State Key Laboratory of Virology, Wuhan Institute of Virology, Center for Biosafety Mega-Science, Chinese Academy of Sciences, Wuhan, 430071, China; University of the Chinese Academy of Sciences, Beijing, 100049, China.
State Key Laboratory of Virology, Wuhan Institute of Virology, Center for Biosafety Mega-Science, Chinese Academy of Sciences, Wuhan, 430071, China.
Antiviral Res. 2022 Aug;204:105365. doi: 10.1016/j.antiviral.2022.105365. Epub 2022 Jun 19.
Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has caused an ongoing pandemic, coronavirus disease-2019 (COVID-19), which has become a major global public health event. Antiviral compounds remain the predominant means of treating COVID-19. Here, we reported that bergamottin, a furanocoumarin originally found in bergamot, exhibited inhibitory activity against SARS-CoV-2 in vitro, ex vivo, and in vivo. Bergamottin interfered with multiple stages of virus life cycles, specifically blocking the SARS-CoV-2 spike-mediated membrane fusion and effectively reducing viral RNA synthesis. Oral delivery of bergamottin to golden Syrian hamsters at dosages of both 50 mg/kg and 75 mg/kg reduced the SARS-CoV-2 load in nasal turbinates and lung tissues. Pathological damage caused by viral infection was also ameliorated after bergamottin treatment. Overall, our study provides evidence of bergamottin as a promising natural compound, with broad-spectrum anti-coronavirus activity, that could be further developed in the fight against COVID-19 infection during the current pandemic.
严重急性呼吸综合征冠状病毒 2 型（SARS-CoV-2）引起了持续的大流行，即 2019 年冠状病毒病（COVID-19），这已成为一个主要的全球公共卫生事件。抗病毒化合物仍然是治疗 COVID-19 的主要手段。在这里，我们报道了佛手柑内酯，一种最初在佛手柑中发现的呋喃香豆素，在体外、体内和体内均显示出对 SARS-CoV-2 的抑制活性。佛手柑内酯干扰病毒生命周期的多个阶段，特别是阻断 SARS-CoV-2 刺突介导的膜融合，并有效减少病毒 RNA 合成。以 50mg/kg 和 75mg/kg 的剂量向金黄地鼠口服佛手柑内酯可降低鼻甲骨和肺组织中的 SARS-CoV-2 载量。佛手柑内酯治疗后，病毒感染引起的病理损伤也得到改善。总的来说，我们的研究为佛手柑内酯作为一种有前途的天然化合物提供了证据，它具有广谱抗冠状病毒活性，可在当前大流行期间进一步开发用于对抗 COVID-19 感染。
