［Ln(Phen)2 (5-Fu)3 (NO3)］(NO3)2的体外抗艾滋病毒活性
In vitro anti-HIV activity of ［Ln(Phen)2 (5-Fu)3 (NO3)］(NO3)2
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摘要: 目的 ： 研究稀土配合物体外抗艾滋病毒作用。 方法 ： 用7种稀土配合物［Ln(Phen)2 (5-Fu)3 (NO3)］(NO3)2作为测试对象，Ln为稀土元素Y，La，Ce，Sm，Gd，Dy，Er，Phen为邻二氮菲，5-Fu为5-氟尿嘧啶。用MTT方法测定它们对C8166细胞的半数抑制浓度(IC500)；用合胞体形成抑制实验测定它们对H9/HIV-1IIIB感染细胞合胞体的半数效应浓度(EC50)。以IC50/EC50计算配合物的治疗指数(TI)，测试结果与抗艾滋病药物齐夫多定(AZT)作阳性对照。 结果 ： 镧(La)配合物的TI为68.03，铈(Ce)配合物的TI为33.1。 结论 ： 镧、铈配合物有一定的体外抗艾滋病毒活性。Abstract: Aim ：To study in vitro anti-HIV activities of ［Ln(Phen)2 (5-Fu)3 (NO3)］(NO3)2. Methods ：Seven kinds of ［Ln(Phen)2 (5-Fu)3 (NO3)］(NO3)2complexes (Ln=Y，La，Ce，Sm，Gd，Dy，Er；Phen=1，10-phenanthroline；5-Fu=fluorouracil) were tested for their potential anti-HIV activities.IC50 of the complexes on C8166 cells was assayed by colorimetric MTT.EC50 was determined through the inhibition of syncytia formation induced by H9/HIV-1IIIB.The therapeutic index (TI，IC50/EC50) were calculated and compared with that of azidothymidine (AZT). Results ：It was found that TI of ［La(Phen)2 (5-Fu)3 (NO3)］(NO3)2 and［Ce(Phen)2 (5-Fu)3 (NO3)］(NO3)2 were 68.03 and 33.13，respectively. Conclusion ：La or Ce doped complexes demonstrated in vitro anti-HIV activity.
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Keywords:
- ［Ln(Phen)2 (5-Fu)3 (NO3)］(NO3)2 /
- 5-fluorouracil /
- anti-HIV activity /
- in vitro
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