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百蕊草保肝成分的预测筛选、活性评价及定量分析
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| 篇名： | 百蕊草保肝成分的预测筛选、活性评价及定量分析 |
| TITLE： | Predictive screening，activity evaluation and quantitative analysis of hepatoprotective constituents from Thesium chinense Turcz. |
| 摘要： | 目的 为百蕊草的质量控制、临床应用及源于百蕊草的保肝药物开发提供实验基础。方法采用网络药理学技术预测、筛选百蕊草中潜在保肝活性成分及其作用靶点；以4mmol/L的异烟肼诱导建立肝脏荧光标记转基因斑马鱼Tg（fabp10a：dsRed）肝损伤模型，以斑马鱼仔鱼肝脏相对荧光面积、相对荧光强度及天冬氨酸氨基转移酶（AST）、丙氨酸氨基转移酶（ALT）、谷胱甘肽（GSH）、白细胞介素6（IL-6）为指标，评价潜在活性成分的保肝活性；采用高效液相色谱法测定17批不同产地百蕊草药材中保肝活性成分的含量。结果通过网络药理学技术筛选出百蕊草素Ⅰ（KOG）、山柰酚-3，7-二葡萄糖苷（KDG）、蒙花苷（BUD）、芹菜素-5-O-新橙皮苷（AON）4种潜在保肝活性成分，其核心作用靶点涉及丝裂原激活的蛋白激酶1、核因子κB亚基1等。药效验证实验结果显示，25μmol/LKOG、BUD、AON以及50μmol/LKDG均可显著增加/增强肝损伤模型仔鱼肝脏的相对荧光面积、相对荧光强度（P＜0.05），降低其AST、ALT、IL-6水平（P＜0.05），升高其GSH水平（P＜0.05）。含量测定结果显示，17批百蕊草药材中KOG均可检出，含量为0.0970～8.0820mg/g；KDG、AON、BUD在部分批次样品中未检出，在检出批次样品中的含量分别为0.0193～0.1232、0.0184～0.1091、0.3851～1.1893mg/g。结论百蕊草中KOG、KDG、AON、BUD可能是其潜在保肝活性成分；其中KOG在不同产地百蕊草药材中均可检出且含量相对较高，可作为百蕊草保肝作用评价的主要指标成分。 |
| ABSTRACT： | OBJECTIVE To provide an experimental basis for quality control， clinical application and development of hepatoprotective drugs derived from Thesium chinense Turcz.METHODS Network pharmacology was adopted to predict and screen potential hepatoprotective constituents and their action targets of T. chinense Turcz. A liver-injured model of transgenic zebrafish Tg （ fabp10a ： dsRed ） with fluorescent-labeled liver was induced by 4 mmol/L isoniazid. The relative liver fluorescence area and relative fluorescence intensity of zebrafish larvae， as well as the levels of aspartate aminotransferase （AST）， alanine aminotransferase （ALT）， glutathione （GSH） and interleukin-6 （IL-6） were taken as indexes to evaluate the hepatoprotective activity of potential active constituents. High-performance liquid chromatography was used to determine the contents of hepatoprotective active constituents in 17 batches of T. chinense Turcz. medicinal materials from different producing areas.RESULTS Four potential hepatoprotective constituents including kaempferol-3- O -glucorhamnoside （KOG）， kaempferol-3，7-di- O -glucoside （KDG）， buddleoside （BUD） and apigenin-5- O -neohesperidoside （AON） were screened out via network pharmacology， and their core targets involved mitogen-activated protein kinase 1， nuclear factor-κB subunit 1， etc. Pharmacodynamic verification results showed that 25 μmol/L KOG， BUD， AON and 50 μmol/L KDG could significantly increase the relative liver fluorescence area and relative fluorescence intensity of liver-injured model larvae （ P ＜0.05）， reduce the levels of AST， ALT and IL-6 （ P ＜0.05）， and elevate the GSH level （ P ＜0.05）. Content determination results indicated that KOG could be detected in all 17 batches of T. chinense Turcz. medicinal materials， with contents ranging from 0.097 0 to 8.082 0 mg/g；KDG， AON and BUD were not detected in partial batches of samples， and their contents in detectable batches were 0.019 3-0.123 2 mg/g， 0.018 4-0.109 1 mg/g and 0.385 1-1.189 3 mg/g， respectively.CONCLUSIONS KOG， KDG， AON and BUD in T.chinense Turcz. may be its potential hepatoprotective active constituents. Among them， KOG can be detected in T.chinense Turcz. medicinal materials from different producing areas with relatively high content， which can be used as the main marker constituent for evaluating the hepatoprotective effect of T.chinense Turcz. |
| 期刊： | 2026年第37卷第19期 |
| 作者： | 李莉；程雪纯；庄秀萍；周朋；张葆青；王信 |
| AUTHORS： | LI Li，CHENG Xuechun，ZHUANG Xiuping，ZHOU Peng，ZHANG Baoqing，WANG Xin |
| 关键字： | 百蕊草;保肝活性成分;网络药理学;斑马鱼;百蕊草素Ⅰ;蒙花苷;山柰酚-3，7-二葡萄糖苷;芹菜素-5-O-新橙皮苷 |
| KEYWORDS： | Thesium chinense Turcz.;hepatoprotective active constituents;Network pharmacology;Zebrafish;kaempferol-3- O -glucorhamnoside;buddleoside;kaempferol-3，7-di- O -glucoside;apigenin-5- O -neohesperidoside |
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