特异性抗肝癌单味中草药提取物的高通量筛选  

High-throughput screening of single Chinese plant extracts on specific anti-hepatoma drugs

作　　者：杨秀颖[1] 张莉[1] 杨海光[1] 李莉 方莲花[1] 杜冠华[1] 

机构地区：[1]中国医学科学院北京协和医学院药物研究所药物靶点研究与新药筛选北京市重点实验室,北京100050

出　　处：《中国药理学与毒理学杂志》2016年第3期243-247,共5页Chinese Journal of Pharmacology and Toxicology

基　　金：国家自然科学基金(81470159);国家科技重大专项(2013ZX09508104)~~

摘　　要：目的利用高通量筛选分析技术评价单味中草药提取物对肝癌细胞及成纤维细胞的作用,以期获得具有特异性抗肝癌作用的中草药提取物。方法将242种常用单味中草药分别应用石油醚、乙醇或水进行提取,共获得554个中草药提取物。采用MTT来评价提取物对人肝癌细胞Bel7402和小鼠成纤维细胞NIH3T3存活的作用。结果提取物对人肝癌细胞Bel7402及成纤维细胞NIH3T3生长抑制作用>50%的样品分别占总样品数的7.4%和14.8%,对2种细胞抑制率同时>50%的样品占总数的4.4%,对Bel7402抑制率为对NIH3T3抑制率2倍以上且对Bel7402抑制率>50%的样品占总样品数的1.6%。复筛结果显示,防己乙醇提取物(DF173)对肝癌细胞的细胞毒作用特异性较好,具有良好的量效关系。DF173对Bel7402细胞毒作用IC50为8.27 mg·L-1,对NIH3T3的细胞毒作用IC50为19.48 mg·L-1。结论肿瘤细胞联合正常成纤维细胞筛选评价中草药提取物特异性抗肿瘤作用,有利于发现高效、低毒抗肿瘤中草药提取物。OBJECTIVE To evaluate the effect of single traditional Chinese medicine（TCM）herb extracts on hepatoma and normal fibroblast cells using high- throughput screening in order to obtain extracts with specific anti-hepatoma effect. METHODS 242 commonly used TCM herbs were extracted by petroleum ether,ethanol and water,respectively. The total number of TCM extracts was 554. The cytotoxicity of samples was evaluated by MTT in human hepatoma cells Bel7402 and mice normal fibroblasts NIH3T3. RESULTS 7.4% of the total extracts had an inhibitory effect greater than 50% for Bel7402,but14.8% for fibroblasts NIH3T3 cells. Extracts with an inhibitory effect above 50% on both Bel7402 and NIH3T3 cells accounted for 4.4% of the total extracts. Our results showed that the sample DF173 had preferable cytotoxicity effect on hepatoma carcinoma cel s in a good dose-effect relationship. DF173 is an ethanol extract from Stephania tetrandra,which is a commonly used herb in TCM. The cytotoxic IC50 of DF173 against Bel7402 was 8.27 mg·L^-1,and 19.48 mg·L^-1on NIH3T3. CONCLUSION The components of TCM herbs are highly complicated. The combination of tumor cells with normal fibroblast cells to evaluate the cytotoxicity effect during anti-tumor drug screening will contribute much to the discovery of TCM drugs with high anti-tumor efficiency and lower toxicity.

关 键 词：高通量筛选分析 中草药提取物 抗肝癌药(中药) Bel7402细胞 NIH3T3细胞 防己 

分 类 号：R284[医药卫生—中药学]