Department of Internal Medicine 3, University of Erlangen-Nuremberg, Erlangen, Germany.
J Bone Miner Res. 2012 Dec;27(12):2442-51. doi: 10.1002/jbmr.1702.
Osteoporosis is characterized by enhanced differentiation of bone-resorbing osteoclasts, resulting in a rapid loss of functional trabecular bone. Bone-forming osteoblasts and osteoblast-derived osteocytes perform a key role in the regulation of osteoclast development by providing both the pro-osteoclastogenic cytokine receptor activator of NF-κB ligand (RANKL) and its natural decoy receptor osteoprotegerin (OPG). By regulating the RANKL/OPG ratio, osteoblasts hence determine the rate of both osteoclast differentiation and bone turnover. Here, we describe a novel role for liver X receptors (LXRs) during the crosstalk of bone-forming osteoblasts and bone-resorbing osteoclasts. By using a system of osteoblast/osteoclast cocultures, we identify LXRs as regulator of RANKL expression and the RANKL/OPG ratio in osteoblasts. Activation of LXRs drastically reduced the RANKL/OPG ratio and interfered with osteoblast-mediated osteoclast differentiation in vitro. During an ovariectomy (OVX)-induced model of postmenopausal osteoporosis, the application of an LXR agonist shifted the RANKL/OPG ratio in vivo, ameliorated the enhanced osteoclast differentiation, and provided complete protection from OVX-induced bone loss. These results reveal an unexpected involvement of LXRs in the regulation of bone turnover and highlight a potential role for LXRs as novel targets in the treatment of osteoporosis and related diseases.
骨质疏松症的特征是破骨细胞的分化增强,导致功能性小梁骨迅速丢失。成骨细胞和成骨细胞衍生的骨细胞在调节破骨细胞发育方面发挥着关键作用,它们通过提供破骨细胞生成细胞因子受体激活物 NF-κB 配体 (RANKL) 和其天然诱饵受体骨保护素 (OPG) 来发挥作用。通过调节 RANKL/OPG 比值,成骨细胞从而决定了破骨细胞分化和骨转换的速度。在这里,我们描述了肝 X 受体 (LXRs) 在成骨细胞和成骨细胞之间相互作用中的一个新作用。通过使用成骨细胞/破骨细胞共培养系统,我们确定 LXRs 是成骨细胞中 RANKL 表达和 RANKL/OPG 比值的调节剂。LXR 的激活大大降低了 RANKL/OPG 比值,并干扰了成骨细胞介导的体外破骨细胞分化。在去卵巢 (OVX) 诱导的绝经后骨质疏松症模型中,LXR 激动剂的应用在体内改变了 RANKL/OPG 比值,改善了增强的破骨细胞分化,并完全防止了 OVX 引起的骨丢失。这些结果揭示了 LXRs 在调节骨转换中的意外作用,并强调了 LXRs 作为骨质疏松症和相关疾病治疗的新型靶点的潜在作用。