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

Takumi Shono; Naoki Ishikawa; Kazufumi Toume; Midori A. Arai; Firoj Ahmed; Samir K. Sadhu; Masami Ishibashi

doi:10.1016/j.bmcl.2015.05.037

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

Takumi Shono, Naoki Ishikawa, Kazufumi Toume, Midori A. Arai, Firoj Ahmed, Samir K. Sadhu, Masami Ishibashi^*

^*この論文の責任著者

和漢医薬学総合研究所薬用資源管理部門

研究成果: ジャーナルへの寄稿 › 学術論文 › 査読

9 被引用数 (Scopus)

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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.

本文言語	英語
ページ（範囲）	2735-2738
ページ数	4
ジャーナル	Bioorganic and Medicinal Chemistry Letters
巻	25
号	14
DOI	https://doi.org/10.1016/j.bmcl.2015.05.037
出版ステータス	出版済み - 2015/06/04

ASJC Scopus 主題領域

生化学
分子医療
分子生物学
薬科学
創薬
臨床生化学
有機化学

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10.1016/j.bmcl.2015.05.037

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

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",

author = "Takumi Shono and Naoki Ishikawa and Kazufumi Toume and Arai, {Midori A.} and Firoj Ahmed and Sadhu, {Samir K.} and Masami Ishibashi",

year = "2015",

month = jun,

day = "4",

doi = "10.1016/j.bmcl.2015.05.037",

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T1 - Boehmenan, a lignan from Hibiscus ficulneus, showed Wnt signal inhibitory activity

AU - Shono, Takumi

AU - Ishikawa, Naoki

AU - Toume, Kazufumi

AU - Arai, Midori A.

AU - Ahmed, Firoj

AU - Sadhu, Samir K.

AU - Ishibashi, Masami

PY - 2015/6/4

Y1 - 2015/6/4

N2 - 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.

AB - 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.

KW - Hibiscus ficulneus

KW - Lignans

KW - Wnt signal

KW - β-Catenin

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DO - 10.1016/j.bmcl.2015.05.037

M3 - 学術論文

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AN - SCOPUS:84930278148

SN - 0960-894X

VL - 25

SP - 2735

EP - 2738

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 14

ER -

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

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