Glycogen Synthase Kinase-3β Inhibition Attenuates the Development of Bleomycin-Induced Lung Injury:

Glycogen synthase kinase-3 (GSK-3) is an ubiquitous serine-threonine protein kinase that participates in a multitude of cellular processes and has recently been implicated in the pathophysiology of a number of diseases. The aim of this study is to investigate the effects of TDZD-8, a potent and selective GSK-3β inhibitor, on the development of lung injury caused by administration of bleomycin (BLM). Mice subjected to intra-tracheal administration of BLM developed significant lung injury characterized by marked neutrophil infiltration and tissue edema. An increase in immunoreactivity to nitrotyrosine, iNOS, TNF-α and IL-1β was also observed in the lungs of BLM-treated mice. In contrast, administration of BLM-treated mice with TDZD-8 (1 mg/kg daily) significantly reduced (I) the degree of lung injury, (II) the increase in staining (immunohistochemistry) for myeloperoxidase (MPO), nitrotyrosine, iNOS, TNF-α and IL-1β and (III) the degree of apoptosis, as evaluated by Bax and Bcl-2 immunoreactivity and TUNEL staining. Taken together, these results clearly demonstrate treatment with the GSK-3β inhibitor TDZD-8 reduces the development of lung injury and inflammation induced by BLM in mice

N -Thiocarbazole-based gold nanoparticles: synthesis, characterization and anti-proliferative activity evaluation

Carbazoles are aromatic heterocyclic compounds derived from the fusion of a benzene ring with an indole nucleus in 2,3 position. Today, many carbazole derivatives are widely studied as anticancer, anti-fungal, antioxidants, photoconductor, anti-bacterial, antimalarials, anti-Alzheimer, anti-tuberculosis, anti-HIV agents and for the treatment of obesity. Some of them, differently substituted on carbazole nucleus, have been synthetized and their biological activity have been evaluated. The purpose of this work is the study of new species obtained binding, a series of carbazole derivatives in which the carbazolic nitrogen has been functionalized with different alkyl-thiol chains, with gold nanoparticles, synthesized in organic solvent. The formation of self-assembled monolayers of these ligands is obtained on the spherical surface of gold nanoparticles, with a stabilizing effect against aggregation. These systems might present a double innovative function, matching an antineoplastic activity typical of carbazoles, with the photothermal effects of gold nanoparticles