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.

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

  • March 2011

Published In

Volume / Issue

  • 2 / 3

Start / End Page

  • 248 - 251

PubMed ID

  • 21666868

Pubmed Central ID

  • 21666868

Electronic International Standard Serial Number (EISSN)

  • 1948-5875

International Standard Serial Number (ISSN)

  • 1948-5875

Digital Object Identifier (DOI)

  • 10.1021/ml1002794


  • eng