Curcumin is a potent DNA hypomethylation agent

Zhongfa Liu, Zhiliang Xie, William Jones, Ryan E. Pavlovicz, Shujun Liu, Jianhua Yu, Pui kai Li, Jiayuh Lin, Jame R. Fuchs, Guido Marcucci, Chenglong Li, Kenneth K. Chan

Research output: Contribution to journalArticlepeer-review

223 Scopus citations

Abstract

Molecular docking of the interaction of curcumin and DNMT1 suggested that curcumin covalently blocks the catalytic thiolate of C1226 of DNMT1 to exert its inhibitory effect. This was validated by showing that curcumin inhibits the activity of M. SssI with an IC50 of 30 nM, but no inhibitory activity of hexahydrocurcumin up to 100 μM. In addition, curcumin can induce global DNA hypomethylation in a leukemia cell line.

Original languageEnglish (US)
Pages (from-to)706-709
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number3
DOIs
StatePublished - Feb 1 2009
Externally publishedYes

Bibliographical note

Funding Information:
This work was partially supported by Grants NIH-NCI RO1 CA102031 (G.M.) and by BioMedical Mass Spectrometry Laboratory, College of Pharmacy.

Keywords

  • Curcumin
  • DNA hypomethylation agent

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