Resumen Diferentes estudios han evaluado la actividad biocida de aceites esenciales (AEs) en larvas de mosquitos de importancia médica. Sin embargo, son limitadas las investigaciones que analizan los efectos de los AEs en todos los estadíos del ciclo de vida de Aedes aegypti. Este estudio evalúa la actividad biológica del AE de Salvia officinalis frente a Ae. aegypti. Se evaluó la actividad ovicida a concentraciones de 1, 5, 37 y 50 mg.L-1 en huevos de 0-12 h y huevos de 0-72 h. La actividad larvicida, pupicida y adulticida fue evaluada a concentraciones exploratorias (CE) y múltiples. Para la actividad repelente se empleó una CE de 1.000 mg.L-1 en intervalos de 0-2 min y de 2-15 min de exposición en antebrazos de voluntarios. La actividad disuasiva de oviposición se estimó a CE de 5, 50 y 200 mg.L-1. El AE causó malformaciones en embriones y alteración de las larvas. La mayor actividad larvicida fue a 63 y 76 mg.L-1 (27 ± 13,4 y 37 ± 18,6 %) a 24 h. La mayor mortalidad pupicida fue a 310 y 390 mg.L-1 (89 ± 1,53 and 100 ± 0 %) a las 48 h. La mortalidad adulticida a 300 mg.L-1 fue de 57,5 ± 0 % y el porcentaje de repelencia fue de 42 ± 4,7 %. La acción disuasiva a 200 mg.L-1fue de 97 ± 4,81 %, con un índice de actividad de ovipostura de -0,94. S. officinalis mostró un efecto biocida en embriones y mortalidad de pupas y adultos, lo que revela que tiene un uso potencial en programas de control focalizados en estos estadios de desarrollo.

Abstract Different studies have evaluated the biocidal activity of essential oils (EO) in mosquito larvae of medical importance. However, limited research focused on analyzing the EO effect at all the stages of the life cycle of Aedes aegypti has been done. This study evaluates the biological activity of the EO Salvia officinalis against Ae. aegypti. The ovicidal activity was evaluated at 1, 5, 37 and 50 mg.L-1 concentrations in eggs from 0-12 h and eggs from 0-72 h. Larvicidal, pupicidal and adulticidal activities were assessed at exploratory concentrations (EC) and multiple concentrations. We employed an EC of 1,000 mg.L-1 for repellent activity and used an exposure time of 0-2 min and 2-15 min on the forearms of volunteers. The deterrent action was estimated at EC of 5, 50 and 200 mg.L-1. The EO caused malformations in embryos as well as larvae alteration. The highest larvicidal activity was at 63 and 76 mg.L-1(27 ± 13.4 and 37 ± 18.6 %) with 24 h exposure. The greatest pupicidal mortality was at 310 and 390 mg.L-1 (89 ± 1.53 and 100 ± 0 %) with 48 h exposure. Adulticidal mortality at 300 mg.L-1 was 57.5 ± 0 % and the percentage of repellency was 42 ± 4.7 %. The dissuasive action at 200 mg.L-1 was 97 ± 4.81 %, with an oviposition activity rate of -0.94. S. officinalis showed a biocidal effect on embryos and mortality of pupae and adults, indicating that its potential use in control programs should be focused on these stages of development.

Resumen Introducción: Análogos del alcaloide girgensohnina, diseñados y sintetizados para inhibir a la enzima acetilcolinesterasa, han presentado efecto insecticida sobre insectos vectores de enfermedades. Objetivo: Determinar la actividad insecticida de 12 análogos sintéticos de gingersohnina sobre ninfas del primer estadio de Triatoma dimidiata. Materiales y Métodos: Se tomó como referencia el protocolo de la OMS 2005. Ninfas del primer estadio de T. dimidiata fueron expuestas a los análogos por aplicación tópica y exposición a superficies para determinar las dosis letales (DL50 y DL95) y verificar alteración en la locomoción mediante el software Videomex V. Resultados: El análogo 6 presentó la mayor actividad insecticida a las 72h con una mortalidad del 20,8% ± 3,57 para el tratamiento de topicación 25% ± 0,00 para las superficies no porosas. Las dosis letales de la molécula 6 fueron: DL50 1036,8 ± 0,38 ng/insecto y DL95 3991,4 ± 0,50 ng/insecto respectivamente. Con respecto a la locomoción, el análogo indujo un comportamiento similar al insecticida comercial deltametrina.

Abstract Introduction: Analogs of the girgensohnine alkaloid, designed and synthesized to inhibit acetylcholinesterase enzyme, have presented an insecticidal effect on vectors insects of diseases. Objective: To determine the insecticidal activity of 12 synthetic analogs of gingersohnine in first stage nymphs of Triatoma dimidiata. Materials and methods: WHO protocol 2005, using exploratory doses, was used to determine the best molecule according to its mortality. First stage nymphs of T. dimidiata were exposed to different doses of the analogs by topical application and surface exposure. Lethal doses (LD50 and DL95) and alterations in locomotion using Videomex V software were determined. Results: Analog 6 presented the highest insecticidal activity at 72 h with a mortality of 20.8% ± 3.57 for topical treatment and 25%±0,0 for non-porous surfaces evaluation. Analog 6 lethal doses were LD50 1036.8 ± 0.38 ng/insecto and DL95 3991.4 ± 0.508 ng/insecto, respectively. With regard to locomotion, analogue 6 induced a similar behavior to that observed for commercial insecticide deltametrin.

Abstract Aedes aegypti is the principal vector of arboviral pathogens that may cause diseases as dengue fever, chikungunya and zika. The harmful environmental effects of commercial pesticides coalesced with the development of insecticide-resistant populations encourage the discovery and generation of new alternative products as a tool to reduce the incidence of vector-borne diseases. In this work, through the classic three component Strecker reaction of commercial benzaldehydes, cyclic secondary amines and KCN, a new series of nine α-amino nitriles, girgensohnine analogs, has been synthetized and screened for larvicide and adulticide properties against A. aegypti, one of the dominant vectors of dengue, chikungunya and zika in tropical and subtropical areas all over the world. Molecules 3 and 4 were identified as potential larvicidal agents with LC50 values of 50.55 and 69.59 ppm, respectively. Molecule 3 showed 100% of mortality after 2 h of treatment when a concentration of 30 ppm in adulticidal assays was evaluated. Additionally, in order to elucidate the mode of action of these molecules, their acetylcholinesterase (AChE) inhibitory properties were evaluated using the Ellman assay. It was found that the molecules possess a weak AChE inhibitory activity with IC50 values between 148.80 and 259.40 µM, indicating that AChE could not be a principal target for insecticide activity.

Abstract The search for new insecticides to control dengue fever, chikungunya, and Zika vectors has gained relevance in the past decades. The aim of the present study was to evaluate the larvicidal action of essential oils (EOs) from Thymus vulgaris, Salvia officinalis, Lippia origanoides, Eucalyptus globulus, Cymbopogon nardus, Cymbopogon martinii, Lippia alba, Pelargonium graveolens, Turnera diffusa, and Swinglea glutinosa on Aedes (Stegomyia) aegypti. The EOs were extracted by microwave-assisted hydrodistillation and characterized by gas chromatography/mass spectrometry (GC/MS). The chemical components of the EOs were identified by linear retention indices and mass spectra. Lethal concentrations (LC50 and LC95) were determined by probit analysis using larvae of Ae. aegypti between the third and the fourth instars. All EOs achieved larvicidal activity at LC50 values lower than 115 mg/L. The lowest LC50 value (45.73 mg/L) corresponded to T. vulgaris EO, whereas C. martinii EO showed the highest LC50 (LC50 = 114.65 mg/L). Some EO mixtures showed lower LC50 than oils used individually, such as the mixtures of L. origanoides + S. glutinosa (LC50 = 38.40 mg/L), T. diffusa + S. glutinosa (LC50 = 63.71 mg/L), and L. alba + S. glutinosa (LC50 = 48.87 mg/L). The main compounds of the EOs with highest larvicidal activity were thymol (42%) and p-cymene (26.4%).

RESUMEN Introducción. El alcaloide natural girgensohnina se ha usado como modelo en la síntesis de nuevos análogos de alcaloidales alfa-aminonitrílicos con efecto insecticida en vectores de enfermedades. Objetivo. Evaluar la actividad biocida de análogos de girgensohnina y de aceites esenciales de las plantas Cymbopogon flexuosus, Citrus sinensis y Eucalyptus citriodora en ninfas de estadios I y V de Rhodnius prolixus. Materiales y métodos. Se empleó la aplicación tópica en terguitos, esternitos y superficies tratadas con diferentes dosis exploratorias de cada una de las moléculas y aceites esenciales para determinar las dosis letales (LD50 y LD95). Resultados. El análogo 3 tuvo la mayor actividad insecticida, con una mortalidad de 83,3±16,7% en los terguitos, de 38,9±4,8 % en los esternitos y de 16,7±0 % a las 72 horas en ninfas de estadioI expuestas a superficies tratadas y 500 mg.L-1. En las ninfas de estadio V solo se presentó mortalidad en los esternitos (11,1±9,6 % con el análogo 6 y 5,5±4,7 % con los análogos 3 y 7 a las 72 h y 1.500 mg.L-1). Las dosis letales para la molécula 3 en los terguitos de ninfas de estadio I fueron las siguientes: DL50, 225,60 mg.L-1 y DL95, 955,90 mg.L-1. En cuanto a los aceites esenciales, el efecto insecticida solo se presentó con C. flexuosus (11,1±4,8%) en los esternitos de ninfas de estadio I expuestas a superficies tratadas; con C. sinensis (5,6±4,8%) en los terguitos y en los esternitos (8,3±0%) a las 72 horas y 1.000 mg.L-1. Conclusión. Los análogos sintéticos del alcaloide girgensohnina y los aceites esenciales de C. flexuosus y C. sinensis exhibieron actividad insecticida en R. prolixus. El análogo 3 exhibió la mayor actividad insecticida de todas las moléculas evaluadas bajo las condiciones de laboratorio.

ABSTRACT Introduction: The alkaloid girgensohnine has been used as a natural model in the synthesis of new alkaloid-like alpha-aminonitriles with insecticidal effect against disease vectors. Objective: To evaluate the biocide activity of girgensohnine analogues and essential oils of Cymbopogon flexuosus, Citrus sinensis and Eucalyptus citriodora in stage I and stage V Rhodnius prolixus nymphs. Materials and methods: We used a topical application model in tergites and sternites, as well as exposure to treated surfaces with different exploratory doses of each of the molecules and essential oils to determine the lethal doses (LD50 and LD95). Results: Analogue 3 showed the highest insecticidal activity with 83.3±16.7% of mortality when applied on tergites, 38.9±4.8% on sternites and 16.7±0% on treated surfaces in stage I nymphs at 72 hours (h) and 500 mg.L-1. In stage V nymphs, the compounds induced mortality only in sternums (11.1±9.6% for analogue 6 and 5.5±4.7% for analogues 3 and 7 at 72 h and 1500 mg.L-1). The lethal doses for molecule 3 on tergites in stage I nymphs were LD50 225.60 mg.L-1 and LD95 955.90 mg.L-1. The insecticidal effect of essential oils was observed only in stage I nymphs, with 11.1±4.8% for C. flexuosus when applied in sternites, while using exposure to surfaces treated it was 5.6±4.8% for C. sinensis applied on tergites and 8.3±0% on sternites at 72 h and 1000 mg.L-1. Conclusion: Synthetic girgensohnine analogues, and C. flexuosus and C. sinensis essential oils showed insecticidal activity in R. prolixus. Analogue 3 showed the greatest insecticidal activity among all molecules and oils evaluated under our laboratory conditions.

Se determino la susceptibilidad de larvas de Aedes albopictus en condiciones de laboratorio de origen del "Vale do Ribeira llha Cumprida" Sao Paulo, Brasil. El producto utilizado fue Bacillus thuringiensis var israelensis H-14 Vectobac-AS con 1.200 unidades internacionales de toxicidad (UIT) por miligramo. Como parametro de comparacion se empleo la colonia Aedes aegypti Rockefeller CDC (Center for Disease Control) de Puerto Rico. Las concentraciones letales obtenidas de Ae. albopictus fueron LC50= 0.12 ppm y LC90= 0,28 ppm y para la especie referenda Ae. aegypti fue CL50 de 0,07 ppm y CL95 de 0,17 ppm. Se puede concluir que Ae. albopictus presento una respuesta al bioinsecticida diferente a Ae. aegypti.

The susceptibility of Aedes albopictus larvae, originating from "Vale do Ribeira llha Cumprida" Sao Paulo, Brasil. was determined under laboratory conditions. The product used was Bacillus thuringiensis var israelensis H-14 Vectobac-AS with 1,200 internacional toxic units (TU) per milligram. An Aedes aegypti Rockefeller colony from CDC (Center for Disease Control) of Puerto Rico was used as a reference. Lethal concentrations determined for Ae. albopictus were LC50= 0.12 ppm and LC95= 0.28 ppm and for the reference species Ae. aegypti they were LC(50)0.07 ppm and LC95 0.17 ppm. It is concluded that Ae. albopictus presented a different response to the bioinsecticide than Ae. aegypti.