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Development of 1-Amino-4-(phenylamino)anthraquinone-2-sulfonate Sodium Derivatives as a New Class of Inhibitors of RANKL-Induced Osteoclastogenesis.
- Source :
-
Archiv der Pharmazie [Arch Pharm (Weinheim)] 2016 May; Vol. 349 (5), pp. 342-55. Date of Electronic Publication: 2016 Apr 13. - Publication Year :
- 2016
-
Abstract
- A series of 1-amino-4-(phenylamino)anthraquinone-2-sulfonate sodium derivatives was synthesized and evaluated for osteoclast inhibition using a TRAP-staining assay. Among them, two compounds, LCCY-13 and LCCY-15, dose-dependently suppressed receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclast formation. Moreover, the cytotoxicity assay on RAW264.7 cells suggested that the inhibition of osteoclastic bone resorption by these compounds was not a result of their cytotoxicity. Further, the inhibitory activities of compounds LCCY-13 and LCCY-15 were further confirmed by including specific inhibition of NFATc1 expression levels in nuclei using an immunofluorescent analysis. In addition, LCCY-13 and LCCY-15 also significantly attenuated the bone resorption activity of osteoclasts according to a pit formation assay. Thus, a new class of 1-amino-4-(phenylamino)anthraquinone-2-sulfonate sodium compounds might be considered as an essential lead structure for the further development of anti-resorptive agents.<br /> (© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Subjects :
- Animals
Bone Resorption
Cell Survival drug effects
Cells, Cultured
Dose-Response Relationship, Drug
Mice
NFATC Transcription Factors biosynthesis
Osteoclasts drug effects
RANK Ligand metabolism
Anthraquinones chemical synthesis
Anthraquinones pharmacology
Osteogenesis drug effects
RANK Ligand antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1521-4184
- Volume :
- 349
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Archiv der Pharmazie
- Publication Type :
- Academic Journal
- Accession number :
- 27071332
- Full Text :
- https://doi.org/10.1002/ardp.201500475