RESUMO
Enantioselective polyclonal antibodies have been produced and characterized to develop a high-throughput screening method for lipase activity fingerprinting, with a view to the enantioselective hydrolysis of azlactones.
Assuntos
Anticorpos/imunologia , Especificidade de Anticorpos , Avaliação Pré-Clínica de Medicamentos/economia , Avaliação Pré-Clínica de Medicamentos/métodos , Catálise , Ensaios de Triagem em Larga Escala , Lactonas/química , Lipase/metabolismo , Estereoisomerismo , Água/químicaRESUMO
We describe the synthesis, the physicochemical characterization and the biological evaluation of three novel pH-sensitive systems prepared derivatizing polysorbate 20 (Tween 20) with glycine, N-methyl-glycine and N,N-dimethyl-glycine (TW20-GLY, TW20-MMG and TW20-DMG). These derivatives form pH-sensitive vesicles and translocate small molecules into cells. The reported systems are efficient drug delivery systems for human hepatoblastoma cells.
Assuntos
Hepatoblastoma/metabolismo , Neoplasias Hepáticas/metabolismo , Polissorbatos/química , Tensoativos/química , Portadores de Fármacos , Glicina/química , Humanos , Concentração de Íons de Hidrogênio , Polissorbatos/administração & dosagem , Sarcosina/análogos & derivados , Sarcosina/química , Tensoativos/administração & dosagem , Células Tumorais CultivadasRESUMO
Polyethylenimine (PEI), an organic branched or linear polyamine polymer, has been successfully used in the past for DNA complexation and transfection in vitro and in vivo into several cell lines and tissues. PEI was also applied in different fields from gene therapy and several studies have emphasized the importance of this polymer in medicinal chemistry. In this brief critical review the uses and applications of this versatile polymeric molecule will be discussed.
Assuntos
Química Farmacêutica/métodos , Polietilenoimina/química , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/química , Anti-Infecciosos/uso terapêutico , Química Farmacêutica/tendências , Materiais Revestidos Biocompatíveis/química , Sistemas de Liberação de Medicamentos/métodos , Estrutura Molecular , Nanopartículas/química , Fotoquimioterapia/métodos , Polietilenoimina/administração & dosagem , Polietilenoimina/uso terapêuticoRESUMO
Near-infrared (NIR) fluorescence light has been applied to monitor several biological events in vivo since it penetrates tissues more efficiently than visible light. Dyes exhibiting NIR fluorescence and having large Stokes shift are key elements for this promising optical imaging technology. Here, we report the synthesis of a novel conjugate between a near-infrared indocyanine dye and an organic polyamine polymer (polyethylenimine, PEI) (IR820-PEI) with high chemical stability and good optical properties. IR820-PEI absorbs at 665 nm, emits at 780 nm, and displays a large Stokes shift (115 nm). Moreover, the reported conjugate is able to bind DNA, and the delivery process can be monitored in vivo with noninvasive optical imaging techniques. These characteristics make IR820-PEI one of the most effective and versatile indocyanine dye polymeric-conjugate reported so far.
