Research Centre for Regenerative Medicine, Department of Orthopaedics, The First Affiliated Hospital of Guangxi Medical University, Nanning, Guangxi 530021, P.R. China.
School of Biomedical Sciences, The University of Western Australia, Perth 6009, Australia.
Int J Mol Med. 2023 May;51(5). doi: 10.3892/ijmm.2023.5246. Epub 2023 Apr 13.
Postmenopausal osteoporosis is a systemic metabolic disease that chronically endangers public health and is typically characterized by low bone mineral density and marked bone fragility. The excessive bone resorption activity of osteoclasts is a major factor in the pathogenesis of osteoporosis; therefore, strategies aimed at inhibiting osteoclast activity may prevent bone decline and attenuate the process of osteoporosis. Casticin (Cas), a natural compound, has anti‑inflammatory and antitumor properties. However, the role of Cas in bone metabolism remains largely unclear. The present study found that the receptor activator of nuclear factor‑κΒ (NF‑κB) ligand‑induced osteoclast activation and differentiation were inhibited by Cas. Tartrate‑resistant acid phosphatase staining revealed that Cas inhibited osteoclast differentiation, and bone resorption pit assays demonstrated that Cas affected the function of osteoclasts. Cas significantly reduced the expression of osteoclast‑specific genes and related proteins, such as nuclear factor of activated T cells, cytoplasmic 1 and c‑Fos at the mRNA and protein level in a concentration‑dependent manner. Cas inhibited osteoclast formation by blocking the AKT/ERK and NF‑κB signaling pathways, according to the intracellular signaling analysis. The microcomputed tomography and tissue staining of tibiae from ovariectomized mice revealed that Cas prevented the bone loss induced by estrogen deficiency and reduced osteoclast activity in vivo. Collectively, these findings indicated that Cas may be used to prevent osteoporosis.
绝经后骨质疏松症是一种慢性危害公众健康的系统性代谢疾病,其特征通常为骨矿物质密度降低和明显的骨骼脆弱。破骨细胞的过度骨吸收活性是骨质疏松症发病机制的一个主要因素;因此,旨在抑制破骨细胞活性的策略可能预防骨量下降并减轻骨质疏松症的进程。紫铆因(Cas)是一种天然化合物,具有抗炎和抗肿瘤特性。然而,Cas 在骨代谢中的作用在很大程度上仍不清楚。本研究发现,Cas 抑制核因子-κB 受体激活剂(NF-κB)配体诱导的破骨细胞激活和分化。酒石酸抗性酸性磷酸酶染色显示 Cas 抑制破骨细胞分化,骨吸收陷窝试验表明 Cas 影响破骨细胞的功能。Cas 显著降低了破骨细胞特异性基因和相关蛋白的表达,如核因子活化 T 细胞、细胞质 1 和 c-Fos,在 mRNA 和蛋白水平上呈浓度依赖性。根据细胞内信号分析,Cas 通过阻断 AKT/ERK 和 NF-κB 信号通路抑制破骨细胞的形成。卵巢切除小鼠的胫骨微计算机断层扫描和组织染色显示,Cas 可预防雌激素缺乏引起的骨丢失,并降低体内破骨细胞的活性。综上所述,这些发现表明 Cas 可用于预防骨质疏松症。