Department of Medicine, Unit of Andrology and Reproductive Medicine, University of Padova, Padova, Italy.
Department of Biochemistry and Microbiology, Faculty of Pharmacy, Damascus University, Damascus, Syrian Arab Republic.
Protein Pept Lett. 2020;27(12):1268-1275. doi: 10.2174/0929866527666200505220459.
During the last decade, the disclosure of systemic effects of osteocalcin (OCN) in its undercarboxylated form contributed to switch the concept of bone from a merely structural apparatus to a fully endocrine organ involved in the regulation of systemic functions. Since that time, the role of OCN as osteokine has been more and more widened appreciated and detailed by the major use of animal models, starting from the original function in the bone extracellular matrix as Gla-protein and spanning from the protective effects towards weight gain, insulin sensitivity and glucose homeostasis, to the anabolic and metabolic roles in skeletal muscle, to the stimulating effects on the testis endocrine function and male fertility, to the most recent preservation from anxious and depressive states through a direct activity on the central nervous system. In this review, experimental data supporting the inter-organ communication roles of this protein are discussed, together with the available data supporting the consistency between experimental data obtained in animals and those reported in humans. In addition, a specific session has been devoted to the possible significance the OCN as a template agonist on its receptor GPRC6A, for the development of novel therapeutic and pharmacological approaches for the treatment of dismetabolic states and male infertility.
在过去的十年中,骨钙素(OCN)未羧化形式的系统性作用的揭示促使人们将骨骼的概念从单纯的结构器官转变为一个涉及全身功能调节的完整内分泌器官。自那时以来,OCN 作为骨钙素的作用通过动物模型的广泛应用得到了越来越多的认可和详细研究,其功能从骨细胞外基质中的 Gla-蛋白的原始功能开始,涵盖了对体重增加、胰岛素敏感性和葡萄糖稳态的保护作用,到在骨骼肌中的合成代谢和代谢作用,再到对睾丸内分泌功能和男性生育能力的刺激作用,以及通过对中枢神经系统的直接作用,最近还发现了其对焦虑和抑郁状态的保护作用。在这篇综述中,讨论了支持这种蛋白质在器官间通讯中的作用的实验数据,以及支持动物实验数据与人类报告数据之间一致性的数据。此外,还专门讨论了 OCN 作为其受体 GPRC6A 的模板激动剂的可能意义,这为治疗代谢紊乱和男性不育的新型治疗和药理学方法的发展提供了可能。