Anti-Inflammatory, Antiallergic, and COVID-19 Main Protease (M<sup>pro</sup>) Inhibitory Activities of Butenolides from a Marine-Derived Fungus <i>Aspergillus terreus</i>.

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Uras I. S., Ebada S. S., Korinek M., Albohy A., Abdulrazik B. S., Wang Y., ...More

Molecules (Basel, Switzerland), vol.26, no.11, 2021 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 26 Issue: 11
  • Publication Date: 2021
  • Doi Number: 10.3390/molecules26113354
  • Journal Name: Molecules (Basel, Switzerland)
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Aerospace Database, Biotechnology Research Abstracts, CAB Abstracts, Chemical Abstracts Core, Communication Abstracts, EMBASE, Food Science & Technology Abstracts, MEDLINE, Metadex, Veterinary Science Database, Directory of Open Access Journals, Civil Engineering Abstracts
  • Keywords: Aspergillus terreus, butenolides, antiallergic, COVID-19 M-pro, elastase, BUTYROLACTONE DERIVATIVES, METABOLIC PRODUCTS, NEUTROPHIL, VERSICOLOR, BIOSYNTHESIS, STRAIN
  • Lokman Hekim University Affiliated: Yes


In December 2020, the U.K. authorities reported to the World Health Organization (WHO) that a new COVID-19 variant, considered to be a variant under investigation from December 2020 (VUI-202012/01), was identified through viral genomic sequencing. Although several other mutants were previously reported, VUI-202012/01 proved to be about 70% more transmissible. Hence, the usefulness and effectiveness of the newly U.S. Food and Drug Administration (FDA)-approved COVID-19 vaccines against these new variants are doubtfully questioned. As a result of these unexpected mutants from COVID-19 and due to lack of time, much research interest is directed toward assessing secondary metabolites as potential candidates for developing lead pharmaceuticals. In this study, a marine-derived fungus Aspergillus terreus was investigated, affording two butenolide derivatives, butyrolactones I (1) and III (2), a meroterpenoid, terretonin (3), and 4-hydroxy-3-(3-methylbut-2-enyl)benzaldehyde (4). Chemical structures were unambiguously determined based on mass spectrometry and extensive 1D/2D NMR analyses experiments. Compounds (1-4) were assessed for their in vitro anti-inflammatory, antiallergic, and in silico COVID-19 main protease (M-pro) and elastase inhibitory activities. Among the tested compounds, only 1 revealed significant activities comparable to or even more potent than respective standard drugs, which makes butyrolactone I (1) a potential lead entity for developing a new remedy to treat and/or control the currently devastating and deadly effects of COVID-19 pandemic and elastase-related inflammatory complications.