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

doi:10.1016/j.bmcl.2008.12.041

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 journal › Article › peer-review

288 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 language	English (US)
Pages (from-to)	706-709
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	3
DOIs	https://doi.org/10.1016/j.bmcl.2008.12.041
State	Published - Feb 1 2009
Externally published	Yes

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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2008.12.041

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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 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.",

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AU - Liu, Zhongfa

AU - Xie, Zhiliang

AU - Jones, William

AU - Pavlovicz, Ryan E.

AU - Liu, Shujun

AU - Yu, Jianhua

AU - Li, Pui kai

AU - Lin, Jiayuh

AU - Fuchs, Jame R.

AU - Marcucci, Guido

AU - Li, Chenglong

AU - Chan, Kenneth K.

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PY - 2009/2/1

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N2 - 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.

AB - 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.

KW - Curcumin

KW - DNA hypomethylation agent

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Curcumin is a potent DNA hypomethylation agent

Abstract

Bibliographical note

Keywords

UN SDGs

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