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叶酸抑制大剂量甲氨蝶呤细胞毒性的试验研究
引用本文:王欢,蔡绍晖,潘琛,梁巧,吴肖蒙,张志敏,王波栋,吴晓松.叶酸抑制大剂量甲氨蝶呤细胞毒性的试验研究[J].中国药房,2012(13):1185-1187.
作者姓名:王欢  蔡绍晖  潘琛  梁巧  吴肖蒙  张志敏  王波栋  吴晓松
作者单位:暨南大学药学院;黑龙江省中医研究院;暨南大学附属第一医院
基金项目:暨南大学中药药效物质基础及创新药物研究广东省高校重点实验室“211”项目资助;暨南大学“国家大学生创新性实验计划”资助
摘    要:目的:研究叶酸抑制大剂量甲氨蝶呤(MTX)细胞毒性的作用。方法:通过体外Caco-2细胞的摄取试验方法结合高效液相联用双质谱技术,分别测定在1、10、100μmol.L-1叶酸存在下,Caco-2细胞与1μmol.L-1MTX共孵育30min后细胞所摄取MTX的量,并设立无叶酸对照组,以细胞中药物量/介质中药物量(C/M)的比值为指标。结果:共孵育30min后,无叶酸对照组C/M=5.13(n=4),而在1、10、100μmol.L-1叶酸存在条件下,C/M比值分别为4.91、4.22、3.74(n=4),与无叶酸对照组比较,100μmol.L-1叶酸存在条件下细胞摄取MTX的比例明显减少(P<0.05)。结论:当叶酸浓度为100μmol.L-1时有抑制大剂量MTX(1μmol.L-1)细胞毒性的作用,对细胞具有一定的保护作用。

关 键 词:甲氨蝶呤  叶酸  Caco-2细胞  细胞毒性  高效液相联用双质谱

Study on the Inhibition Effect of Folic Acid on the Cytotoxicity of High-dose Methotrexate
WANG Huan,CAI Shao-hui,LIANG Qiao,WU Xiao-meng,ZHANG Zhi-min,WANG Bo-dongCollege of Pharmacy,Jinan University,Guangzhou,China PAN ChenHeilongjiang Academy of Traditional Chinese Medicine,Harbin,China WU Xiao-song.Study on the Inhibition Effect of Folic Acid on the Cytotoxicity of High-dose Methotrexate[J].China Pharmacy,2012(13):1185-1187.
Authors:WANG Huan  CAI Shao-hui  LIANG Qiao  WU Xiao-meng  ZHANG Zhi-min  WANG Bo-dongCollege of Pharmacy  Jinan University  Guangzhou  China PAN ChenHeilongjiang Academy of Traditional Chinese Medicine  Harbin  China WU Xiao-song
Institution:WANG Huan,CAI Shao-hui,LIANG Qiao,WU Xiao-meng,ZHANG Zhi-min,WANG Bo-dong(College of Pharmacy,Jinan University,Guangzhou 510632,China) PAN Chen(Heilongjiang Academy of Traditional Chinese Medicine,Harbin 150036,China) WU Xiao-song(The First Affiliated Hospital of Jinan University,Guangzhou 510630,China)
Abstract:OBJECTIVE:To study the inhibition effect of folic acid(FA) on cytotoxicity of high-dose methotrexate(MTX).METHODS:The amount of MTX uptake was determined by cell uptake experiment of Caco-2 cells with HPLC-MS/MS technology after Caco-2 cells incubated with 1 μmol·L-1 MTX in 1,10,100 μmol·L-1 of FA for 30 min.Control group without FA was established with the drug uptake of cell/medium(C/M) ratio as index.RESULTS:After 30 min incubation,C/M=5.13(n=4) in control group without FA,while the C/M=4.91,4.22 or 3.74 in 1,10,100 μmol·L-1 of FA(n=4),respectively.Compared with the control group without FA,the proportion of MTX uptake decreased significantly(P<0.05) in the group with 100 μmol·L-1 FA.CONCLUSION:When the concentration of FA is up to 100 μmol·L-1,it can inhibit the cytotoxicity of high-dose MTX(1 μmol·L-1) and protect the cells to some extent.
Keywords:Methotrexate  Folic acid  Caco-2 cells  Cytotoxicity  HPLC-MS/MS
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