1,597 research outputs found

    Finasteride quantification in human plasma by high-performance liquid chromatography coupled to electrospray ionization tandem mass spectrometry. application to a comparative pharmacokinetics study

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    A specific, fast and sensitive LC-MS/MS assay was developed for the determination of finasteride in human plasma using betamethsone dipropionate as the internal standard (IS). The limit of quantification was 1.0 ng/ml and the method was linear in the range of 1.0–25.0 ng/ml. The retention times were 0.75 min for finasteride and 0.85 min for IS. Method intra-batch precision and accuracy ranged from 3.6 to 7.1%, and 96.6 to 103.9%, respectively. Inter-batch precision ranged from 2.5 to 3.4%, while Inter-batch accuracy ranged from 100.3 to 103.5%. The analytical method was applied to evaluate the pharmacokinetic and relative bioavailability of 2 different pharmaceutical formulations containing 1.0 mg of finasteride. This study evaluated 38 volunteers in a randomized, 2-period crossover study with 7 days washout period between doses. The geometric mean and respective 90% CI of finasteride test/reference percent ratios were 95.68% (91.2 – 104.6%) for Cmax, 97.5% (92.1 –103.3%) for AUC0-t and 98.1 (92.67−103.8) for AUC0-inf. Based on the 90% confidence interval of the individual ratios (test formulation/reference formulation) for Cmax and AUC0-inf, it was concluded that the test formulation is bioequivalent to the reference one with respect to the rate and extent of absorption of finasteride65944945

    The predictive value of serum concentrations of anti-Mullerian hormone for oocyte quality, fertilization, and implantation

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    Objective: This study aimed to identify a possible correlation between serum levels of anti-.Mullerian hormone (AMH) and oocyte quality, embryo developmental competence, and implantation potential. Methods: 4488 oocytes obtained from 408 patients undergoing ICSI cycles were evaluated. Oocyte dimorphisms, embryo quality on days two and three, blastocyst formation competence, fertilization rates, implantation rates, and pregnancy rates were correlated with serum levels of AMH using Pearson's correlation coefficient and regression analysis. Results: A positive correlation was observed between serum levels of AMH and number of retrieved oocytes (CC: 0.600, p<0.001), fertilization rate (CC: 0.595, p=0.048), and number of obtained embryos (CC: 0.495, p<0.001). AMH did not affect the quality of cleavage stage embryos or the chance of blastocyst formation. However, AMH levels affected oocyte quality (OR: 0.75, CI 0.44-.0.96, p<0.001), and implantation (CC: 0,116, p=0.031) and pregnancy (OR: 1.22, CI: 1.03-.1.53, p<0.001) rates. Conclusion: Serum levels of AMH are a useful predictor of ovarian response to COS, oocyte quality, and fertilization. However, AMH levels may also compromise clinical outcomeslower AMH levels did not impair embryo development.Fertil Med Grp, Sao Paulo, SP, BrazilCtr Estudos & Pesquisa Reprod Assistida, Inst Sapientiae, Sao Paulo, SP, BrazilUniv Fed Sao Paulo, Dept Cirurgia, Area Reprod Humana, Disciplina Urol, Sao Paulo, SP, BrazilUniv Fed Sao Paulo, Dept Cirurgia, Area Reprod Humana, Disciplina Urol, Sao Paulo, SP, BrazilWeb of Scienc

    Avaliação de sete genótipos de sorgo (Sorghum bicolor (L.) Moench) para producao de silagem. III. Valor nutricional.

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    Foram estudadas a digestibilidade in vitro da matéria seca (DIVMS), a proteína bruta e os componentes da parede celular de sete genótipos de sorgo de diferentes portes e suculência do colmo para produção de silagem. A colheita do material a ser ensilado foi realizada durante o estádio de grão leitoso/pastoso, com 102 dias de idade. Na ensilagem utilizaram-se silos de laboratório, feitos de PVC. Os silos foram abertos após 7, 14,28 e 56 dias de fermentação. O teor de PB oscilou de 4,8 a 9,1 % entre os diferentes tipos de sorgo. A altura da planta não retratou a proporção de grãos e principalmente a digestibilidade do material, já que os dois sorgos de porte médio apresentaram as mais altas porcentagens de panícula e os menores valores de DIVMS. A correlação entre DIVMS e porcentagem de folhas foi positiva e entre DIVMS e componentes da parede celular foi negativa

    Avaliação da silagem de sete genótipos de sorgo (Sorghum bicolor (L) Moench. III. Valor nutritivo.

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    Foram estudadas as silagens de quatro genótipos de sorgo de porte alto, colmo suculento e com açúcar e três de porte baixo, colmo seco e sem açúcar com o objetivo de estudar fibra em detergente neutro (FDN), fibra em detergente ácido (FDA), hemicelulose, celulose, lignina e digestibilidade in vitro da matéria seca (DIVMS). A percentagem média de FDN foi de 63,3% para os sorgos de porte alto e 65,5% para os de porte baixo. Os valores de FDA variaram de 33,1 a 35,7% no material original e de 30,1 a 34,3% aos 56 dias de ensilagem. Houve redução nos teores de hemicelulose com o avanço do processo fermentativo indicando sua utilização como fonte adicional de carboidratos. Observou-se variação nos conteúdos de celulose ao longo da fermentação em alguns dos genótipos avaliados. Os teores médios de lignina encontrados no material original e aos 56 dias de fermentação foram, respectivamente, de 5,9 e 4,6%. Em relação à DIVMS apenas o sorgo BR506 não modificou os valores com a fermentação, e o teor médio nas silagens aos 56 dias de fermentação foi de 54,8%, variação de 51,3 a 58,5%

    Identifying new isatin derivatives with GSK-3 inhibition capacity through molecular docking and bioassays

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    The semi-synthesis of 11 isatin derivatives was achieved through bimolecular nucleophilic substitution and click chemistry. Seven new compounds were obtained. All chemical structures were determined by infrared spectroscopy (IR), nuclear magnetic resonance spectrometry (NMR) and high-resolution mass spectrometry (HRMS) data. These derivatives were evaluated for their anti-GSK-3 activity and all isatin derivatives (N-alkyl and 1,2,3-triazolic) exhibited strong inhibitory activity, with 2b and 4h exhibiting remarkable potency. In addition, docking studies were performed with 2b and 2e models to unravel the molecular mechanism underlying the polar interactions on the GSK-3 ATP-binding site.This study was funded by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, Brasil (CAPES), Finance Code 001, by the National Council of Scientific and Technological Development (CNPq) and Foundation of Support to Research and Innovation of Espírito Santo (FAPES PPE-Agro No. 76418880/16). We also would like to acknowledge INCTBioNat (CNPq 465637/2014-0) for additional support and NCQP-UFES, as well as the Portuguese Foundation for Science and Technology (FCT) under the scope of the strategic funding of UID/BIO/04469/2019 unit and BioTecNorte operation (NORTE-01-0145-FEDER-000004) funded by the European Regional Development Fund under the scope of Norte2020, Programa Operacional Regional do Norte. L. R. R. also acknowledges her sabbatical leave fellowship (SFRH/BSAB/142991/2018) funded by FCT. D. F. is recipient of a doctoral fellowship (call NORTE-69-2015-15) funded by the European Social Fund under the scope of Norte2020, Programa Operacional Regional do Norte.info:eu-repo/semantics/publishedVersio
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