Rhein is a lipophilic anthraquinone extensively found in medicinal herbs. Apoptosis was induced by adjunctive use of rhein with epidermal growth factor receptor (EGFR) inhibitors in pancreatic cancer cells. Suppression of the phosphorylation of STAT3 and EGFR (epidermal growth factor receptor) were also observed as a result of the treatment with a combination of rhein and EGFR inhibitors. Rhein considerably sensitized cells to erlotinib, thus suppressing tumor growth in PANC-1 and BxPC-3 xenograft models[3]. Rhein possesses pharmacological activity to suppress caspase-1 protease activity and IL-1 βproduction by interfering with the formation of NLRP3 multiprotein complex. Rhein has therapeutic potential for treating NLRP3 inflammasome-mediated diseases such as gouty arthritis[4]. Rhein exhibits various renoprotective functions, rhein remarkably reversed renal Klotho (a renal-specific antiaging protein) deficiency in adenine-treated mice. The renal protective effects of rhein were largely abolished when Klotho was knocked-down by RNA interferences, suggesting that rhein reversal of Klotho deficiency is essential for its renoprotective actions[5]. Rhein could effectively block the ATP-induced [Ca2+]c increases in a dose-dependent manner. Besides, rhein also suppressed the production of intracellular reactive oxygen species (ROS) induced by ATP in synoviocytes that was resulted from P2X4-mediated Ca2+ entry. Both rhein and BBG (Brilliant blue G) attenuated these inflammatory gene expressions enhanced by ATP[6].
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