[Inhibitory effect of diacerein on osteoclastic bone destruction and its possible mechanism of action].
OBJECTIVE
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.


METHODS
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.


RESULTS
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.


CONCLUSIONS
Diacerein may inhibit osteoclastic bone destruction through the inhibition of RANKL expression and the increase of OPG expression in MC3T3-E1 cells.
Wang
Lin
L
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union, Medical College, Beijing 100050, China.
Mao
Yu-Jia
YJ
Wang
Wen-Jie
WJ
D000818:Animals; D000831:Animals, Newborn; D000880:Anthraquinones / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D001854:Bone Marrow Cells / Q000502:physiology; D001862:Bone Resorption; D002460:Cell Line; D018920:Coculture Techniques; D051379:Mice; D008810:Mice, Inbred C57BL; D010006:Osteoblasts / Q000166:cytology / Q000378:metabolism* / Q000502:physiology; D010010:Osteoclasts / Q000502:physiology*; D053244:Osteoprotegerin / Q000096:biosynthesis* / Q000235:genetics; D053245:RANK Ligand / Q000096:biosynthesis* / Q000235:genetics; D012333:RNA, Messenger / Q000096:biosynthesis / Q000235:genetics
D000880:Anthraquinones; D000893:Anti-Inflammatory Agents; D053244:Osteoprotegerin; D053245:RANK Ligand; D012333:RNA, Messenger; C025292:diacerein