Yayınlanmış 1 Ocak 2022 | Sürüm v1
Dergi makalesi Açık

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

  • 1. Kaohsiung Med Univ, Coll Pharm, Grad Inst Nat Prod, Kaohsiung 80708, Taiwan
  • 2. Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
  • 3. Ain Shams Univ, Fac Pharm, Dept Pharmacognosy, Cairo 11566, Egypt

Açıklama

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-gamma-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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