Carbenoxolone

Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties[3]. Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the treatment of chronic liver disease[2]. Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD[1]. Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop[4].Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself[6].

[1]. Sharma S, et al. Inhibition of Alzheimer's amyloid-beta aggregation in-vitro by carbenoxolone:Insight into mechanism of action. Neurochem Int. 2017 Sep;108:481-493. [2]. Crespo Yanguas S, et al. TAT-Gap19 and Carbenoxolone Alleviate Liver Fibrosis in Mice. Int J Mol Sci. 2018 Mar 12;19(3). pii: E817. [3]. Hirata K, et al. Formulation of carbenoxolone for delivery to the skin. Int J Pharm. 2013 May 20;448(2):360-5. [4]. Michalski K, et al. Carbenoxolone inhibits Pannexin1 channels through interactions in the first extracellular loop. J Gen Physiol. 2016 Feb;147(2):165-74. [5]. Kim J, et al. Protective effect of carbenoxolone on ER stress-induced cell death in hypothalamic neurons. Biochem Biophys Res Commun. 2015 Dec 25;468(4):793-9. [6]. Pu J, et al. Antiviral activity of Carbenoxolone disodium against dengue virus infection. J Med Virol. 2017 Apr;89(4):571-581