纤细薯蓣皂苷衍生物及其抗肿瘤活性研究

Study on gracillin derivatives and their antitumor activity

基于纤细薯蓣皂苷母体结构,通过水解和酯化反应制备了11个纤细薯蓣皂苷衍生物,通过波谱学方法(NMR、MS)确证了其化学结构,其中化合物Ⅰ、Ⅱ、Ⅴ、Ⅵ、Ⅸ、Ⅺ均为新化合物.采用改良MTT法对衍生物进行了体外抗肿瘤活性试验,结果显示,纤细薯蓣皂苷衍生物对人慢性骨髓性白血病细胞K562、人肝癌细胞Hep G-2均表现出一定的抗肿瘤活性,一些化合物表现出优于纤细薯蓣皂苷元的抗肿瘤活性,其中的化合物Ⅸ、Ⅺ表现出明显的抗肿瘤活性趋势,尤其化合物Ⅸ,对2种肿瘤细胞的IC50值分别为3.66μg/m L和21.47μg/m L;而且发现糖基部分糖的数量影响化合物抑制肿瘤细胞的活性.

By the means of hydrolysis and esterification, 11 gracillin derivatives were prepared. Six of them （ I , II, V, VI, IX, XI） were new compounds. Their spectrum.Their in vitro antitumor activity were tested IX and XI had interesting activity.ICso of compounds structures were confirmed by ^1H NMR, ^13C NMR, and MS on K562 and HepG-2 cells.Resuh showed that compounds IX on two kinds of tumor cells were 3.66 μg/mL and 21.47 μg/mL,respectively.It was also found that the quantity of sugar on compounds could affect the inhibiting activity of tumor cells.