Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 15, Pages 4150-4154Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.06.058
Keywords
Natural products; Inhibitor; Hedgehog signal; Artocarpus communis; Hyptis suaveolens
Funding
- Japan Society for the Promotion of Science (JSPS)
- Ministry of Education, Culture, Sports, Science and Technology, Japan (MEXT)
- Terumo Life Science Foundation
- Tokyo Biochemical Research Foundation (TBRF)
- Grants-in-Aid for Scientific Research [15H04650] Funding Source: KAKEN
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The hedgehog (Hh) signaling pathway plays crucial roles in cell maintenance and proliferation during embryonic development. Naturally occurring Hh inhibitors were isolated from Artocarpus communis and Hyptis suaveolens using our previously constructed cell-based assay system. Bioactivity guided fractionation led to the isolation of 15 compounds, including seven new compounds (4, 5, 6, 7, and 9-11). The isolated compounds showed cytotoxicity against a cancer cell line (PANC1) in which Hh signaling was abnormally activated. Several compounds (12-14; GLI1 transcriptional inhibition IC50 = 7.6, 4.7, and 4.0 mu M, respectively) inhibited Hh related protein (BCL2) expression. Moreover, compounds 1, 12, and 13 disrupted GLI1 and DNA complex formation. (C) 2015 Elsevier Ltd. All rights reserved.
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