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schaftoside有助于提取物在脂多糖诱导的RAW 264.7细胞中的抗炎活性。

Schaftoside contributed to anti-inflammatory activity of extract in lipopolysaccharide-induced RAW 264.7 cells.

作者信息

Thongyim Saruda, Sattayawat Pachara, Pongamornkul Wittaya, Jangsutthivorawat Siriphorn, Tragoolpua Yingmanee, Panya Aussara

机构信息

Office of Research Administration, Chiang Mai University, Chiang Mai, Thailand.

National Extracts and Innovative Products for Alternative Healthcare Research Group, Chiang Mai University, Chiang Mai, Thailand.

出版信息

Front Pharmacol. 2025 Jun 10;16:1584620. doi: 10.3389/fphar.2025.1584620. eCollection 2025.

Abstract

INTRODUCTION

: a plant listed in the Thai Herbal Pharmacopoeia, is well recognized for its medicinal properties, particularly its anti-inflammatory and antiviral activities. Among its known bioactive constituents, schaftoside has been reported to exhibit anti-inflammatory effects in various disease models. However, comparative studies between pure schaftoside and crude extracts, as well as comprehensive investigations into the underlying mechanisms of action, remain limited. Moreover, the relationship between the quantity and diversity of bioactive compounds and their corresponding anti-inflammatory activity which could serve as potential quality biomarkers has not been fully elucidated.

METHODS

In this study, we investigated the anti-inflammatory effects of schaftoside and evaluated its content in ethanolic extracts collected from ten geographically distinct regions of Thailand. First, the anti-inflammatory activity of schaftoside was assessed in LPS-induced RAW 264.7 macrophage cells. Subsequently, ten ethanolic extracts were tested for their anti-inflammatory activity in the same cell model. To further explore the potential contribution of schaftoside and other bioactive compounds to anti-inflammatory activity, molecular docking analysis was performed.

RESULTS AND DISCUSSION

At a concentration of 40 μM, schaftoside significantly downregulated the expression of key inflammation-related genes, including . All extracts demonstrated a consistent trend of reducing iNOS protein expression, which was accompanied by a corresponding decrease in nitric oxide (NO) production, indicating their potential anti-inflammatory properties. However, no significant correlation was observed between schaftoside content and the magnitude of anti-inflammatory activity, suggesting that schaftoside may not be the sole active compound responsible for the observed effects. The results of molecular docking analysis revealed that, in addition to schaftoside, other flavonoids such as isoorientin and isovitexin also exhibited binding affinity toward the iNOS protein, indicating that these compounds may contribute to the overall anti-inflammatory activity of extracts.

摘要

引言

作为泰国草药药典中列出的一种植物,其药用特性,特别是抗炎和抗病毒活性广为人知。在其已知的生物活性成分中,schaftoside已被报道在各种疾病模型中具有抗炎作用。然而,纯schaftoside与粗提物之间的比较研究以及对其潜在作用机制的全面研究仍然有限。此外,生物活性化合物的数量和多样性与其相应的抗炎活性之间的关系,而这种关系可作为潜在的质量生物标志物,尚未得到充分阐明。

方法

在本研究中,我们研究了schaftoside的抗炎作用,并评估了从泰国十个地理上不同地区收集的乙醇提取物中其含量。首先,在LPS诱导的RAW 264.7巨噬细胞中评估schaftoside的抗炎活性。随后,在同一细胞模型中测试了十种乙醇提取物的抗炎活性。为了进一步探索schaftoside和其他生物活性化合物对抗炎活性的潜在贡献,进行了分子对接分析。

结果与讨论

在浓度为40μM时,schaftoside显著下调了关键炎症相关基因的表达,包括……所有提取物均显示出降低iNOS蛋白表达的一致趋势,同时一氧化氮(NO)生成相应减少,表明它们具有潜在的抗炎特性。然而,未观察到schaftoside含量与抗炎活性大小之间存在显著相关性,这表明schaftoside可能不是导致观察到的效果的唯一活性化合物。分子对接分析结果表明,除schaftoside外,其他黄酮类化合物如异荭草素和异牡荆素也对iNOS蛋白表现出结合亲和力,表明这些化合物可能有助于提取物的整体抗炎活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2590/12186155/707d3cc83e9d/fphar-16-1584620-g001.jpg

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