Department of Comparative Biomedical Sciences, The Royal Veterinary College, London, United Kingdom.
Department of Comparative Biomedical Sciences, The Royal Veterinary College, London, United Kingdom; Experimental Histopathology, The Francis Crick Institute, London, United Kingdom.
Am J Pathol. 2019 Apr;189(4):753-761. doi: 10.1016/j.ajpath.2018.12.007. Epub 2019 Jan 19.
Glucocorticoid-induced secondary osteoporosis is the most predictable side effect of this anti-inflammatory. One of the main mechanisms by which glucocorticoids achieve such deleterious outcome in bone is by antagonizing Wnt/β-catenin signaling. Sclerostin, encoded by Sost gene, is the main negative regulator of the proformative and antiresorptive role of the Wnt signaling pathway in the skeleton. It was hypothesized that the partial inactivation of sclerostin function by genetic manipulation will rescue the osteopenia induced by high endogenous glucocorticoid levels. Sost-deficient mice were crossed with an established mouse model of excess glucocorticoids, and the effects on bone mass and structure were evaluated. Sost haploinsufficiency did not rescue the low bone mass induced by high glucocorticoids. Intriguingly, the critical manifestation of Sost deficiency combined with glucocorticoid excess was sporadic, sudden, unprovoked, and nonconvulsive death. Detailed histopathologic analysis in a wide range of tissues identified peracute hemopericardium and cardiac tamponade to be the cause. These preclinical studies reveal outcomes with direct relevance to ongoing clinical trials that explore the use of antisclerostin antibodies as a treatment for osteoporosis. They particularly highlight a potential for increased cardiovascular risk and may inform improved stratification of patients who might otherwise benefit from antisclerostin antibody treatment.
糖皮质激素诱导的继发性骨质疏松症是这种抗炎药最可预测的副作用。糖皮质激素在骨骼中产生这种有害后果的主要机制之一是拮抗 Wnt/β-连环蛋白信号。骨硬化蛋白(由 Sost 基因编码)是 Wnt 信号通路在骨骼中促进形成和抗吸收作用的主要负调节剂。据推测,通过遗传操作部分失活骨硬化蛋白的功能将挽救由内源性糖皮质激素水平升高引起的骨质疏松症。Sost 缺陷型小鼠与过量糖皮质激素的已建立的小鼠模型杂交,并评估其对骨量和结构的影响。Sost 杂合不足不能挽救由高糖皮质激素引起的低骨量。有趣的是,Sost 缺乏与糖皮质激素过量结合的关键表现是偶发性、突发性、无诱因和非惊厥性死亡。在广泛的组织中进行详细的组织病理学分析确定为急性血性心包积液和心脏压塞。这些临床前研究揭示了与正在探索使用抗骨硬化蛋白抗体作为骨质疏松症治疗的临床试验具有直接相关性的结果。它们特别强调了心血管风险增加的可能性,并可能为那些可能受益于抗骨硬化蛋白抗体治疗的患者提供更好的分层。