Biotechnology Department, Facultad de Ciencias Químicas, Universidad Nacional de Asunción, San Lorenzo 111421, Paraguay.
Phytochemistry Department, Facultad de Ciencias Químicas, Universidad Nacional de Asunción, San Lorenzo 111421, Paraguay.
Molecules. 2022 Mar 7;27(5):1743. doi: 10.3390/molecules27051743.
The COVID-19 pandemic has led to the search for new molecules with antiviral activity against SARS-CoV-2. The entry of the virus into the cell is one of the main targets for inhibiting SARS-CoV-2 infection. Natural products are an important source of new therapeutic alternatives against diseases. Pseudotyped viruses allow the study of SARS-CoV-2 viral entry inhibitors, and due to their simplicity, they allow the screening of a large number of antiviral candidates in Biosafety Level 2 facilities. We used pseudotyped HIV-1 with the D614G SARS-CoV-2 spike glycoprotein to test its ability to infect ACE2-expressing HEK 293T cells in the presence of diverse natural products, including 21 plant extracts, 7 essential oils, and 13 compounds from plants and fungi. The 50% cytotoxic concentration (CC) was evaluated using the resazurin method. From these analyses, we determined the inhibitory activity of the extract of , which had a half-maximal inhibitory concentration (IC) of 91.65 µg/mL, a CC of 693.5 µg/mL, and a selectivity index (SI) of 7.57, indicating its potential use as an inhibitor of SARS-CoV-2 entry. Moreover, our work indicates the usefulness of the pseudotyped-virus system in the screening of SARS-CoV-2 entry inhibitors.
新型冠状病毒肺炎疫情促使人们寻找具有抗 SARS-CoV-2 活性的新型分子。病毒进入细胞是抑制 SARS-CoV-2 感染的主要靶点之一。天然产物是治疗疾病的新疗法的重要来源。假型病毒允许研究 SARS-CoV-2 病毒进入抑制剂,并且由于其简单性,允许在生物安全 2 级设施中筛选大量的抗病毒候选物。我们使用带有 D614G SARS-CoV-2 刺突糖蛋白的假型 HIV-1 来测试其在存在多种天然产物的情况下感染表达 ACE2 的 HEK 293T 细胞的能力,这些天然产物包括 21 种植物提取物、7 种精油和 13 种植物和真菌化合物。使用 Resazurin 法评估 50%细胞毒性浓度 (CC)。通过这些分析,我们确定了 的提取物具有抑制活性,其半数最大抑制浓度 (IC) 为 91.65 µg/mL,CC 为 693.5 µg/mL,选择性指数 (SI) 为 7.57,表明其可能用作 SARS-CoV-2 进入抑制剂。此外,我们的工作表明假型病毒系统在筛选 SARS-CoV-2 进入抑制剂方面的有用性。