title: The phytoestrogenic compound cajanol from Pigeonpea roots is associated with the activation of estrogen receptor α-dependent signaling pathway in human prostate cancer cells.
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.
authors: Engineering Research Center of Forest Bio-Preparation, Ministry of Education, Northeast Forestry University, Harbin, 150040, PR China; Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin, 150040, PR China.
authors: Lu
authors: L
authors: Liang
authors: Chang
authors: C
authors: Gao
authors: Meng
authors: M
authors: Luo
authors: Chunjian
authors: C
authors: Zhao
authors: Wei
authors: W
authors: Wang
authors: Chengbo
authors: C
authors: Gu
authors: Jinghua
authors: J
authors: Yu
authors: Yujie
authors: Y
authors: Fu
mesh_terms: D017360:Arabidopsis; D036561:Cajanus / Q000737:chemistry; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D019938:Cyclin D1 / Q000378:metabolism; D047628:Estrogen Receptor alpha / Q000378:metabolism*; D038362:Glycogen Synthase Kinase 3 / Q000378:metabolism; D006801:Humans; D007529:Isoflavones / Q000494:pharmacology*; D008297:Male; D019869:Phosphatidylinositol 3-Kinases / Q000378:metabolism; D048789:Phytoestrogens / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry; D030821:Plants, Genetically Modified; D011471:Prostatic Neoplasms / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects*; D000094162:Phytoalexins
chemical_list: D019938:Cyclin D1; D047628:Estrogen Receptor alpha; D038362:Glycogen Synthase Kinase 3; D007529:Isoflavones; D019869:Phosphatidylinositol 3-Kinases; D048789:Phytoestrogens; C530104:CCND1 protein, human; C506487:ESR1 protein, human; C471767:cajanol; D000094162:Phytoalexins
keywords: apoptosis; cajanol; estrogenic activity; pER8-GFP transgenic Arabidopsis