Research Institute of Medicine and Pharmacy, Qiqihar Medical University, 161006, Qiqihar, China.
College of Pharmacy, Qiqihar Medical University, 161006, Qiqihar, China.
J Ethnopharmacol. 2025 Jan 30;337(Pt 1):118769. doi: 10.1016/j.jep.2024.118769. Epub 2024 Aug 31.
Trollius chinensis Bunge has a long history of use in China as traditional Chinese medicine and functional tea for the treatment of respiratory infections, such as pharyngitis, tonsillitis and bronchitis. Pharyngitis can impact the entire throat and adjacent lymphoid tissues, and may lead to significant systemic complications. However, the active components and mechanism of Trollius chinensis Bunge for treating acute pharyngitis remains unclear.
Trollius chinensis Bunge is recognized in China both as a medicinal herb and a functional tea. Research into its properties aimed to establish its effectiveness against pharyngitis and to pinpoint the active components and mechanism.
A 70% ethanol extract from the herb was prepared, which was refined using chromatography through a column containing D101 macroporous resin and varying ethanol solutions. The efficacy of the initial and refined extracts was tested using a rat model of ammonia-induced acute pharyngitis. Pathological examination, HE staining and ELISA were applied to screen activity fraction. The compounds were isolated by silica gel, sephadex LH-20 column chromatography and semi-preparative HPLC chromatography from active fraction. All of the isolated compounds were assessed for anti-inflammatory activity by acting on LPS-induced RAW 264.7 macrophage cells in vitro. Cytotoxicity of compounds was detected by CCK-8 assay. The Griess reaction was applied to evaluate the inhibitory effects of isolated compounds on NO production in RAW 264.7 cells induced by LPS. TNF-α, IL-6, IL-1β and PGE levels in macrophage supernatant were detected by ELISA. Molecular docking and western blot analysis were applied to study the anti-inflammatory mechanism of active compound.
The fraction extracted with 30% ethanol proved particularly effective, significantly reducing pharyngitis symptoms. This was evidenced by decreased levels of cytokines (TNF-α, IL-6, IL-1β and PGE) and visible improvements in the pharyngeal tissue histology. In pursuit of pharyngitis treatments, 23 phenolic acids and 13 flavonoids were isolated from the 30% ethanol fraction and identified using spectral analysis. Of these, three were newly discovered compounds and eight were first-time isolates from the Trollius genus. These compounds were further investigated for their ability to suppress nitric oxide production in RAW 264.7 cells triggered by lipopolysaccharide. Compounds 3, 19, and 26 exhibited strong anti-inflammatory properties. HPLC analysis of the 30% ethanol fraction revealed that orientin was the predominant component, accounting for 44.4% of this fraction. Western blot analysis demonstrated that orientin reduced the expression levels of the protein p-p65 relative to p65, p-IκBα relative to IκBα and iNOS, indicating an anti-inflammatory effect potentially through the modulation of the NF-κB signaling pathway.
The finding of this study provided strong support for the use of T. chinensis as a potential functional food for treating pharyngitis.
金莲花在中国有悠久的药用和功能茶使用历史，用于治疗呼吸道感染，如咽炎、扁桃体炎和支气管炎。咽炎可影响整个喉咙和相邻的淋巴组织，并可能导致严重的全身并发症。然而，金莲花治疗急性咽炎的活性成分和机制仍不清楚。
金莲花在中国既是一种草药，也是一种功能茶。研究其特性旨在确定其对咽炎的疗效，并确定活性成分和机制。
从该植物中提取 70%乙醇提取物，通过 D101 大孔树脂柱和不同浓度乙醇溶液的色谱法进行精制。使用氨诱导的急性咽炎大鼠模型测试初始和精制提取物的功效。通过病理检查、HE 染色和 ELISA 从活性部位筛选活性成分。用硅胶、葡聚糖 LH-20 柱色谱和半制备 HPLC 从活性部位分离化合物。通过 LPS 诱导的 RAW 264.7 巨噬细胞体外评估所有分离化合物的抗炎活性。通过 CCK-8 测定法检测化合物的细胞毒性。采用 Griess 反应评估分离化合物对 LPS 诱导的 RAW 264.7 细胞中 NO 产生的抑制作用。通过 ELISA 检测巨噬细胞上清液中 TNF-α、IL-6、IL-1β 和 PGE 的水平。采用分子对接和 Western blot 分析研究活性化合物的抗炎机制。
30%乙醇提取的馏分效果特别显著，明显减轻了咽炎症状。这表现在细胞因子（TNF-α、IL-6、IL-1β 和 PGE）水平降低，以及咽部组织组织学明显改善。为了寻找咽炎治疗方法，从 30%乙醇馏分中分离并鉴定了 23 种酚酸和 13 种类黄酮，其中 3 种为新发现的化合物，8 种为首次从金莲花属中分离出来的化合物。进一步研究了这些化合物抑制脂多糖诱导的 RAW 264.7 细胞中一氧化氮产生的能力。化合物 3、19 和 26 表现出较强的抗炎作用。30%乙醇馏分的 HPLC 分析表明，木犀草苷是该馏分的主要成分，占 44.4%。Western blot 分析表明，木犀草苷降低了蛋白 p-p65 相对于 p65、p-IκBα 相对于 IκBα 和 iNOS 的表达水平，表明其抗炎作用可能是通过调节 NF-κB 信号通路实现的。
本研究结果为金莲花作为治疗咽炎的潜在功能性食品提供了有力支持。
