Rhein

Rhein is an anthraquinone derivative that has been found in R. rhabarbarum and is an active metabolite of diacerein (Item No. 11710) that has diverse biological activities, including anticancer, antioxidant, and anti-inflammatory activities.^1,2,3,4 It induces cell cycle arrest at the S phase and inhibits the proliferation of HepG2 cells when used at concentrations of 40 and 100 µM, respectively.¹ Rhein (100 and 200 µM) also inhibits proliferation of MCF-7 and MDA-MB-435s breast cancer cells under normoxic and hypoxic conditions.² It reduces controlled cortical impact-induced decreases in catalase and superoxide dismutase (SOD) activity and malondialdehyde (MDA), glutathione, and glutathione disulfide levels in the brain in a rat model of traumatic brain injury when administered at a dose of 12 mg/kg.³ Rhein (50 mg/kg per day) reduces cerulein-induced increases in serum TNF-α, IL-1β, and amylase levels, as well as reduces pancreatic glandular atrophy and fibrosis, in a mouse model of chronic pancreatitis.⁴

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1. Liu, S., Wang, J., Shao, T., et al. The natural agent rhein induces β-catenin degradation and tumour growth arrest. J. Cell. Mol. Med. 22(1), 589-599 (2018).

2. Fernand, V.E., Losso, J.N., Traux, R.E., et al. Rhein inhibits angiogenesis and the viability of hormone-dependent and -independent cancer cells under normoxic or hypoxic conditions in vitro. Chem. Biol. Interact. 192(3), 220-232 (2011).

3. Xu, X., Lv, H., Xia, Z., et al. Rhein exhibits antioxidative effects similar to Rhubarb in a rat model of traumatic brain injury. BMC Complement. Altern. Med. 17(1), 140 (2017).

4. Tsang, S.W., Zhang, H., Lin, C., et al. Rhein, a natural anthraquinone derivative, attenuates the activation of pancreatic stellate cells and ameliorates pancreatic fibrosis in mice with experimental chronic pancreatitis. PLoS One 8(12), e82201 (2013).