Niclosamide and its derivative DK-520 inhibit RANKL-induced osteoclastogenesis.
DK-520
Niclosamide
RANKL
differentiation
osteoclast
Journal
FEBS open bio
ISSN: 2211-5463
Titre abrégé: FEBS Open Bio
Pays: England
ID NLM: 101580716
Informations de publication
Date de publication:
08 2020
08 2020
Historique:
received:
01
11
2019
revised:
05
06
2020
accepted:
09
06
2020
pubmed:
1
7
2020
medline:
5
11
2021
entrez:
1
7
2020
Statut:
ppublish
Résumé
Niclosamide is a potent inhibitor of osteoclastogenesis and bone remodeling. DK-520 is an acyl derivative of Niclosamide and significantly increased both the plasma concentration and the duration of exposure of Niclosamide when dosed orally. However, at present the effect of DK-520 on osteoclastogenesis has not been reported. Here, we investigated whether DK-520 can regulate receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis of bone marrow macrophages (BMMs) in vitro. Following induction of BMMs with RANKL for three days, we detected differentiated osteoclasts with typical morphology and high levels of tartrate-resistant acid phosphatase (TRAP), RANKL, and cathepsin K (CTSK) expression. Treatment with either Niclosamide or DK-520 did not affect the viability of osteoclast precursors (OCPs), but significantly inhibited RANKL-induced transdifferentiation of macrophages into OCPs, particularly in the early stage of osteoclastogenesis. Both Niclosamide and DK-520 significantly decreased the relative levels of transcription factor PU.1 mRNA transcripts and dendritic cell-specific transmembrane protein (DC-STAMP), but not v-ATPasev
Identifiants
pubmed: 32602250
doi: 10.1002/2211-5463.12921
pmc: PMC7396435
doi:
Substances chimiques
Anthelmintics
0
RANK Ligand
0
Tnfsf11 protein, mouse
0
Niclosamide
8KK8CQ2K8G
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1685-1697Informations de copyright
© 2020 The Authors. Published by FEBS Press and John Wiley & Sons Ltd.
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