Nucleic acids-based therapies have recently developed as next-generation agents for treating and preventing viral infection, cancer, and genetic disorders, but their use is still limited due to its relatively poor delivery into targeted cells. We designed and synthesized new amphiphilic amino acid derivatives (cysteine-based) of low molecular weight, formed by the same pentapeptide (AG2: WWCOO) N-acylated, with different hydrophobic chains containing from 12 to 18 carbons, named AG2-C n (N), which dimerize by oxidation in the presence of pLenti-CMV-GFP Puro plasmid (P) in the respective gemini. We determined transfection efficiency, critical micelle concentration, particle size, ζ-potential and cytotoxicity for the derivatives obtained. We found that all the synthesized compounds were active for DNA delivery and had greater ability to transfect CHO-K1 cells. In particular, AG2-C 18 is a promising carrier for gene delivery because it showed no cytotoxicity and its activity was greater than or equal to the commercial actives currently used.
ResumenSe ha sintetizado y evaluado la actividad antimicrobiana de nuevos compuestos gemini derivados de un tetrapéptido. La síntesis se realizó utilizando química en fase sólida y N-δ-alquilación directa e indirecta de los residuos peptídicos de ornitina. La actividad antimicrobiana se ensayó frente a cepas ATCC (American Type Culture Collection) mediante difusión en agar y determinación de la concentración inhibitoria mínima. El método directo de N-alquilación con carbonato de potasio fue el más adecuado con rendimientos del 40 % permitiendo obtener compuestos mono y di alquilados biológicamente activos. La baja masa molecular de estos compuestos, su forma simple de obtención y su actividad hacia bacterias causantes de enfermedades de transmisión alimentaria los hace tecnológicamente atractivos para ser utilizados como preservadores alimentarios. La presencia de ornitina en las moléculas les otorga resistencia enzimática y vida media biológica mayor, por que podrían ser utilizados para el desarrollo de drogas con fines terapéuticos.Palabras clave: péptido, gemini, actividad antimicrobiana, N-δ-alquilación, L-Ornitina. AbstractThe antimicrobial activity of new gemini derived from a tetrapeptide has been evaluated. The synthesis was carried out using solid phase chemistry and N-δ-direct and indirect alkylation of the ornithine peptide residue. The antimicrobial activity was tested against ATCC strains (American Type Culture Collection) by well-diffusion assay and determination of minimal inhibitory concentration. The method of N-alkylation with potassium carbonate was the best with yields of 40% allows achieving biologically active mono and dialkylate surfactants. The low molecular weight of these compounds, their simple way of preparation and their activity towards bacteria causing food-borne diseases makes them technologycally attractive for use as food preservatives. The presence in the molecules of ornithine gives them enzymatic resistance and a longer biological half-life and thus may be used to develop drugs for therapeutic purposes.
RESUMEN.La incógnita planteada en el título reunió a un grupo de investigadores en el simposio "Ecología de residuos plásticos: ¿Qué estudiamos en Argentina?", llevado a cabo en la XXVIII Reunión Argentina de Ecología. En esta comunicación hacemos un análisis del contexto nacional sobre residuos plásticos. Nuestros estudios en ecología de plásticos buscaron mitigar, por un lado, y cuantificar los residuos plásticos, por otro lado. Estos estudios ocurrieron en la mitad norte del país, en ambientes terrestres y acuáticos, y se enfocaron en diferentes materiales plásticos y en distintos organismos, aunque las bacterias fueron de interés para la mayoría de nosotros. Concluimos con preguntas guía para ecólogos, basadas en los Objetivos de Desarrollo Sostenible (ODS) de la ONU. Estas preguntas se relacionan con los ODS Agua Limpia y Saneamiento, Ciudades y Comunidades Sostenibles, Producción y Consumo Responsable y Vida Submarina y Sobre la Tierra.[Palabras clave: ambientes acuáticos y terrestres, comunidades animales, contaminación plástica, Reunión Argentina de Ecología] ABSTRACT. What do we ecologists study when we investigate plastic waste in terrestrial and freshwater environments of Argentina? What kind of research questions do ecologists make in relation to plastic waste in Argentina? This question gathered a group of researchers at the symposium "Ecology of plastic waste: What do we study in Argentina?", held at the XXVIII Argentinian Ecology Meeting. In this communication we analyze the national context on plastic waste. Our studies on the ecology of plastics sought to mitigate, on the one hand, and to quantify plastic waste, on the other hand. These studies occurred in the northern half of the country, in terrestrial and aquatic environments, and were focused on different plastic materials and diverse organisms, though bacteria were of interest for the majority of us. We conclude with guiding questions for ecologists, based on the Sustainable Development Objectives of the UN. These questions are related to: Clean Water and Sanitation, Sustainable Cities and Communities, Responsible Consumption and Production, and Life Below Water and on Land.
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