Advanced search×

Evodiamine as a novel antagonist of aryl hydrocarbon receptor

Hui H Yu, Yongjiu Y Tu, Chun C Zhang, Xia X Fan, Xi X Wang, Zhanli Z Wang, and Huaping H Liang

Biochem Biophys Res Commun 402(1):5 (2010) PMID 20888792

Evodiamine, the major bioactive alkaloid isolated from Wu-Chu-Yu, has been shown to interact with a wide variety of proteins and modify their expression and activities. In this study, we investigated the interaction between evodiamine and the aryl hydrocarbon receptor (AhR). Molecular modeling results revealed that evodiamine directly interacted with the AhR. Cytosolic receptor binding assay also provided the evidence that evodiamine could interact with the AhR with the K"i value of 28.4+/-4.9nM. In addition, we observed that evodiamine suppressed the 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) induced nuclear translocation of the AhR and the expression of CYP1A1 dose-dependently. These results suggested that evodiamine was able to bind to the AhR as ligand and exhibit antagonistic effects.

Copyright © 2010 Elsevier Ltd. All rights reserved.

DOI: 10.1016/j.bbrc.2010.09.122
Version: za2963e q8za1 q8zbb q8zcb q8zd2 q8zec q8zfd q8zgd

Similar articles you may find interesting…

  1. A novel domino strategy for forming poly-substituted quaternary imidazoles through a Cs2CO3-promoted aryl migration process.
    Hai-Wei Xu, Wei Fan, and Shu-Jiang Tu

    Org Biomol Chem (2013) PMID 23648485

    A new domino strategy for the synthesis of highly functionalized quaternary imidazole derivatives via [3 + 2] heterocyclization, involving aryl migration and ring-opening of oxirane, has been developed. This domino reaction enables the successful assembly of three new sigma bonds inc...
  2. Xenoestrogenic and dioxin-like activity in blood of East Greenland polar bears (Ursus maritimus).
    Simon E Erdmann, Rune Dietz, and Eva C Bonefeld-Jørgensen

    Chemosphere (2013) PMID 23648332

    The aims of the project were to (i) extract the lipophilic persistent organic pollutants (POPs) from the blood of 99 East Greenland polar bears and assess the combined mixture effect on the estrogen receptor (ER) and the aryl hydrocarbon receptor (AhR) mediated transactivity; (ii) To...
  3. Downregulation of aryl hydrocarbon receptor expression decreases gastric cancer cell growth and invasion.
    Xiao-Fei Yin, Jie Chen, and Min-Hu Chen

    Oncol Rep (2013) PMID 23604401

    We explored the effects of the inhibition of AhR expression by RNA interference on the biological behavior of gastric cancer cells (MKN45 and SGC7901), and elucidated the specific mechanisms of AhR action in the development of gastric cancer. Results showed that small interfering RNA (siRNA) against...