Behmardi Abtin, Zolghadr Leila, Rajaei Farzad, Gholamzadeh Khoei Saeideh, Gheibi Nematollah
Cellular and Molecular Research Center, Research Institute for Prevention of Non-Communicable Disease, Qazvin University of Medical Sciences, Qazvin, Iran.
Department of Chemistry, Imam Khomeini International University, Qazvin, Iran.
Rep Biochem Mol Biol. 2025 Jan;13(4):484-494. doi: 10.61186/rbmb.13.4.484.
The kidneys are a potential target for SARS-CoV-2 infection. Ascorbic acid (vitamin C) has been shown to play an important role in reducing the symptoms of SARS-CoV-2. Recently liposomal drug delivery platforms have demonstrated promising results in enhancing the effectiveness of various therapeutics including infectious diseases. In this study, we designed a liposomal delivery system containing vitamin C to evaluate its antiviral efficacy in COVID-19, focusing on its effects on viral entry gene expression in Vero cells.
Vitamin C was loaded into a liposome made up of hydrogenated soybean phosphatidylcholine, cholesterol, and 1,2-distearoyl-sn-glycero-3 phosphoethanolamine-N-[methoxy (polyethylene glycol)-2000], and their physicochemical properties were assessed. Next, the cytotoxicity of free and liposomal vitamin C on the survival of the Vero cell line was evaluated using the MTT assay. In addition, the expression of viral entry genes, (ACE2) and (TMPRSS2), key mediators of SARS-CoV-2 entry into kidney cells, was investigated using RTq-PCR.
Liposomes were successfully loaded with vitamin C, achieving an encapsulation efficiency of 88.03%. The liposomal vitamin C formulation exhibited a brilliant surface morphology as observed by SEM. Both free and liposomal forms of vitamin C showed cytotoxic effects at higher concentrations. Moreover, both forms downregulated the expression of viral entry genes, although the liposomal form showed superior inhibitory performance compared to the free form.
The study suggests liposomal vitamin C as a safe, effective treatment for COVID-19 by targeting viral entry genes in kidney cells, protecting them from viral damage and inflammation.
肾脏是严重急性呼吸综合征冠状病毒2（SARS-CoV-2）感染的潜在靶点。已证明抗坏血酸（维生素C）在减轻SARS-CoV-2症状方面发挥重要作用。最近，脂质体药物递送平台在提高包括传染病在内的各种治疗药物的有效性方面已显示出有前景的结果。在本研究中，我们设计了一种含有维生素C的脂质体递送系统，以评估其在2019冠状病毒病（COVID-19）中的抗病毒功效，重点关注其对非洲绿猴肾（Vero）细胞中病毒进入基因表达的影响。
将维生素C负载到由氢化大豆磷脂酰胆碱、胆固醇和1,2-二硬脂酰-sn-甘油-3-磷酸乙醇胺-N-[甲氧基（聚乙二醇）-2000]组成的脂质体中，并评估其物理化学性质。接下来，使用噻唑蓝（MTT）法评估游离和脂质体形式的维生素C对Vero细胞系存活的细胞毒性。此外，使用逆转录定量聚合酶链反应（RTq-PCR）研究SARS-CoV-2进入肾细胞的关键介质病毒进入基因血管紧张素转换酶2（ACE2）和跨膜丝氨酸蛋白酶2（TMPRSS2）的表达。
脂质体成功负载了维生素C，包封率达到88.03%。扫描电子显微镜（SEM）观察显示，脂质体维生素C制剂呈现出良好的表面形态。游离和脂质体形式的维生素C在较高浓度下均表现出细胞毒性作用。此外，两种形式均下调了病毒进入基因的表达，尽管脂质体形式与游离形式相比表现出更优异的抑制性能。
该研究表明，脂质体维生素C通过靶向肾细胞中的病毒进入基因，保护它们免受病毒损伤和炎症，是一种安全、有效的COVID-19治疗方法。
