2. Academic Validation
  3. Boehmenan, a lignan from Hibiscus ficulneus, showed Wnt signal inhibitory activity

Boehmenan, a lignan from Hibiscus ficulneus, showed Wnt signal inhibitory activity

  • Bioorg Med Chem Lett. 2015 Jul 15;25(14):2735-8. doi: 10.1016/j.bmcl.2015.05.037.
Takumi Shono 1,  Naoki Ishikawa 1,  Kazufumi Toume 1,  Midori A Arai 1,  Firoj Ahmed 2,  Samir K Sadhu 3,  Masami Ishibashi 4
Affiliations

Affiliations

  • 1 Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan.
  • 2 Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan; Department of Pharmaceutical Chemistry, University of Dhaka, Dhaka 1000, Bangladesh.
  • 3 Pharmacy Discipline, Life Science School, Khulna University, Khulna 9208, Bangladesh.
  • 4 Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan. Electronic address: mish@chiba-u.jp.
PMID: 26026364 DOI: 10.1016/j.bmcl.2015.05.037
Abstract

The Wnt signal pathway modulates numerous biological processes, and its aberrant activation is related to various diseases. Therefore, inhibition of the Wnt signal may provide an effective (or efficient) strategy for these diseases. Cell-based luciferase assay targeting the Wnt signal (TOP assay) revealed that Hibiscus ficulneus extract inhibited the Wnt signal. The activity-guided isolation of the MeOH extract of H. ficulneus stems yielded four known (1-4) Lignans along with myriceric acid (5). Compounds 1-4 potently inhibited the Wnt signal with TOPflash IC50 values of 1.0, 4.5, 6.3, and 1.9 μM, respectively. Compound 1 exhibited cytotoxicity against both Wnt-dependent (HCT116) and Wnt-independent (RKO) cells. Western blot analysis showed that 1 decreased the expression of full, cytosolic and nuclear β-catenin along with c-Myc in STF/293 cells. Our results suggested that 1 may have inhibited the Wnt signal by decreasing β-catenin levels.

Keywords

Hibiscus ficulneus; Lignans; Wnt signal; β-Catenin.

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