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来自Myrtaceae的Myrtucommulones和相关的乙黄醇作为多目标SARS-CoV-2循环抑制剂的有希望的来源

Simony Carvalho Mendonça¹, Brendo Araujo Gomes^1,2, Mariana Freire Campos^1,2

¹Departamento de Produtos Naturais e Alimentos, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro 21941-902, RJ, Brazil.

Pharmaceuticals (Basel, Switzerland)

|April 27, 2024

概括

巴西米尔塔科植物提取物显示出针对SARS-CoV-2点的显著抗病毒活性. 尤金尼亚·莫塞尼和E.普拉西纳证明了病毒蛋白和复制的强有力的抑制,米尔图库穆隆被确定为有前途的治疗化合物.

科学领域:

自然产品化学自然产品化学
抗病毒药物发现发现
分子生物学分子生物学

背景情况:

SARS-CoV-2 病毒依赖于关键蛋白质,如 Spike 蛋白和蛋白酶 (3CLpro,PLpro) 进行感染.
LABEXTRACT植物提取物银行,丰富于来自巴西的Myrtaceae物种,为生物勘探新型抗病毒剂提供了一个来源.
之前的研究表明,在Myrtaceae家族内具有潜在的抗病毒特性.

研究的目的:

为了研究巴西木植物提取物对抗SARS-CoV-2点的抗病毒潜力.
为了将特定的Myrtaceae物种与对Spike蛋白,3CLpro和PLpro.pro的抑制作用相关联.
通过in vitro和in silico方法识别潜在的活性化合物并评估其有效性.

主要方法:

在体外测试以评估SARS-CoV-2点和病毒复制的抑制.
液体染色学-质谱学/质谱学 (LC-MS/MS) 与化学分析相结合,用于化合物识别.
在基分子对接,以评估已识别的化合物与病毒标和ACE2的结合亲和力.

主要成果:

尤金尼亚普拉西纳和尤金尼亚莫塞尼提取物对SARS-CoV-2点表现出显著的抑制作用.
E. mosenii 显示针对 Spike,3CLpro 和 PLpro 的多目标抑制 (>72%) 并抑制病毒复制 (EC50 < 8.3 μg·mL-1).
LC-MS/MS和分子网络识别了myrtucommulones作为潜在的活性化合物;对接分析突出了一个未经描述的myrtucommulone,它与病毒标和ACE2具有很高的结合亲和力.

结论:

木植物提取物,特别是来自E. mosenii和E. prasina的提取物,在抑制SARS-CoV-2感染的关键阶段方面显示出相当大的前景.
myrtucommulones被确定为潜在的抗SARS-CoV-2药物,需要进一步研究治疗开发.
这项研究强调了巴西生物多样性对于发现新型抗病毒策略的价值.

关键词:

在 COVID-19 疫情中,费特·弗雷特 (FRET FRET) 是一家在美国的船只.在PLS回归过程中,回归的结果是:伪型病毒伪型病毒

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