Abstract
The rhizome of Davallia formosana is commonly used to treat bone disease including bone fracture, arthritis, and osteoporosis in Chinese herbal medicine. Here, we report the effects of WL1101, the ethanol extracts of fresh rhizomes of Davallia formosana on ovariectomy-induced osteoporosis. In addition, excess activated bone-resorbing osteoclasts play crucial roles in inflammation-induced bone loss diseases, including rheumatoid arthritis and osteoporosis. In this study, we examined the effects of WL1101 on receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis. Treatment with WL1101 significantly inhibited RANKL-stimulated osteoclastogenesis. Two isolated active compounds, ((−)-epicatechin) or WL14 (4-hydroxy-3-aminobenzoic acid) could also inhibit RANKL-induced osteoclastogenesis. WL1101 suppressed the RANKL-induced nuclear factor-κB (NF-κB) activation and nuclear translocation, which is the key process during osteoclastogenesis, by inhibiting the activation of IκB kinase (IKK) and IκBα. In animal model, oral administration of WL1101 (50 or 200 mg/kg/day) effectively decreased the excess bone resorption and significantly antagonized the trabecular bone loss in ovariectomized rats. Our results demonstrate that the ethanol extracts of fresh rhizomes of Davallia formosana inhibit osteoclast differentiation via the inhibition of NF-κB activation and effectively ameliorate ovariectomy-induced osteoporosis. WL1101 may thus have therapeutic potential for the treatment of diseases associated with excessive osteoclastic activity.
Highlights
Bone is an important organ which can provide mechanical support to soft tissues such as brain and spinal cord
We first examined the effect of ethanol extracts derived from fresh rhizome of Davallia formosana, WL1101, on RANKL-induced osteoclast differentiation
Excess activity of osteoclasts contributes to many bone diseases including osteoporosis, arthritis, and cancer bone metastasis [13,14,15]
Summary
Bone is an important organ which can provide mechanical support to soft tissues such as brain and spinal cord. Bone participates in maintaining blood calcium, phosphate, and hematopoiesis as well. Both osteoblast-mediated synthesis and osteoclast-mediated resorption contribute to the dynamic remodeling process in bone tissue [1, 2]. Osteoblasts are derived from mesenchymal stem cells and are responsible for bone matrix formation including bone mineralization [1]. On the other hand, multinucleated osteoclasts which are differentiated from hematopoietic cells are responsible for bone resorption [2]. Both cell types are regulated by circulating hormones, mechanical stress, and inflammatory mediators. Once the amount of osteoclast-mediated bone resorption is more than that of bone formation, osteoporosis ensures
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