Voriconazole (VCZ), a triazole with a large spectrum of action is one of the most recommended antifungal agents as the first line therapy against several clinically important systemic fungal ...infections, including those by Candida albicans. This antifungal has moderate water solubility and exhibits a nonlinear pharmacokinetic (PK) profile. By entrapping VCZ into liposomes, it is possible to circumvent certain downsides of the currently available product such as a reduction in the rate of its metabolization into an inactive form, avoidance of the toxicity of the sulfobutyl ether-beta-cyclodextrin (SBECD), vehicle used to increase its solubility. PKs and biodistribution of VCZ modified by encapsulation into liposomes resulted in improved antifungal activity, due to increased specificity and tissue penetration. In this work, liposomal VCZ resulted in AUC
0-24
/MIC ratio of 53.51 ± 11.12, whereas VFEND
®
resulted in a 2.5-fold lower AUC
0-24
/MIC ratio (21.51 ± 2.88), indicating favorable antimicrobial systemic activity. VCZ accumulation in the liver and kidneys was significantly higher when the liposomal form was used. Protection of the drug from biological degradation and reduced rate of metabolism leads to a 30% reduction of AUC of the inactive metabolite voriconazole-N-oxide (VNO) when the liposomal drug was administered. Liposomal VCZ presents an alternative therapeutic platform, leading to a safe and effective treatment against systemic fungal infections.
BRAZIL ROAD-KILL Grilo, Clara; Coimbra, Michely R.; Cerqueira, Rafaela C. ...
Ecology (Durham),
11/2018, Volume:
99, Issue:
11
Journal Article
Peer reviewed
Open access
Mortality from collision with vehicles is the most visible impact of road traffic on wildlife. Mortality due to roads (hereafter road-kill) can affect the dynamic of populations of many species and ...can, therefore, increase the risk of local decline or extinction. This is especially true in Brazil, where plans for road network upgrading and expansion overlaps biodiversity hotspot areas, which are of high importance for global conservation. Researchers, conservationists and road planners face the challenge to define a national strategy for road mitigation and wildlife conservation. The main goal of this dataset is a compilation of geo-referenced road-kill data from published and unpublished road surveys. This is the first Data Paper in the BRAZIL series (see ATLANTIC, NEOTROPICAL, and BRAZIL collections of Data Papers published in Ecology), which aims make public road-kill data for species in the Brazilian Regions. The dataset encompasses road-kill records from 45 personal communications and 26 studies published in peer-reviewed journals, theses and reports. The road-kill dataset comprises 21,512 records, 83% of which are identified to the species level (n = 450 species). The dataset includes records of 31 amphibian species, 90 reptile species, 229 bird species, and 99 mammal species. One species is classified as Endangered, eight as Vulnerable and twelve as Near Threatened. The species with the highest number of records are: Didelphis albiventris (n = 1,549), Volatinia jacarina (n = 1,238), Cerdocyon thous (n = 1,135), Helicops infrataeniatus (n = 802), and Rhinella icterica (n = 692). Most of the records came from southern Brazil. However, observations of the road-kill incidence for non-Least Concern species are more spread across the country. This dataset can be used to identify which taxa seems to be vulnerable to traffic, analyze temporal and spatial patterns of road-kill at local, regional and national scales and also used to understand the effects of road-kill on population persistence. It may also contribute to studies that aims to understand the influence of landscape and environmental influences on road-kills, improve our knowledge on road-related strategies on biodiversity conservation and be used as complementary information on large-scale and macroecological studies. No copyright or proprietary restrictions are associated with the use of this data set other than citation of this Data Paper.
BRAZIL ROAD-KILL Grilo, Clara; Coimbra, Michely R.; Cerqueira, Rafaela C. ...
Bulletin of the Ecological Society of America,
01/2019, Volume:
100, Issue:
1
Journal Article
Clinical, surgical, and percutaneous strategies similarly prevent major cardiovascular events in patients with stable coronary artery disease (CAD). The possibility that these strategies have ...differential effects on health-related quality of life (HRQoL) has been debated, particularly in patients treated outside clinical trials. We assigned 454 patients diagnosed with CAD during an elective diagnostic coronary angiography to coronary artery bypass grafting (CABG), percutaneous coronary intervention (PCI), or optimal medical treatment (OMT), and followed them for an average of 5.2 + or - 1.5 years. HRQoL was assessed using a validated Brazilian version of the 12-Item Short-Form Health Survey questionnaire. The association between therapeutic strategies and quality of life scores was tested using variance analysis and adjusted for confounders in a general linear model. There were no differences in the mental component summary scores in the follow-up evaluation by therapeutic strategies: 51.4, 53.7, and 52.3 for OMT, PCI, and CABG, respectively. Physical component summary scores were higher in the PCI group than the CABG and OMT groups (46.4 vs. 42.9 and 43.8, respectively); however, these differences were no longer different after adjustment for confounding variables. In a long-term follow-up of patients with stable CAD, HRQoL did not differ in patients treated by medical, percutaneous, or surgical treatments.
An ethnopharmacological survey indicates that the genus
Byrsonima
has some medicinal species that are commonly found in the Brazilian Cerrado and has been used as an anti-inflammatory and for ...gastroduodenal disorders. The aim of this study was to evaluate the anti-inflammatory and antioxidant activity along with qualitative chemical characterization of the methanolic extract of the leaves of
Byrsonima verbascifolia
(BvME) obtained by exhaustive percolation. The data from the chemical analyses by liquid chromatography–mass spectrometry led to tentative identification of 42 compounds belonging to proanthocyanidins, galloyl quinic acid derivatives, flavonoids, and triterpene glycoside derivatives. BvME contain flavonoids and show an antioxidative activity. The methanolic extract administered intraperitoneally at doses of 50, 100, or 300 mg/kg showed a significant reduction in paw edema and modulated the neutrophil influx in a mouse model. Furthermore, the anti-edematogenic activity of the extract provided in smaller doses (12.5 and 25 mg/kg) was also demonstrated in a mouse paw edema model. The extract inhibited NO production by macrophages induced by lipopolysaccharide. We presume that the anti-inflammatory effects of BvME are due to a combination of compounds present in
B. verbascifolia
, including catechins (procyanidins), flavonoids, and triterpene glycosides and that these anti-inflammatory actions should be mediated, at least partly, through the inhibition of NO production. This study supports and validates the ethnopharmacological uses of
B. verbascifolia
as an anti-inflammatory.
The main objective of this work is to evaluate the occurrence of bromophenols (2bromophenol, 4bromophenol, 2,4dibromophenol, 2,6dibromophenol and 2,4,6tribromophenol), in the flesh and guts in two ...species of the LutjanidaeFamily: Lutjanus synagris and Ocyurus chrysurus. The bromophenols were extracted by steam distillation with pentaneether (7:3 v/v), identified by reverse phase High Performance Liquid Chromatography (HPLCUV), and quantified bythe externalstandard method. Total bromophenol concentrations were similar in the muscle of both species, rangingfrom 36 ng g(1) to 349 ng g(1). The total bromophenol concentrations in stomach (ranging from 12 ng g(1) to 586 ng g(1))were slightly higher than in muscle. The presence of bromophenol in the muscles of the species under study may occuras a result of their diet. The results of this work are therefore expected to contribute toward a better understanding ofthe path of bromophenol absorption from the fish's stomach to the rest of its body.
Objective: Liver fibrosis results from the perpetuation of the normal wound healing response to several types of injury. Despite the wealth of knowledge regarding the involvement of intracellular and ...extracellular signaling pathways in liver fibrogenesis, information about the role of intercellular communication mediated by gap junctions is scarce.
Methods: In this study, liver fibrosis was chemically induced by carbon tetrachloride in mice lacking connexin32, the major liver gap junction constituent. The manifestation of liver fibrosis was evaluated based on a series of read-outs, including collagen morphometric and mRNA analysis, oxidative stress, apoptotic, proliferative and inflammatory markers.
Results: More pronounced liver damage and enhanced collagen deposition were observed in connexin32 knockout mice compared to wild-type animals in experimentally triggered induced liver fibrosis. No differences between both groups were noticed in apoptotic signaling nor in inflammation markers. However, connexin32 deficient mice displayed decreased catalase activity and increased malondialdehyde levels.
Conclusion: These findings could suggest that connexin32-based signaling mediates tissue resistance against liver damage by the modulation of the antioxidant capacity. In turn, this could point to a role for connexin32 signaling as a therapeutic target in the treatment of liver fibrosis.
The perception of the flavor is an important attribute of quality in marine fish and other seafoods, being the first and main factor of discrimination for the evaluation, later acceptance and ...preference of the product by the consumer. Recently, the simple bromophenols have been considered an important group of key flavor compounds occurring in a wide variety of seafood species like fishes, mollusks, crustaceans and algae. When present in high concentration, in seafood, the bromophenols produce an undesirable flavor and are associated with inferior quality. Meanwhile, when present in low concentration levels (for example ng g-1) these compounds produce a desirable marine - or ocean-like - flavor and enhance the existing flavor in seafood. Indeed, simple bromophenols are widespread in seafood but virtually absent in freshwater fish. Herein we present a review on these flavor components found in the marine environment.
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