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03-02-2025 | SARS-CoV-2 | Original Paper

Potent SARS-CoV-2 3C-like protease inhibitor ( +)-eupenoxide-3,6-diketone (IC50: 0.048 μM) was synthesized based on ( +)-eupenoxide; lead from ( +)-eupenoxide analogs study by endophytic fermentation

Authors: Shoji Maehara, Moeka Kumamoto, Shogo Nakajima, Yuhzo Hieda, Koichi Watashi, Toshiyuki Hata

Published in: Journal of Natural Medicines

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Abstract

Since the coronavirus disease 2019 (COVID-19) outbreak, research has been conducted on treatment and countermeasures against the causative severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). However, the development of new seeds is urgently needed because viruses have the characteristic of becoming resistant through mutation. We hypothesize that endophytes produce antiviral substances to combat foreign viruses in host plants. According to this hypothesis, the seeds of therapeutic agents for infectious diseases could be obtained from endophytes by culture experiments. This report found that Aspergillus sp. endophyte isolated from Catharanthus roseus produced ( +)-eupenoxide and its 3-ketone form with anti-SARS-CoV-2 activity. In addition, ( +)-eupenoxide-3,6-diketon was discovered as a new compound with potent 3C-like protease inhibitory activity (IC50: 0.048 μM) by synthesis based on ( +)-eupenoxide. This finding could be an important evidence that endophytic fungi symbiosis with medicinal plants is useful as antiviral producers.

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Literature
4.
go back to reference Nejidat A (1987) Effect of ophiobolin A on stomatal movement: role of calmodulin. Plant Cell Physiol 28:455–460 Nejidat A (1987) Effect of ophiobolin A on stomatal movement: role of calmodulin. Plant Cell Physiol 28:455–460
Metadata
Title
Potent SARS-CoV-2 3C-like protease inhibitor ( +)-eupenoxide-3,6-diketone (IC50: 0.048 μM) was synthesized based on ( +)-eupenoxide; lead from ( +)-eupenoxide analogs study by endophytic fermentation
Authors
Shoji Maehara
Moeka Kumamoto
Shogo Nakajima
Yuhzo Hieda
Koichi Watashi
Toshiyuki Hata
Publication date
03-02-2025
Publisher
Springer Nature Singapore
Keyword
SARS-CoV-2
Published in
Journal of Natural Medicines
Print ISSN: 1340-3443
Electronic ISSN: 1861-0293
DOI
https://doi.org/10.1007/s11418-024-01874-3