Complessi di rutenio con attività chemioterapica antitumorale

La presente invenzione riguarda l’utilizzo di complessi di rutenio come agenti chemioterapici antitumorali. I complessi dell’invenzione sono utili nel trattamento di pazienti con tumori solidi metastatici molto spesso resistenti ai farmaci antitumorali comunemente utilizzati. I complessi dell’invenzione mostrano meno effetti collaterali per l'ospite rispetto a quelli sviluppati da altri agenti chemioterapici a base metallica

Antiproliferative Activity of a New (Arene)Ruthenium(II) Complex on a Model of Breast Cancer

Following our previous studies,1 novel (arene)ruthenium(II) complexes containing neutral chelating nitrogen ligands, with general formula [Ru(arene)(L’)Cl]Cl, have been prepared by reacting the ligands L’ (L’ in general; in detail, L1 = bis(pyrazol-1-yl)methane; L2 = bis(3,5-dimethylpyrazol-1-yl) methane) with some dinuclear organometallic acceptors of ruthenium, such as (para-cymene)ruthenium(II) dichloride, (benzene)ruthenium(II) dichloride and (hexamethylbenzene)ruthenium(II) dichloride. The solid-state structures of these half-sandwich organometallic complexes were determined by X-ray crystallographic studies.1 Their antiproliferative properties were assessed in vitro and in vivo screening assays and it was found that the Ru(II) complexes exhibit potent antiproliferative activity against different human malignant cancer cells, even in comparison with cisplatin and NAMI-A (Figure 1). Moreover, our data clearly that some Ru(II) complexes are characterized by a strong ability to block cells migration associated with a low toxicity

Association of osteopontin regulatory polymorphisms with systemic sclerosis

To test the involvement of osteopontin gene (OPN) in systemic sclerosis (SSc) susceptibility, two OPN single nucleotide polymorphisms previously reported to be associated with systemic lupus erythematosus, namely -156G/GG (proximal promoter) and +1239A/C (3' untranslated region (UTR)), were tested in 357 Italian patients and 864 matched control subjects. OPN serum levels were determined by enzyme-linked immunosorbent assay in 32 patients and 116 controls. Compared with the controls, in SSc patients there was a significantly increased frequency of the alleles -156G (p = 0.0086), and +1239C (p = 0.00064), paralleling the association reported for systemic lupus erythematosus. According to logistic regression analysis, this association is primarily due to the effect of +1239 single nucleotide polymorphism. OPN serum levels were significantly higher in SSc patients than in controls (p = 0.00025). These data suggest that OPN genetic variations have a role in SSc susceptibility, reporting for the first time an involvement of this molecule in SSc pathogenesis and emphasizing that SSc shares pathogenetic mechanisms with other autoimmune diseases