Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, China Pharmaceutical University , 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.
Syngenta, Jealott's Hill International Research Centre , Bracknell, Berkshire RG42 6EY, United Kingdom.
Org Lett. 2017 Oct 6;19(19):5410-5413. doi: 10.1021/acs.orglett.7b02681. Epub 2017 Sep 28.
Artemisians A-D (1-4), the first examples of [4 + 2] Diels-Alder type adducts presumably biosynthesized from a rare 1, 10-4, 5-diseco-guaianolide and a guaianolide diene, along with their possible precursor 5, were isolated from the traditional Chinese medicine Artemisia argyi. The structures of 1-4 were elucidated by extensive spectroscopic analyses and calculated electronic circular dichroism. Compound 2, with an IC value of 3.21 μM, exhibited significant antiproliferative activity via apoptosis induction and G2/M arrest in MDA-MB-468 cells.
青蒿素 A-D（1-4），是从传统中药青蒿中分离得到的首例[4+2]Diels-Alder 型加合物，可能由罕见的 1,10-4,5-去甲-11,12-环氧-愈创木烷内酯和愈创木烷二烯生物合成而来，同时还分离到它们的可能前体 5。通过广泛的光谱分析和计算电子圆二色性，确定了 1-4 的结构。化合物 2 的 IC 值为 3.21 μM，通过诱导 MDA-MB-468 细胞凋亡和 G2/M 期阻滞，表现出显著的抗增殖活性。
