In vitro and in vivo osteogenic activity of largazole

Journal Article

Due to their capability of modifying chromatin structure and thereby regulating gene transcription, histone deacetylases (HDACs) have been reported to play important roles in osteogenesis and considered a promising potential therapeutic target for bone diseases, including osteoporosis. We showed that the novel marine-derived HDAC inhibitor largazole exhibits in vitro and in vivo osteogenic activity. Largazole significantly induced the expression of ALP and OPN. The osteogenic activity of largazole was mediated through the increased expression of Runx2 and BMPs. Importantly, largazole showed in vivo bone-forming efficacy in the mouse calvarial bone formation assay and the rabbit calvarial bone fracture healing model. The dual action of largazole to stimulate bone formation and inhibit bone resorption would be a useful feature in drug development for bone-related disorders. © 2011 American Chemical Society.

Full Text

Duke Authors

Cited Authors

  • Lee, S-U; Kwak, HB; Pi, S-H; You, H-K; Byeon, SR; Ying, Y; Luesch, H; Hong, J; Kim, SH

Published Date

  • 2011

Published In

Volume / Issue

  • 2 / 3

Start / End Page

  • 248 - 251

PubMed ID

  • 21666868

International Standard Serial Number (ISSN)

  • 1948-5875

Digital Object Identifier (DOI)

  • 10.1021/ml1002794