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  2. Dehydrodiconiferyl alcohol promotes BMP-2-induced osteoblastogenesis through its agonistic effects on estrogen receptor

Dehydrodiconiferyl alcohol promotes BMP-2-induced osteoblastogenesis through its agonistic effects on estrogen receptor

  • Biochem Biophys Res Commun. 2018 Jan 15;495(3):2242-2248. doi: 10.1016/j.bbrc.2017.12.079.
Wonwoo Lee 1 Kyeong Ryang Ko 1 Hyun-Keun Kim 2 Seonung Lim 2 Sunyoung Kim 3
Affiliations

Affiliations

  • 1 Department of Biological Sciences, Seoul National University, Seoul 151-742, South Korea; ViroMed Co., Ltd., Seoul 151-747, South Korea.
  • 2 Department of Biological Sciences, Seoul National University, Seoul 151-742, South Korea.
  • 3 Department of Biological Sciences, Seoul National University, Seoul 151-742, South Korea; ViroMed Co., Ltd., Seoul 151-747, South Korea. Electronic address: sunyoung@snu.ac.kr.
Abstract

Estrogen deficiency results in an imbalance between the levels of bone-resorping osteoclasts and bone-forming osteoblasts, eventually leading to overall bone loss. Dehydrodiconiferyl alcohol (DHCA), a lignan compound originally isolated from Cucurbita moschata, has been shown to bind to Estrogen Receptor, and indeed exhibits various activities of estrogen, such as anti-inflammatory and anti-oxidative stress effects. In this study, we tested whether synthetic DHCA could affect the BMP-2-induced osteoblastogenesis in vitro. In MC3T3-E1 cells, DHCA promoted BMP-2-induced differentiation of osteoblasts. Consistently, the expression of three osteoblastogenic genes known to be induced by BMP-2, ALP, osteocalcin and OPG, was up-regulated by DHCA treatment. DHCA was also shown to activate the production of RUNX2 by activating Smad1/5/9 and AMPK. Data from transient transfection assays suggested that DHCA might activate the Estrogen Receptor signaling pathway. Effects of DHCA on BMP-2-induced osteoblastogenesis were reduced when cells were treated with a specific siRNA to ERα or ERβ. Taken together, our results suggest that DHCA may be developed as an efficient therapeutic for osteoporosis by regulating osteoblastogenesis through its estrogenic effects.

Keywords

Bone morphogenetic protein-2; Dehydrodiconiferyl alcohol; Differentiation; Estrogen receptor; Osteoblasts.

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