Synthesis, crystal structures, antimicrobial, antifungal and antituberculosis activities of mixed ligand silver(I) complexes

The biological activity of some new mixed silver-phosphane-thio-ligand complexes, with 1:1:2, 1:1:1 and 1:2:1 (Ag:phospine:ligand) compositions, have been examined. Ten compounds were prepared using a series of silver(I) salts [AgX, where X = NO3, ClO4, PF6 and Br], tertiary phosphines and the ligands thi-osemicarbazide, 2-(propan-2-ylidene) hydrazinecarbothioamide, and thiazolidine-2-thione. The syntheses were carried out under ambient conditions, and the ten complexes obtained were found to be light stable. All 10 compounds were characterized by elemental analysis, FTIR, and NMR spectroscopy, whereas nine compounds were characterized by X-ray diffraction analysis. The anti-proliferative activities were evaluated by minimum inhibitory concentration (MIC: lg/mL) in an aqueous suspension system and they all show promising potential activity against selective strains of Gram-positive and Gram-negative bacteria, fungous and Mycrobaterium tuberculosis H37Rv. © 2013 Elsevier Ltd. All rights reserved.

Isolation, homology modeling and renal effects of a C-type natriuretic peptide from the venom of the Brazilian yellow scorpion (Tityus serrulatus)

Mammalian natriuretic peptides (NPs) have been extensively investigated for use as therapeutic agents in the treatment of cardiovascular diseases. Here, we describe the isolation, sequencing and tridimensional homology modeling of the first C-type natriuretic peptide isolated from scorpion venom. In addition, its effects on the renal function of rats and on the mRNA expression of natriuretic peptide receptors in the kidneys are delineated. Fractionation of Tityusserrulatus venom using chromatographic techniques yielded a peptide with a molecular mass of 2190.64Da, which exhibited the pattern of disulfide bridges that is characteristic of a C-type NP (TsNP, T. serrulatus Natriuretic Peptide). In the isolated perfused rat kidney assay, treatment with two concentrations of TsNP (0.03 and 0.1μg/mL) increased the perfusion pressure, glomerular filtration rate and urinary flow. After 60min of treatment at both concentrations, the percentages of sodium, potassium and chloride transport were decreased, and the urinary cGMP concentration was elevated. Natriuretic peptide receptor-A (NPR-A) mRNA expression was down regulated in the kidneys treated with both concentrations of TsNP, whereas NPR-B, NPR-C and CG-C mRNAs were up regulated at the 0.1μg/mL concentration. In conclusion, this work describes the isolation and modeling of the first natriuretic peptide isolated from scorpion venom. In addition, examinations of the renal actions of TsNP indicate that its effects may be related to the activation of NPR-B, NPR-C and GC-C. © 2013 Elsevier Ltd.

Structure-function relationships of the peptide Paulistine: A novel toxin from the venom of the social wasp Polybia paulista

Background: The peptide Paulistine was isolated from the venom of wasp Polybia paulista. This peptide exists under a natural equilibrium between the forms: oxidised - with an intra-molecular disulphide bridge; and reduced - in which the thiol groups of the cysteine residues do not form the disulphide bridge. The biological activities of both forms of the peptide are unknown up to now. Methods: Both forms of Paulistine were synthesised and the thiol groups of the reduced form were protected with the acetamidemethyl group [Acm-Paulistine] to prevent re-oxidation. The structure/activity relationships of the two forms were investigated, taking into account the importance of the disulphide bridge. Results: Paulistine has a more compact structure, while Acm-Paulistine has a more expanded conformation. Bioassays reported that Paulistine caused hyperalgesia by interacting with the receptors of lipid mediators involved in the cyclooxygenase type II pathway, while Acm-Paullistine also caused hyperalgesia, but mediated by receptors involved in the participation of prostanoids in the cyclooxygenase type II pathway. Conclusion: The acetamidemethylation of the thiol groups of cysteine residues caused small structural changes, which in turn may have affected some physicochemical properties of the Paulistine. Thus, the dissociation of the hyperalgesy from the edematogenic effect when the actions of Paulistine and Acm-Paulistine are compared to each other may be resulting from the influence of the introduction of Acm-group in the structure of Paulistine. General significance: The peptides Paulistine and Acm-Paulistine may be used as interesting tools to investigate the mechanisms of pain and inflammation in future studies. © 2013 Elsevier B.V.

Síntese e estudos estrutura/função de um peptídeo extraído da rã Hypsiboas albopunctatus e análogos

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Arrabidaea chica (HBK) Verlot: phytochemical approach, antifungal and trypanocidal activities

Arrabidaea chica (HBK.) Verlot (Bignoniaceae) popularmente, "Pariri", é um arbusto escandente, distribuído do sul do México até a Guiana e Brasil central e é tradicionalmente indicado para tratar sintomas de inflamações e afecções da pele. Seu extrato etanólico foi quimicamente investigado e testado contra leveduras e fungos dermatófitos. A atividade tripanocida do mesmo extrato foi também avaliada. Este trabalho reporta o isolamento de três flavonóides, a inibição total do crescimento de Trichophyton mentagrophytes e um significante efeito tripanocida do extrato etanólico e de suas frações. Não foi detectada qualquer toxicidade aguda relevante, mesmo a uma dose de 1000 mg/kg

Environmental isolation, biochemical identification, and antifungal drug susceptibility of Cryptococcus species

Introduction The incidence of opportunistic fungal infections has increased in recent years and is considered an important public health problem. Among systemic and opportunistic mycoses, cryptococcosis is distinguished by its clinical importance due to the increased risk of infection in individuals infected by human immunodeficiency virus. Methods To determine the occurrence of pathogenic Cryptococcus in pigeon excrement in the City of Araraquara, samples were collected from nine environments, including state and municipal schools, abandoned buildings, parks, and a hospital. The isolates were identified using classical tests, and susceptibility testing for the antifungal drugs (fluconazole, itraconazole, voriconazole, and amphotericin B) independently was also performed. After collection, the excrement samples were plated on Niger agar and incubated at room temperature. Results A total of 87 bird dropping samples were collected, and 66.6% were positive for the genus Cryptococcus. The following species were identified: Cryptococcus neoformans (17.2%), Cryptococcus gattii (5.2%), Cryptococcus ater (3.5%), Cryptococcus laurentti (1.7%), and Cryptococcus luteolus (1.7%). A total of 70.7% of the isolates were not identified to the species level and are referred to as Cryptococcus spp. throughout the manuscript. Conclusions Although none of the isolates demonstrated resistance to antifungal drugs, the identification of infested areas, the proper control of birds, and the disinfection of these environments are essential for the epidemiological control of cryptococcosis.

B-type natriuretic peptide in the evaluation of cardiac function

B type natriuretic peptide (BNP) and its precursor, the inactive form of NT-pro-BNP, are currently the most studied laboratory parameters in the heart disease spectrum. The assessment of their blood concentrations provides invaluable information on the likelihood, severity and prognosis of the disease. The present review aims to describe the biological determinants, the factors that influence these peptide concentrations, the suggested cutoff values for the diagnosis of heart failure and the use of this biomarker in the assessment of cardiac function.

Antifungal activity of flavonoids from Heteropterys byrsonimifolia and a commercial source against Aspergillus ochraceus: In silico interactions of these compounds with a protein kinase

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Susceptibility variation of Malassezia pachydermatis to antifungal agents according to isolate source

Malassezia pachydermatis is associated with dermatomycoses and otomycosis in dogs and cats. This study compared the susceptibility of M. pachydermatis isolates from sick (G1) and healthy (G2) animals to azole and polyene antifungals using the M27-A3 protocol. Isolates from G1 animals were less sensitive to amphotericin B, nystatin, fluconazole, clotrimazole and miconazole.