The synthesis, characterization, acute toxicity, antitumor activity, and histopathological analysis of a novel dinuclear platinum(2+) complex - [Pt(DACH-κ2N)µ-(C4H2O6-κ4O)Pt(DACH-κ2N)] - is reported. Through acute toxicity tests, it was possible to place the platinum complexes into categories according to the OECD protocol. The dinuclear complex was classified in category 2 (cisplatin - category 1; and oxaliplatin - category 2). Analyzing the interaction between dsDNA and dinuclear complex was observed an Tm increase, suggesting that the dinuclear complex-dsDNA interact probably through of the interstrand form. Evaluations of tumor masses extracted from mice inoculated with Ehrlich carcinoma demonstrated a percent of tumor inhibition similar for cisplatin and oxaliplatin, but statistically different and superior for the case of the dinuclear complex. Cisplatin and oxaliplatin showed 41.4 and 40.8% inhibition, respectively, while the dinuclear complex presented 66.3%. The histopathological analysis demonstrated that the group treated with cisplatin showed more significant tissue damage, moderate hepatic steatosis, and nephritis. The livers, spleens, and kidneys of the animals treated with the dinuclear complex were within the normality range with no tissue lesions, and absence of metastasis.

In this article the synthesis, characterization, acute toxicity, and antitumor activity of the novel Ru3+ complex are described. Through the acute toxicity tests, it was possible to fit the complexes into categories according to the OECD protocol guideline 423. The cisplatin complex was classified in category 1 and the sodium diaquodimalonateruthenate(3+) - Na[Ru(H2O)2(Mal-κ2O)2] - was classified in category 4. This result demonstrates the lower toxicity achieved by the ruthenium complex in comparison with metallopharmaceuticals compound. Evaluations of tumor masses extracted from mice inoculated with Ehrlich ascites carcinoma demonstrated percent inhibition lowest to cisplatin. Cisplatin showed 58% inhibition (1 mg/kg), while Na[Ru(H2O)2(Mal-κ2O)2] complex (5 mg/kg) presented 77%.

The synthesis, characterization, cytotoxicity and antitumor activity of platinum(II) complexes coordinated to O-glycoside and analogous is reported. Through the acute toxicity tests, it was possible to fit the complexes into categories according to the OECD protocol. The cis-[PtCl2(C6H14S2O2)-κ2S] complex was classified in category 3 and the cis-[PtCl2(C26H38O12S2)-κ2S] complex was classified in category 4. This result demonstrates the lower toxicity achieved by the glycoside in comparison with its analogous system. Evaluations of tumor masses extracted from mice inoculated with Ehrlich carcinoma demonstrated percent inhibition similar to cisplatin and synthesized platinum complexes. Cisplatin showed 59% inhibition, while cis-[PtCl2(C6H14S2O2)-κ2S] and cis-[PtCl2(C26H38O12S2)-κ2S] complexes presented 57% and 59%, respectively. Although the glycosidic compounds exhibit tumor activity, reported in the literature, the presence of platinum ion was shown to be determinant for antitumor action according with the compounds tested, since the glycosidic ligand presented tumor inhibition of only 38%, with a similar antitumor activity in relation to cisplatin.

ABSTRACT In this work, a matrix based on silica xerogel, synthesized from TEOS, water, ibuprofen (as template) and acetic acid at room temperature, was used for ibuprofen (IBF) incorporation, aiming to create a drug delivery system capable of releasing this compound under a basic pH condition (considering desirable and optimal release in the intestines). The IBF release was checked at different pH values (ranging from 2 to 8), using appropriate buffered solutions. After observing the IBF release performance from the silica xerogel and its dependence on the pH, the same matrix containing IBF was submitted to a novel assay, using only a pH 7 buffered solution as the best way to check the chronological release. This was carried out at 1, 2, 5 and 10 minutes to determine aliquot removal, as well as IBF concentration at each elapsed period.

The synthesis, characterization and antimicrobial activity of novel vanadium (IV) complex derived of amide natural piplartine is reported. The minimum inhibitory concentrations (MIC) of complex, piplartine and vanadyl sulphate used in the synthesis were determined against six bacteria and one fungus. The complex exhibited good activity with minimal inhibitory concentration values ranging from 156.2 to 625 µg mL-1, it was observed the lowest value for the Escherichia coli bacteria with MIC 156.2 µg mL-1 and Microsporum gypseum fungus with MIC 312.5 µg/mL. In overall, the complex showed better antimicrobial activity than the piplartine. Additionally, the V-PIP complex was completely soluble in water, on the contrary of the piplartine free; which means that the proposal complex consists in a potential candidate to drug.