• 제목/요약/키워드: o-Hydroxycinnamaldehyde

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Study on the Protein Binding of Anti-cancer Agent, 2"-O-benzoylcinnamaldehyde, using Ultrafilteration and Flurescence Spectrometry

  • Ren , Shan;Kim, Dae-Duk;Lee, Chi-Ho
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.242.3-243
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    • 2003
  • The compound of 2"-O-benzoylcinnamaldehyde(CB-ph) is a derivative of 2"-hydroxycinnamaldehyde whcih is a methanol extract of cinnamomum cassia blume. It"s a new anti-cancer agent which has been showed to inhibit the growth of various tumor cells in vitro and in vivo. In order to investigate the effective drug concentration and bio-distribution of CB-ph, the plasma protein binding was studied. In this study, the degree of the binding of Cb-ph to various serum proteins, the binding parameters, the binding site of CB-ph in human serum albumin, and the effect of some extensive protein-binding drugs on the protein binding of CB-ph in human serum ablumin were investigated respectively by ultrafilteration and fluorescence spectrometry. (omitted)

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Inhibition of Farnesyl Protein Transferase by Ortho-substituted Cinnamaldehyde Derivatives

  • Sung, Nack-Do;Kwon, Byoung-Mog;Lim, Chi-Hwan;Cho, Young-Kwon
    • Applied Biological Chemistry
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    • 제41권4호
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    • pp.218-221
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    • 1998
  • Various cinnamaldehyde derivatives were synthesized and their inhibition activity $(pI_{50})$ of farnesyl protein transferase (FPTase) was measured to examine the structure-activity relationships (SAR) on the basis that FPTase was inhibited by ortho-hydroxycinnamaldehyde derived from extracts of the bark of Cinnamomum cassia Blume. The ortho-substituents on the phenyl backbone of cinnamaldehyde showed higher activity than those with meta- and para-substituents, and the side chain required unsaturated aldehyde. In particular, 2-chlorocinnamaldehyde, 5 showed the highest inhibition activity on the FPTase among them and its inhibition activity $(pI_{50})$ value was 4.45.

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