The Phytoestrogenic Compound Cajanol from Pigeonpea Roots is Associated with the Activation of Estrogen Receptor α-dependent Signaling Pathway in Human Prostate Cancer Cells

Authors

  • Lu Liang,

    1. Engineering Research Center of Forest Bio-Preparation, Ministry of Education, Northeast Forestry University, Harbin, PR China
    2. Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin, PR China
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  • Chang Gao,

    1. College of Basic Medical Science, Peking University Health Science Center, Beijing, PR China
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  • Meng Luo,

    1. Engineering Research Center of Forest Bio-Preparation, Ministry of Education, Northeast Forestry University, Harbin, PR China
    2. Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin, PR China
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  • Chunjian Zhao,

    1. Engineering Research Center of Forest Bio-Preparation, Ministry of Education, Northeast Forestry University, Harbin, PR China
    2. Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin, PR China
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  • Wei Wang,

    1. Engineering Research Center of Forest Bio-Preparation, Ministry of Education, Northeast Forestry University, Harbin, PR China
    2. Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin, PR China
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  • Chengbo Gu,

    1. Engineering Research Center of Forest Bio-Preparation, Ministry of Education, Northeast Forestry University, Harbin, PR China
    2. Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin, PR China
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  • Jinghua Yu,

    Corresponding author
    1. Engineering Research Center of Forest Bio-Preparation, Ministry of Education, Northeast Forestry University, Harbin, PR China
    2. Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin, PR China
    • Correspondence to: Prof. Dr. Yujie Fu and Prof. Dr. Jinghua Yu, Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, and Engineering Research Center of Forest Bio-Preparation, Ministry of Education, Northeast Forestry University, Hexin Road, Harbin 150040, China.

      E-mail: yujie_fu2002@yahoo.com; yujh@mail.nefu.edu.cn

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  • Yujie Fu

    Corresponding author
    1. Engineering Research Center of Forest Bio-Preparation, Ministry of Education, Northeast Forestry University, Harbin, PR China
    2. Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin, PR China
    • Correspondence to: Prof. Dr. Yujie Fu and Prof. Dr. Jinghua Yu, Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, and Engineering Research Center of Forest Bio-Preparation, Ministry of Education, Northeast Forestry University, Hexin Road, Harbin 150040, China.

      E-mail: yujie_fu2002@yahoo.com; yujh@mail.nefu.edu.cn

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Abstract

In the present study, the main natural estrogen-agonist/antagonist from Pigeonpea roots was studied by the estrogen receptor α-dependent signaling pathway in human prostate cancer cell. First, the natural products with estrogenic activity in Pigeonpea roots were screened by pER8-GFP transgenic Arabidopsis, and cajanol (5-hydroxy-3-(4-hydroxy-2-methoxyphenyl)-7-methoxychroman-4-one) was confirmed as the active compound. Further study showed that cajanol significantly arrested the cell cycle in the G1 and G2/M phase and induced nuclei condensation, fragmentation and the formation of apoptotic bodies. Western blotting showed that cajanol modulated the ERα-dependent PI3K pathway and induced the activation of GSK3 and CyclinD1 closely following the profile of PI3K activity. Based on above results, we proposed a mechanism through which cajanol could inhibit survival and proliferation of estrogen-responsive cells (PC-3 cells) by interfering with an ERα-associated PI3K pathway, following a process that could be dependent of the nuclear functions of the ERα. Above all, we conclude that cajanol represents a valuable natural phytoestrogen source and may potentially be applicable in health food industry. Copyright © 2013 John Wiley & Sons, Ltd.

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