Description
Lisofylline (6493-06-7, racemic) displays anti-inflammatory activity. Regulates immune cell function and autoimmune response by inhibition of IL-12 signalling and cytokine production.1 Protects pancreatic beta cells and prevents type I diabetes in non-obese diabetic mice.2 Lisofylline reduces LPS-induced TNF alpha levels in CD-1 mice.3?Cell permeable.
Chemical Properties
White Solid
Uses
A major oxidative metabolite of Pentoxifylline.
Definition
ChEBI: 1-(5-hydroxyhexyl)-3,7-dimethyl-3,7-dihydro-1H-purine-2,6-dione is a dimethylxanthine that is 3,7-dihydro-1H-purine-2,6-dione which is substituted at positions 1,3 and 7 by a 5-hydroxyhexyl group, methyl group and methyl group, respectively. It is a secondary alcohol and a dimethylxanthine.
Brand name
ProTec (Cell
Therapeutics).
Biological Activity
A potent inhibitor of phosphatidic acid generation (IC50=0.6 μM). It protects mice from endotoxic shock and attenuates sepsis-induced acute lung injury in the pig. Anti-inflammatory agent. Enhances glucose-stimulated insulin secretion. Inhibits IL-12-mediated STAT4 activation.
in vitro
(±)-lisofylline is a potent anti-inflammatory agent in which only the (-) optical isomer is biologically active. (±)-lisofylline was found to inhibit the generation of phosphatidic acid from cytokine-activated lysophosphatidic acyl transferase. (±)-lisofylline could also suppress the production of the proinflammatory cytokine ifn-γ, inhibit il-12-mediated stat-4 activation, as well as enhance glucose-stimulated β-cell insulin secretion [1].
in vivo
in a previous study, lisofylline was administered to female non-obese diabetic mice for 3 weeks. cytokines and blood glucose concentrations were monitored. histology and immunohistochemistry were also carried out in pancreatic sections. results showed that lisofylline was able to suppress ifn-γ production, reduce the onset of insulitis and diabetes, and inhibit diabetes [1].
References
1) Yang?et al. (2005),?Lisofylline: a potential lead for the treatment of diabetes; Biochem. Pharmacol., 69?1
2) Yang?et al. (2002),?The anti-inflammatory compound lisofylline prevents Type I diabetes in non-obese diabetic mice; Diabetologia,?45?1307
3) Wyska?et al. (2010),?Pharmacokinetic-pharmacodynamic modeling of methylxanthine derivatives in mice challenged with high-dose lipopolysaccharide; Pharmacology,?85?264
