Monovalent Gb_3-/Gb_2-Derivatives Conjugated with a Phosphatidyl Residue : A Novel Class of Shiga Toxin-Neutralizing Agent(Microbiology)

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概要

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• Shiga toxin (Stx) exerts toxic activity by binding to glycosphingolipids, mainly globotriaosyl (Gb_3) ceramide, on the surface of target cells. The inhibition of toxin-receptor binding is a promising therapeutic approach to prevent Stx-mediated diseases. In this study, we synthesized monovalent Stx-ligands of phosphatidylethanolamine dipalmitoyl-Gb_3 (Gb_3-PEDP) and galabiosyl (Gb_2)-PEDP and we examined their neutralizing activity against Stx-1 and Stx-2 in vitro. Both Gb_3-PEDP and Gb_2-PEDP strongly neutralized the cytotoxicity of Stx-1 and Stx-2. It is likely that the mechanism of neutralization involved formation of liposomes and consequently clustering of sugar units. We propose monovalent Gb_3-/Gb_2-derivatives conjugated with phosphatidyl residue as a novel class of Stx-neutralizing agent.

• 公益社団法人日本薬学会の論文
• 2007-09-01

著者

• Inazu Toshiyuki

  Department Of Applied Chemistry School Of Engineering Tokai University

• Yokoyama Shin-ichiro

  Laboratory Of Microbiology Department Of Public Health Pharmacy Gifu Pharmaceutical University

• Murata Takeomi

  Department Of Applied Biological Chemistry Faculty Of Agriculture Shizuoka University

• Murata Takeomi

  Departmentof Environmental Science For Human Life Faculty Of Agriculture Shizuoka University

• Murata Takeomi

  Department Of Applied Biological Cemistry Faculty Of Agriculture Shizuoka University

• MORI Hiroshi

  Laboratory of Microbiology, Gifu Pharmaceutical University

• Neri Paola

  Laboratory Of Microbiology Department Of Public Health Pharmacy Gifu Pharmaceutical University

• Nishida Yoshihiro

  Department Of Molecular Design And Engineering Graduate School Of Engineering Nagoya University

• TOKORO Shunji

  Laboratory of Microbiology, Department of Public Health Pharmacy, Gifu Pharmaceutical University

• MIURA Tsuyoshi

  The Noguchi Institute

• NISHIDA Yoshihiro

  Division of Molecular Bioorganic Chemistry, Department of Horticulture, Chiba University

• KAJIMOTO Tetsuya

  Kyoto Pharmaceutical University

• TSUJINO Satoshi

  The Noguchi Institute

• USUI Taiichi

  Departmentof Environmental Science for Human Life, Faculty of Agriculture, Shizuoka University

• Usui Taiichi

  Departmentof Environmental Science For Human Life Faculty Of Agriculture Shizuoka University

• Tokoro Shunji

  Laboratory Of Microbiology Department Of Public Health Pharmacy Gifu Pharmaceutical University

• Yokoyama Shin-ichiro

  Gifu Prefectural Research Institute For Bioengineering Department Of Applied Microbiology

• Sugiyama Tsuyoshi

  Laboratory Of Microbiology Department Of Public Health Pharmacy Gifu Pharmaceutical University

• Mori Hiroshi

  Laboratory Of Microbiology Department Of Public Health Pharmacy Gifu Pharmaceutical University

• Usui Taiichi

  Department of Applied Biological Chemistry, Faculty of Agriculture, Shizuoka University

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