黄花夹竹桃的强心苷类化合物和无患子的三萜皂苷类化合物作为克服TRAIL耐药性的化合物。

Cardenolide glycosides of Thevetia peruviana and triterpenoid saponins of Sapindus emarginatus as TRAIL resistance-overcoming compounds.

作者信息

Miyagawa Takashi, Ohtsuki Takashi, Koyano Takashi, Kowithayakorn Thaworn, Ishibashi Masami

机构信息

Graduate School of Pharmaceutical Sciences, Chiba University, 1-33 Yayoi-cho, Inage-ku, Chiba 263-8522, Japan, Temko Corporation, 4-27-4 Honcho, Nakano, Tokyo 164-0012, Japan.

出版信息

J Nat Prod. 2009 Aug;72(8):1507-11. doi: 10.1021/np900202n.

DOI:10.1021/np900202n

PMID:19594141

Abstract

A screening study for TRAIL resistance-overcoming activity was carried out, and activity-guided fractionations of Thevetia peruviana and Sapindus emarginatus led to the isolation of four cardenolide glycosides (1-4) and four triterpenoid saponins (5-8), respectively. In particular, cardenolide glycosides (1 and 2) from T. peruviana were shown to have a significant reversal effect on TRAIL resistance in human gastric adenocarcinoma cells, and real-time PCR showed that thevefolin (2) enhanced mRNA expression of death receptor 4 (DR4) and DR5. In addition, 1H and 13C NMR characterizations are shown for thevefolin (2) for the first time.

摘要

开展了一项针对克服TRAIL抗性活性的筛选研究，对黄花夹竹桃和无患子进行活性导向分离，分别得到了四种强心苷糖苷（1-4）和四种三萜皂苷（5-8）。特别地，黄花夹竹桃中的强心苷糖苷（1和2）对人胃腺癌细胞的TRAIL抗性具有显著的逆转作用，实时PCR显示，毒毛旋花子苷元（2）可增强死亡受体4（DR4）和DR5的mRNA表达。此外，首次给出了毒毛旋花子苷元（2）的1H和13C NMR表征。