Isolation and evaluation of hedgehog inhibitors from christmas grass (themeda arguens)

Tatsuro Yoneyama, Midori A. Arai, Takashi Koyano, Thaworn Kowithayakorn, Masami Ishibashi

研究成果: Article査読

2 被引用数 (Scopus)

抄録

The hedgehog (Hh) signaling pathway is an important regulator of embryonic development, tissue patterning, cellular proliferation and differentiation. However, aberrant activation of the pathway is associated with tumorigenesis. In this study, the Hh signal inhibitory activity of plant extracts was measured with a cell-based assay system that targets GLI1-mediated transcription. Activity guided analysis of MeOH extracts of christmas grass (Themeda arguens) led to the isolation of four inhibitory compounds: Aciculatin (1), 7-de-O-methylaciculatin (2), 8-C-D-boivinopyranosylapigenin (3) and aciculatinone (4). Compound 1 strongly inhibited Hh/GLI1-mediated transcriptional activity with an IC50 value of 1.8 ΓM, and disrupted the formation of the GLI1-DNA complex by EMSA. 1 and 3 were cytotoxic for human prostate (DU-145) and breast (MCF-7) cancer cells. These compounds may serve as new tools for the molecular dissection of Hh pathway activation.

本文言語English
ページ(範囲)210-222
ページ数13
ジャーナルHeterocycles
95
1
DOI
出版ステータスPublished - 2017
外部発表はい

ASJC Scopus subject areas

  • 分析化学
  • 薬理学
  • 有機化学

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