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毛蕊花糖苷通过反相微乳剂清除活性氧增强体外抑制肝星状细胞激活的功效。

Enhanced In Vitro Efficacy of Verbascoside in Suppressing Hepatic Stellate Cell Activation via ROS Scavenging with Reverse Microemulsion.

作者信息

Xiao Xiao, Yang Feiyu, Huang Yuling, Liu Shaohui, Hu Zhenhua, Liao Shanggao, Li Yuanyuan

机构信息

School of Pharmacy, Guizhou Medical University, Guiyang 550025, China.

Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Zhongshan 528400, China.

出版信息

Antioxidants (Basel). 2024 Jul 27;13(8):907. doi: 10.3390/antiox13080907.

Abstract

Numerous approaches targeting hepatic stellate cells (HSCs) have emerged as pivotal therapeutic strategies to mitigate liver fibrosis and are currently undergoing clinical trials. The investigation of herbal drugs or isolated natural active compounds is particularly valuable, due to their multifaceted functions and low risk of side effects. Recent studies have hinted at the potential efficacy of verbascoside (VB) in ameliorating renal and lung fibrosis, yet its impact on hepatic fibrosis remains to be elucidated. This study aims to evaluate the potential effects of VB on liver fibrosis by assessing its ability to inhibit HSC activation. VB demonstrated significant efficacy in suppressing the expression of fibrogenic genes in activated LX-2 cells. Additionally, VB inhibited the migration and proliferation of these activated HSCs by scavenging reactive oxygen species (ROS) and downregulating the AMPK pathway. Furthermore, a biosafe reverse microemulsion loaded with VB (VB-ME) was developed to improve VB's instability and low bioavailability. The optimal formulation of VB-ME was meticulously characterized, revealing substantial enhancements in cellular uptake, ROS-scavenging capacity, and the suppression of HSC activation.

摘要

许多针对肝星状细胞(HSCs)的方法已成为减轻肝纤维化的关键治疗策略,目前正在进行临床试验。对草药或分离出的天然活性化合物的研究特别有价值,因为它们具有多方面的功能且副作用风险低。最近的研究暗示了毛蕊花糖苷(VB)在改善肾纤维化和肺纤维化方面的潜在疗效,但其对肝纤维化的影响仍有待阐明。本研究旨在通过评估VB抑制HSC活化的能力来评价其对肝纤维化的潜在作用。VB在抑制活化的LX-2细胞中纤维化基因的表达方面显示出显著疗效。此外,VB通过清除活性氧(ROS)和下调AMPK途径来抑制这些活化的HSCs的迁移和增殖。此外,还开发了一种负载VB的生物安全反向微乳(VB-ME),以改善VB的不稳定性和低生物利用度。对VB-ME的最佳配方进行了细致表征,结果显示其在细胞摄取、ROS清除能力和抑制HSC活化方面有显著增强。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/adaf/11351154/72c2ec0eda2e/antioxidants-13-00907-g001.jpg

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