https://scholars.lib.ntu.edu.tw/handle/123456789/634489
標題: | Isolation of Anti-SARS-CoV-2 Natural Products Extracted from Mentha canadensis and the Semi-synthesis of Antiviral Derivatives | 作者: | Chou, Osbert Juang, Yu-Pu TAI-LING CHAO Tsai, Sheng-Fa Chiu, Pei-Fang Chiou, Chun-Tang Tsai, Keng-Chang SUI-YUAN CHANG PI-HUI LIANG Wong, Chi-Huey |
公開日期: | 23-六月-2023 | 卷: | 86 | 期: | 6 | 起(迄)頁: | 1428 | 來源出版物: | Journal of natural products | 摘要: | Traditional herbal medicine offers opportunities to discover novel therapeutics against SARS-CoV-2 mutation. The dried aerial part of mint (Mentha canadensis L.) was chosen for bioactivity-guided extraction. Seven constituents were isolated and characterized by nuclear magnetic resonance (NMR) and mass spectrometry (MS). Syringic acid and methyl rosmarinate were evaluated in drug combination treatment. Ten amide derivatives of methyl rosmarinate were synthesized, and the dodecyl (13) and 3-ethylphenyl (19) derivatives demonstrated significant improvement in the anti-SARS-CoV-2 plaque reduction assay, achieving IC50 of 0.77 and 2.70 μM, respectively, against Omicron BA.1 as compared to methyl rosmarinate's IC50 of 57.0 μM. Spike protein binding and 3CLpro inhibition assays were performed to explore the viral inhibition mechanism. Molecular docking of compounds 13 and 19 to 3CLpro was performed to reveal potential interaction. In summary, natural products with anti-Omicron BA.1 activity were isolated from Mentha canadensis and derivatives of methyl rosmarinate were synthesized, showing 21- to 74-fold improvement in antiviral activity against Omicron BA.1. |
URI: | https://scholars.lib.ntu.edu.tw/handle/123456789/634489 | ISSN: | 01633864 | DOI: | 10.1021/acs.jnatprod.3c00104 |
顯示於: | 醫學檢驗暨生物技術學系 |
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