Morichika Takita
   Department   School of Medicine, School of Medicine
   Position   Assistant Professor
Article types Original article
Language English
Peer review Peer reviewed
Title A novel carborane analog, BE360, with a carbon-containing polyhedral boron-cluster is a new selective estrogen receptor modulator for bone.
Journal Formal name:Biochemical and Biophysical Research Commmunications
Abbreviation:Biochem. Biophys. Res. Commn.
ISSN code:0006291X
Domestic / ForeginForegin
Publisher Elsevier
Volume, Issue, Page 380,pp.218-222
Author and coauthor Hirata Michiko†, Inada Masaki, Matsumoto Chiho, Takita Morichika, Ogawa Takumi, Endo Yasuyuki, Miyaura Chisato*
Publication date 2009/01
Summary Carboranes are a class of carbon-containing polyhedral boron-cluster compounds with globular geometry and hydrophobic surface that interact with hormone receptors. Estrogen deficiency results in marked bone loss due to increased osteoclastic bone resorption in females, but estrogen replacement therapy is not generally used for postmenopausal osteoporosis due to the risk of uterine cancer. We synthesized a novel carborane compound BE360 to clarify its anti-osteoporosis activity. BE360 showed a high binding affinity to estrogen receptors (ER), ERalpha and ERbeta. In ovariectomized (OVX) mice, femoral bone volume was markedly reduced and BE360 dose-dependently restored bone loss in OVX mice. However, BE360 did not exhibit any estrogenic activity in the uterus. BE360 also restored bone loss in orchidectomized mice without androgenic action in the sex organs. Therefore, BE360 is a novel selective estrogen receptor modulator (SERM) that may offer a new therapy option for osteoporosis.
DOI 10.1016/j.bbrc.2009.01.033
PMID 19159615