Hedgehog inhibitors from Artocarpus communis and Hyptis suaveolens

Midori A. Arai, Kyoko Uchida, Samir K. Sadhu, Firoj Ahmed, Takashi Koyano, Thaworn Kowithayakorn, Masami Ishibashi

研究成果: Article

10 引用 (Scopus)

抜粋

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 μM, respectively) inhibited Hh related protein (BCL2) expression. Moreover, compounds 1, 12, and 13 disrupted GLI1 and DNA complex formation.

元の言語English
ページ(範囲)4150-4154
ページ数5
ジャーナルBioorganic and Medicinal Chemistry
23
発行部数15
DOI
出版物ステータスPublished - 2015 7 23
外部発表Yes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • これを引用

    Arai, M. A., Uchida, K., Sadhu, S. K., Ahmed, F., Koyano, T., Kowithayakorn, T., & Ishibashi, M. (2015). Hedgehog inhibitors from Artocarpus communis and Hyptis suaveolens. Bioorganic and Medicinal Chemistry, 23(15), 4150-4154. https://doi.org/10.1016/j.bmc.2015.06.058