Nanoparticles increase the efficacy of cancer chemopreventive agents in cells exposed to cigarette smoke condensate

Lung cancer is a leading cause of death in developed countries. Although smoking cessation is a primary strategy for preventing lung cancer, former smokers remain at high risk of cancer. Accordingly, there is a need to increase the efficacy of lung cancer prevention. Poor bioavailability is the main factor limiting the efficacy of chemopreventive agents. The aim of this study was to increase the efficacy of cancer chemopreventive agents by using lipid nanoparticles (NPs) as a carrier. This study evaluated the ability of lipid NPs to modify the pharmacodynamics of chemopreventive agents including N-acetyl-L-cysteine, phenethyl isothiocyanate and resveratrol (RES). The chemopreventive efficacy of these drugs was determined by evaluating their abilities to counteract cytotoxic damage (DNA fragmentation) induced by cigarette smoke condensate (CSC) and to activate protective apoptosis (annexin-V cytofluorimetric staining) in bronchial epithelial cells both in vitro and in ex vivo experiment in mice. NPs decreased the toxicity of RES and increased its ability to counteract CSC cytotoxicity. NPs significantly increased the ability of phenethyl isothiocyanate to attenuate CSC-induced DNA fragmentation at the highest tested dose. In contrast, this potentiating effect was observed at all tested doses of RES, NPs dramatically increasing RES-induced apoptosis in CSC-treated cells. These results provide evidence that NPs are highly effective at increasing the efficacy of lipophilic drugs (RES) but are not effective towards hydrophilic agents (N-acetyl-L-cysteine), which already possess remarkable bioavailability. Intermediate effects were observed for phenethyl isothiocyanate. These findings are relevant to the identification of cancer chemopreventive agents that would benefit from lipid NP delivery.

Efficiency comparison of hyperbranched polymers as toughening agents for a one-part epoxy resin

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Thermal stability and thermal decomposition of the antihypertensive drug amlodipine besylate

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

The effect of non-antihypertensive doses of angiotensin converting enzyme inhibitor on myocardial necrosis and hypertrophy in young rats with renovascular hypertension

In renovascular hypertensive rats, low doses of angiotensin converting enzyme (ACE) inhibitors have been found to prevent myocardial hypertrophy independent of blood pressure level. This finding would suggest humoral rather than mechanical control of myocyte growth. The aim of this study was to examine the effect of nonantihypertensive doses of ACE inhibitor on myocardial hypertrophy and necrosis in hypertensive rats. Renovascular hypertension (RHT) was induced in four-week-old Wistar rats. Twenty-eight animals were treated for four weeks with three doses of ramipril (0.01, 0.1 or 1. 0 mg/kg/day, which are unable to lower blood pressure. Fourteen animals were not treated (RHT group). A sham operated, age/sex-matched group was used as control (n = 10). Myocardial histology was analysed in 3 microm thick sections of the ventricle stained with either haematoxylin-eosin, reticulin silver stain or Masson's trichrome. There was a significant correlation between systolic blood pressure and left ventricular to body weight ratio in both sets of animals: untreated plus controls and ramipril-treated rats. ACE inhibition prevented myocyte and perivascular necrosis and fibrosis in a dose-dependent manner. We conclude that myocardial hypertrophy in rats with renovascular hypertension is directly related to arterial pressure, and that this relationship is not affected by nonantihypertensive doses of ACE inhibitor. Myocardial necrosis/fibrosis and coronary artery damage induced by angiotensin II are prevented by ACE inhibitor in a dose-dependent manner, despite the presence of arterial hypertension.

Effect of incorporation of remineralizing agents into bleaching gels on the microhardness of bovine enamel in situ

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents

In the search for new therapeutic tools against tuberculosis and to further address the therapeutic potential of pyridine-2-thiol 1-oxide (Hmpo) metal complexes, two new octahedral [M(III)(mpo)3] complexes, with M = Ga or Bi, were synthesized and characterized in the solid state and in solution. Attempts to crystallize [Ga(III)(mpo)3] in CH2Cl2 led to single crystals of the reaction product [GaCl(mpo)2], where the gallium(III) ion is in a square basis pyramidal environment, trans-coordinated at the basis to two pyridine-2-thiolato 1-oxide anions acting as bidentate ligands through their oxygen and sulfur atoms. The biological activity of the new [M(III)(mpo)3] complexes together with that of the previously reported Fe(III) analogous compound and the pyridine-2-thiol 1-oxide sodium salt (Na mpo) was evaluated on Mycobacterium tuberculosis. The compounds showed excellent activity, both in the standard strain H37Rv ATCC 27294 (pan-susceptible) and in five clinical isolates that are resistant to the standard first-line anti-tuberculosis drugs isoniazid and rifampicin. These pyridine-2-thiol 1-oxide derivatives are promising compounds for the treatment of resistant tuberculosis.

Effect of collagen matrix saturation on the surface free energy of dentin using different agents

The surface free energy of conditioned-dentin is one of the factors that interfere with monomeric infiltration of the interfibrillar spaces. Saturation of the tooth matrix with different substances may modulate this energy and, consequently, the wettability of the dentin. To evaluate the influence of different substances used to saturate conditioned-dentin on surface free energy (SFE) of this substrate. Dentin blocks (4 × 7 × 1 mm, n = 6/ group), obtained from the roots of bovine incisors, were etched using phosphoric acid for 15 seconds, rinsed and gently dried. The surfaces were treated for 60 seconds with: ultra-purified water (H20-control); ethanol (EtOH), acetone (ACT), chlorhexidine (CHX), ethylenediaminetetraacetic acid (EDTA); or sodium hypochlorite (NaOCl). The tooth surfaces were once again dried with absorbent paper and prepared for SFE evaluation using three standards: water, formamide and bromonaphthalene. Analysis of variance (ANOVA) and Dunnet's tests (a = 0.05) were applied to the data. Ethylenediaminetetraacetic acid was the only substance that caused a change to the contact angle for the standards water and formamide, while only EtOH influenced the angles formed between formamide and the dentin surface. None of the substances exerted a significant effect for bromonaphtha-lene. In comparison to the control, only EDTA and NaOCl altered both polar components of the SFE. Total SFE was increased by saturation of the collagen matrix by EDTA and reduced when NaOCl was used. Saturation of the collagen matrix by EDTA and EtOH changed the surface free energy of the dentin. In addition, the use of NaOCl negatively interfered with the properties evaluated. The increase of surface free energy and wettability of the dentin surface would allow higher penetration of the the adhesive system, which would be of importance to the clinical success of resin-dentin union.

Anti-dementia medications: current prescriptions in clinical practice and new agents in progress

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Tick-borne agents in domesticated and stray cats from the city of Campo Grande, state of Mato Grosso do Sul, midwestern Brazil

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Vanadium complexes with hydrazone or thiosemicarbazone ligands as potential anti-mycobacterium tuberculosis agents

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Toxic heritage: maternal transfer of pyrethroid insecticides and sunscreen agents in dolphins from Brazil

Pyrethroids (PYR) and UV filters (UVF) were investigated in tissues of paired mother-fetus dolphins from Brazilian coast in order to investigate the possibility of maternal transfer of these emerging contaminants. Comparison of PYR and UVF concentrations in maternal and fetal blubber revealed Franciscana transferred efficiently both contaminants to fetuses (F/M > 1) and Guiana dolphin transferred efficiently PYR to fetuses (F/M > 1) different than UVF (F/M < 1). PYR and UVF concentrations in fetuses were the highest-ever reported in biota (up to 6640 and 11,530 ng/g lw, respectively). Muscle was the organ with the highest PYR and UVF concentrations (p < 0.001), suggesting that these two classes of emerging contaminants may have more affinity for proteins than for lipids. The high PYR and UVF concentrations found in fetuses demonstrate these compounds are efficiently transferred through placenta. This study is the first to report maternal transfer of pyrethroids and UV filters in marine mammals.

Brazilian community health agents and qualitative primary healthcare information

The aim of this study was to explore female community health agents’ views about the value of recording qualitative information on contextual health issues they observe during home visits, data that are not officially required to be documented for the Brazilian System of Primary Healthcare Information. Background: The study was conducted in community primary healthcare centres located in the cities of Araçatuba and Coroados (state of São Paulo) and Rio de Janeiro (state of Rio de Janeiro), Brazil. Methods: The design was a qualitative, exploratory study. The purposeful sampling criteria were being female, with a minimum of three years of continuous service in the same location. Data collection with 62 participants was conducted via 11 focus groups (in 2007 and 2008). Audio files were transcribed and submitted to the method of thematic analysis. Four themes guided the analysis: working with qualitative information and undocumented observation; reflecting on qualitative information; integrating/analysing quantitative and qualitative information; and information-sharing with agents and family health teams. In 2010, 25 community health agents verified the final interpretation of the findings. Findings: Participants valued the recording of qualitative, contextual information to expand understanding of primary healthcare issues and as an indicator of clients’ improved health behaviour and health literacy. While participants initiated the recording of additional health information, they generally did not inform the family health team about these findings. They perceived that team members devalued this type of information by considering it a reflection of the clientele’s social conditions or problems beyond the scope of medical concerns. Documentation of qualitative evidence can account for the effectiveness of health education in two ways: by improving preventative care, and by amplifying the voices of underprivileged clients who live in poverty to ensure the most appropriate and best quality primary healthcare for them.

Microhardness of luting agents used for fiber post cementation submitted to thermo cycling

Aims and Objectives: The aim of this study was to analyze the microhardness of three resin cements used in cementing glass fiber posts in bovine incisor. The microhardness was analyzed in cervical, middle and apical thirds before and after thermocycling process. Materials and Methods: Bovine teeth were instrumented and divided into 3 groups composed of 10 teeth each. Then, the teeth were sectioned and obturated and had their canals prepared at a depth of 12mm. Once proceeded the desobturation, the roots and glass fiber posts were prepared for adhesive cementation. After cementation, the microhardness reading was carried out. After initial reading, the samples were placed in a thermocycler and subjected to 2,000 cycles and a new microhardness reading. The data collected were subjected to analysis of variance (ANOVA) and Turkey’s test. Results: It was observed a statistical difference among the microhardness of resin cements. However, the statistical difference of microhardness before and after thermocycling appeared only in group U-200. Conclusion: Thermocycling reduced microhardness values in all cements evaluated in this study. The autopolymerizing cement Multilink presented the most stable microhardness mean values after thermocycling in the coronal, middle and apical thirds.

Effect of light-activation on the antibacterial activity of dentin bonding agents

Aim: This study evaluated the effect of light-activation on the antibacterial activity of dentin bonding systems. Methods: Inocula of Streptococcus mutans and Lactobacillus casei cultures were spread on the surface of BHI agar and the materials were applied and subjected or not to light-activation. Zones of bacterial growth inhibition around the discs were measured. Results: Excite, Single Bond and the bond of Clearfil SE Bond (SE) and Clearfil Protect Bond (CP) did not show any antibacterial activity. The strongest inhibitory activity was observed for the primers of CP and Prompt (PR) against S. mutans and the primers of SE and PB against L. casei. Conclusion: Light-activation significantly reduced or suppressed the antibacterial activity of the initially active uncured dentin bonding systems.