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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
引用本文:郑小红,李伟,张昕宇,程训官,夏铸,汤为学,余瑜.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[J].世界科技研究与发展,2011,33(3):477-480.
作者姓名:郑小红  李伟  张昕宇  程训官  夏铸  汤为学  余瑜
作者单位:重庆医科大学药学院药物化学与生物材料研究室,重庆,400016
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。

关 键 词:手性药物  MTT法  油红0染色  QCY-7701  优对映体

Researches on Anti-tumor Activity of Novel Chiral Compound TNBG in Vitro
ZHENG Xiaohong,LI Wei,ZHANG Xinyu,CHENG Xunguan,XIA Zhu,TANG Weixue,YU Yu.Researches on Anti-tumor Activity of Novel Chiral Compound TNBG in Vitro[J].World Sci-tech R & D,2011,33(3):477-480.
Authors:ZHENG Xiaohong  LI Wei  ZHANG Xinyu  CHENG Xunguan  XIA Zhu  TANG Weixue  YU Yu
Institution:( Research Lab. of Pharmacochemistry and Biomaterial, School of Pharmacy, Chongqing Medical University, Chongqing 400016)
Abstract: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.
Keywords:chiral drugs  MTT assay  oil red O stain  QGY-7701  eutomer
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