含天然化合物脂质体抗CHIKV病毒活性的研究。

IF 5.5 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Marília Freitas Calmon, Luiza Araújo Gusmão, Thalles Fernando Rocha Ruiz, Guilherme Rodrigues Fernandes Campos, Gabriela Miranda Ayusso, Tamara Carvalho, Isabella do Vale Francisco Bortolato, Pâmela Joyce Previdelli Conceição, Sebastião Roberto Taboga, Ana Carolina Gomes Jardim, Andres Merits, Paula Rahal, Antonio Claudio Tedesco
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引用次数: 0

摘要

背景/目的:基孔肯雅病毒(CHIKV)是一种由蚊子传播的单链RNA病毒,属于甲病毒属(托加病毒科),可引起大规模暴发。然而,目前还没有针对CHIKV感染的特异性治疗方法。小檗碱和大黄素是具有抗chikv活性的植物源化合物。本研究旨在评估含有小檗碱(LB)或大黄素(LE)的脂质体在体外对CHIKV的抗病毒效果,因为已知含有两性离子聚合物的纳米载体可以增强候选药物的生物稳定性、生物相容性和治疗效果。方法:合成并表征脂质体,并评估细胞活力以确定后续检测的合适浓度。对BHK-21和Huh7细胞进行共聚焦显微镜、抗病毒实验和western blotting。结果:在BHK-21和Huh7细胞中,浓度分别为5µM和10µM的LB和LE具有良好的耐受性。在这两种细胞类型中,脂质体被内化;LE主要定位于细胞质,而LB也在细胞核中检测到。EGCG作为抗病毒实验的标准药物,在BHK-21和Huh7细胞中表现出抗病毒活性,抑制RNA复制和CHIKV复制周期的多个阶段。纳米制剂和EGCG均能抑制CHIKV复制酶和病毒粒子蛋白的表达。结论:这些发现突出了载小檗碱和大黄素脂质体作为抗CHIKV感染的抗病毒药物的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Antiviral Activity of Liposomes Containing Natural Compounds Against CHIKV.

Antiviral Activity of Liposomes Containing Natural Compounds Against CHIKV.

Antiviral Activity of Liposomes Containing Natural Compounds Against CHIKV.

Antiviral Activity of Liposomes Containing Natural Compounds Against CHIKV.

Background/Objectives: Chikungunya virus (CHIKV), a mosquito-borne single-stranded RNA virus belonging to the genus Alphavirus (family Togaviridae), causes large-scale outbreaks. However, no specific treatment for CHIKV infections is currently available. Berberine and emodin are plant-derived compounds with anti-CHIKV activities. This study aimed to evaluate the antiviral efficacy of liposomes containing berberine (LB) or emodin (LE) against CHIKV in vitro, since nanocarriers incorporating zwitterionic polymers are known to enhance the biostability, biocompatibility, and therapeutic efficacy of drug candidates. Methods: Liposomes were synthesized and characterized, and cell viability was assessed to determine appropriate concentrations for subsequent assays. Confocal microscopy, antiviral assays, and western blotting were performed in BHK-21 and Huh7 cells. Results: In BHK-21 and Huh7 cells, LB and LE were well tolerated at concentrations of 5 and 10 µM, respectively. In both cell types, liposomes were internalized; LE was predominantly localized in the cytoplasm, whereas LB was also detected in the nucleus. EGCG, used as a standard drug against CHIKV in antiviral assays, exhibited virucidal activity and inhibited RNA replication and multiple stages of the CHIKV replication cycle in BHK-21 and Huh7 cells. Both the nanoformulations and EGCG consistently suppressed the expression of CHIKV replicase and virion proteins. Conclusions: These findings highlight the potential of berberine- and emodin-loaded liposomes as antiviral agents against CHIKV infection.

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来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
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