探索葡萄籽提取物对抑郁症的抗炎作用:临床前和网络药理学方法

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Marina Rigotti, Laura Ferrazzi Finger, Júlia Maiara dos Santos, Luciana Bavaresco Andrade Touguinha, Adriano Costa De Camargo, Alina Concepción-Alvarez, Raquel Bridi, Michel Mansur Machado, Lucielli Savegnago, Catia Santos Branco
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引用次数: 0

摘要

葡萄籽提取物(GSE)是一种生物技术投入,以其抗炎和神经保护特性而闻名。本研究旨在利用计算机方法对GSE进行化学表征,并评估其对抑郁症中肠-脑轴相关靶点的影响。还评估了酚类物质的生物可及性和体外和体内安全性。采用网络药理学(Network pharmacology, NP)方法鉴定GSE主要生物活性化合物的性质和潜在靶点,并采用高效液相色谱-二极管阵列检测(HPLC-DAD)技术对其进行鉴定。分子对接与抑郁相关toll样受体(TLR)信号通路相关的靶蛋白。在所有消化阶段评估GSE的生物可及性、抗氧化活性和总多酚含量,并将BV-2小胶质细胞暴露于最终消化代谢物中。重要的化合物儿茶素和芦丁与蛋白AKT1和MAPK8表现出分子亲和力,表明GSE具有抗炎作用。生物可及性分析显示,酚类化合物在胃和十二指肠消化阶段减少,在空肠和回肠消化阶段恢复到对照组水平。消化提取物(浓度≤50µg/mL; 24 h)对BV-2细胞无细胞毒性,不改变一氧化氮(NO)或活性氧(ROS)的产生(p > 0.05)。这些结果表明,GSE可能是调节炎症相关疾病的有希望的候选者。此外,使用盐蒿模型的体内毒性评估表明,提取物在体内应用是安全的。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Exploring the Anti-Inflammatory Effects of Grape Seed Extract on Depressive Disorder: A Preclinical and Network Pharmacology Approach

Exploring the Anti-Inflammatory Effects of Grape Seed Extract on Depressive Disorder: A Preclinical and Network Pharmacology Approach

Grape seed extract (GSE) is a biotechnological input known for its anti-inflammatory and neuroprotective properties. This study aimed to chemically characterize GSE and evaluate their effects on targets associated with the gut-brain axis in depression using in silico methods. Phenolic bioaccessibility and in vitro and in vivo safety profiles were also assessed. Network pharmacology (NP) was employed to identify the properties and potential targets of GSE’s main bioactive compounds, which were identified via High-Performance Liquid Chromatography with Diode-Array Detection (HPLC-DAD). Molecular docking was performed with target proteins involved in depression-related toll-like receptor (TLR) signaling pathways. The bioaccessibility, antioxidant activity, total polyphenol content of GSE were evaluated across all digestive stages, and BV-2 microglial cells were exposed to the final digestion metabolites. The significant compounds catechin and rutin exhibited molecular affinity with the proteins AKT1 and MAPK8, suggesting an anti-inflammatory effect of GSE. Bioaccessibility assays revealed a reduction of phenolic compounds during the gastric and duodenal digestion phases, which were reestablished to levels like the control in the jejunal and ileal phases. The digested extract (concentrations ≤ 50 µg/mL; 24 h) was non-cytotoxic to BV-2 cells and did not alter the production of nitric oxide (NO) or reactive oxygen species (ROS) (p > 0.05). These results suggest that GSE may be a promising candidate for modulating inflammation-related conditions. Additionally, in vivo toxicity assessments using the Artemia salina model indicated that the extract is safe for in vivo applications.

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来源期刊
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
审稿时长
>12 weeks
期刊介绍: The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.
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