夏枯草抗肿瘤转移活性成分及其作用机制研究  

Study on Anti-tumor Constituents of Spica Prunellae and Their Anti-tumor Activity

作　　者：徐华影 金妍[1] 

机构地区：[1]天津医科大学第二医院,天津300211

出　　处：《中药新药与临床药理》2015年第3期351-355,共5页Traditional Chinese Drug Research and Clinical Pharmacology

摘　　要：目的研究夏枯草抗肿瘤的活性成分。方法夏枯草全草用75%乙醇提取,利用硅胶、凝胶等柱色谱及制备液相色谱对其化学成分进行分离和鉴定,进一步通过MTT细胞毒实验、划痕实验及蛋白质免疫印迹实验来评价各化合物的细胞毒性及抗肿瘤转移的活性。结果从夏枯草中分离鉴定了9个化合物,并对化合物进行了体外抗肿瘤转移活性的筛选,细胞毒性MTT实验结果表明,化合物1和2对人乳腺癌细胞MDA-MB-231没有明显毒性,进一步划痕实验结果显示化合物1和2均能剂量依赖性抑制抗肿瘤的迁移,此外化合物2能抑制与迁移相关PI3k/Akt通路的Akt和PKC的磷酸化水平。结论化合物1和2具有较强的抗肿瘤转移活性,化合物2通过抑制PI3k/Akt通路而抑制肿瘤细胞的迁移。Objective To study the chemical constituents from the whole plant of Spica Prunellae and to observe their anti-tumor activity. Methods Extracted with 75 % ethyl alcohol,the constituents were isolated from Spica Prunellae through chromatography of silica gel,Toyopearl HW-40 and p-HPLC. Their structures were identified on the basis of the physical properties and spectral analysis such as UV,1H NMR,13 C NMR and ESI-MS. Furthermore,cytotoxicity assay and wound healing assay were carried out to evaluate the anti-tumor activity of compounds 1~9. Results Nine compounds were isolated from Spica Prunellae. MTT cytotoxicity assay exhibited that compounds 1 and 2 had no cytotoxicity on MDA-MB-231 human breast cancer cells. Further wound healing assay showed that compounds 1 and 2inhibited cell migration in dose-dependent manner. And compound 2 could significantly inhibit the phosphorylation of Akt and PKC in migration-related PI3k/Akt signaling pathway. Conclusion Compounds 1 and 2 have exhibited excellent anti-tumor migration activities, and compound 2 might exhibit anti-tumor migration function through inhibiting the PI3k/Akt pathway.

关 键 词：夏枯草 细胞毒性 抗肿瘤迁移 PI3K/AKT 

分 类 号：R284.1[医药卫生—中药学]