Wang Lin, Mao Yu-Jia, Wang Wen-Jie
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union, Medical College, Beijing 100050, China.
Yao Xue Xue Bao. 2006 Jun;41(6):555-60.
To study the inhibitory action of diacerein on the formation of osteoclasts (OCLs) and their activity in bone resorption as well as the relationship between this action and the expression of osteoprotegerin (OPG) and receptor activator of NF-kappaB ligand (RANKL) in MC3T3-E1 cells.
A coculture system constituted with MC3T3-E1 cells and bone marrow cells for osteoclasts formation was established in vitro. TRAP-positive and multinucleated cells with three or more nuclei in each cell were counted as osteoclasts and the number of pits formed on the dentine slices was determined to judge the activity of osteoclasts. Western blotting, RT-PCR and flow cytometer were used to detect the expression of OPG and RANKL in MC3T3-E1 cells.
Diacerein significantly inhibited the formation and function of the cultured osteoclasts stimulated by IL-1beta. sRANKL could reverse the effect of diacerein. Diacerein inhibited protein and mRNA expression of RANKL but enhanced those of OPG in MC3T3-E1 cells.
Diacerein may inhibit osteoclastic bone destruction through the inhibition of RANKL expression and the increase of OPG expression in MC3T3-E1 cells.
研究双醋瑞因对破骨细胞（OCLs）形成及其骨吸收活性的抑制作用，以及该作用与MC3T3-E1细胞中骨保护素（OPG）和核因子κB受体活化因子配体（RANKL）表达之间的关系。
体外建立由MC3T3-E1细胞和骨髓细胞组成的用于破骨细胞形成的共培养体系。将每个细胞中含有三个或更多核的抗酒石酸酸性磷酸酶（TRAP）阳性多核细胞计为破骨细胞，并测定牙本质切片上形成的凹坑数量以判断破骨细胞的活性。采用蛋白质免疫印迹法、逆转录-聚合酶链反应（RT-PCR）和流式细胞仪检测MC3T3-E1细胞中OPG和RANKL的表达。
双醋瑞因显著抑制白细胞介素-1β（IL-1β）刺激的培养破骨细胞的形成和功能。可溶性RANKL（sRANKL）可逆转双醋瑞因的作用。双醋瑞因抑制MC3T3-E1细胞中RANKL的蛋白质和mRNA表达，但增强OPG的表达。
双醋瑞因可能通过抑制MC3T3-E1细胞中RANKL的表达和增加OPG的表达来抑制破骨细胞性骨破坏。
