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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 27, Number 4
BKCSDE 27(4)
April 20, 2006 

 
Title
Inhibitory Effects of Momordin I Derivatives on the Formation of Fos-Jun-AP-1 DNA Complex
Author
Juhyung Lee, Chi-Hoon Park, Wook-Hwan Kim, Yun Ha Hwang, Kyungchae Jeong, Chul-Hak Yang*
Keywords
Fos-Jun, Momordin I, Curcumin, AP-1, EMSA
Abstract
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 IC50 values of momordin I derivatives were about 4.0 μM 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.
Page
535 - 538
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