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Acredinone C and the Effect of Acredinones on Osteoclastogenic and Osteoblastogenic Activity

Yeon, Jeong-Tae, Kim, Hiyoung, Kim, Kwang-Jin, Lee, Jihye, Won, Dong Hwan, Nam, Sang-Jip, Kim, Seong Hwan, Kang, Heonjoong, Son, Young-Jin
Journal of natural products 2016 v.79 no.7 pp. 1730-1736
benzophenones, transcription factor NF-kappa B, osteoclasts, nuclear magnetic resonance spectroscopy, dose response, xanthone, cytotoxicity, ligands, bone formation, osteoblasts, Acremonium, spectral analysis, culture media, animal disease models, fungi
A new inhibitor, acredinone C (1), of receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclast differentiation was isolated from the culture broth of the fungus Acremonium sp. (F9A015) along with acredinones A (2) and B (3). The structure of acredinone C (1), which incorporates benzophenone and xanthone moieties, was established by the analyses of combined spectroscopic data including 1D and 2D NMR and MS. All of the acredinones studied efficiently inhibited the RANKL-induced formation of TRAP⁺-MNCs in a dose-dependent manner without any cytotoxicity up to 10 μM. Acredinone A showed dual activity in both osteoclast and osteoblast differentiation in vitro and good efficacy in an animal disease model of bone formation.