Abstract

Bone remodeling is a renewal process regulated by bone synthesis (osteoblasts) and bone destruction (osteoclasts). A previous study demonstrated that Lycii radicis cortex (LRC) extract inhibited ovariectomized (OVX)-induced bone loss in mice. This study investigated the anti-osteoporotic effects of bioactive constituent(s) from the LRC extract. The effective compound(s) were screened, and a single compound, scopolin, which acts as a phytoalexin, was chosen as a candidate component. Scopolin treatment enhanced alkaline phosphatase activity and increased mineralized nodule formation in MC3T3-E1 pre-osteoblastic cells. However, osteoclast differentiation in primary-cultured monocytes was reduced by treatment with scopolin. Consistently, scopolin treatment increased osteoblast differentiation in the co-culture of monocytes (osteoclasts) and MC3T3-E1 (osteoblast) cells. Scopolin treatment prevented bone mineral density loss in OVX-induced osteoporotic mice. These results suggest that scopolin could be a therapeutic bioactive constituent for the treatment and prevention of osteoporosis.

Highlights

  • Bone remodeling during vertebrate development is governed by the coordinated action of bone formation and resorption [1,2]

  • Alkaline phosphatase (ALP) is a glycoprotein located on the cell membrane of osteoblasts, and is a reliable and sensitive marker of bone metabolism; we conducted an alkaline phosphatase (ALP) assay to screen for bone formation-enhancing effects [22,23]

  • We investigated the effect of scopolin treatment on OVX-induced bone loss in an osteoporotic animal model

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Summary

Introduction

Bone remodeling during vertebrate development is governed by the coordinated action of bone formation (osteoblasts) and resorption (osteoclasts) [1,2]. Bone formation is initiated by high alkaline phosphatase (ALP) activity and is regulated by mineralization, collagen synthesis, and osteoblastic proliferation and differentiation [3]. Bone resorption is associated with osteoclastic proliferation and tartrate-resistant acid phosphatase (TRAP) activity [4]. Old or damaged bone tissue is removed by the action of osteoclasts on the bone surface, followed by the formation of new bone tissue by osteoblasts [1,5]. Imbalanced regulation of the two bone remodeling sub-processes results in many metabolic bone diseases, such as osteoporosis [6]. Osteoporosis is a progressive bone disease characterized by excessive bone resorption, decreased bone mass and density, and associated

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