期刊
MOLECULES
卷 26, 期 11, 页码 -出版社
MDPI
DOI: 10.3390/molecules26113354
关键词
Aspergillus terreus; butenolides; antiallergic; COVID-19 M-pro; elastase
资金
- TUB.ITAK-BMBF [114S916]
- Ministry of Science and Technology [MOST 106-2320-B-255-003MY3, MOST 108-2320-B-255-003-MY3, MOST 109-2327-B-255-001, MOST 109-2327-B-182-002]
- Chang Gung Memorial Hospital [CMRPF1G0241~3, CMRPF1J0051~3, BMRP450]
- Chang Gung University, Taiwan [104-6576A3]
A marine-derived fungus was found to contain two potentially active compounds that could be developed into new remedies for treating COVID-19 and related inflammatory complications.
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.
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