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排序方式: 共有321条查询结果,搜索用时 15 毫秒
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Lara Soares Aleixo de Carvalho Lívia Mara Silva Vinícius Carius de Souza Marcos Paulo Nascimento da Silva Priscila V. S. Z. Capriles Priscila de Faria Pinto Josué de Moraes Ademar Alves Da Silva Filho 《化学与生物多样性》2021,18(11):e2100604
Schistosomiasis, a neglected tropical disease caused by Schistosoma species, harms over 250 million people in several countries. The treatment is achieved with only one drug, praziquantel. Cardamonin, a natural chalcone with in vitro schistosomicidal activity, has not been in vivo evaluated against Schistosoma. In this work, we evaluated the in vivo schistosomicidal activities of cardamonin against Schistosoma mansoni worms and conducted enzymatic apyrase inhibition assay, as well as molecular docking analysis of cardamonin against potato apyrase, S. mansoni NTPDase 1 and S. mansoni NTPDase 2. In a mouse model of schistosomiasis, the oral treatment with cardamonin (400 mg/kg) showed efficacy against S. mansoni, decreasing the total worm load in 46.8 % and reducing in 54.5 % the number of eggs in mice. Cardamonin achieved a significant inhibition of the apyrase activity and the three-dimensional structure of the potato apyrase, obtained by homology modeling, showed that cardamonin may interact mainly through hydrogen bonds. Molecular docking studies corroborate with the action of cardamonin in binding and inhibiting both potato apyrase and S. mansoni NTPDases. 相似文献
3.
Daniel Silva Torres Bruna Alves de Oliveira Lígia Souza d Silveira Marcos Paulo da Silva Vinícius Rodrigues Durães Pereira Josué Moraes Mara Rúbia Costa Couri Rafaella Fortini Grenfell e Queiroz Patrícia Martins Parreiras Márcio Roberto Silva Lara Azevedo Alves Vinícius Carius de Souza Priscila Vanessa Zabala Capriles Goliatt Eveline Gomes Vasconcelos Ademar Alves da Silva Filho Priscila de Faria Pinto 《化学与生物多样性》2021,18(11):e2100439
In this work, two synthetic aurones revealed moderate schistosomicidal potential in in vitro and in vivo assays. Aurones ( 1 ) and ( 2 ) promoted changes in tegument integrity and motor activity, leading to death of adult Schistosoma mansoni worms in in vitro assays. When administered orally (two doses of 50 mg/kg) in experimentally infected animals, synthetic aurones ( 1 ) and ( 2 ) promoted reductions of 56.20 % and 57.61 % of the parasite load and stimulated the displacement towards the liver of the remaining adult worms. The oogram analysis revealed that the treatment with both aurones interferes with the egg development kinetics in the intestinal tissue. Seeking an action target for compounds ( 1 ) and ( 2 ), the connection with NTPDases enzymes, recognized as important therapeutic targets for S. mansoni, was evaluated. Molecular docking studies have shown promising results. The dataset reveals the anthelmintic character of these compounds, which can be used in the development of new therapies for schistosomiasis. 相似文献
4.
Alice Simon Vinícius Raphael de Almeida Borges Lucio Mendes Cabral Valéria Pereira de Sousa 《AAPS PharmSciTech》2013,14(1):425-434
The intramuscular administration of the injectable suspension betamethasone sodium phosphate (BSP) and betamethasone dipropionate (BD) has immediate therapeutic activity due to solubilized BSP and prolonged activity resulting from the slow release of BD micro-crystals. The purpose of this study was to develop and validate a dissolution method for BD in intramuscular injectable suspensions with detection by high-performance liquid chromatography (HPLC) method. Five commercial products presented a distribution of particle sizes, ranging between 7.43 and 40.25 μm as measured by laser diffraction. It was also found that particle sizes differed between batches of the same product. The different products were tested using the paddle apparatus, with stirring speeds of 25 and 50 rpm in 300 mL of phosphate buffer; simulated body fluid, muscle fluid, and synovial fluid were used as biorelevant dissolution media at 37 ± 0.5°C. It was verified that not only does average particle size affect the dissolution rate, but also the mode and the polydispersity index of the particles. Discriminatory power was obtained using the in vitro dissolution method with 0.1 M sodium phosphate buffer pH 7.4 containing 0.1% sodium lauryl sulfate and a stirring speed of 50 rpm. The HPLC-method is linear, precise, selective, and accurate for the quantification of BSP and BD in dissolution profile testing. This dissolution method can be utilized as a method to control the quality of these injectable suspensions.Key words: dipropionate betamethasone, dissolution test, intramuscular injectable suspensions, simulated muscular fluid, sodium phosphate betamethasone 相似文献
5.
Marcelo Santos da Silva Jomar Patrício Monteiro Vinícius Santana Nunes Elton José Vasconcelos Arina Marina Perez Lúcio de Holanda Freitas-Júnior Maria Carolina Elias Maria Isabel Nogueira Cano 《PloS one》2013,8(11)
Here, we show the morphological events associated with organelle segregation and their timing in the cell cycle of a reference strain of Leishmania (L.) amazonensis promastigotes, the main causative agent of Tegumentary leishmaniasis in the Americas. We show evidences that during the cell cycle, L. amazonensis promastigotes present two distinct modes of nucleus and kinetoplast segregation, which occur in different temporal order in different proportions of cells. We used DAPI-staining and EdU-labeling to monitor the segregation of DNA-containing organelles and DNA replication in wild-type parasites. The emergence of a new flagellum was observed using a specific monoclonal antibody. The results show that L. amazonensis cell cycle division is peculiar, with 65% of the dividing cells duplicating the kinetoplast before the nucleus, and the remaining 35% doing the opposite or duplicating both organelles concomitantly. In both cases, the new flagellum appeared during S to G2 phase in 1N1K cells and thus before the segregation of both DNA-containing organelles; however, we could not determine the exact timing of flagellar synthesis. Most of these results were confirmed by the synchronization of parasites using hydroxyurea. Altogether, our data show that during the cell cycle of L. amazonensis promastigotes, similarly to L. donovani, the segregation of nucleus and kinetoplast do not follow a specific order, especially when compared to other trypanosomatids, reinforcing the idea that this characteristic seems to be species-specific and may represent differences in cellular biology among members of the Leishmania genus. 相似文献
6.
Luciano Pereira Paulo R.L. Bittencourt Vinícius S. Pacheco Marcela T. Miranda Ya Zhang Rafael S. Oliveira Peter Groenendijk Eduardo C. Machado Melvin T. Tyree Steven Jansen Lucy Rowland Rafael V. Ribeiro 《Plant, cell & environment》2020,43(1):131-142
Xylem vulnerability to embolism represents an important trait to determine species distribution patterns and drought resistance. However, estimating embolism resistance frequently requires time-consuming and ambiguous hydraulic lab measurements. Based on a recently developed pneumatic method, we present and test the “Pneumatron”, a device that generates high time-resolution and fully automated vulnerability curves. Embolism resistance is estimated by applying a partial vacuum to extract air from an excised xylem sample, while monitoring the pressure change over time. Although the amount of gas extracted is strongly correlated with the percentage loss of xylem conductivity, validation of the Pneumatron was performed by comparison with the optical method for Eucalyptus camaldulensis leaves. The Pneumatron improved the precision of the pneumatic method considerably, facilitating the detection of small differences in the (percentage of air discharged [PAD] < 0.47%). Hence, the Pneumatron can directly measure the 50% PAD without any fitting of vulnerability curves. PAD and embolism frequency based on the optical method were strongly correlated (r2 = 0.93) for E. camaldulensis. By providing an open source platform, the Pneumatron represents an easy, low-cost, and powerful tool for field measurements, which can significantly improve our understanding of plant–water relations and the mechanisms behind embolism. 相似文献
7.
Leandro Nolé Eduardo Michael Maia Mincarone Flávia Lucena-Frédou Júlia Rodrigues Martins Gabriel Vinícius Felix Afonso Bárbara Teixeira Villarins Thierry Frédou Alex Souza Lira Arnaud Bertrand 《Zeitschrift fur angewandte Ichthyologie》2020,36(6):845-848
Length-weight relationship parameters were calculated for twelve mesopelagic fish species from the western Tropical Atlantic: Diretmus argenteus, Melamphaes polylepis, Bolinichthys distofax, Diaphus lucidus, Diaphus splendidus, Electrona risso, Hygophum taaningi, Taaningichthys bathyphilus, Melanolagus bericoides, Winteria telescopa, Diplophos taenia, Astronesthes similus. Data was collected off northeastern Brazil from April 9th to May 6th, 2017. Hauls were conducted during day and night at 47 stations by using a micronekton trawl (body mesh: 40 mm, cod-end mesh: 10 mm) from 10 to 1,113 m depth. The material was fixed in a 4% formalin solution for 1 month and then preserved in a 70% alcohol solution for proximally 6 months before processing for length (nearest 0.1 cm of standard length) and weight (nearest 0.01 g of total weight). A new maximum standard length for Winteria telescopa is also provided. 相似文献
8.
Glaucio Monteiro Ferreira Juliana Gallottini de Magalhães Vinícius Gonçalves Maltarollo Thales Kronenberger Arasu Ganesan Flávio da Silva Emery 《Journal of biomolecular structure & dynamics》2020,38(2):354-363
AbstractSirtuin 2 is a key enzyme in gene expression regulation that is often associated with tumor proliferation control and therefore is a relevant anticancer drug target. Anilinobenzamide derivatives have been discussed as selective sirtuin 2 inhibitors and can be developed further. In the present study, hologram and three-dimensional quantitative structure–activity relationship (HQSAR and 3D-QSAR) analyses were employed for determining structural contributions of a compound series containing human sirtuin-2-selective inhibitors that were then correlated with structural data from the literature. The final QSAR models were robust and predictive according to statistical validation (q2 and r2pred values higher than 0.85 and 0.75, respectively) and could be employed further to generate fragment contribution and contour maps. 3D-QSAR models together with information about the chemical properties of sirtuin 2 inhibitors can be useful for designing novel bioactive ligands.Communicated by Ramaswamy H. Sarma 相似文献
9.
Jean Ricardo Simões Vitule Flávia Francine Gazola da Silva Hugo Bornatowski Vinícius Abilhoa 《Environmental Biology of Fishes》2013,96(9):1029-1044
Feeding ecology of fish assemblage in a costal river of the Atlantic Rain Forest in Southern Brazil was investigated. Monthly samples using different fishing techniques were completed on a section of the river characterized as a freshwater environment, and an adjacent tide-influenced estuarine section. Species were grouped into three major Feeding Mode Functional Groups: Zoobenthivore, Omnivore and Detritivore. The river section with the greatest occurrence was the site where the most abundant species are likely to feed most intensively. Freshwater strangler species (Cyphocharax santacatarinae - detritivorous, Rhamdia quelen and Oligosarcus hepsetus - zoobenthivorous) presented higher stomach repletion in the freshwater environment while marine migrants (Genidens genidens and Etropus crossotus - zoobenthivorous) and estuarine residents (Bairdiella ronchus - zoobenthivorous) presented higher repletion in the tide-influenced estuarine stretch. Use of food resources was influenced by spatial and temporal variations linked to environmental characteristics such as salinity, habitat heterogeneity, life history evolution, feeding specialization and resource partitioning. Hypotheses concerning potential keystone species, ecosystem engineers or strong interactors were also discussed. 相似文献
10.
Vinícius de L. Dantas Juli G. Pausas Marco Antônio Batalha Priscilla de Paula Loiola Marcus Vinicius Cianciaruso 《Oecologia》2013,171(2):487-494
Intraspecific trait variability plays a fundamental role in community structure and dynamics; however, few studies have evaluated its relative importance to the overall response of communities to environmental pressures. Since fire is considered a key factor in Neotropical savannas, we investigated to what extent the functional effects of fire in a Brazilian savanna occurs via intra- or interspecific trait variability. We sampled 12 traits in communities subjected to three fire regimes in the last 12 years: annual, biennial, and protected. To evaluate fire’s relative effects, we fitted a general linear mixed models with species as random and fire as fixed factors, using: (1) all species in the communities (i.e., considering intra- and interspecific variabilities); (2) 18 species common to all fire regimes (i.e., intraspecific variability only); and (3) all species with their overall average trait values (i.e., interspecific variability only). We assessed the relative role of intra- or interspecific variability by comparing the significance of each trait in the three analyses. We also compared the within and between fire variabilities with a variance component analysis. Five traits presented larger intraspecific than interspecific variability, and the main effect of fire occurred at the intraspecific level. These results confirm that it is important to consider intraspecific variability to fully understand fire-prone communities. Moreover, trait variability was larger within than among fire regimes. Thus, fire may act more as an external filter, preventing some of the species from the regional pool from colonizing the cerrado, than as an internal factor structuring the already filtered cerrado communities. 相似文献