Description
Rhein is an active metabolite of diacerein and an anthraquinone found in Rheus (rhubarb). Rhein exhibits pro-inflammatory, anti-inflammatory, anti-diabetic, anticancer, antioxidative, anti-atherosclerotic, and anti-angiogenic activities. Rhein inhibits LPS-induced activation of NF-κB and production of IL-6 and IL-1β by inhibiting degradation of IκB kinase. Rhein also inhibits hyperglycemia-induced apoptosis in β cells in animal models of diabetes. In gastric cancer cells, rhein increases the Bax/Bcl-2 ratio and levels of cytochrome c, inducing mitochondria-mediated apoptosis and inhibiting cell proliferation. This compound also inhibits vessel plexus formation and endothelial cell migration. Additionally, rhein decrease H2O2-induced increases in malondialdehyde and lactate dehydrogenase levels and decreases in superoxide dismutase and glutathione activity, inhibiting apoptosis and oxidative injury.
References
Gao Y, Chen X, Fang L, et al. Rhein exerts pro- and anti-inflammatory actions by targeting IKKβ inhibition in LPS-activated macrophages. Free Radic Biol Med. 2014 Jul;72:104-12. PMID: 24721152.
Liu J, Chen Z, Zhang Y, et al. Rhein protects pancreatic β-cells from dynamin-related protein-1-mediated mitochondrial fission and cell apoptosis under hyperglycemia. Diabetes. 2013 Nov;62(11):3927-35. PMID: 23919963.
Li Y, Xu Y, Lei B, et al. Rhein induces apoptosis of human gastric cancer SGC-7901 cells via an intrinsic mitochondrial pathway. Braz J Med Biol Res. 2012 Nov;45(11):1052-9. PMID: 22850871.
Zhong XF, Huang GD, Luo T, et al. Protective effect of rhein against oxidative stress-related endothelial cell injury. Mol Med Rep. 2012 May;5(5):1261-6. PMID: 22344690.
He ZH, Zhou R, He MF, et al. Anti-angiogenic effect and mechanism of rhein from Rhizoma Rhei. Phytomedicine. 2011 Apr 15;18(6):470-8. PMID: 21112197.
