Mendes Sabrina, Guimarães Lays Cordeiro, Costa Pedro Augusto Carvalho, Fernandez Clara Couto, Figueiredo Maria Marta, Teixeira Mauro Martins, Dos Santos Robson Augusto Souza, Guimarães Pedro Pires Goulart, Frézard Frédéric
Department of Physiology and Biophysics, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte, Minas Gerais, Brazil.
Department of Biochemistry and Immunology, Universidade Federal de Minas Gerais, Belo Horizonte, Minas Gerais, Brazil.
Antimicrob Agents Chemother. 2024 Dec 5;68(12):e0083524. doi: 10.1128/aac.00835-24. Epub 2024 Oct 29.
To effectively reduce the health impact of coronavirus disease (COVID-19), it is essential to adopt comprehensive strategies to protect individuals from severe acute respiratory syndrome. In that sense, much effort has been devoted to the discovery and repurposing of effective antiviral and anti-inflammatory molecules. The endogenous peptide angiotensin-(1-7) [Ang-(1-7)] has been recently proposed as a promising anti-inflammatory agent to control respiratory infections. Liposomes also emerged as a safe and effective drug carrier system for local drug delivery to the lungs. In this context, the aim of this study was to develop a liposomal formulation of Ang-(1-7) [LAng (1-7)] and investigate its impact on animal survival as well as its antiviral and anti-inflammatory efficacies after intranasal administration in transgenic K18-hACE2 mice infected with SARS-CoV-2. The liposomal formulation was prepared by the ethanol injection method, exhibiting a mean diameter of 100 nm and a polydispersity index of 0.1. Following treatment of infected mice every 12 hours for 5 days, LAng (1-7) extended animal survival compared to the control groups that received either empty liposomes, free Ang-(1-7), or phosphate-buffered saline. Furthermore, the treatment with LAng (1-7) significantly decreased the viral load, as well as IL-6 and tumor necrosis factor levels in the lungs. Conventional treatment with remdesivir by parenteral route used as a positive control promoted similar effects, leading to improved survival rates and reduced viral load in the lungs without significant effects on IL-6 level. In conclusion, liposomal Ang-(1-7) emerges as a promising formulation to improve the treatment and decrease the severity of respiratory infections, such as COVID-19.
为有效降低冠状病毒病(COVID-19)对健康的影响,采取全面策略保护个体免受严重急性呼吸综合征的侵害至关重要。从这个意义上讲,人们已投入大量精力来发现和重新利用有效的抗病毒和抗炎分子。内源性肽血管紧张素 -(1 - 7)[Ang -(1 - 7)]最近被提议作为一种有前景的抗炎剂来控制呼吸道感染。脂质体也成为一种安全有效的药物载体系统,用于肺部局部给药。在此背景下,本研究的目的是开发一种Ang -(1 - 7)的脂质体制剂[LAng(1 - 7)],并研究其对感染严重急性呼吸综合征冠状病毒2(SARS-CoV-2)的转基因K18-hACE2小鼠经鼻给药后的动物存活率、抗病毒和抗炎功效的影响。该脂质体制剂通过乙醇注入法制备,平均直径为100 nm,多分散指数为0.1。在对感染小鼠每12小时治疗一次,持续5天之后,与接受空脂质体、游离Ang -(1 - 7)或磷酸盐缓冲盐水的对照组相比,LAng(1 -7)延长了动物存活时间。此外,LAng(1 - 7)治疗显著降低了肺部的病毒载量以及白细胞介素-6和肿瘤坏死因子水平。作为阳性对照的经肠胃外途径使用瑞德西韦的常规治疗也产生了类似效果,提高了存活率并降低了肺部病毒载量,但对白细胞介素-6水平无显著影响。总之,脂质体Ang -(1 - 7)成为一种有前景的制剂,可改善治疗并降低呼吸道感染(如COVID-19)的严重程度。