Division of Pharmaceutics, College of Pharmacy, The Ohio State University, 500 W. 12th St., Columbus, OH 43210, USA.
Bioorg Med Chem Lett. 2009 Feb 1;19(3):706-9. doi: 10.1016/j.bmcl.2008.12.041. Epub 2008 Dec 14.
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.
姜黄素与 DNMT1 相互作用的分子对接表明，姜黄素通过共价结合 DNMT1 的 C1226 巯基来发挥其抑制作用。这一点通过实验得到了验证，即姜黄素能抑制 M. SssI 的活性，其 IC50 为 30 nM，但六氢姜黄素在 100 μM 时没有抑制活性。此外，姜黄素可诱导白血病细胞系中全基因组 DNA 低甲基化。
