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5-Lipoxygenase inhibitors suppress RANKL-induced osteoclast formation via NFATc1 expression

Title
5-Lipoxygenase inhibitors suppress RANKL-induced osteoclast formation via NFATc1 expression
Authors
Kang, Ju-HeeTing, ZhengMoon, Mi-ranSim, Jung-SeonLee, Jung-MinDoh, Kyung-EunHong, SunhyeCui, MinghuaChoi, SunChang, Hyeun WookChoo, Hea-Young ParkYim, Mijung
Ewha Authors
박혜영최선
SCOPUS Author ID
박혜영scopus; 최선scopus
Issue Date
2015
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN
0968-0896JCR Link1464-3391JCR Link
Citation
vol. 23, no. 21, pp. 7069 - 7078
Keywords
5-LipoxygenaseBenzoxazole scaffoldRANKL-induced osteoclast formationNFATc1Lipopolysaccharide (LPS)-induced osteoclast formation
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
5-Lipoxygenase synthesizes leukotrienes from arachidonic acid. We developed three novel 5-LO inhibitors having a benzoxazole scaffold as a potential anti-osteoclastogenics. They significantly suppressed RANKL-induced osteoclast formation in mouse bone marrow-derived macrophages. Furthermore, one compound, K7, inhibited the bone resorptive activity of osteoclasts. The anti-osteoclastogenic effect of K7 was mainly attributable to reduction in the expression of NFATc1, an essential transcription factor for osteoclast differentiation. K7 inhibited osteoclast formation via ERR and p38 MAPK, as well as NF-kappa B signaling pathways. K7 reduced lipopolysaccharide (LPS)-induced osteoclast formation in vivo, corroborating the in vitro data. Thus, K7 exerted an inhibitory effect on osteoclast formation in vitro and in vivo, properties that make it a potential candidate for the treatment of bone diseases associated with excessive bone resorption. (C) 2015 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2015.09.025
Appears in Collections:
약학대학 > 약학과 > Journal papers
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