天然产物研究与开发2013，Vol.25Issue(2)：156-160,5.
异土木香内酯及土木香内酯的结构修饰研究
Structural Modification of Isoalantolactone and Alantolactone Isolated from Inula helenium
摘要
Abstract
The objective of this study was to modify the structures of isoalantolactone (1) and alantolactone (2). All the derivatives were screened for antiproliferative activity against HepG2 cell line in vitro to explore the structure-antiprolif-erative activity relationship. In total, 11 compounds were obtained,of which 13α-methoxymethyl-alanlactone (2d) was reported for the first time. The results showed that epoxyisoalantolactone (1b) and 5α,6a-epoxyalantolactone (2b) performed higher antiproliferative activity against HepG2 than compounds 1 and 2 while others performed weaker. Hence it was speculated that the 11,13-dehydrolactone fraction played a key role in keeping the antiproliferative activity against HepG2 cancer cells and the addition of an oxygen atom to form an epoxy group on the skeleton of isoalantolactone (1) and alantolactone (2) could further stimulate the antiproliferative activity.关键词
土木香/异土木香内酯/土木香内酯/结构修饰/抗增殖活性Key words
Inula helenium/isoalantolactone/alantolactone/structural modification/antiproliferative activity分类
医药卫生引用本文复制引用
杜会静,史海明,王梦月,彭崇胜,李晓波..异土木香内酯及土木香内酯的结构修饰研究[J].天然产物研究与开发,2013,25(2):156-160,5.基金项目
国家科技重大专项"重大新药创制"项目(2009ZX09502013,2012ZX09103201-038) （2009ZX09502013,2012ZX09103201-038）
上海交通大学"晨星青年学者奖励计划"(A10CX60) （A10CX60）
