期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 2, 页码 718-722出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.11.126
关键词
Excoecaria agallocha; Hedgehog; GLI1-mediated transcriptional activity; Inhibitor
资金
- Japan Society for the Promotion of Science (JSPS)
- Grants-in-Aid for Scientific Research [22310133, 23310149, 23404007, 23102008] Funding Source: KAKEN
The inhibition of the Hedgehog (Hh) signaling pathway has emerged as an anti-cancer strategy. Three flavonoid glycosides including 2 new compounds (1-2) were isolated from Excoecaria agallocha as Hedgehog/GLI1-mediated transcriptional inhibitors and exhibited cytotoxicity against human pancreatic (PANC1) and prostate (DU145) cancer cells. Our data revealed that compound 1 clearly inhibited the expression of GLI-related proteins (PTCH and BCL-2) and blocked the translocation of GLI1 transcription factors into the nucleus in PANC1. Deleting the Smoothened (Smo) function in PANC1 treated with 1 led to downregulation of the mRNA expression of Ptch. This study describes the first Hh signaling inhibitor which blocks GLI1 movement into the nucleus without interfering with Smo. (C) 2010 Elsevier Ltd. All rights reserved.
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