Adenosine A3 Receptor (A3AR) Agonist for the Treatment of Bleomycin-Induced Lung Fibrosis in Mice

Adenosine receptors (ARs) are involved in the suppression and development of inflammatory and fibrotic conditions. Specifically, AR activation promotes differentiation of lung fibroblasts into myofibroblasts, typical of a fibrotic event. Pulmonary fibrosis is a severe disease characterized by inflammation and fibrosis of unknown etiology and lacking an effective treatment. The present investigation explored the action of MRS5980, a new, highly potent and selective A₃AR agonist, in an established murine model of lung fibrosis. The effects of either vehicle or MRS5980 were studied in mice following intratracheal bleomycin administration. We evaluated the role of the A₃AR agonist on lung stiffness, studying the airway resistance to inflation, oxidative stress (8-OHdG and MDA), inflammation, pro- and anti-inflammatory marker levels (IL-1β, IL-6, TNF-α, IL-10 and IL-17A) and fibrosis establishment, evaluating transforming growth factor (TGF)-β expression and α-smooth muscle actin (α-SMA) deposition in lungs. Bleomycin administration increased lung stiffness, TGF-β levels, α-SMA deposition, and inflammatory and oxidative stress markers. The treatment with MRS5980 attenuated all the analyzed functional, biochemical and histopathological markers in a dose-dependent manner. Our findings support the therapeutic potential of A₃AR agonists in lung fibrosis by demonstrating reduced disease progression, as indicated by decreased inflammation, TGF-β expression and fibrotic remodeling.     

Nano-CdZr4(PO4)6 as a reusable and robust catalyst for the synthesis of bis-thiazolidinones by a multicomponent reaction of aldehydes,ethylenediamine and thioglycolic acid

Nano-CdZr₄(PO₄)₆ has been used as an efficient catalyst for the preparation of bis-thiazolidinones by pseudo-five-component reaction of aldehydes, ethylenediamine and thioglycolic acid under reflux conditions in toluene. The present synthetic protocol has several advantages, such as simplicity, excellent yields, short reaction times, reusability of the catalyst and low catalyst loading.     

Surface alteration of (VO)2P2O7 by α-Sb2O4 as a route to control the n-butane selective oxidation

The catalytic properties of (VO)₂P₂O₇/α-Sb₂O₄ mixed oxides system for n-butane mild oxidation have been investigated on two mechanical mixtures (M1 and M2) of the same well crystallized (VO)₂P₂O₇ (reference vanadyl pyrophosphate) with two different morphologies of α-Sb₂O₄.The M1 mixture of (VO)₂P₂O₇ with α-Sb₂O₄ (1), prepared by oxidation of Sb₂O₃, leads to the oxidative dehydrogenation (ODH) of n-butane, whereas the M2 mixture of (VO)₂P₂O₇ with a commercial α-Sb₂O₄ (2) (Aldrich) with a different morphology improves the maleic anhydride selectivity as compared to the reference (VO)₂P₂O₇ catalyst (synergetic effect). After reaction, no ternary VPSbO phase is detected by XRD and DTA and it was controlled that the two α-Sb₂O₄ oxides are catalytically inactive.The (VO)₂P₂O₇ reference catalyst which produced only maleic anhydride as mild oxidation product shows by XPS a slightly oxidized surface (14% V⁵⁺–86% V⁴⁺).Contamination of the (VO)₂P₂O₇ phase by migration of Sb species occurs after catalytic reaction in the case of the M1 mixture as shown by XPS, LEIS and TEM–EDX analysis. XPS showed that (VO)₂P₂O₇ is partially superficially reduced (86% V⁴⁺–14% V³⁺). This feature is consistent with the decrease of acidity as observed by pyridine adsorption–desorption.In opposition with the M1 mixture, no contamination of the (VO)₂P₂O₇ phase is observed after catalytic reaction in the case of the M2 mixture. The XPS study shows, in this case, that (VO)₂P₂O₇ is partially oxidized (30% V⁵⁺–70% V⁴⁺) at a higher level than for the reference (VO)₂P₂O₇ catalyst. This situation is associated with the increase of selectivity observed for maleic anhydride (synergetic effect).The difference in the catalytic results for the two M1 and M2 mixtures, as compared to the (VO)₂P₂O₇ reference catalyst, can be explained by the alteration of the surface composition of (VO)₂P₂O₇ and the distribution of vanadium oxidation state due to different interaction between Sb₂O₄and (VO)₂P₂O₇, depending on the orientation of the α-Sb₂O₄ crystals.