Novel bromomelatonin derivatives suppress osteoclastic activity and increase osteoblastic activity: Implications for the treatment of bone diseases

フォーマット:

論文

責任表示:

Suzuki, Nobuo ; Somei, Masanori ; Kitamura, Keiichiro ; Reiter, Russel J. ; Hattori, Atsuhiko

言語:

英語

出版情報:

Blackwell Publishing, 2008-04-01

著者名:

• Suzuki, Nobuo
• Somei, Masanori
• Kitamura, Keiichiro
• Reiter, Russel J.
• Hattori, Atsuhiko

掲載情報:

Journal of Pineal Research

ISSN:

0742-3098      

巻:

44

通号:

3

開始ページ:

326

終了ページ:

334

バージョン:

author

概要:

金沢大学環日本海域環境研究センター生物多様性研究部門<br />The teleost scale is a calcified tissue that contains osteoclasts, osteoblasts, and bone matrix, all of which are similar to those found in mammalian membrane bone. Using the goldfish scale, we recently … developed a new in vitro assay system and previously demonstrated that melatonin suppressed both osteoclastic and osteoblastic activities in this assay system. In mammals, 2-bromomelatonin possesses a higher affinity for the melatonin receptor than does melatonin. Using a newly developed synthetic method, we synthesized 2-bromomelatonin, 2,4,6-tribromomelatonin and novel bromomelatonin derivatives (1-allyl-2,4,6-tribromomelatonin, 1-propargyl-2,4,6-tribromomelatonin, 1-benzyl-2,4,6-tribromomelatonin, and 2,4,6,7-tetrabromomelatonin) and then examined the effects of these chemicals on osteoclasts and osteoblasts. All bromomelatonin derivatives, as well as melatonin, had an inhibitory action on osteoclasts. In particular, 1-benzyl-2,4,6-tribromomelatonin (benzyl-tribromomelatonin) possessed a stronger activity than melatonin. At an in vitro concentration of 10-10 m, benzyl-tribromomelatonin still suppressed osteoclastic activity after 6 hr of incubation. In reference to osteoblasts, all bromomelatonin derivatives had a stimulatory action, although melatonin inhibited osteoblastic activity. In addition, estrogen receptor mRNA expression (an osteoblastic marker) was increased in benzyl-tribromomelatonin (10-7 m)-treated scales. Taken together, the present results strongly suggest that these novel melatonin derivatives have significant potential for use as beneficial drug for bone diseases such as osteoporosis. © 2007 The Authors. 全文公開200904 続きを見る

URL:

http://hdl.handle.net/2297/17120