Pentoxifylline is a methylxanthine derivative. It has been shown to have anti-inflammatory activity, inhibiting LPS-induced TNF-α production in isolated peripheral blood mononuclear cells (IC50 = 85 ?M) and suppressing LPS-induced leukopenia in mice.1 Pentoxifylline weakly inhibits the generation of phosphatidic acid (IC50 = 500 ?M) from LPS-activated lysophosphatidic acyl transferase (LPAAT), and weakly antagonizes A1 and A2 adenosine receptors.2,3 It also inhibits human acidic mammalian chitinase, human chitotriosidase, and chitinase B1 from Aspergillus fumigatus (IC50s = 49, 98, and 126 ?M, respectively).4
1.Cottam, H.B., Shih, H., Tehrani, L.R., et al.Substituted xanthines, pteridinediones, and related compounds as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor αJ. Med. Chem.392-9(1996) 2.Rice, G.C., Brown, P.A., Nelson, R.J., et al.Protection from endotoxic shock in mice by pharmacologic inhibition of phosphatidic acidProc. Natl. Acad. Sci. USA91(9)3857-3861(1994) 3.Schwabe, U., Ukena, D., and Lohse, M.J.Xanthine derivatives as antagonists at A1 and A2 adenosine receptorsNaunyn Schmiedebergs Arch. Pharmacol.330(3)212-221(1985) 4.Rao, F.V., Andersen, O.A., Vora, K.A., et al.Methylxanthine drugs are chitinase inhibitors: Investigation of inhibition and binding modesChem. Biol.12(9)973-980(2005)