The Open Bioactive Compounds Journal

2009, 2 : 37-42
Published online 2009 November 26. DOI: 10.2174/1874847300902010037
Publisher ID: TOBCJ-2-37

RESEARCH ARTICLE
 Methyl Ganoderic Acid DM: A Selective Potent Osteoclastogenesis Inhibitor

Jie Liu1 , Jun Shiono1 , Yukiko Tsuji2 , Kuniyoshi Shimizu1, * and Ryuichiro Kondo1
1 Department of Forest and Forest Products Science, Faculty of Agriculture, Kyushu University, Fukuoka, 812-8581, Japan
2 Bio-Architecture Center, Kyushu University, Fukuoka, 812-8581, Japan

* Address correspondence to this author at the Department of Forest and Forest Products Science, Faculty of Agriculture, Kyushu University, Fukuoka, 812-8581, Japan; Tel: +81-92-642-3002; Fax: +81-92-642-3002; E-mail: shimizu@agr.kyushu-u.ac.jp

ABSTRACT

Increased osteoclastic bone resorption plays a central role in the pathogenesis of many bone diseases, and osteoclast inhibitors are the most widely used treatments for these diseases. Ganoderic acid DM, the main component of Ganoderma lucidum, has been known for its medicinal effects such as anti-androgen and anti-proliferative activities. In this study, we investigated the inhibitory effects of ganoderic acid DM and its analog (methyl ganoderic acid DM and 7-oxo-methyl ganoderic acid Z) on osteoclastogenesis using RAW264 cell in vitro. Methyl ganoderic acid DM blocked osteoclastogenesis completely at 12.5 μM with low cytotoxicity less than 30%. On the other hands, ganoderic acid DM blocked osteoclastogenesis completely at the higher concentration of 50 μM, but 7-oxo-methyl ganoderic acid Z did not up to 100 μM. These results implicated the carbonyl group at C-3 is essentially for selective osteoclastogenesis inhibitory activity, and methyl esters at C-26 should play an important role in enhancing its osteoclastogenesis inhibitory activity

Keyword:

, methyl ganoderic acid DM, osteoporosis, rheumatoid arthritis.