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In this study, we report the synthesis and evaluation of in vitro and in vivo antitrypanosomal activity of styrylquinoline-like compounds (SQ) 3a-h . Synthesis was carried out by using quinaldine and 8- hydroxyquinaldine with a variety of aromatic aldehydes. The structure of SQs was corroborated by one and two-dimension NMR spectroscopy. In vitro antitrypanosomal activity on T. cruzi Talahuen strain was evaluated using β-galactosidase enzymatic method; cytotoxicity on U-937 cells was assessed by using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] method. On the other hand, in vivo therapeutical response to 3a-f compounds was evaluated in BALB/c mice ( Mus musculus ) experimentally infected with T. cruzi blood trypomastigotes and then orally administered with 100 mg/kg weight day for 20 days. All of the compounds showed in vitro activity with EC 50 values ranging between 4.6 ± 0.1 μg/mL (14.4 μM) and 36.6 ± 6.1 μg/mL (91 μM). Furthermore, treatment with 3a-f compounds for 20 days resulted in improvement in all of the mice, with a 83–96% decrease in parasitic load at day 90 post-treatment. Treatment with benznidazol (BZ) managed to cure 100% of the mice at the end of treatment. None of the treatments affected the weight of the animals or alanine aminotransferase (ALT), blood urea nitrogen (BUN) and creatinine levels in serum. These results suggest a therapeutic potential of 3a-f compounds as treatment for the infection.

ResumenEl presente estudio reporta la síntesis de cinco (E)-estirilquinolinas (Q.1, Q.2, Q.3, Q.5, Q.6) y tres derivados O-alquilados (Q.1a, Q.6a, Q.6b) y la evaluación de su actividad antimalárica y citotóxica in vitro. Para obtener las estirilquinolinas se empleó la reacción de condensación tipo Perkin a partir de 8-hidroxiquinaldina con aldehídos aromáticos. La actividad antimalárica se realizó empleando el método Radioisotópico con cepas FCB-2 de Plasmodium falciparum (resistente a la cloroquina) y para la actividad citotóxica se empleó el método del MTT con células HepG2. La mayoría de los compuestos mostraron ser activos antimaláricos. Los que presentan mayor actividad son el Q.3 (IC50 6.4µM), y el Q.5 (IC5010.8 µM) aunque todos mostraron ser citotóxicos a concentraciones superiores a 1µg/mL. Las estructuras de estos compuestos se confirmaron empleando técnicas espectroscópicas de Infrarrojo y Resonancia Magnética Nuclear en una y dos dimensiones. Palabras clave: estirilquinolinas, actividad antimalárica, reacción de Perkin, compuestos o-alquilados, citotoxicidad Evaluation of Antimalarial and Cytotoxic Activity of Styrylquinolines obtained from 8-Hydroxyquinaldine with Aromatic Aldehydes AbstractThis study reports the synthesis of five (E)-Styrylquinolines (Q.1, Q.2, Q.3, Q.5, Q.6) and three O-alkylated derivatives (Q.1a, Q.6a, Q 6 b) and the evaluation of its antimalarial activity and cytotoxic in vitro. For Styrylquinolines Perkin condensation reaction type from 8-hydroxyquinaldine with aromatic aldehydes was used. Antimalarial activity was performed using the method Radioisotope with FCB-2 strains of Plasmodium falciparum (chloroquine-resistant) and for the cytotoxic activity the MTT method with HepG2 cells was employed. Most compounds showed to be active antimalarial. Those with higher activity were Q.3 (IC50 6.4μM) and Q.5 (IC5010.8 µM), although all of them were cytotoxic at concentrations above 1 µg / mL. The structures of these compounds were confirmed using infrared spectroscopy techniques and MRI in one and two dimensions.

Biopesticides are pest and pathogen management agents based on living microorganisms or natural products (botanical origin). Due to their natural origins, they stand out as an environmentally friendly tool, since they quickly decompose and minimize pollution problems produced by synthetic pesticides. However, these products present significant challenges that affect the bioactivities of the active components, due to the degradation of the biomass or bioactive metabolite by factors such as air, light, and temperature. Therefore, in this study, a systematic search of the Scopus database was conducted and scientometric tools were used to evaluate formulation techniques and approaches that seek to improve the bioactivities of natural preparations. The results showed that published research on biopesticides has significantly increased by 71.24% in the last decade (2011–2021). Likewise, the bibliometrics showed, through temporal flow analysis, and in the period from 2010 to 2021, investigations evolved have toward the use of nanotechnology, with the purpose of improving and potentiating the formulations of biopesticides. Consequently, nanotechnology tools can be classified as current strategies of interest that allow the increase and protection of bioefficacy to a greater extent than traditional biopesticide preparations. This review constitutes an important contribution to future research and expands the panorama in relation to biopesticide formulations for the control of agricultural pests.

ResumenEn este trabajo se evalúa el efecto de la concentración de nitrógeno y fósforo sobre la acumulación de Astaxantina en Haematococcus pluvialis UTEX 2505, utilizando un diseño de experimentos factorial 3 2 . Las variables de respuestas cuantificadas fueron el crecimiento celular, la producción de Astaxantina, perfil lipídico y el módulo de Young de la membrana celular. Se encontró que la productividad celular aumenta al incrementar los niveles de nitrógeno, en contraste con las bajas concentraciones de nitrógeno y fósforo que muestra un efecto positivo sobre la producción de Astaxantina. El estrés generado por la limitación de nutrientes (fuente de nitrógeno y fósforo) disminuye la rigidez de la pared celular en la microalga. Como conclusión, para obtener concentraciones más altas de Astaxantina, es necesario limitar los niveles de nitrógeno y fósforo. AbstractIn this study, the effect of the concentration of nitrogen and phosphorus on the accumulation of Astaxanthin in Haematococcus pluvialis UTEX 2505 was evaluated using a factorial 3 2 design. The dependent variables were cell growth, Astaxanthin production, lipid profile and Young's modulus of the cell membrane. It was found that cellular productivity increases when nitrogen levels were high, in contrast to low concentrations of nitrogen and phosphorus that showed a positive effect on Astaxanthin production. The stress generated by the source of nutrients decreases the rigidity of the cellular wall in the microalgae. As a conclusion, to obtain higher concentrations of Astaxanthin it is necessary to limit the nitrogen and phosphorus levels.