Bulletin of the Korean Chemical Society

  • 제27권4호
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  • Pages.535-538
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  • 2006
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  • 0253-2964(pISSN)
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  • 1229-5949(eISSN)
대한화학회 (Korean Chemical Society)
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Inhibitory Effects of Momordin I Derivatives on the Formation of Fos-Jun-AP-1 DNA Complex

  • Lee, Ju-hyung (Department of Chemistry and Molecular Engineering, College of Natural Sciences, Seoul National University) ;
  • Park, Chi-Hoon (Department of Chemistry and Molecular Engineering, College of Natural Sciences, Seoul National University) ;
  • Kim, Wook-Hwan (Department of Chemistry and Molecular Engineering, College of Natural Sciences, Seoul National University) ;
  • Hwang, Yun-Ha (Department of Chemistry and Molecular Engineering, College of Natural Sciences, Seoul National University) ;
  • Jeong, Kyung-chae (Department of Chemistry and Molecular Engineering, College of Natural Sciences, Seoul National University) ;
  • Yang, Chul-Hak (Department of Chemistry and Molecular Engineering, College of Natural Sciences, Seoul National University)
  • 발행 : 2006.04.20
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초록

In our previous studies, we have observed that curcumin and momordin I isolated from Ampelopsis radix inhibit the formation of Fos-Jun-activation protein-1 (AP-1) DNA complex. We have screened more effective compounds which have a 5-membered ring framework like momordin I and have modified disaccharide or carboxylic acid portions in momordin I. We synthesized momordin I derivatives according to the published method with slight modification. Synthetic momordin I derivatives showed remarkable inhibitory activities on Fos-Jun-AP-1 DNA complex formation results in in vitro assays. The $IC_{50}$ values of momordin I derivatives were about 4.0 $\mu$M in an electrophoretic mobility shift assay (EMSA). This value is about 125 times higher than that of curcumin and about 12 times higher than that for curcumin derivative C1, and moreover about 30 times higher than that for momordin I. We found momordin I derivatives (a) and (b) are the strongest inhibitory compound for Fos-Jun-AP-1 DNA complex formation.

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참고문헌

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피인용 문헌

  1. Small Molecule Inhibitors Targeting Activator Protein 1 (AP-1) vol.57, pp.16, 2014, https://doi.org/10.1021/jm5004733