Analysis of bone selective estrogen and androgen receptor modulators.

• Project/Area Number: 22790062
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: Biological pharmacy
• Research Institution: Tokyo University of Agriculture and Technology
• Principal Investigator: HIRATA Michiko 東京農工大学, 大学院・工学研究院, 助教 (40544060)
• Project Period (FY): 2010 – 2011
• Project Status: Completed (Fiscal Year 2011)
• Budget Amount: ¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000); Fiscal Year 2011: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000); Fiscal Year 2010: ¥2,990,000 (Direct Cost: ¥2,300,000、Indirect Cost: ¥690,000)
• Keywords: 骨粗鬆症 / エストロゲン / アンドロゲン / 受容体作働薬

Research Abstract

Bone remodeling is regulated by osteoclastic bone resorption and new bone formation. Estrogen deficiency induced by menopause results in marked bone loss in women. The elderly men exhibit marked bone loss due to androgen deficiency. We developed the new anti-osteoporosis drugs with minimal undesired effects on reproductive tissues. Carboranes restored bone loss in ovariectomized mice and orchidectomized mice without estrogenic activity or androgenic action in the sex organs. Therefore, Carboranes are novel selective estrogen receptor modulators(SERM) that may offer a new therapy option for osteoporosis.

Research Products

• [Journal Article] Polymethoxy flavonoids, nobiletin and tangeretin, prevent lipopolysaccharide-induced inflammatory bone loss in an experimental model for periodontitis (2012)
  • Author(s): Tominari T, Hirata M, Matsumoto C, Inada M, Miyaura C
  • Journal Title: J. Pharmacol. Sci Volume: (印刷中)
  • NAID: 10031071717
  • Peer Reviewed
• [Journal Article] The correlation between postmenopausal osteoporosis and inflammatory periodontitis regarding bone loss in experimental models (2012)
  • Author(s): Kobayashi M, Matsumoto C, Hirata M, Tominari T, Inada M and Miyaura C
  • Journal Title: Exp. Anim Volume: 61(2) Pages: 183-187
  • NAID: 10030556018
  • Peer Reviewed
• [Journal Article] Capsaicin, a TRPV1 ligand, suppresses boneresorption n by inhibiting theprostaglandin E production of osteoblasts, and attenuates the inflammatory bone loss induced by lipopolysaccharide (2012)
  • Author(s): Kobayashi M, Watanabe K, Yokoyama S, Matsumoto C, Hirata M, Tominari T, Inada M and Miyaura C
  • Journal Title: ISRN. Phamacol Volume: 2012 Pages: 439860-439860
  • DOI: 10.5402/2012/439860
  • Peer Reviewed
• [Journal Article] Polymethoxy flavonoids, nobiletin and tangeretin, prevent lipopolysaccharide-induced inflammatory bone loss in an experimental model for periodontitis (2012)
  • Author(s): Tominari T
  • Journal Title: J.Pharmacol.Sci Volume: (印刷中)
  • Peer Reviewed
• [Journal Article] The correlation between postmenopausal osteoporosis and inflammatory periodontitis regarding bone loss in experimental models (2012)
  • Author(s): Kobayashi M
  • Journal Title: Exp.Anim Volume: 61(2) Pages: 183-187
  • Peer Reviewed
• [Journal Article] Nobiletin, a polymethoxy flavonoid, suppresses bone resorption by inhibiting NFκB-dependent prostaglandin E synthesis in osteoblasts, and prevents bone loss due to estrogen deficiency (2011)
  • Author(s): Harada S, Tominari T, Matsumoto C, Hirata M, Takita M, Inada M, Miyaura C
  • Journal Title: J. Pharmacol. Sci Volume: 115(1) Pages: 89-93
  • NAID: 10029891678
  • Peer Reviewed
• [Journal Article] Nobiletin, a polymethoxy flavonoid, suppresses bone resorption by inhibiting NF κ B-dependent prostagland in E synthesis in osteoblasts, and prevents bone loss due to estrogen deficiency. (2011)
  • Author(s): Harada S
  • Journal Title: J.Pharmacol.Sci. Volume: 115 Pages: 89-93
  • Peer Reviewed
• [Journal Article] Cell Shape and Matrix Production of Fibroblasts cultured on fibroin-organized scaffold with type-II-turn structured(Ala-Gly-Ala-Gly-Ser-Gly) n sequences (2010)
  • Author(s): Hirata M, Kobayashi M, Matsumoto C, Miyaura C, Asakura T, Inada M
  • Journal Title: J. Health Sci Volume: 56(6) Pages: 738-744
  • Peer Reviewed
• [Journal Article] Cell Shape and Matrix Production of Fibroblasts cultured on fibroin-organized scaffold with type-II -turn structured (Ala-Gly-Ala-Gly-Ser-Gly)_n sequences. (2010)
  • Author(s): Hirata M
  • Journal Title: J.Health Sci. Volume: 56 Pages: 1-7
  • Peer Reviewed
• [Presentation] Toll-like receptor 2へテロ受容体(TLR1/2, TLR 2/6)シグナルによる炎症性骨吸収の亢進 (2011)
  • Author(s): 松本千穂
  • Organizer: 第29回日本骨代謝学会学術集会
  • Place of Presentation: 大阪国際会議場(大阪府)
  • Year and Date: 2011-07-30
• [Presentation] Toll-like receptor 2ヘテロ受容体(TLR1/2,TLR2/6)シグナルによる炎症性骨吸収の亢進 (2011)
  • Author(s): 松本千穂
  • Organizer: 第29回日本骨代謝学会学術集会
  • Place of Presentation: 大阪国際会議場(大阪府)
  • Year and Date: 2011-07-30
• [Presentation] β-Cryptoxanthin, A Citrus Xanthophyl Carotenoid Prevents Inflammatory Bone Loss of Alveolar Bone in the Model for Periodontal Disease (2011)
  • Author(s): Hirata M
  • Organizer: American Society For Bone and Mineral Research 2011
  • Place of Presentation: California, USA
• [Presentation] Toll-like Receptor 2 Heterodimer, TLR1/2 and TLR2/6, Induces Inflammatory Bone Loss via PGE2 Production by Osteoblasts (2011)
  • Author(s): Matsumoto C
  • Organizer: American Society For Bone and Mineral Research 2011
  • Place of Presentation: California, USA
• [Presentation] Daidzeinの皮膚細胞に対する生理活性 (2011)
  • Author(s): 高木梨名
  • Organizer: 第84回日本生化学会大会
  • Place of Presentation: 国立京都国際会館(京都府)
• [Presentation] ビタミンD3の脂肪細胞分化への影響 (2011)
  • Author(s): 青木崇史
  • Organizer: 第84回日本生化学会大会
  • Place of Presentation: 国立京都国際会館(京都府)
• [Presentation] 抗酸化物質の細胞に与える影響の解析 (2011)
  • Author(s): 門間奈津希
  • Organizer: 第84回日本生化学会大会
  • Place of Presentation: 国立京都国際会館(京都府)
• [Presentation] β-Cryptoxanthin, A Citrus Xanthophyl Carotenoid Prevents Inflammatory Bone Loss of Alveolar Bone in the Model for Periodontal Disease (2011)
  • Author(s): Hirata M
  • Organizer: American Society For Bone and Mineral Research 2011
  • Place of Presentation: San diego, California, USA
• [Presentation] Toll-like Receptor 2 Heterodimer, TLR1/2 and TLR2/6, Induces Inflammatory Bone Loss via PGE2 Production by Osteoblasts (2011)
  • Author(s): Matsumoto C
  • Organizer: American Society For Bone and Mineral Research 2011
  • Place of Presentation: San diego, California, USA
• [Presentation] 皮膚細胞の増殖と分化を制御するステロイド性因子の解析 (2010)
  • Author(s): 清水和
  • Organizer: 第83回日本生化学会大会
  • Place of Presentation: 神戸ポートアイランド(兵庫県)
  • Year and Date: 2010-12-10
• [Presentation] 脂肪細胞の分化と脂肪蓄積におけるプロスタグランジンE2の関与 (2010)
  • Author(s): 高田秀春
  • Organizer: 第83回日本生化学会大会
  • Place of Presentation: 神戸ポートアイランド(兵庫県)
  • Year and Date: 2010-12-10
• [Presentation] 血管内皮細胞による管腔形成制御の解析 (2010)
  • Author(s): 増井聡美
  • Organizer: 第83回日本生化学会大会
  • Place of Presentation: 神戸ポートアイランド(兵庫県)
  • Year and Date: 2010-12-10
• [Presentation] 脂肪前駆細胞の分化成熟におけるコラーゲン産生の解析 (2010)
  • Author(s): 小林愛
  • Organizer: 第83回日本生化学会大会
  • Place of Presentation: 神戸ポートアイランド(兵庫県)
  • Year and Date: 2010-12-10
• [Presentation] 脂肪細胞の分化と脂肪蓄積におけるプロスタグランジンE_2の関与 (2010)
  • Author(s): 高田秀春
  • Organizer: 第83回日本生化学会大会
  • Place of Presentation: 神戸ポートアイランド(兵庫県)
  • Year and Date: 2010-12-10
• [Presentation] Catechins with Gallate Moiety Suppress Bone Resorption by Inhibiting Prostaglandin Biosynthesis and RANKL Expression in Osteoblasts, Tumor Growth and Bone Metastasis of Cancer (2010)
  • Author(s): Chiho Matsumoto
  • Organizer: ASBMR 2010
  • Place of Presentation: Toronto, Ontario, Canada
  • Year and Date: 2010-10-17
• [Presentation] ガレート基含有カテキンは骨芽細胞におけるプロスタグランジンE産生を制御して炎症性骨吸収を抑制する (2010)
  • Author(s): 松本千穂
  • Organizer: 日本骨代謝学会学術集会
  • Place of Presentation: 京王プラザホテル(東京都)