大花紫玉盘中的新抗肿瘤活性番荔枝内酯及其绝对构型研究

STUDIES ON NEW CYTOTOXIC ANNONACEOUS ACETOGENINS FROM UVARIA GRANDIFLORA AND ABSOLUTE CONFIGURATIONS

从番荔枝科紫玉盘属植物大花紫玉盘（ＵｖａｒｉａｇｒａｎｄｉｆｌｏｒａＲｏｘｂ．）根茎中分得两种新的抗肿瘤活性番荔枝内酯（１和３），用Ｘｒａｙ衍射分析和Ｍｏｓｈｅｒ方法对１的绝对构型进行了研究，全部６个手性碳的构型分别是１５Ｓ，１７Ｒ，１８Ｒ，２１Ｒ，２２Ｒ，３６Ｓ。命名为大花紫玉盘素（ｕｖａｒｉｇｒｉｎ）。用Ｍｏｓｈｅｒ方法对３的绝对构型也进行了测定，命名为大花紫玉盘素Ａ（ｕｖａｒｉｇｒａｎｄｉｎＡ）。对以前得到的大花紫玉盘脂素（ｕｖａｒｉｇｒａｎｉｎ，２）的相对构型进行了修正。

Two new cytotoxic annonaceous acetogenins, named uvarigrin(1) and uvarigrandin A(3), were obtained from the roots of Uvaria grandiflora Roxb(Annonaceae). Based on X ray analysis and Mosher's methodology, the overall absolute configuration of 1 was established as 15 S ,17 R ,18 R ,21 R ,22 R ,36 S . The absolute configuration of 3 was also resolved by Mosher's methodology. The relative configuration of the previously reported uvarigranin(2) was revised. Compound 1 showed cytotoxicity against HCT 8, Bel 7402 and A 2780 human tumor cell lines at ED 50 levels of 0 15, 0 21 and 0 41 μg·ml -1 , respectively.