大黄对瘢痕成纤维细胞增殖抑制作用及其有效成分研究  

Active ingredients in rhubarb with anti-proliferative effects on scar fibroblasts

作　　者：王倩[1] 张楠楠[2] 李红艳 姜民[4] 高洁[4] 白钢[4] 

机构地区：[1]河南广播电视大学,河南郑州450008 [2]天津中医药大学,天津300193 [3]天津嘉氏堂科技有限公司,天津300457 [4]南开大学药学院,天津300071

出　　处：《药学学报》2012年第12期1618-1622,共5页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81173638;81102835)

摘　　要：探索中药大黄抗瘢痕成纤维细胞(HSF)增殖作用的有效成分。采用索氏提取法将大黄药材按照极性依次提取不同的部位;以MTS法筛选大黄各溶剂提取物(25μg·mL-1)抗人增生性瘢痕成纤维细胞增殖的作用,结合流式细胞仪检测其对细胞周期的影响;进一步采用HPLC对其有效成分进行谱效分析,将其中高活性成分进行UPLC-Q/TOF鉴定及验证。结果显示,大黄乙酸乙酯提取物的有较高的抗细胞增殖活性(P<0.01),能显著增加G0/G1期细胞的比例(P<0.01),降低增殖指数(PI)(P<0.01),其中主要活性成分为蒽醌类化合物;以大黄素、大黄酸和没食子酸为例的验证结果显示,这3种成分均能抑制细胞的增殖且呈剂量依赖性。结果提示,大黄乙酸乙酯提取物对瘢痕成纤维细胞增殖有抑制作用,主要成分为其中的蒽醌类化合物。This study is to explore the active ingredients of traditional Chinese medicine rhubarb with anti- proliferative activity on hypertrophic scar fibroblasts （HSF）. Rhubarb was extracted with Soxhlet extraction method by different polar solvents. MTS method was used to screen rhubarb solvent extracts （25 μg-mL-1） with anti-proliferative activity on HSF, and flow cytometry was used to detect their influences on cell cycle. Then, the active ingredients were analyzed by HPLC. The components with high activity were identified by UPLC-Q/TOF and verified by HE staining. The results showed that the ethyl acetate extract of rhubarb had higher anti-proliferative activity （P〈0.01）, increased significantly the proportion of cells in G0/G1 phase （P〈0.01）, and reduced the proliferation index （PI） （P〈0.01）. The main active ingredients were anthraquinones. The results of confirming experiment showed that emodin, rhein and gallic acid could inhibit cell proliferation in a dose-dependent manner. In conclusion, the ethyl acetate extract of rhubarb showed anti-proliferative activity on HSF, and the anti-proliferative ingredients might be anthraquinones.

关 键 词：大黄 瘢痕成纤维细胞 谱效关系 UPLC-Q TOF 

分 类 号：R285[医药卫生—中药学]