determined based on exhaustive spectral analyses including 1D/2D NMR and mass spectrometry. The isolated compounds (1-6) were assessed for their in vitro anti-inflammatory, antiallergic, elastase inhibitory activities and in silico SARS-CoV-2 main protease (M(pro)). Results exhibited that only butenolides (1 and 2) revealed potent activities similar to or more than reference drugs unlike butyrolactone V (3) suggesting them as plausible chemical entities for developing lead molecules.

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