Synthesis of 4-Hydroxy-3(2H)-furanone Acyl Derivatives and Their Anti-cataract Effect on Spontaneous Cataract Rats (ICR/f)

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概要

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• 4-Hydroxy-2,5-dimethyl-3(2H)-furanone (HDMF)and 2(or 5)-ethyl-4-hydroxy-5(or 2)-methyl-3(2H)-furanone (EHMF) are known to inhibit cataract development in spontaneous cataract rats (ICR/f). Forty-five acylated hydroxyfuranone derivatives were designed and synthesized for an anti-cataract test, and their hydrophobic con-stants were also tested. Among these derivatives, 2,5-dimethyl-4-pivaloyloxy-3(2H)-furanone (HDMF pivalate) exerted a marked protective effect against the development of cataract in a galactose-induced model using cultured rat lens (in vitro). When tested on an ICR/f cataract model (in vivo), HDMF pivalate showed more significant inhibition of cataract development than parent compound HDMF. This derivative is more lipophilic than HDMF, so that HDMF pivalate can penetrate the cornea more easily than HDMF. The inhibition of cataract development by HDMF converted from HDMF pivalate is supported by the fact that HDMF was observed in the lens of ICR/f rats treated with HDMF pivalate.

• 社団法人日本農芸化学会の論文
• 1998-11-23

著者

• Sakai Takafumi

  Division Of Applied Life Sciences Graduate School Of Agriculture Kyoto University

• Sakai T

  Kyoto Univ. Kyoto Jpn

• YAMAKOSHI Jun

  Research and Development Division, Kikkoman Corporation

• SAITO Makoto

  Research and Development Division, Kikkoman Corporation

• KIKUCHI Mamoru

  Research and Development Division, Kikkoman Corporation

• Mori Kenji

  Department of Biochemistry, National Cardiovascular Center Research Institute

• Sakai T

  Kikkoman Corp. Chiba Jpn

• KASAI Kouichi

  Research and Development Division, Kikkoman Corporation

• Saito Makoto

  Research And Development Division Kikkoman Corporation

• Kasai K

  Research And Development Division Kikkoman Corporation

• Kasai Kouichi

  Research And Development Division Kikkoman Corporation

• Koga Takuro

  Biochemical Division Kikkoman Corporation

• Koga Takuro

  Noda Institute For Scientific Research

• Saito M

  Department Of Biotechnology And Life Science Tokyo University Of Agriculture And Technology

• 松浦 克子

  キッコーマン株式会社 研究本部

• SASAKI Tsutomu

  Research and Development Division, Kikkoman Corporation

• MATSUDO Takanao

  Research and Development Division, Kikkoman Corporation

• Matsudo T

  Kikkoman Corp. Chiba Jpn

• Matsudo Takanao

  Research And Development Division Kikkoman Corporation

• Kikuchi Masanori

  Department Of Food Production And Utility Development Graduate School Of Dairy Science Research Raku

• Takagi S

  Ehime Prefectural Fisheries Experimental Station

• Koga T

  National Institute Of Advanced Industrial Science And Technology

• Kikuchi M

  Kikkoman Corp. Chiba Jpn

• Yamakoshi Jun

  Research And Development Division Kikkoman Corporation

• Kikuchi Mamoru

  Res. And Dev. Div. Kikkoman Corp.

• Kikuchi Mamoru

  Research & Development Division Kikkoman Corporation

• Mori K

  Sci. Univ. Tokyo Tokyo Jpn

• Kikuchi M

  Res. And Dev. Div. Kikkoman Corp.

• Saito M

  Research And Development Division Kikkoman Corporation

• Yamakoshi J

  Research And Development Division Kikkoman Corporation

• Mori Kenji

  Department Of Biochemistry National Cardiovascular Center Research Institute

• Mori Kenji

  Department Of Agricultural Chemistry The University Of Tokyo

• Mori Kenji

  Department Of Agricultural Chemistry Nagoya University

• Saito Makoto

  Research & Development Division Kikkoman Corporation

• Mori Kenji

  Department Of Agricultural Chemistry College Of Science And Technology The University Of Tokyo

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