文献类型：期刊文献

中文题名：L02肝细胞膜生物亲和材料快速筛选大黄降血脂活性成分

英文题名：L02 liver membrane bioaffinity material for rapid screening of lipid-lowering active constituents from Rheum palmatum L.

作者：武晓玉[1,2,3];段文达[1];夏鹏飞[1];边惠琴[1];王玉霞[1];李少泓[4];赵磊[1,2,3]

第一作者：武晓玉

机构：[1]甘肃中医药大学,兰州730000;[2]西北中藏药省部共建协同创新中心,兰州730000;[3]甘肃省高校中(藏)药化学与质量研究省级重点实验室,兰州730000;[4]江苏省无锡市第二人民医院,无锡214000

第一机构：甘肃中医药大学

年份：2022

卷号：42

期号：9

起止页码：1511

中文期刊名：药物分析杂志

外文期刊名：Chinese Journal of Pharmaceutical Analysis

收录：CSTPCD;;北大核心:【北大核心2020】；CSCD:【CSCD2021_2022】；

基金：国家自然科学基金资助项目(82160457);甘肃省“双一流”科研重点项目(GSSYLXM-05);甘肃省教育厅青年博士基金项目(2021QB-079);甘肃中医药大学引进人才科研启动基金(2018YJRC-02)。

语种：中文

中文关键词：大黄;L02肝脂肪变性细胞;生物亲和材料;降血脂;活性成分;快速筛选:网络药理学;分子对接

外文关键词：Rheum palmatum L.;L02 hepatic steatosis cells;bioaffinity material;hypolipidemic effects;active ingredient;rapid screening;network pharmacology;molecular docking

摘要：目的:为实现天然产物中活性成分的高通量筛选,制备物理吸附L02肝脂肪变性细胞膜生物亲和材料,并将其应用于大黄降血脂活性成分的快速筛选。方法:油酸诱导L02肝细胞,建立L02肝脂肪变性细胞模型;利用细胞膜自身的融合作用和硅胶表面硅羟基的吸附作用制备生物亲和材料,扫描电镜和红外光谱进行表征;并对大黄30%乙醇提取液进行吸附,HPLC分析吸附结果。结果:扫描电镜证实材料表面覆盖有1层细胞膜,红外光谱也出现3 442.41、1 549.35、1 106.23 cm^(-1)的-NH键特征吸收峰,表明材料制备成功;与正常L02细胞膜生物亲和材料相比,L02肝脂肪变性细胞膜生物亲和材料对大黄30%乙醇提取液中11个化学成分有特异性吸附,分别为:芦荟大黄素-8-O-β-D葡萄糖苷、大黄酸-8-O-β-D葡萄糖苷、大黄酚-8-O-β-D葡萄糖苷、大黄素甲醚-8-O-β-D葡萄糖苷、芦荟大黄素、大黄酸、大黄素、大黄酚、大黄素甲醚及2种未知成分。网络药理学预测出大黄降血脂主要作用靶标包括:PPARα、HMGCR、AKT1、TNF、MTOR、APOE等;分子对接模拟显示大黄素、大黄酚、大黄素甲醚对PPARα靶蛋白的结合能力高于HMGCR靶蛋白。结论:制备的物理吸附L02肝脂肪变性细胞膜生物亲和材料能够快速筛选出大黄降血脂活性成分,可弥补传统药物筛选中成分分离与活性筛选无法结合的缺点,为其他降血脂中药活性成分的快速筛选提供参考。
Objective: To realize the high-throughput screening of active ingredients in natural products, a kind of bioaffinity material of L02 hepatic steatosis cell membrane was prepared by physical adsorption, and it wasapplied to the rapid screening of active components of Rheum palmatum L. for lowering blood lipid. Methods: Model of L02 liver steatosis cells was established by oleic acid. Bioaffinity material was prepared by physical adsorption of hydroxyl on silica gel and amino on cell membrane, and characterized by scan electron microscopy and infrared spectroscopy. The 30% ethanol extract of Rheum palmatum L. was adsorbed, and the adsorption results were analyzed by HPLC. Results: Scanning electron microscope confirmed that the surface of the material was covered with a membrane obviously. Representative peaks at 3 442.41, 1 549.35 and 1 106.23 cm^(-1) were assigned to the adsorption of vibration by-NH bond, indicating that the material was successfully prepared. Compared with bioaffinity materials of normal L02 cell membrane, bioaffinity material of L02 hepatic steatosis cell membrane specifically adsorbed 11 chemical components from 30% ethanol extract of Rheum palmatum L., respectively: aloe-emodin-8-O-β-D glucopyranoside, rhein-8-O-β-D glucopyranoside, emodin-8-O-β-D glucoside, physcion-8-O-β-D-monoglucoside, aloe-emodin, rhein, emodin, chrysophanol, physcion and two unknown components. Network pharmacology predicted the main targets of Rheum palmatum L. for lowering blood lipid were PPARα, HMGCR, AKT1, TNF, MTOR and APOE, etc. Molecular docking simulation showed that the binding ability of emodin, chrysophanol and physcion to PPARα protein was higher than that of HMGCR protein. Conclusion: The bioaffinity material of L02 hepatic steatosis cell membrane by physical adsorption can quickly screen out the hypolipidemic active components of Rheum palmatum L.. It can make up for the shortcoming of the combination of component separation and activity screening in traditional drug screening, and provides reference for the rapid screening of other active constituents of lipid-lowering of traditional Chinese medicine.