title: Curcumin is a potent DNA hypomethylation agent.
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 IC(50) of 30 nM, but no inhibitory activity of hexahydrocurcumin up to 100 microM. In addition, curcumin can induce global DNA hypomethylation in a leukemia cell line.
authors.affiliation: Division of Pharmaceutics, College of Pharmacy, The Ohio State University, 500 W. 12th St., Columbus, OH 43210, USA. liu.550@osu.edu
authors.forename: Zhongfa
authors.initials: Z
authors.lastname: Liu
authors.forename: Zhiliang
authors.initials: Z
authors.lastname: Xie
authors.forename: William
authors.initials: W
authors.lastname: Jones
authors.forename: Ryan E
authors.initials: RE
authors.lastname: Pavlovicz
authors.forename: Shujun
authors.initials: S
authors.lastname: Liu
authors.forename: Jianhua
authors.initials: J
authors.lastname: Yu
authors.forename: Pui-kai
authors.initials: PK
authors.lastname: Li
authors.forename: Jiayuh
authors.initials: J
authors.lastname: Lin
authors.forename: Jame R
authors.initials: JR
authors.lastname: Fuchs
authors.forename: Guido
authors.initials: G
authors.lastname: Marcucci
authors.forename: Chenglong
authors.initials: C
authors.lastname: Li
authors.forename: Kenneth K
authors.initials: KK
authors.lastname: Chan
mesh_terms: D002384:Catalysis; D020134:Catalytic Domain; D045744:Cell Line, Tumor; D003474:Curcumin / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D003596:Cytosine / Q000737:chemistry; D000076123:DNA (Cytosine-5-)-Methyltransferase 1; D004248:DNA (Cytosine-5-)-Methyltransferases / Q000737:chemistry; D019175:DNA Methylation; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D007938:Leukemia / Q000188:drug therapy; D008956:Models, Chemical; D008968:Molecular Conformation
chemical_list: C096277:tetrahydrocurcumin; D003596:Cytosine; D000076123:DNA (Cytosine-5-)-Methyltransferase 1; D004248:DNA (Cytosine-5-)-Methyltransferases; C000619380:DNMT1 protein, human; D003474:Curcumin