Shao Yu, Hernandez-Buquer Selene, Childress Paul, Stayrook Keith R, Alvarez Marta B, Davis Hannah, Plotkin Lilian I, He Yongzheng, Condon Keith W, Burr David B, Warden Stuart J, Robling Alexander G, Yang Feng-Chun, Wek Ronald C, Allen Matthew R, Bidwell Joseph P
Department of Medical and Molecular Genetics, Indiana University School of Medicine, Indianapolis, Indiana 46202.
Department of Anatomy and Cell Biology, Indiana University School of Medicine, Indianapolis, Indiana 46202.
Endocrinology. 2017 Sep 1;158(9):2722-2740. doi: 10.1210/en.2017-00355.
Combining anticatabolic agents with parathyroid hormone (PTH) to enhance bone mass has yielded mixed results in osteoporosis patients. Toward the goal of enhancing the efficacy of these regimens, we tested their utility in combination with loss of the transcription factor Nmp4 because disabling this gene amplifies PTH-induced increases in trabecular bone in mice by boosting osteoblast secretory activity. We addressed whether combining a sustained anabolic response with an anticatabolic results in superior bone acquisition compared with PTH monotherapy. Additionally, we inquired whether Nmp4 interferes with anticatabolic efficacy. Wild-type and Nmp4-/- mice were ovariectomized at 12 weeks of age, followed by therapy regimens, administered from 16 to 24 weeks, and included individually or combined PTH, alendronate (ALN), zoledronate (ZOL), and raloxifene (RAL). Anabolic therapeutic efficacy generally corresponded with PTH + RAL = PTH + ZOL > PTH + ALN = PTH > vehicle control. Loss of Nmp4 enhanced femoral trabecular bone increases under PTH + RAL and PTH + ZOL. RAL and ZOL promoted bone restoration, but unexpectedly, loss of Nmp4 boosted RAL-induced increases in femoral trabecular bone. The combination of PTH, RAL, and loss of Nmp4 significantly increased bone marrow osteoprogenitor number, but did not affect adipogenesis or osteoclastogenesis. RAL, but not ZOL, increased osteoprogenitors in both genotypes. Nmp4 status did not influence bone serum marker responses to treatments, but Nmp4-/- mice as a group showed elevated levels of the bone formation marker osteocalcin. We conclude that the heightened osteoanabolism of the Nmp4-/- skeleton enhances the effectiveness of diverse osteoporosis treatments, in part by increasing hyperanabolic osteoprogenitors. Nmp4 provides a promising target pathway for identifying barriers to pharmacologically induced bone formation.
在骨质疏松症患者中,将抗分解代谢药物与甲状旁腺激素(PTH)联合使用以增加骨量,结果喜忧参半。为了提高这些治疗方案的疗效,我们测试了它们与转录因子Nmp4缺失联合使用的效用,因为使该基因失活可通过增强成骨细胞分泌活性来放大PTH诱导的小鼠小梁骨增加。我们探讨了与PTH单一疗法相比,将持续的合成代谢反应与抗分解代谢作用相结合是否能带来更好的骨量增加。此外,我们还研究了Nmp4是否会干扰抗分解代谢疗效。野生型和Nmp4基因敲除小鼠在12周龄时进行卵巢切除术,随后在16至24周期间给予治疗方案,包括单独或联合使用PTH、阿仑膦酸盐(ALN)、唑来膦酸盐(ZOL)和雷洛昔芬(RAL)。合成代谢治疗效果一般为PTH + RAL = PTH + ZOL > PTH + ALN = PTH > 载体对照。Nmp4缺失增强了PTH + RAL和PTH + ZOL治疗下股骨小梁骨的增加。RAL和ZOL促进了骨修复,但出乎意料的是,Nmp4缺失增强了RAL诱导的股骨小梁骨增加。PTH、RAL和Nmp4缺失的联合使用显著增加了骨髓骨祖细胞数量,但不影响脂肪生成或破骨细胞生成。RAL增加了两种基因型的骨祖细胞,但ZOL没有。Nmp4状态不影响骨血清标志物对治疗的反应,但作为一个群体的Nmp4基因敲除小鼠显示骨形成标志物骨钙素水平升高。我们得出结论,Nmp4基因敲除小鼠骨骼中增强的骨合成代谢提高了多种骨质疏松症治疗的有效性,部分原因是增加了高合成代谢的骨祖细胞。Nmp4为识别药理学诱导骨形成的障碍提供了一个有前景的靶标途径。