Syntheses of PET probes of Chinese medicinal plants, and those pharmacokinetics analysis

• Project/Area Number: 22790265
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: General pharmacology
• Research Institution: The Institute of Physical and Chemical Research
• Principal Investigator: ISHII Hideki 独立行政法人理化学研究所, 分子イメージング創薬化学研究チーム, 副チームリーダー (80425610)
• Project Period (FY): 2010 – 2011
• Project Status: Completed (Fiscal Year 2011)
• Budget Amount: ¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000); Fiscal Year 2011: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000); Fiscal Year 2010: ¥3,120,000 (Direct Cost: ¥2,400,000、Indirect Cost: ¥720,000)
• Keywords: 生薬 / 天然物薬理学 / PET

Research Abstract

β-Sitosterol, 6-gingerol, curcumin, parthenolide, and evodiamine, which have used for the synthesis of PET-probe precursors or standard samples, have isolated using column chromatography after the extraction with organic solvents of corresponding powders from the commercially available Chinese medicinal plants : Pinellia tuber, Zingiber siccatum, Curcuma longa, Feverfew, and Evodiae fructus. Corresponding^<11> C-PET probe precursors(boronic acid esters) ofβ-sitosterol and curcumin have successfully synthesized.

Research Products

• [Journal Article] PET Imaging. Based Evaluation of Hepatobiliary Transport in Humans with(15R)-^<11> C-TIC-Me (2012)
  • Author(s): Tadayuki Takashima, Satoshi Kitamura, Yasuhiro Wada, Masaaki Tanaka, Yoshihito Shigihara, Hideki Ishii, Ryosuke Ijuin, Susumu Shiomi, Takahiro Nakae, Yumiko Watanabe, Yilong Cui, Hisashi Doi, Masaaki Suzuki, Kazuya Maeda, Hiroyuki Kusuhara, Yuichi Sugiyam
  • Journal Title: J. Nucl. Med Volume: 53 Pages: 741-748
  • Peer Reviewed
• [Journal Article] Synthesis and biological evaluation of deoxy-hematoxylin derivatives as a novel class of anti-HIV-1 agents (2012)
  • Author(s): ideki Ishii, Hiroko Koyama, Kyoji Hagiwara, Tomoyuki Miura, Guangai Xue, Yoshie Hashimoto, Genta Kitahara, Yoko Aida, Masaaki Suzuki
  • Journal Title: Bioorg. Med. Chem. Lett. Volume: 22 Pages: 1469-1474
  • Peer Reviewed
• [Journal Article] Synthesis and biological evaluation of deoxy-hematoxylin derivatives as a novel class of anti-HIV-1 agents. (2012)
  • Author(s): Ishii H, Koyama H, Hagiwara K, Miura T, Xue G, Hashimoto Y, Kitahara G, Aida Y, Suzuki M.
  • Journal Title: Bioorg. Med. Chem Volume: 1; 22(3) Issue: 3 Pages: 1469-74
  • DOI: 10.1016/j.bmcl.2011.06.066
  • Peer Reviewed
• [Journal Article] Positron emission tomography (PET) imaging-based evaluation of hepatobiliary transport in humans using 15R-[^<11>C]TIC-Me (2012)
  • Author(s): Tadayuki Takashima, Satoshi Kitamura, Yasuhiro Wada, Masaaki Tanaka, Yoshihito, Shigihara, Hideki Ishii, Ryosuke Ijuin, Susumu Shiomi, Takahiro Nakae, Yumiko Watanabe, Yilong Cui, Hisashi Doi, Masaaki Suzuki, Kazuya Maeda, Hiroyuki Kusuhara, Yuichi Sugiyama, Yasuyoshi Watanabe
  • Journal Title: The Journal of Nuclear Medicine Volume: (in press)
  • Peer Reviewed
• [Presentation] SAR studies of(-)-cytoxazone as potent anti-hepatic-fibrosis agents and development of its radioisotope-free photoaffinity probes (2012)
  • Author(s): Hideki Ishii
  • Organizer: The 1st International Symposium on Latent TGF-βActivation Reaction
  • Place of Presentation: RIKEN Kobe Inst, Japan
  • Year and Date: 2012-02-25
• [Presentation] TGF-βシグナル伝達系を阻害する新規サイトキサゾン誘導体の合成および標的タンパク質探索用光標識プローブの開発 (2012)
  • Author(s): 羽毛田匡,石井英樹,服部明,掛谷秀昭,小嶋聡一,鈴木正昭
  • Organizer: 日本薬学会第132年会
  • Place of Presentation: 札幌、北海道
• [Presentation] SAR studies of (-)-cytoxazone as potent anti-hepatic-fibrosis agents and development of its radioisotope-free photoaffinity probes (2011)
  • Author(s): Hideki Ishii
  • Organizer: The 1st International Symposium on Latent TGF-ss Activation Reaction
  • Place of Presentation: RIKEN Kobe Inst, Japan(招待講演)
  • Year and Date: 2011-02-25
• [Presentation] Synthesis of[C^^<11>] all-trans-retinoic acid via an alkenylboron precursor by Pd(0)-mediated rapid C-[C^^<11>] methylation (2011)
  • Author(s): Masaaki Suzuki, Misato Takashima-Hirano, Chika Watanabe, Hideki Ishii, Kengo Sumi, Hiroko Koyama, Hisashi 1 Doi
  • Organizer: 19^<th> International Symposiuon Radiopharmaceutical Sciences
  • Place of Presentation: Amsterdam, The Netherlands
• [Presentation] Vpr Helix3領域と結合する新規HIV-1阻害剤の開発 (2011)
  • Author(s): 萩原恭二、村上知行、石井英樹、近藤恭光、本田香織、長田裕之、横田恭子、鈴木正昭、間陽子
  • Organizer: 第25回日本エイズ学会学術集会・総会
  • Place of Presentation: ハイアットリージェンシー東京,東京都
• [Presentation] Synthesis of [^<11>C]all-trans-retinoic acid via an alkenylboron precursor by Pd(O)-mediated rapid C-[^<11>C]methylation (2011)
  • Author(s): Masaaki Suzuki, Misato Takashima-Hirano, Chika Watanabe, Hideki Ishii, Kengo Sumi, Hiroko Koyama, Hisashi Doi
  • Organizer: 19^<th> International Symposiuon Radiophar maceutical Sciences
  • Place of Presentation: Amsterdam, The Netherlands
• [Presentation] Vpr Helix3領域と結合する新規HIV-1阻害剤の開発 (2011)
  • Author(s): 萩原恭二、村上知行、石井英樹、近藤恭光、本田香織、長田裕之、横田恭子、鈴木正昭、間陽子
  • Organizer: 第25回日本エイズ学会学術集会・総会
  • Place of Presentation: ハイアットリージェンシー東京(東京都)
• [Presentation] EVALUATION OF IN VIVO HEPATOBILIARY TRANSPORT USING POSITRON EMISSION TOMOGRAPHY(PET): STUDIES IN RATS AND APPLICATION TO MICRODOSING CLINICAL STUDIES (2010)
  • Author(s): Tadayuki Takashima, Hiroko Nagata, Hideki Ishii, Ryosuke Ijuin, Takahiro Nakae, Masaaki Tanaka, Yoshihito Shigihara, Suzuka Ataka, Hisashi Doi, Yasuhiro Wada, Masaaki Suzuki, Kazuya Maeda, Hiroyuki Kusuhara, Yuichi Sugiyama, Yasuyoshi Watanabe
  • Organizer: 9^<th> ISSX international symposioum
  • Place of Presentation: Istanbul