Institut de Chimie des Substances Naturelles, CNRS, UPR 2301, Université Paris-Saclay, 91198 Gif-sur-Yvette, France.
Unité Mixte Processus Infectieux en Milieu Insulaire Tropical, Université de la Réunion, INSERM U1187, CNRS UMR 9192, IRD UMR 249, Plateforme Technologique CYROI, 94791 Sainte Clotilde, France.
Molecules. 2023 Jul 14;28(14):5414. doi: 10.3390/molecules28145414.
Induced by the spread of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the COVID-19 pandemic underlined the clear need for antivirals against coronaviruses. In an effort to identify new inhibitors of SARS-CoV-2, a screening of 824 extracts prepared from various parts of 400 plant species belonging to the Rutaceae and Annonaceae families was conducted using a cell-based HCoV-229E inhibition assay. Due to its significant activity, the ethyl acetate extract of the leaves of was selected for further chemical and biological investigations. Mass spectrometry-guided fractionation afforded three undescribed phenolic lipids (-), whose structures were determined via spectroscopic analysis. The absolute configurations of and were determined by analyzing Mosher ester derivatives. The antiviral activity against SARS-CoV-2 was subsequently shown, with IC values of 0.20 and 0.05 µM for and , respectively. The mechanism of action was further assessed, showing that both and are inhibitors of coronavirus entry by acting directly on the viral particle. Phenolic lipids from might be a source of new antiviral agents against human coronaviruses.
严重急性呼吸综合征冠状病毒 2（SARS-CoV-2）的传播引发了 COVID-19 大流行，这清楚地表明需要针对冠状病毒的抗病毒药物。为了寻找针对 SARS-CoV-2 的新型抑制剂，我们使用基于细胞的 HCoV-229E 抑制测定法，对来自 400 种植物的 824 种不同部位提取物进行了筛选，这些植物属于芸香科和番荔枝科。由于其显著的活性，选择了 的叶的乙酸乙酯提取物进行进一步的化学和生物学研究。质谱引导的分段得到了三种未描述的酚类脂质（-），通过光谱分析确定了它们的结构。通过分析 Mosher 酯衍生物确定了 和 的绝对构型。随后显示了对 SARS-CoV-2 的抗病毒活性， 和 的 IC 值分别为 0.20 和 0.05 µM。进一步评估了作用机制，表明 和 都是通过直接作用于病毒颗粒来抑制冠状病毒进入的抑制剂。可能是针对人类冠状病毒的新型抗病毒药物的来源。
