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Pharmacological topics of bone metabolism: a novel bisphosphonate for the treatment of periodontitis Shinoda H; Takeyama S; Suzuki K; Murakami S; Yamada SJ Pharmacol Sci 2008[Apr]; 106 (4): 555-8It has been reported that the pharmacological characteristics of bisphosphonates vary depending on the side chain attached to the carbon atom of the P-C-P bond. TRK-530 is a novel synthetic bisphosphonate with an anti-oxidant methylthio-phenylthio side chain. This compound has been suggested to have both anti-inflammatory and anti-bone-resorbing effects. Such a compound could be effective for the treatment of diseases with excessive bone resorption accompanied by inflammation. We have been studying this compound as a potential therapeutic agent for periodontitis. To date, we have found that 1) TRK-530 inhibited osteoclastic bone resorption in animals and in bone organ culture, 2) both systemic and topical administration of TRK-530 prevented alveolar bone loss in animals with experimental periodontitis, 3) TRK-530 prevented prostaglandin E(2) synthesis by inhibiting the expression of cyclooxygenase (COX)-2 mRNA, and 4) TRK-530 inhibited the formation of dental calculus. The above results suggest that TRK-530 might be useful for the treatment of alveolar bone loss in periodontitis.|Administration, Topical[MESH]|Animals[MESH]|Anti-Inflammatory Agents/administration & dosage/*therapeutic use[MESH]|Bone Density Conservation Agents/administration & dosage/*therapeutic use[MESH]|Bone Resorption/enzymology/etiology/*prevention & control[MESH]|Cyclooxygenase 2/genetics/metabolism[MESH]|Dental Calculus/etiology/prevention & control[MESH]|Dinoprostone/metabolism[MESH]|Diphosphonates/administration & dosage/*therapeutic use[MESH]|Disease Models, Animal[MESH]|Down-Regulation[MESH]|Humans[MESH]|Mice[MESH]|Organ Culture Techniques[MESH]|Periodontitis/complications/*drug therapy/enzymology[MESH]|RNA, Messenger/metabolism[MESH]|Rats[MESH] |
