Pharmacology of the glucagon-like peptide-1 analog exenatide extended-release in healthy cats

Exenatide extended-release (ER) is a microencapsulated formulation of the glucagon-like peptide 1-receptor agonist exenatide: It has a protracted pharmacokinetic profile that allows a once-weekly injection with comparable efficacy to insulin with an improved safety profile in type II diabetic people. Here, we studied the pharmacology of exenatide ER in 6 healthy cats. A single subcutaneous injection of exenatide ER (0.13 mg/kg) was administered on day 0. Exenatide concentrations were measured for 12 wk. A hyperglycemic clamp (target = 225 mg/dL) was performed on days 7 (clamp I) and 21 (clamp II) with measurements of insulin and glucagon concentrations. Glucose tolerance was defined as the amount of glucose required to maintain hyperglycemia during the clamp. Continuous glucose monitoring was performed on weeks 0, 2, and 6 after injection. Plasma concentrations of exenatide peaked at 1 h and 4 wk after injection. Comparing clamp I with clamp II, fasting blood glucose decreased (mean standard deviation = 11 8 mg/dL, P = 0.02), glucose tolerance improved (median [range] +33% 14%-138%], P = 0.04), insulin concentrations increased (+36.5% [-9.9% to 274.1%], P = 0.02), and glucagon concentrations decreased (-4.7% [0%-12.1%], P = 0.005). Compared with preinjection values on continuous glucose monitoring, glucose concentrations decreased and the frequency of readings <50 mg/dL increased at 2 and 6 wk after injection of exenatide ER. This did not correspond to clinical hypoglycemia. No other side effects were observed throughout the study. Exenatide ER was safe and effective in improving glucose tolerance 3 wk after a single injection. Further evaluation is needed to determine its safety, efficacy, and duration of action in diabetic cats. (C) 2015 Elsevier Inc. All rights reserved.

Evaluation of sodium diclofenac release using natural rubber latex as carrier

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

Effect of recasting procedure upon corrosion behavior and metallic ion release of Co-Cr-Mo dental alloy in physiological

Recasting process influence upon corrosion behavior of Co-Cr-Mo dental alloy in simulated physiological serum has been investigated using chemical and electrochemical techniques. Recast Co-Cr-Mo alloy by induction (IND) or by blowtorch (FLAME) has exhibited similar dendritic structures. Both IND and FLAME alloys have presented good corrosion resistance in physiological serum. Passivation process provides this corrosion resistance. Codissolution makes this process difficult. Passive films, formed on these alloys, have been analyzed as a dual layer consisting of an inner barrier and an outer porous layer. Passive film protective characteristics are higher in FLAME than in IND alloy. On this last alloy, the passive film is more porous due to a higher Codissolution. ©Carl Hanser Verlag, München.

Purification and characterization of a unique pectin lyase from aspergillus giganteus able to release unsaturated monogalacturonate during pectin degradation

A pectin lyase, named PLIII, was purified to homogeneity from the culture filtrate of Aspergillus giganteus grown in submerged culture containing orange peel waste as carbon source. PLIII was able to digest apple pectin and citrus pectins with different degrees of methyl esterification. Interestingly, the PLIII activity was stimulated in the presence of some divalent cations including Pb(2+) and was not significantly affected by Hg(2+). Like other pectin lyases, PLIII is stimulated by but is not dependent on Ca(2+). The main soluble product released during the degradation of pectic substances promoted by the PLIII is compatible with an unsaturated monogalacturonate. PLIII is a unique enzyme able to release unsaturated monogalacturonate as the only soluble product during the degradation of pectic substances; therefore, PLIII was classified as an exo-pectin lyase. To our knowledge, this is the first characterization of an exo-pectin lyase. The PLIII described in this work is potentially useful for ethanol production from pectin-rich biomass, besides other common applications for alkaline pectinases like preparation of textile fibers, coffee and tea fermentation, vegetable oil extraction, and the treatment of pulp in papermaking.

Anthocyanin incorporated dental copolymer: bacterial growth inhibition, mechanical properties, and compound release rates and stability by (1)h NMR

Objective. To evaluate bacterial growth inhibition, mechanical properties, and compound release rate and stability of copolymers incorporated with anthocyanin (ACY; Vaccinium macrocarpon). Methods. Resin samples were prepared (Bis-GMA/TEGDMA at 70/30 mol%) and incorporated with 2 w/w% of either ACY or chlorhexidine (CHX), except for the control group. Samples were individually immersed in a bacterial culture (Streptococcus mutans) for 24 h. Cell viability (n = 3) was assessed by counting the number of colony forming units on replica agar plates. Flexural strength (FS) and elastic modulus (E) were tested on a universal testing machine (n = 8). Compound release and chemical stability were evaluated by UV spectrophotometry and (1)H NMR (n = 3). Data were analyzed by one-way ANOVA and Tukey's test ( α = 0.05). Results. Both compounds inhibited S. mutans growth, with CHX being most effective (P < 0.05). Control resin had the lowest FS and E values, followed by ACY and CHX, with statistical difference between control and CHX groups for both mechanical properties (P < 0.05). The 24 h compound release rates were ACY: 1.33 μg/mL and CHX: 1.92 μg/mL. (1)H NMR spectra suggests that both compounds remained stable after being released in water. Conclusion. The present findings indicate that anthocyanins might be used as a natural antibacterial agent in resin based materials.

Polymeric and solid lipid nanoparticles for sustained release of carbendazim and tebuconazole in agricultural applications

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

Trypanosoma cruzi and Its soluble antigens induce NET release by stimulating toll-like receptors

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

Participation of dectin-1 receptor on NETs release against Paracoccidioides brasiliensis: role on extracellular killing

Paracoccidioides brasiliensis is a dimorphic fungus from the Paracoccidioides genus, which is the causative agent of paracoccidioidomycosis, a chronic, subacute or acute mycosis, with visceral and cutaneous involvement. This disease that is acquired through inhalation primarily attacks the lungs but, can spread to other organs. Phagocytic cells as neutrophils play an important role during innate immune response against this fungus, but studies on antifungal activities of these cells are scarce. In addition to their ability to eliminate pathogens by phagocytosis and antimicrobial secretions, neutrophils can trap and kill microorganisms by release of extracellular structures composed by DNA and antimicrobial proteins, called neutrophil extracellular traps (NETs). Here, we provide evidence that P. brasiliensis virulent strain (P. brasiliensis 18) induces NETs release. These structures were well evidenced by scanning electron microscopy, and specific NETs compounds such as histone, elastase and DNA were shown by confocal microscopy. In addition, we have shown that dectin-1 receptor is the main PRR to which fungus binds to induce NETS release. Fungi were ensnared by NETs, denoting the role of these structures in confining the fungus, avoiding dissemination. NETs were also shown to be involved in fungus killing, since fungicidal activity detected before and mainly after neutrophils activation with TNF-α, IFN-γ and GM-CSF was significantly inhibited by cocultures treatment with DNAse.

Controlled swollen and drug release from urea-cross-linked polyether/siloxane hybrids

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Insights into the swelling process and drug release mechanisms from cross-linked pectin/high amylose starch matrices

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Amorphous calcium phosphate sealants: remineralization of carious lesions in the enamel can be achieved with use of pit-and-fissure sealants containing amorphous calcium phosphate

New pit-and-fissure sealants with the capacity to release calcium and phosphate because of the presence of ACP have been introduced into the dental marketplace. With the continuous introduction of new dental materials, it is important not only to research and confirm their properties, but also to propose modifications or associations that may contribute to their improvement.

Estimating the number of whales entering trade using DNA profiling and capture-recapture analysis of market products

Surveys of commercial markets combined with molecular taxonomy (i.e. molecular monitoring) provide a means to detect products from illegal, unregulated and/or unreported (IUU) exploitation, including the sale of fisheries bycatch and wild meat (bushmeat). Capture-recapture analyses of market products using DNA profiling have the potential to estimate the total number of individuals entering the market. However, these analyses are not directly analogous to those of living individuals because a ‘market individual’ does not die suddenly but, instead, remains available for a time in decreasing quantities, rather like the exponential decay of a radioactive isotope. Here we use mitochondrial DNA (mtDNA) sequences and microsatellite genotypes to individually identify products from North Pacific minke whales (Balaenoptera acutorostrata ssp.) purchased in 12 surveys of markets in the Republic of (South) Korea from 1999 to 2003. By applying a novel capture-recapture model with a decay rate parameter to the 205 unique DNA profiles found among 289 products, we estimated that the total number of whales entering trade across the five-year survey period was 827 (SE, 164; CV, 0.20) and that the average ‘half-life’ of products from an individual whale on the market was 1.82 months (SE, 0.24; CV, 0.13). Our estimate of whales in trade (reflecting the true numbers killed) was significantly greater than the officially reported bycatch of 458 whales for this period. This unregulated exploitation has serious implications for the survival of this genetically distinct coastal population. Although our capture-recapture model was developed for specific application to the Korean whale-meat markets, the exponential decay function could be modified to improve the estimates of trade in other wildmeat or fisheries markets or abundance of living populations by noninvasive genotyping.

Draft U.S. Pacific Marine Mammal Stock Assessments: 2009

Under the 1994 amendments to the Marine Mammal Protection Act (MMPA), the National Marine Fisheries Service (NMFS) and the U.S. Fish and Wildlife Service (USFWS) are required to publish Stock Assessment Reports for all stocks of marine mammals within U.S. waters, to review new information every year for strategic stocks and every three years for non-strategic stocks, and to update the stock assessment reports when significant new information becomes available. This report presents stock assessments for 13 Pacific marine mammal stocks under NMFS jurisdiction, including 8 “strategic” stocks and 5 “non-strategic” stocks (see summary table). A new stock assessment for humpback whales in American Samoa waters is included in the Pacific reports for the first time. New or revised abundance estimates are available for 9 stocks, including Eastern North Pacific blue whales, American Samoa humpback whales, five U.S. west coast harbor porpoise stocks, the Hawaiian monk seal, and southern resident killer whales. A change in the abundance estimate of Eastern North Pacific blue whales reflects a recommendation from the Pacific Scientific Review Group to utilize mark-recapture estimates for this population, which provide a better estimate of total population size than the average of recent line-transect and mark-recapture estimates. The ‘Northern Oregon/Washington Coast Stock’ harbor porpoise stock assessment includes a name change (‘Oregon’ is appended to ‘Northern Oregon’) to reflect recent stock boundary changes. Changes in abundance estimates for the two stocks of harbor porpoise that occur in Oregon waters are the result of these boundary changes, and do not reflect biological changes in the populations. Updated information on the three stocks of false killer whales in Hawaiian waters is also included in these reports. Information on the remaining 50 Pacific region stocks will be reprinted without revision in the final 2009 reports and currently appears in the 2008 reports (Carretta et al. 2009). Stock Assessments for Alaskan marine mammals are published by the National Marine Mammal Laboratory (NMML) in a separate report. Pacific region stock assessments include those studied by the Southwest Fisheries Science Center (SWFSC, La Jolla, California), the Pacific Islands Fisheries Science Center (PIFSC, Honolulu, Hawaii), the National Marine Mammal Laboratory (NMML, Seattle, Washington), and the Northwest Fisheries Science Center (NWFSC, Seattle, WA). Northwest Fisheries Science Center staff prepared the report on the Eastern North Pacific Southern Resident killer whale. National Marine Mammal Laboratory staff prepared the Northern Oregon/Washington coast harbor porpoise stock assessment. Pacific Islands Fisheries Science Center staff prepared the report on the Hawaiian monk seal. Southwest Fisheries Science Center staff prepared stock assessments for 9 stocks. The stock assessment for the American Samoa humpback whale was prepared by staff from the Center for Coastal Studies, Hawaiian Islands Humpback National Marine Sanctuary, the Smithsonian Institution, and the Southwest Fisheries Science Center. Draft versions of the stock assessment reports were reviewed by the Pacific Scientific Review Group at the November 2008, Maui meeting. The authors also wish to thank those who provided unpublished data, especially Robin Baird and Joseph Mobley, who provided valuable information on Hawaiian cetaceans. Any omissions or errors are the sole responsibility of the authors. This is a working document and individual stock assessment reports will be updated as new information on marine mammal stocks and fisheries becomes available. Background information and guidelines for preparing stock assessment reports are reviewed in Wade and Angliss (1997). The authors solicit any new information or comments which would improve future stock assessment reports. These Stock Assessment Reports summarize information from a wide range of sources and an extensive bibliography of all sources is given in each report. We strongly urge users of this document to refer to and cite original literature sources rather than citing this report or previous Stock Assessment Reports. If the original sources are not accessible, the citation should follow the format: [Original source], as cited in [this Stock Assessment Report citation].

An Evaluation of Diazacon as a Potential Contraceptive in Non-Native Rose-Ringed Parakeets

Rose-ringed parakeets (Psittacula krameri) have become widely established outside their native range through accidental or deliberate release. Potential economic impacts on agriculture, conservation concerns, and mixed public opinion regarding the species have highlighted the need to develop effective but humane management options. Fertility control might provide such a solution if a safe and environmentally benign contraceptive was available. The chemical 20,25-diazacholesterol dihydrochloride (diazacon) has previously been used to reduce reproductive output in avian species through reduction of blood cholesterol and cholesterol-dependent reproductive hormones. We orally dosed captive rose-ringed parakeets with a solution of either 9 mg/kg or 18 mg/kg of diazacon for up to 10 days and found that a dose of 18 mg/kg for 10 days temporarily reduced blood cholesterol levels with no adverse side effects. We evaluated this dose level in a captive population in semi-natural conditions during the 2008 breeding season and found a significant decrease in fertility. We concluded that diazacon has potential for fertility control in this species if a suitable formulation and delivery system is developed for free-living populations.