Đukić Ivana, Kaličanin Nevena, Sencanski Milan, Pajovic Snezana B, Milicevic Jelena, Prljic Jelena, Paessler Slobodan, Prodanović Radivoje, Glisic Sanja
University of Belgrade-Faculty of Chemistry, 11000 Belgrade, Serbia.
University of Belgrade-Institute of Chemistry, Technology and Metallurgy, 11000 Belgrade, Serbia.
Front Biosci (Landmark Ed). 2023 Jan 13;28(1):8. doi: 10.31083/j.fbl2801008.
Drug resistance is a critical problem in health care that affects therapy outcomes and requires new approaches to drug design. SARS-CoV-2 Mpro mutations are of concern as they can potentially reduce therapeutic efficacy. Viral infections are amongst the many disorders for which nutraceuticals have been employed as an adjunct therapy. The aim of this study was to examine the potential activity of L-arginine and vitamin C against SARS-CoV-2 Mpro.
The Mpro inhibition assay was developed by cloning, expression, purification, and characterization of Mpro. Selected compounds were then screened for protease inhibition.
L-arginine was found to be active against SARS-CoV-2 Mpro, while a vitamin C/L-arginine combination had a synergistic antiviral action against Mpro. These findings confirm the results of our previous repurposing study that showed L-arginine and vitamin C were potential Mpro inhibitors. Moreover, they suggest a possible molecular mechanism to explain the beneficial effect of arginine in COVID patients.
The findings of the current study are important because they help to identify COVID-19 treatments that are efficient, inexpensive, and have a favorable safety profile. The results of this study also suggest a possible adjuvant nutritional strategy for COVID-19 that could be used in conjunction with pharmacological agents.
耐药性是医疗保健中的一个关键问题，它会影响治疗效果，需要新的药物设计方法。严重急性呼吸综合征冠状病毒2（SARS-CoV-2）主蛋白酶（Mpro）突变令人担忧，因为它们可能会降低治疗效果。病毒感染是众多使用营养保健品作为辅助治疗的疾病之一。本研究的目的是研究L-精氨酸和维生素C对SARS-CoV-2 Mpro的潜在活性。
通过Mpro的克隆、表达、纯化和表征建立Mpro抑制试验。然后筛选选定的化合物的蛋白酶抑制作用。
发现L-精氨酸对SARS-CoV-2 Mpro有活性，而维生素C/L-精氨酸组合对Mpro有协同抗病毒作用。这些发现证实了我们之前的重新利用研究结果，即L-精氨酸和维生素C是潜在的Mpro抑制剂。此外，它们还提示了一种可能的分子机制来解释精氨酸对新冠肺炎患者的有益作用。
本研究的结果很重要，因为它们有助于确定高效、廉价且安全性良好的新冠肺炎治疗方法。本研究结果还提示了一种可能用于新冠肺炎的辅助营养策略，可与药物联合使用。
