苦荞麦黄酮对人食管癌细胞EC9706增殖的影响

目的研究苦荞麦黄酮在体外对EC9706细胞增殖的影响。方法 MTT法观察苦荞麦黄酮对EC9706细胞的毒性,荧光染色法观察细胞核的改变,流式细胞术观察细胞周期和细胞内活性氧水平,Western blotting分析凋亡蛋白表达。结果苦荞麦黄酮明显抑制EC9706细胞的增殖,其抑制率与药物浓度和作用时间呈正相关。经DAPI染色,电镜观察细胞核,可见多个凋亡小体的形成。流式细胞仪检测发现,苦荞麦黄酮使细胞发生G2/M期周期停滞,细胞内活性氧水平明显增加,且呈浓度依赖效应。Western blotting分析表明,苦荞麦黄酮能上调细胞内的促凋亡蛋白Bax,并下调抗凋亡蛋白Bcl-2的表达量。结论苦荞麦黄酮对人食管癌细胞株EC9706增殖具有明显的抑制作用,使细胞发生周期阻滞,并能通过调节活性氧水平及改变凋亡蛋白的表达量诱导其发生凋亡。

Virtual evaluation on activities of flavonoids from Scutellaria baicalensis

Objective To explore the investigation method of complicated Chinese materia medica (CMM), the potential action mechanisms of flavonoids from Scutellaria baicalensiswere studied by docking calculation. Methods In total, eight flavonoids (aglycones and their glycosides) from S. baicalensiswere selected as ligand. The crystalline structures of targets related to common diseases were used as the receptors for calculation. The calculations were conducted with Schrodinger software package. The grading standard of selectivity was developed according to G-score between ligands and receptors. Results The total number of reported pharmacologic actions was 26. Among all effects in literatures, nine of them can be deduced from the docking calculation of aglycone. Form of glycosides with grade ++, 25 reported effects can be estimated from calculation. Apparently, the target selectivity of aglycones and their glycosides were different form the virtual evaluation. The virtual evaluation results of glycosides were more close to the reported effects. Conclusion The proposed virtual evaluation method seems an effective way to investigate the complicated system of CMM. It suggests that aglycones may be effective as the form of glucoside in vivo, and metabolism is a very important factor for virtual evaluation.