Department of Immunology, Forsyth Institute, Cambridge, MA 02142, USA.
Exp Cell Res. 2011 Jun 10;317(10):1454-64. doi: 10.1016/j.yexcr.2011.03.014. Epub 2011 Mar 21.
Tetracycline antibiotics, including doxycycli\e (DOX), have been used to treat bone resorptive diseases, partially because of their activity to suppress osteoclastogenesis induced by receptor activator of nuclear factor kappa B ligand (RANKL). However, their precise inhibitory mechanism remains unclear. Therefore, the present study examined the effect of Dox on osteoclastogenesis signaling induced by RANKL, both in vitro and in vivo. Although Dox inhibited RANKL-induced osteoclastogenesis and down-modulated the mRNA expression of functional osteoclast markers, including tartrate-resistant acid phosphatase (TRAP) and cathepsin K, Dox neither affected RANKL-induced MAPKs phosphorylation nor NFATc1 gene expression in RAW264.7 murine monocytic cells. Gelatin zymography and Western blot analyses showed that Dox down-regulated the enzyme activity of RANKL-induced MMP-9, but without affecting its protein expression. Furthermore, MMP-9 enzyme inhibitor also attenuated both RANKL-induced osteoclastogenesis and up-regulation of TRAP and cathepsin K mRNA expression, indicating that MMP-9 enzyme action is engaged in the promotion of RANKL-induced osteoclastogenesis. Finally, Dox treatment abrogated RANKL-induced osteoclastogenesis and TRAP activity in mouse calvaria along with the suppression of MMP9 enzyme activity, again without affecting the expression of MMP9 protein. These findings suggested that Dox inhibits RANKL-induced osteoclastogenesis by its inhibitory effect on MMP-9 enzyme activity independent of the MAPK-NFATc1 signaling cascade.
四环素类抗生素,包括强力霉素(DOX),已被用于治疗骨吸收性疾病,部分原因是其抑制核因子κB 受体激活物配体(RANKL)诱导的破骨细胞生成的活性。然而,其确切的抑制机制尚不清楚。因此,本研究在体外和体内研究了 DOX 对 RANKL 诱导的破骨细胞生成信号的影响。尽管 DOX 抑制了 RANKL 诱导的破骨细胞生成,并下调了功能性破骨细胞标志物(包括抗酒石酸酸性磷酸酶(TRAP)和组织蛋白酶 K)的 mRNA 表达,但 DOX 既不影响 RANKL 诱导的 MAPKs 磷酸化,也不影响 RAW264.7 鼠单核细胞中 NFATc1 基因的表达。明胶酶谱和 Western blot 分析表明,DOX 下调了 RANKL 诱导的 MMP-9 的酶活性,但不影响其蛋白表达。此外,MMP-9 酶抑制剂也减弱了 RANKL 诱导的破骨细胞生成和 TRAP 和组织蛋白酶 K mRNA 表达的上调,表明 MMP-9 酶的作用参与了 RANKL 诱导的破骨细胞生成的促进。最后,DOX 处理消除了 RANKL 诱导的小鼠颅骨破骨细胞生成和 TRAP 活性,同时抑制了 MMP9 酶活性,而不影响 MMP9 蛋白的表达。这些发现表明,DOX 通过抑制 MMP-9 酶活性而非 MAPK-NFATc1 信号级联来抑制 RANKL 诱导的破骨细胞生成。
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