title: Pharmacological topics of bone metabolism: a novel bisphosphonate for the treatment of periodontitis.
abstract: It 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.
authors.affiliation: Department of Applied Pharmacology, Tohoku University Graduate School of Dentistry, Sendai, Japan. shinodah@mail.tains.tohoku.ac.jp
authors.forename: Hisashi
authors.initials: H
authors.lastname: Shinoda
authors.forename: Sadaaki
authors.initials: S
authors.lastname: Takeyama
authors.forename: Keiko
authors.initials: K
authors.lastname: Suzuki
authors.forename: Shinobu
authors.initials: S
authors.lastname: Murakami
authors.forename: Shoji
authors.initials: S
authors.lastname: Yamada
mesh_terms: D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D050071:Bone Density Conservation Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D001862:Bone Resorption / Q000201:enzymology / Q000209:etiology / Q000517:prevention & control*; D051546:Cyclooxygenase 2 / Q000235:genetics / Q000378:metabolism; D003728:Dental Calculus / Q000209:etiology / Q000517:prevention & control; D015232:Dinoprostone / Q000378:metabolism; D004164:Diphosphonates / Q000008:administration & dosage / Q000627:therapeutic use*; D004195:Disease Models, Animal; D015536:Down-Regulation; D006801:Humans; D051379:Mice; D009924:Organ Culture Techniques; D010518:Periodontitis / Q000150:complications / Q000188:drug therapy* / Q000201:enzymology; D012333:RNA, Messenger / Q000378:metabolism; D051381:Rats
chemical_list: D000893:Anti-Inflammatory Agents; D050071:Bone Density Conservation Agents; D004164:Diphosphonates; D012333:RNA, Messenger; C109548:TRK 530; D051546:Cyclooxygenase 2; D015232:Dinoprostone