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目的:研究手性药物氨甲蝶呤(MTX)消旋体与单一对映体对ECV304内皮细胞的细胞毒性。方法:设置溶剂对照组及氨甲蝶呤(MTX)单一体与消旋体不同浓度组、时间组,采用四甲基偶氮唑蓝(MTT)比色法检测各组细胞存活和生长情况,分析量效关系、时效关系。结果:在0.1~50μmol.L-1浓度范围内,(+)MTX、(±)MTX对ECV304内皮细胞有明显抑制作用(P<0.01),而(-)MTX相对抑制较弱。在药物作用72h后各组的细胞抑制率均达到高峰。结论:在一定浓度范围,(±)MTX、(+)MTX对ECV304内皮细胞有细胞毒性,而(-)MTX则相对不明显。
Objective: To study the cytotoxicity of chiral drug methotrexate (MTX) racemate and single enantiomer on ECV304 endothelial cells. Methods: Solvent control group and methotrexate (MTX) single unit and racemic mixture of different concentrations of time group, using MTT assay cell viability and growth of each group, Analysis of the relationship between quantity and efficiency, aging relationship. Results: (+) MTX and (±) MTX significantly inhibited the ECV304 endothelial cells (P <0.01) in the concentration range of 0.1 ~ 50μmol.L-1, while the inhibition of (-) MTX was relatively weak. 72h after the drug effect in each group reached a peak cell inhibition rate. CONCLUSION: (±) MTX and (+) MTX are cytotoxic to ECV304 endothelial cells in a certain concentration range, while (-) MTX is relatively insignificant.