新型手性抗肿瘤药物德氮吡格(TNBG)体外抗肿瘤活性初步研究  

Researches on Anti-tumor Activity of Novel Chiral Compound TNBG in Vitro

作　　者：郑小红[1] 李伟[1] 张昕宇[1] 程训官[1] 夏铸[1] 汤为学[1] 余瑜[1] 

机构地区：[1]重庆医科大学药学院药物化学与生物材料研究室,重庆400016

出　　处：《世界科技研究与发展》2011年第3期477-480,共4页World Sci-Tech R&D

基　　金：国家自然科学基金(30772595)

摘　　要：目的观察手性旋光异构体德氮吡格(TNBG)对6株人体肿瘤细胞增殖的影响,初步探讨其抗肿瘤作用机制。方法运用MTT法检测手性TNBG对6株肿瘤细胞生长抑制情况;油红O染色法观察QGY-7701细胞中脂质聚集情况;流式细胞仪检测手性TNBG对人肝癌细胞株QGY-7701细胞周期分布和凋亡影响。结果手性TNBG能不同程度抑制肿瘤细胞增殖,且呈剂量依赖性;油红O染色提取显示QGY-7701细胞内脂质量与给药剂量呈正相关;流式细胞仪检测到有S期细胞增加,并且手性TNBG还能诱导QGY-7701细胞发生凋亡。结论手性TNBG在体外具有良好的抗肿瘤活性,其抗肿瘤作用机制可能是通过促使肿瘤细胞产生脂质聚集,抑制肿瘤细胞增殖、诱导其凋亡从而达到抗肿瘤效应。总体看(+)TNBG体外抗肿瘤活性比(-)TNBG更强。Objective To investigate the effects of the two ehiral leading compounds, （-） TNBG and （ ＋ ）TNBG on proliferation of 6 human carcinoma cells, and approach the mechanism of their anti-tumor effects. Methods MTT assay was used to test the effects of anti-proliferation of 6 tumor cells. Oil Red O stain was used to observe the deposition of lipid substance. The flow eytometrlc analysis was used to detect the cell cycle and apoptosis information on QGY-7701. Results The proliferation was depressed in different degree after the intervention of chiral TNBGs in concentration-dependent manners. Oil Red O stain showed that the quantity of lipid substance while the dosage had a positive correlation. The cells showed S arrest in QGY-7701 ,with apoptosis induced in QGY-7701. Conclusion Chiral TNBGs had good anti-tumor activities in vitro, which may result from inducing the deposition of lipid substance in addition to inhibiting proliferation and inducing to apoptosis on QGY-7701. In general,the anti-tumor effect of （ ＋ ）TNBG was better than （-）TNBG in vitro.

关 键 词：手性药物 MTT法 油红O染色 QGY-7701 优对映体 

分 类 号：R96[医药卫生—药理学]