LIPID MAPS

Emodin is a naturally-occurring anthraquinone found in a variety of plants used in traditional Chinese medicine. Purified emodin has diverse effects, including the suppression of inflammation, dyslipidemia, and cancer.^1,2,3 At a molecular level, emodin directly and selectively inhibits casein kinase II (IC50 = 0.89 μM).^4,5 Through this action, it inhibits the COP9 signalosome, causing the stabilization of the tumor suppressor p53.5 Moreover, emodin acts as a phytoestrogen, binding human estrogen receptors and blocking 17β-estradiol binding with Ki values of 0.77 and 1.5 μM for ERα and ERβ, respectively.⁶

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References

1. Alisi, A., Pastore, A., Ceccarelli, S., et al. Emodin prevents intrahepatic fat accumulation, inflammation and redox status imbalance during diet-induced hepatosteatosis in rats. Int. J. Mol. Sci. 13(2), 2276-2289 (2012).

2. Lin, S.Z., Wei, W.T., Chen, H., et al. Antitumor activity of emodin against pancreatic cancer depends on its dual role: Promotion of apoptosis and suppression of angiogenesis. PLoS One 7(8), 1-15 (2012).

3. Tzeng, T.F., Lu, H.J., Liou, S.S., et al. Emodin, a naturally occurring anthraquinone derivative, ameliorates dyslipidemia by activating AMP-activated protein kinase in high-fat-diet-fed rats. Evid. Based Complement. Alternat. Med. 781812 (2012).

4. Füllbeck, M., Huang, X., Dumdey, R., et al. Novel curcumin- and emodin-related compounds identified by in silico 2D/3D conformer screening induce apoptosis in tumor cells. BMC Cancer 5(97), 1-14 (2005).

5. Matsuda, H., Shimoda, H., Morikawa, T., et al. Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): Structure-requirement of hydroxyanthraquinones for estrogenic activity. Bioorg. Med. Chem. Lett. 11(14), 1839-1842 (2001).

6. Sarno, S., De Moliner, E., Ruzzene, M., et al. Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA). Biochem. J. 374(Pt 3), 639-646 (2003).