八种稀土金属配合物和铂配合物抗HIV活性的研究

The anti-HIV-1 activity of 8 rare earth complexes and platinum complex

为了寻找治疗艾滋病的新药,研究了8种稀土金属(镧、铒、镝、钆、镨、镱、钐、钕)配合物和铂配合物的抗HIV活性。我们以C8166细胞系为指示细胞,测定样品对HIV-1IIIB诱导的细胞合胞体形成的抑制作用,并以MTT方法测定它们对细胞存活率的影响,以研究稀土和铂配合物对细胞的毒性。根据公式,计算出其CC50和EC50值,并进一步计算出其TI值。结果表明,镧配合物、钐配合物和铂配合物的EC50值分别为0.006μg/ml、74.28μg/ml和21.54μg/ml,它们的治疗指数分别为63、21和45,具有一定的抗HIV-1活性。其它的配合物具有很低或者不具有抗HIV-1活性。

To find a novel anti-HIV/AIDS drug, we detected the anti-HIV-1 activity of rare earth lanthanum, erbium, dysprosium, gadolinium, praseodymium, ytterbium, samarium, neodymium complexes, and platinum complex. The anti-HIV activity and cytotoxicity of these complexes were determined by the inhibitory assay of HIV-1 induced syncytial formation and MTT colorimetric assay, respectively. For these assay, a T cell adapted HIV-1IIIB viral strain and C8166 cells were used. The CC_(50) (50% cytotoxic concentration)、 EC_(50) (50% effective concentration) and TI (therapeutic index) of the above compounds were further calculated. The results showed that the EC_(50) of the lanthanum and samarium complexes and platinum complex were 0.006μg/ml, 74.28μg/ml and 21.54μg/ml, respectively; And their therapeutic indexes were 63, 21 and 45,respectively. The other rare earth complexes showed very low therapeutic index or no anti-HIV activity.