A novel carborane analog, BE360, with a carbon-containing polyhedral boron-cluster is a new selective estrogen receptor modulator for bone

作者：Hirata Michiko; Inada Masaki; Matsumoto Chiho; Takita Morichika; Ogawa Takumi; Endo Yasuyuki; Miyaura Chisato^*

来源：Biochemical and Biophysical Research Communications, 2009, 380(2): 218-222.

DOI：10.1016/j.bbrc.2009.01.033

• Osteoporosis
• Bone mass
• Carborane compound
• Ovariectomized mice
• Selective estrogen receptor modulator
• Estrogen

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-osteoporsis activity. BE360 showed a high binding affinity to estrogen receptors (ER), ER alpha. and ER beta. 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.

• 出版日期2009-3-6