水溶性C_(60)-脱氢枞胺衍生物的合成及生物活性

Synthesis and bioactivity study of water-soluble C_(60)-dehydroabietylamine derivatives

以C60-脱氢枞胺吡咯烷衍生物和C60-脱氢枞胺氮烯加成物为原料,通过两种不同的水性化途径分别合成了两种水溶性的C60-脱氢枞胺富勒醇衍生物和两种水溶性的C60-脱氢枞胺甘氨酸衍生物。产物经TEM、FT-IR、ESI-MS、1H NMR和HPLC等分析方法检测确认为目标产物,且为加成度不同的混合物。对合成出的4种水溶性C60-脱氢枞胺衍生物进行了生物活性测试。结果表明,4种水溶性C60-脱氢枞胺衍生物对rTaq DNA聚合酶和HIV-1反转录酶均表现出一定的抑制作用,对卵巢癌细胞株几乎不表现出抑制活性。

Two water-soluble C60-dehydroabietylamine fullerenol derivatives and two water-soluble glycine derivatives were synthesized by different water-borne modification method,with C60-dehydroabietylamine pyrrolidine derivative and nitrene addition derivative as the raw materials.The structures were characterized by TEM,FT-IR,ESI-MS,1H NMR and HPLC.The products were confirmed to be mixtures of components with different additional group numbers.These four derivatives were each given a bioactivity test.The results showed that they had different inhibition against both rTaq DNA polymerase and HIV-1 reverse transcriptase,while they showed less inhibition against the Hey 1B ovarian cancer cell line than HIV-1 reverse transcriptase.