Synthesis and biological evaluation of a polyglutamic acid-dopamine conjugate: a new antiangiogenic agent

Dopamine has previously been shown to inhibit angiogenesis in vitro and in vivo, but its clinical applications in this context are severely limited by its short half-life. Here we report the synthesis of a polyglutamic acid-dopamine conjugate and show that conjugation significantly extends (from 1 to 24 h) dopamine’s antiangiogenic activity in vitro and in vivo. These findings form the basis for the development of a new class of agents for the treatment of angiogenesis-dependent diseases.

Liquid-vapour homogenisation of fluid inclusions in stalagmites: Evaluation of a new thermometer for paleoclimate research

We present a new approach to determine palaeotemperatures (mean annual surface temperatures) based on measurements of the liquid–vapour homogenisation temperature of fluid inclusions in stalagmites. The aim of this study is to explore the potential and the limitations of this new palaeothermometer and to develop a reliable methodology for routine applications in palaeoclimate research. Therefore, we have investigated recent fluid inclusions from the top part of actively growing stalagmites that have formed at temperatures close to the present-day cave air temperature. A precondition for measuring homogenisation temperatures of originally monophase inclusions is the nucleation of a vapour bubble by means of single ultra-short laser pulses. Based on the observed homogenisation temperatures (Th(obs)) and measurements of the vapour bubble diameter at a known temperature, we calculated stalagmite formation temperatures (Tf) by applying a thermodynamic model that takes into account the effect of surface tension on liquid–vapour homogenisation. Results from recent stalagmite samples demonstrate that calculated stalagmite formation temperatures match the present-day cave air temperature within ± 0.2 °C. To avoid artificially induced changes of the fluid density we defined specific demands on the selection, handling and preparation of the stalagmite samples. Application of the method is restricted to stalagmites that formed at cave temperatures greater than ~ 9–11 °C.

Polysialic acid as a drug carrier: evaluation of a new polysialic acid–epirubicin conjugate and its comparison against established drug carriers

This paper explores the potential of polysialic acid (PSA) as a carrier for low molecular weight anticancer drugs. A PSA–epirubicin (Epi) conjugate was synthesized and compared against Epi conjugates containing established carriers, namely: N-(2-hydroxypropyl) methacrylamide (HPMA) copolymers, poly(ethylene glycol) (PEG) and polyglutamic acid (PGA). Biological assessments in the breast cancer cell line MCF-7 and in the anthracycline resistant MCF-7/DX showed that the PSA–Epi conjugate had the highest activity (40% and 30% cell death in the two cell lines at 1 mM Epi equiv., respectively). FACS studies confirmed internalization of all conjugates by cholesterol-dependent endocytosis. PSA–Epi showed release of Epi (40% at 5 h) when incubated with lysosome extracts. In vivo evaluation showed that all conjugates had a significantly longer half-life compared to free Epi. This study also allowed an investigation on the effect of the polymeric carrier on the biological activity of a conjugate, with the biodegradability of the carrier emerging as an important feature.

Synthesis and in vitro evaluation of potential antichagasic hydroxymethyinitrofurazone (NFOH-121): A new nitrofurazone prodrug

The synthesis of mutual prodrugs of nitrofurazone with primaquine, using specific and nonspecific spacer groups, has been previously attempted seeking selective antichagasic agents. The intermediate reaction product, hydroxymethylnitrofurazone (NFOH-121), was isolated and tested in LLC-MK2 culture cells infected with trypomastigotes forms of Trypanosoma cruzi showing higher trypanocidal activity than nitrofurazone and benznidazol in all stages. The mutagenicity tests showed that the prodrug was less toxic than the parent drug. Degradation assays were carried out in pH 1.2 and 7.4. (C) 2003 Elsevier Ltd. All rights reserved.

Synthesis, Characterization and Pharmacological Evaluation of 1-(2-Chloro-6-Fluorophenyl)-5-Methylindolin-2-One: A New Anti-Inflammatory Compound with Reduced Gastric Ulceration Properties

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Radiopacity evaluation of new root canal filling materials by digitalization of images

The aim of this study was to evaluate the radiopacity of five root canal filling materials (AH Plus, Intrafill, Roeko Seal, Epiphany, and EndoRez). Following the International Organization of Standardization 687612001, five circular specimens (10 X 1 mm) were made from each material. After the material set, radiographs were made using occlusal film and a graduated aluminum step-wedge varying in thickness from 2 to 16 mm. The dental X-ray unit (GE1000) was set at 50 Kvp, 10 mA, 18 pulses/second, and distance of 33.5 cm. The radiographs were digitized, and the radiopacity was compared with the aluminum step-wedge, using WIXWIN-2000 software (Gendex). Data (mm Al) were analyzed using ANOVA and Tukey tests. AH Plus and Epiphany were the most radiopaque materials (9.8 and 8.8 mm Al, respectively), followed by EndoRez (7.2 mm Al). Roeko Seal and Intrafill presented the lowest radiopacity values (5.7 and 6.1 mm Al, respectively). Although the materials evaluated demonstrated different radiopacities, all had values above the minimum recommended by the international Organization of Standardization.

Evaluation of new red winemaking technologies through consumer liking

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Isolation and structure elucidation of two new flavonoid glycosides from the infusion of Maytenus aquifolium leaves. Evaluation of the antiulcer activity of the infusion

Droplet countercurrent chromatography and high-performance liquid chromatography fractionation of the aqueous infusion from Maytenus aquifolium Martius leaves afforded two flavonoid tetrasaccharides: quercetin 3-O-alpha-L-rhamnopyranosyl(1-->6)-O-[beta-D-glucopyranosyl(1-->3)-O-alpha-L-rhamnopranosyl( 1-->2)-O-beta-D-galactopyranoside and kaempferol 3-O-alpha-L-rhamnopyranosyl(1-->6)-O-[beta-D-glucopyranosyl( 1-->3)-O-alpha-L-rhamnopyranosy(1-->2-2)-O-beta-D-galactopyranoside. All structures were elucidated by spectroscopic methods. Pharmacological essays of the infusion showed antiulcer activity in rats.

Development of new standard procedures for the evaluation of dental composite abrasive wear

This article discusses the development of a test bench and a methodology for the study of composite resin abrasive wear. To evaluate the operation of the test bench and to compare the proposed methodology with other existing ones, a study was made of the five composites most commonly used by dentists.The one-way ANOVA method and the Tukey test were used to statistically analyze the results by multiple comparisons of the groups of resins tested. Using the proposed methodology, these resins were classified in an increasing order of abrasive wear strength, as follows: Charisma (the lowest abrasive wear strength), Tetric, TPH, Herculite and Z-100 (the highest abrasive wear strength) (P < 0.05). In comparison to other methodologies, the results of the proposed methodology presented the lowest coefficient of variation. (C) 2002 Elsevier B.V. B.V. All rights reserved.

P elements in the saltans group of Drosophila: a new evaluation of their distribution and number of genomic insertion sites

Few are studies on P elements that have addressed the saltans group. These studies had shown that species from the cordata and elliptica subgroups were devoid of any discernible P homologous sequences, while species from the parasaltans, sturtevanti, and saltans subgroups all contain P element sequences. Our analyses showed the presence of one to 15 P element insertion sites in species of the saltans group, including Drosophila neocordata and Drosophila emarginata (cordata and elliptica subgroups, respectively). From these species, only those from the parasaltans, sturtevanti, and saltans subgroups harbor canonical P elements and, only those of the last two subgroups seem to harbor putative full-sized elements. Due to the low similarity of the sequences found in D. neocordata and D. emarginata to those earlier described, we suggest that these sequences might be rudimental P element derivatives that were present in the ancestral of the subgenus Sophophora. (C) 2004 Elsevier B.V. All rights reserved.

Electromyographic evaluation of masseter and anterior temporalis muscles in resting position and during maximum tooth clenching of edentulous patients before and after new complete dentures.

The aim of this study was to assess the electrical activity of the masseter and anterior temporal muscles in patients with severe bone resorption, with complete dentures worn for over ten years, and five months after having new dentures put in place. The RDC questionnaire was applied to twelve asymptomatic patients, before and five months after new dentures were put in place. The electrical activity recordings were made in the mandibular position at rest, and during maximum tooth clenching. The electrical activity of the masseter and anterior temporal muscles in the position at rest presented no statistically significant difference after five months of wearing the new complete dentures. Electrical activity during tooth clenching exhibited a statistically significant reduction only in the right temporal muscle. A period longer than five months of wearing the new complete dentures is required for adaptation and the acquisition of functional capacity.

Evaluation of a new intraoral paralleling device for creating guiding planes: A pilot study

Aim: The aim of the study was to assess the accuracy of a new intraoral paralleling device for creating proximal guiding planes for removable partial dental prostheses. Methods and Materials: Thirty gypsum casts were divided into two groups in which the proximal surfaces of selected teeth were prepared using either a surveying device (Group 1) or the new ParalAB paralleling device (Group 2). In each cast guiding planes were prepared on the distal surface of the maxillary left canine (A), on the mesial and distal surfaces of the maxillary left second molar (B and C), and on the distal surface of the maxillary right canine (D). Each prepared surface formed an angle related to the occlusal plane that was measured five times and averaged by one operator using a tridimensional coordinate machine. Results: The mean guiding plane angles (± standard deviation) for the prepared surfaces were A=91.82° (±0.48°, B=90.47° (±0.47°, C=90.21° (±0.76°, and D=90.50° (±0.73°) for the dental surveyor (Group 1) and A=92.18° (±0.87°), B=90.90° (±0.85°), C=90.07° (±0.92°), and D=90.66° (±0.76°) for the ParalAB paralleling device (Group 2). A two-way ANOVA, Tukey's, and Levène's tests (at p<0.05) revealed statistically significant differences among surfaces prepared by both groups and that one surface Conclusions: The ParalAB device was able to prepare parallel surfaces and despite significant difference between groups, the ParalAB presented a small deviation from absolute parallelism and can be considered a valid method to transfer guide plans in the fabrication of removable partial dentures. Clinical Significance: The preparation of suitable guiding planes on abutment teeth during the fabrication of removable partial dentures is dependent on the ability of the operator and requires considerable chair time. When multiple teeth are involved, achieving parallelism between abutment surfaces can be technically challenging, especially in posterior regions of the mouth. The ParalAB prototype intraoral paralleling device can aid the clinician during the preparation of accurate guiding planes with a minimum degree of occlusal divergence. © 2010 Seer Publishing LLC.