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

摘要: 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HepG-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3.66 μg/mL和21.47 μg/mL;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.

Abstract: 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 structures were confirmed by 1H NMR,13C NMR,and MS spectrum.Their in vitro antitumor activity were tested on K562 and HepG-2 cells.Result showed that compounds Ⅸ and Ⅺ had interesting activity.IC50 of 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.