Abstract
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 (Mpro) 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.
Highlights
For more than a year since 2019, the whole world has been faced with the Coronavirus Disease 2019 (COVID-19) pandemic, believed to be caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV 2), a zoonotic viral infection that first emerged and was reported in Wuhan, China in December 2019 [1,2]
This mission was accomplished in December 2020 when the U.S Food and Drug Administration (FDA) issued the first Emergency Use Authorization (EUA) for the Pfizer–BioNTech vaccine [3] and the United Kingdom approved the emergency use of the Oxford–AstraZeneca vaccine for the prevention of the COVID-19 in individuals 16 years of age or older [4]
We performed an in vitro human coronavirus 229E (HCoV-229) assay to determine possible protective effects of compounds 1–4 (10 μM) against the HCoV-229 infection in Huh7 cells; none of the compounds exerted effects. These results suggest a potential role of these isolated compounds in the inhibition of the SARS-CoV-2 main protease with a possible role in controlling the new virus and late stage of coronavirus-associated acute respiratory distress syndrome (ARDS) inflammation
Summary
For more than a year since 2019, the whole world has been faced with the Coronavirus Disease 2019 (COVID-19) pandemic, believed to be caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV 2), a zoonotic viral infection that first emerged and was reported in Wuhan, China in December 2019 [1,2] During this year, scientists from all around the globe set new horizons for collaborations to race against time to produce a dependable and a reliable vaccine. For C26H31O9, 487.1968), indicating the existence of 11 degrees of unsaturation Both 1D and 2D NMR spectra of 3 revealed a similar pattern to those presented by terretonin, a meroterpenoid previously reported from A. terreus fungus [30,31]. The viability assays towards the cells used in the tests were performed
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
