A novel μ-oxo-diruthenium(III,III)-ibuprofen-(4-aminopyridine) chloride derived from the diruthenium(II,III)-ibuprofen paddlewheel metallodrug shows anticancer properties.

Diruthenium(II,III) metal-metal multiply bonded paddlewheel complexes bearing non-steroidal anti-inflammatory drugs are promising anticancer metallodrugs. The [Ru(Ibp)Cl] (Ibp, ibuprofenate anion from HIbp ibuprofen drug), free or encapsulated, shows anticancer activity against glioblastoma (in vitro, in vivo), and against human breast and prostate cancer cells. Herein we report the interaction of [Ru(Ibp)Cl] and of [Ru(Ac)(HO)]PF (Ac, acetate) with the 4-aminopyridine (4Apy) drug.

Plasma estradiol and progesterone concentrations during the female reproductive cycle in a highly placentotrophic viviparous lizard, Mabuya sp.

The neotropical genus Mabuya are obligate placentotrophic viviparous lizards, which have a short vitellogenesis that produces microlecithal oocytes and a prolonged time of gestation (9 to 10 months). The hormonal control of female reproductive activity during follicular growth and pregnancy has not been studied, although it is known that the corpus luteum can produce progesterone, but regresses early in pregnancy, being replaced in this function by the placenta. Through enzyme immunoassay (EIA) we measured the plasma concentrations of estradiol (E) and progesterone (P) in females of a population of Mabuya sp at different stages of their reproductive cycle.

Validation of an enzyme immunoassay for the quantification of testosterone in green iguana males (Iguana iguana).

The endocrinological study by immunological methods allows elucidating mechanisms of response to environmental challenges and reproductive regulatory mechanisms in animals. However, it is often overlooked that immunological assays for the detection and quantification of steroid hormones require prior validation tests. In this study, the efficacy of a commercial enzyme immunoassays (EIA) was evaluated for the quantification of plasma testosterone (T) in males from a population of green iguanas (Iguana iguana) in semi-captivity.

Growth inhibitory effects of the Diruthenium-Ibuprofen compound, [Ru2Cl(Ibp) 4], in human glioma cells in vitro and in the rat C6 orthotopic glioma in vivo.

The Diruthenium-Ibuprofen compound [Ru2Cl(Ibp)4] (or RuIbp) is known to cause significant inhibition of C6 rat glioma cell proliferation in vitro. RuIbp increased the expression of cell cycle-related proteins such as p21 and p27 and the pro-apoptotic protein Bax, as well as causing a reduction in mitochondrial membrane potential and a modest increase in apoptosis in vitro. The present study extended these findings by (i) investigating the effects of RuIbp on human glioma cell line proliferation in vitro and (ii) investigating the acute and chronic toxicology of the compound in normal Wistar rats.

Kinetic and mechanistic studies on reactions of diruthenium(II,III) with biologically relevant reducing agents.

Diruthenium(ii,iii)-tetracarboxylates have shown promising anticancer properties as metallotherapeutics. On the basis of the role that bio-reducing agents may play on the mode of action of ruthenium-based anticancer drugs, we performed detailed kinetic studies on the reaction of ascorbic acid and glutathione with the [Ru2(RCOO)4](+) paddlewheel framework by using the non-drug, diaqua complex ion [Ru2(CH3COO)4(H2O)2](+). In the presence of the reducing agents, the diaqua-Ru2 species first undergo a ligand substitution reaction by which the axially-coordinated water is displaced by the reducing agent.

Thermodynamics of axial substitution and kinetics of reactions with amino acids for the paddlewheel complex tetrakis(acetato)chloridodiruthenium(II,III).

The known paddlewheel, tetrakis(acetato)chloridodiruthenium(II,III), offers a versatile synthetic route to a novel class of antitumor diruthenium(II,III) metallo drugs, where the equatorial ligands are nonsteroidal anti-inflammatory carboxylates. This complex was studied here as a soluble starting prototype model for antitumor analogues to elucidate the reactivity of the [Ru(2)(CH(3)COO)(4)](+) framework. Thermodynamic studies on equilibration reactions for axial substitution of water by chloride and kinetic studies on reactions of the diaqua complexes with the amino acids glycine, cysteine, histidine, and tryptophan were performed.