Department of Medical Microbiology, Leiden University Medical Center, 2333 ZA Leiden, The Netherlands.
Department of Pulmonology, Leiden University Medical Center, 2333 ZA Leiden, The Netherlands.
Int J Mol Sci. 2023 Feb 27;24(5):4588. doi: 10.3390/ijms24054588.
The SARS-CoV-2 pandemic highlighted the need for broad-spectrum antivirals to increase our preparedness. Patients often require treatment by the time that blocking virus replication is less effective. Therefore, therapy should not only aim to inhibit the virus, but also to suppress pathogenic host responses, e.g., leading to microvascular changes and pulmonary damage. Clinical studies have previously linked SARS-CoV-2 infection to pathogenic intussusceptive angiogenesis in the lungs, involving the upregulation of angiogenic factors such as ANGPTL4. The β-blocker propranolol is used to suppress aberrant ANGPTL4 expression in the treatment of hemangiomas. Therefore, we investigated the effect of propranolol on SARS-CoV-2 infection and the expression of ANGPTL4. SARS-CoV-2 upregulated ANGPTL4 in endothelial and other cells, which could be suppressed with R-propranolol. The compound also inhibited the replication of SARS-CoV-2 in Vero-E6 cells and reduced the viral load by up to ~2 logs in various cell lines and primary human airway epithelial cultures. R-propranolol was as effective as S-propranolol but lacks the latter's undesired β-blocker activity. R-propranolol also inhibited SARS-CoV and MERS-CoV. It inhibited a post-entry step of the replication cycle, likely via host factors. The broad-spectrum antiviral effect and suppression of factors involved in pathogenic angiogenesis make R-propranolol an interesting molecule to further explore for the treatment of coronavirus infections.
SARS-CoV-2 大流行凸显了我们需要广谱抗病毒药物来提高应对能力。当阻止病毒复制的效果降低时,患者通常需要治疗。因此,治疗不仅要抑制病毒,还要抑制致病的宿主反应,例如导致微血管变化和肺损伤。临床研究先前将 SARS-CoV-2 感染与肺部的病理性内套叠血管生成联系起来,涉及血管生成因子如 ANGPTL4 的上调。β受体阻滞剂普萘洛尔用于抑制血管畸形中异常的 ANGPTL4 表达,因此我们研究了普萘洛尔对 SARS-CoV-2 感染和 ANGPTL4 表达的影响。SARS-CoV-2 在上皮细胞和其他细胞中上调了 ANGPTL4,R-普萘洛尔可以抑制其表达。该化合物还抑制了 SARS-CoV-2 在 Vero-E6 细胞中的复制,并在各种细胞系和原代人气道上皮培养物中将病毒载量减少了约 2 个对数级。R-普萘洛尔与 S-普萘洛尔一样有效,但缺乏后者不想要的β受体阻滞剂活性。R-普萘洛尔还抑制了 SARS-CoV 和 MERS-CoV。它抑制了复制周期的进入后步骤,可能通过宿主因子。广谱抗病毒作用和抑制与病理性血管生成相关的因素使 R-普萘洛尔成为一种有趣的分子,可进一步探索用于治疗冠状病毒感染。