Description
Carbenoxolone is a synthetic derivative of glycyrrhizin that exhibits anti-ulcerative, anti-inflammatory, neuromodulatory, neuroprotective, anti-hyperlipidemic, hepatoprotective, and immunosuppressive activities. Carbenoxolone is clinically used to treat ulcers and inflammation; it inhibits 11β-hydroxysteroid dehydrogenase as well as connexins, limiting gap junction communication. In animal models of cerebral ischemia/reperfusion, carbenoxolone decreases infarct volume and neuronal damage. Carbenoxolone also increases NO levels in other animal models, preventing gastric injury. In animal models of experimental autoimmune encephalitis (EAE), carbenoxolone delays disease onset and suppresses production of IL-23 and Th17 cells. In other animal models, this compound decreases levels of triglycerides, free fatty acids, SREBP-1c, LXR, and fatty acid synthase and suppresses hepatocyte apoptosis and inflammatory cytokine expression.
References
Chen G, Park CK, Xie RG, et al. Connexin-43 induces chemokine release from spinal cord astrocytes to maintain late-phase neuropathic pain in mice. Brain. 2014 Aug;137(Pt 8):2193-209. PMID: 24919967.
Beraki S, Litrus L, Soriano L, et al. A pharmacological screening approach for discovery of neuroprotective compounds in ischemic stroke. PLoS One. 2013 Jul 18;8(7):e69233. PMID: 23874920.
Rhee SD, Kim CH, Park JS, et al. Carbenoxolone prevents the development of fatty liver in C57BL/6-Lep ob/ob mice via the inhibition of sterol regulatory element binding protein-1c activity and apoptosis. Eur J Pharmacol. 2012 Sep 15;691(1-3):9-18. PMID: 22742899.
Endong L, Shijie J, Sonobe Y, et al. The gap-junction inhibitor carbenoxolone suppresses the differentiation of Th17 cells through inhibition of IL-23 expression in antigen presenting cells. J Neuroimmunol. 2011 Dec 15;240-241:58-64. PMID: 22036952.
Chávez-Piña AE, Tapia-Álvarez GR, Reyes-Ramínrez A, et al. Carbenoxolone gastroprotective mechanism: participation of nitric oxide/(c) GMP/K(ATP) pathway in ethanol-induced gastric injury in the rat. Fundam Clin Pharmacol. 2011 Dec;25(6):717-22. PMID: 21105909.
