Synthesis and Biological Evaluation of Papain‐Family Cathepsin L‐Like Cysteine Protease Inhibitors Containing a 1,4‐Benzodiazepine Scaffold as Antiprotozoal Agents

Novel papain‐family cathepsin L‐like cysteine protease inhibitors endowed with antitrypanosomal and antimalarial activity were developed, through an optimization study of previously developed inhibitors. In the present work, we studied the structure–activity relationships of these derivatives, with the aim to develop new analogues with a simplified and more synthetically accessible structure and with improved antiparasitic activity. The structure of the model compounds was significantly simplified by modifying or even eliminating the side chain appended at the C3 atom of the benzodiazepine scaffold. In addition, a simple methylene spacer of appropriate length was inserted between the benzodiazepine ring and the 3‐bromoisoxazoline moiety. Several rhodesain and falcipain‐2 inhibitors displaying single‐digit micromolar or sub‐micromolar antiparasitic activity against one or both parasites were identified, with activities that were one order of magnitude more potent than the model compounds.     

Effect of APE1 T2197G (Asp148Glu) Polymorphism on APE1, XRCC1, PARP1 and OGG1 Expression in Patients with Colorectal Cancer

It has been hypothesized that genetic variation in base excision repair (BER) might modify colorectal adenoma risk. Thus, we evaluated the influence of APE1 T2197G (Asp148Glu) polymorphism on APE1, XRCC1, PARP1 and OGG1 expression in normal and tumor samples from patients with colorectal cancer. The results indicate a downregulation of OGG1 and an upregulation of XRCC1 expression in tumor tissue. Regarding the anatomical location of APE1, OGG1 and PARP-1, a decrease in gene expression was observed among patients with cancer in the rectum. In patients with or without some degree of tumor invasion, a significant downregulation in OGG1 was observed in tumor tissue. Interestingly, when taking into account the tumor stage, patients with more advanced grades (III and IV) showed a significant repression for APE1, OGG1 and PARP-1. XRCC1 expression levels were significantly enhanced in tumor samples and were correlated with all clinical and histopathological data. Concerning the polymorphism T2197G, GG genotype carriers exhibited a significantly reduced expression of genes of the BER repair system (APE1, XRCC1 and PARP1). In summary, our data show that patients with colorectal cancer present expression changes in several BER genes, suggesting a role for APE1, XRCC1, PARP1 and OGG1 and APE1 polymorphism in colorectal carcinogenesis.     

Hyperbranched polyglycerols,obtained from environmentally benign monomer,as reactive clays inhibitors for water‐based drilling fluids

To prevent the degradation of the borehole and also the disintegration and dispersion of drilled cuttings, different shale stabilizing additives are used in water‐based drilling fluids (WBFs). Glycols, poly(ethylene glycol), glycerols, and polyglycerol derivatives, also called polyols, have been used to inhibit shales containing reactive clays in WBF. These additives are normally used in conjunction with KCl to reduce clay swelling and dispersion of drilled cuttings. Highly branched polymers have become an important field in current polymer science. Such materials typically exhibit compact, globular structures in combination with an exceptionally high number of sites with functional groups. They have unique properties that differ significantly from their linear counterparts, and the hyperbranched polyglycerol (hPG) is an important hyperbranched polymer that can be produced from an environmentally benign monomer, the glycerol carbonate. In this article, the clay inhibitive properties of hPG were evaluated by different test methods including bentonite inhibition test, cuttings recovery, and X‐ray diffraction measurements. The results show that the hPG has a great potential to be used as an environmental friendly inhibitor additive in WBFs. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 40384.     

Processing and thermal properties of composites based on recycled PET,sisal fibers,and renewable plasticizers

This investigation focuses on the preparation of bio‐based composites from recycled poly (ethylene terephthalate) (PET) and sisal fibers (3 cm, 15 wt %), via thermopressing process. Plasticizers derived from renewable raw materials are used, namely, glycerol, tributyl citrate (TBC) and castor oil (CO), to decrease the melting point of the recycled PET (T_m ∼ 265°C), which is sufficiently high to initiate the thermal decomposition of the lignocellulosic fiber. All used materials are characterized by thermogravimetric analysis and differential scanning calorimetry, and the composites are also characterized via dynamic mechanical thermal analysis. The storage modulus (30°C) and the tan δ peak values of CT [PET/sisal/TBC] indicate that TBC also acts as a compatibilizing agent at the interface fiber/PET, as well as a plasticizer. To compare different processing methods, rheometry/thermopressing and compression molding are used to prepare the recycled PET/sisal/glycerol/CO composites. These two different methods of processing show no significant influence on the thermal properties of these composites. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 40386.     

Different bacterial models for in vitro induction of non‐cavitated enamel caries‐like lesions: Microhardness and polarized light miscroscopy analyses

The aim of this study was to compare different bacterial models for in vitro induction of non‐cavitated enamel caries‐like lesions by microhardness and polarized light microscopy analyses. One hundred blocks of bovine enamel were randomly divided into four groups (n = 25) according to the bacterial model for caries induction: (A) Streptococcus mutans, (B) S. mutans and Lactobacillus acidophilus, (C) S. mutans and L. casei, and (D) S. mutans, L. acidophilus, and L. casei. Within each group, the blocks were randomly divided into five subgroups according to the duration of the period of caries induction (4–20 days). The enamel blocks were immersed in cariogenic solution containing the microorganisms, which was changed every 48 h. Groups C and D presented lower surface hardness values (SMH) and higher area of hardness loss (ΔS) after the cariogenic challenge than groups A and B (P < 0.05). As regards lesion depth, under polarized light microscopy, group A presented significantly lower values, and groups C and D the highest values. Group B showed a higher value than group A (P < 0.05). Groups A and B exhibited subsurface caries lesions after all treatment durations, while groups C and D presented erosion‐type lesions with surface softening. The model using S. mutans, whether or not it was associated with L. acidophilus, was less aggressive and may be used for the induction of non‐cavitated enamel caries‐like lesions. The optimal period for inducing caries‐like lesions was 8 days. Microsc. Res. Tech. 78:444–451, 2015. © 2015 Wiley Periodicals, Inc.     

Novel intelligent real-time position tracking system using FPGA and fuzzy logic

The main aim of this paper is to test if FPGAs are able to achieve better position tracking performance than software-based soft real-time platforms. For comparison purposes, the same controller design was implemented in these architectures. A Multi-state Fuzzy Logic controller (FLC) was implemented both in a Xilinx^®${\mathrm{Xilinx}}^{\circledR }$ Virtex-II FPGA (XC2v1000) and in a soft real-time platform NI CompactRIO^®-9002${\mathrm{CompactRIO}}^{\circledR }\mathrm{-}9002$. The same sampling time was used. The comparative tests were conducted using a servo-pneumatic actuation system. Steady-state errors lower than 4 μm were reached for an arbitrary vertical positioning of a 6.2 kg mass when the controller was embedded into the FPGA platform. Performance gains up to 16 times in the steady-state error, up to 27 times in the overshoot and up to 19.5 times in the settling time were achieved by using the FPGA-based controller over the software-based FLC controller.     

New carbon composite adsorbents for the removal of textile dyes from aqueous solutions: Kinetic,equilibrium, and thermodynamic studies

New carbon composite materials were prepared by pyrolysis of mixture of coffee wastes and red mud at 700 °C with the inorganic: organic ratios of 1.9 (CC-1.9) and 2.2 (CC-2.2). These adsorbents were used to remove reactive orange 16 (RO-16) and reactive red 120 (RR-120) textile dyes from aqueous solution. The CC-1.9 and CC-2.2 materials were characterized using Fourier transform infrared spectroscopy, Nitrogen adsorption/desorption curves, scanning electron Microscopy and X-ray diffraction. The kinetic of adsorption data was fitted by general order kinetic model. A three-parameter isotherm model, Liu isotherm model, gave the best fit of the equilibrium data (298 to 323 K). The maximum amounts of dyes removed at 323 K were 144.8 (CC-1.9) and 139.5 mg g^?1 (CC-2.2) for RO-16 dye and 95.76 (CC-1.9) and 93.80 mg g^?1 (CC-2.2) for RR-120 dye. Two simulated dyehouse effluents were used to investigate the application of the adsorbents for effluent treatment.     

Follicular development and morphological changes in the vaginal epithelium during the estrous cycle of Galea spixii

The current study aimed to determine if characteristics observed in vaginal cytology during the estrous cycle of female SYT cavies corresponded with proliferation of the vaginal epithelium, characterized by proliferating cell nuclear antigen (PCNA) immunolocalization, and with follicular development at different phases of the estrous cycle. After determining estrous cycle phases by vaginal cytology, females were euthanized at metestrus, diestrus, proestrus, and estrus. Histological study of the vaginal epithelium and ovary were then performed. Immunohistochemistry for PCNA in vaginal tissue at each cycle phase was also performed. Superficial cornified cells and early post‐ovulatory follicles were found at estrus. Few nuclei below the enucleate superficial cells were immunoreactive to PCNA. At metestrus, the vaginal epithelium underwent desquamation and lost the superficial cornified cells; basal and intermediate cells appeared, and the post‐ovulatory follicle formed an early corpus luteum. No PCNA immunoreactivity was observed. At diestrus, the corpus luteum was developed, and the vaginal epithelium contained basal and intermediate cells. There was PCNA immunoreactivity in the cellular nucleus in the germinative stratum of the epithelium. Because of the growth and maturation of ovarian follicles, the vaginal epithelium suffered intense proliferation at proestrus. Vaginal cytology revealed large intermediate cells and nucleated and enucleated superficial cornified cells. In the ovary, mature follicles were present. More apparent immunoreactivity of PCNA in the germinative layer was found. In summary, we inferred that vaginal exfoliative findings matched the proliferation process of the vaginal epithelium. PCNA immunolocalization occurred as well as corresponding follicular development in the ovaries.     

Influence of acceleration setting reaction by halogen light‐curing on GIC–dentin interface: Qualitative analysis by SEM

The aim of this study was to evaluate by scanning electron microscope (SEM) photomicrographs the influence of application of halogen light‐curing for fastening the set reaction of high‐viscosity glass ionomer cements (GIC) by assessing the material/dentin interface. Twelve human primary canines were assigned in four groups (n = 3) according to the GIC (Fuji IX, GC or Maxxion R, FGM) and application of halogen light‐curing (60 sec or control—no external energy). Blocks with approximately 6 mm of height were buildup on previously pre‐treated dentin surface in according to the experimental group. After storage at 37 °C, 100% humidity for 48 h, the specimens were then sectioned in slices with 1‐mm thick. The slices were qualitative analyzed using SEM to evaluate possible structural changes. Two examiners independently evaluated the images in order to observe the spherical hollow spaces of each tooth. The photomicrographs revealed the presence of spherical hollow spaces in all experimental groups. However, in both groups that received halogen light‐curing application, it was possible to observe that the presence of these hollow spaces decreased in size and quantity. It can be concluded that the halogen light‐curing application positively decreases in size and quantity in the presence of spherical hollow spaces in GIC.