Polymer-based nanostructures loaded with piperine as a platform to improve the larvicidal activity against Aedes aegypti.

Piperine is an alkaloid extracted from the seed of Piper spp., which has demonstrated a larvicidal effect against Ae. aegypti. The incorporation of piperine into nanostructured systems can increase the effectiveness of this natural product in the control of Ae. aegypti larvae. In this study, we evaluated the effectiveness of piperine loaded or not into two nanostructured systems (named NS-A and NS-B) prepared by the nanoprecipitation method. The Ae. aegypti larvae were exposed to different concentrations of piperine loaded or not (2 to 16 ppm) and the mortality was investigated after 24, 48, and 72 hours. The nanostructures prepared were spherical in shape with narrow size distribution and great encapsulation efficiency. The lethal concentration 50 (LC50) for non-loaded piperine were 13.015 ppm (24 hours), 8.098 ppm (48 hours), and 7.248 ppm (72 hours). The LC50 values found for NS-A were 35.378 ppm (24 hours), 12.091 ppm (48 hours), and 8.011 ppm (72 hours), whereas the values found for NS-B were 21.267 ppm (24 hours), 12.091 ppm (48 hours), and 8.011 ppm (72 hours). Collectively, these findings suggested that non-loaded piperine caused higher larval mortality in the first hours of exposure while the nanostructured systems promoted the slow release of piperine and thereby increased the larvicidal activity over time. Therefore, loading piperine into nanostructured systems might be an effective tool to improve the larval control of vector Ae. aegypti.

Change in susceptibility response of Aedes aegypti (Diptera: Culicidae) to organophosphate insecticide and Copaifera oleoresin.

The growth of resistance in vector mosquitoes to insecticides, especially the organophosphate Temephos can facilitate the transmission of various disease agents worldwide. Consequently, it arises a challenge to public health agencies, which is the urgency use of other possibilities as botanical insecticides. Such insecticides have specific properties against insects due to the plant's ability to synthesize products derived from its secondary metabolism. The diversity and complexity of active compounds of botanical insecticides can help reduce the selection of resistant individuals and consequently not change susceptibility. To corroborate this hypothesis, the aim of this study was to compare two populations of Aedes aegypti treated with Temephos and Copaifera oleoresin. Thus, Ae. aegypti larvae were exposed from (F1) up to tenth generation (F10) with sublethal doses (±LC25) of these products (Copaifera oleoresin: 40 mg/L and Temephos: 0.0030 mg/L). The triplicates and control groups were monitored every 48 hours and the surviving larvae were separated until the emergence of the adults. Each new population were then subjected to a series of concentrations (LC50 and LC95) of Temephos and Copaifera oleoresin to calculate the Resistance Ratio (RR) of each exposed generation. The population of Ae. aegypti exposed to Temephos had an increase in RR from 05 (considered low) to 13 (considered high). Those population exposed to Copaifera oleoresin, had no increasing in RR and continued susceptible to the oil in all generations. There was a significant difference in mortality between the generations exposed to the two products. The results presented here show that the change in the susceptibility status of Ae. aegypti population to Temephos was already expected. So, we believe that this work will be of great contribution to research related to mosquito control with plant products, and resistance to chemical insecticides.

Effect of Free and Nanoencapsulated Copaiba Oil on Monocrotaline-induced Pulmonary Arterial Hypertension.

Copaiba oil comes from an Amazonian tree and has been used as an alternative medicine in Brazil. However, it has not been investigated yet in the treatment of cardiovascular diseases. This study was designed to test whether copaiba oil or nanocapsules containing this oil could modulate monocrotaline (MCT)-induced pulmonary arterial hypertension (PAH). Male Wistar rats (170 ± 20 g) received oil or nanocapsules containing this oil (400 mg/kg) by gavage daily for 1 week. At the end of this period, a single injection of MCT (60 mg/kg i.p.) was administered and measurements were performed after 3 weeks. The animals were divided into 6 groups: control, copaiba oil, nanocapsules with copaiba oil, MCT, oil + MCT, and nanocapsules + MCT. Afterward, echocardiographic assessments were performed, and rats were killed to collect hearts for morphometry and oxidative stress. MCT promoted a significant increase in pulmonary vascular resistance, right ventricle (RV) hypertrophy, and RV oxidative stress. Both oil and copaiba nanocapsules significantly reduced RV hypertrophy and oxidative stress. Pulmonary vascular resistance was reduced by copaiba oil in natura but not by nanocapsules. In conclusion, copaiba oil seems to offer protection against MCT-induced PAH. Our preliminary results suggest that copaiba oil may be an important adjuvant treatment for PAH.

Larvicidal activity of lipophilic extract of Hypericum carinatum (Clusiaceae) against Aedes aegypti (Diptera: Culicidae) and benzophenones determination.

In this study, the larvicidal activity of an enriched fraction of the major lipophilic phenolic compounds from Hypericum carinatum Griseb. (Clusiaceae) was investigated against larvae of Aedes aegypti (Diptera: Culicidae), the main vector of dengue virus in Brazil. The larval mortality rate ranged 37.33 to 72.00 % at concentrations of 66-200 µg/mL. The effect demonstrated to be dose-dependent. The lethal concentration 50 % and confidence interval were 100 and 88-111 µg/mL, respectively. The results could be attributed to the presence of cariphenone A and cariphenone B in concentrations of 1.24 ± 0.04 and 0.56 ± 0.01 %, respectively, determined by high-performance liquid chromatography. Besides, the results reinforce the potential of genus Hypericum as source of alternative insecticides.

Larvicidal activity of Copaifera sp. (Leguminosae) oleoresin microcapsules against Aedes aegypti (Diptera: Culicidae) larvae.

Studies have demonstrated the potential of Copaifera sp. oleoresin to control Aedes aegypti proliferation. However, the low water solubility is a factor that limits its applicability. Thus, the micro- or nanoencapsulation could be an alternative to allow its use in larval breeding places. The purpose of this study was to evaluate if achievable lethal concentrations could be obtained from Copaifera sp. oleoresin incorporated into polymers (synthetic or natural) and, mainly, if it can be sustained in the residual activity compared to the pure oil when tested against the A. aegypti larvae. Microcapsules were prepared by the process of emulsification/precipitation using the polymers of cellulose acetate (CA) and poly(ethylene-co-methyl acrylate) (PEMA), yielding four types of microcapsules: MicPEMA1 and MicPEMA2, and MicCA1 and MicCA2. When using only Copaifera sp. oleoresin, the larvicidal activity was observed at concentrations of LC50 = 48 mg/L and LC99 = 149 mg/L. For MicPEMA1, the LC50 and LC99 were 78 and 389 mg/L, respectively. Using MicPEMA2, the LC50 was 120 mg/L and LC99 > 500 mg/L. For microcapsules MicCA1 and MicCA2, the LC50 and LC99 were 42, 164, 140, and 398 mg/L, respectively. For a dose of 150 mg/L of pure oleoresin, the residual activity remained above 20% for 10 days, while the dose of 400 mg/L remained above 40% for 21 days. The MicPEMA1 microcapsules showed a loss in residual activity up to the first day; however, it remained in activity above 40% for 17 days. The microcapsules of MicCA1 showed similar LC50 of pure oil with 150 mg/L.

Larvicidal effect of dried leaf extracts from Pinus caribaea against Aedes aegypti (Linnaeus, 1762) (Diptera: Culicidae).

In this study, the larvicidal activity of dried leaf extracts from Pinus caribaea Morelet against Aedes aegypti was evaluated for the first time. Pinus caribaea extracts were obtained by macerating dried leaves in alkaline hydroethanol, ethanol and acetone solutions followed by evaporation under reduced pressure. The lignin content was quantified using the thioglycolic acid complexation method. Lethality bioassays (LC(50) and LC(90)) were carried out in accordance with the recommendations of the World Health Organization. The results showed that the acetone extract from Pinus caribaea was more active, and that larvicidal activity was associated with lignin concentration.

Larvicidal effect of dried leaf extracts from Pinus caribaea against Aedes aegypti (Linnaeus, 1762) (Diptera: Culicidae) / Efeito larvicida dos extratos de folhas secas de Pinus caribaea contra Aedes aegypti (Linnaeus, 1762) (Diptera: Culicidae)

In this study, the larvicidal activity of dried leaf extracts from Pinus caribaea Morelet against Aedes aegypti was evaluated for the first time. Pinus caribaea extracts were obtained by macerating dried leaves in alkaline hydroethanol, ethanol and acetone solutions followed by evaporation under reduced pressure. The lignin content was quantified using the thioglycolic acid complexation method. Lethality bioassays (LC50 and LC90) were carried out in accordance with the recommendations of the World Health Organization. The results showed that the acetone extract from Pinus caribaea was more active, and that larvicidal activity was associated with lignin concentration.

Neste trabalho foi avaliada pela primeira vez a atividade larvicida contra Aedes aegypti de extratos obtido a partir de folhas secas de Pinus caribae. Os extratos de Pinus caribaea foram obtidos a partir da maceração de folhas secas em solução hidroetanólica alcalina, etanol e acetona, seguido de evaporação sob pressão reduzida. O teor de lignina foi quantificado usando o método de complexação com ácido tioglicóliclo. Os ensaios de letalidade foram conduzidos de acordo com a recomendação da Organização Mundial da Saúde. Os resultados demonstraram que o extrato obtido com acetona foi mais ativo, e a atividade larvicida esta associada com a concentração de ligninas.

Leaf extracts of Melia azedarach Linnaeus (Sapindales: Meliaceae) act as larvicide against Aedes aegypti (Linnaeus, 1762) (Diptera: Culicidae) / Extratos de folhas de Melia azedarach Linnaeus (Sapindales: Meliaceae) atuam como larvicida de Aedes aegypti (Linnaeus, 1762) (Diptera: Culicidae)

The objective of this study was to compare the larvicidal effect of hydroethanolic extracts of fresh and dry leaves of Melia azedarach Linnaeus (Sapindales: Meliaceae) on Aedes aegypti (Linnaeus, 1762) (Diptera: Culicidae). All the extracts evaluated induced mortality among the third and fourth instar larvae of Aedes aegypti after 24 and 48 hours of exposure to the products. Although previous studies had demonstrated the action of seeds and fruits of Melia azedarach against the larvae of different Aedes aegypti populations, the present report is the first to show the larvicidal effect of the fresh and dry leaves of this plant.

O objetivo deste trabalho foi comparar o efeito larvicida de extratos hidro-etanólicos de folhas verdes e secas de Melia azedarach Linnaeus (Sapindales: Meliaceae) em Aedes aegypti (Linnaeus, 1762) (Diptera: Culicidae). Todos os extratos avaliados induziram mortalidade em larvas de 3º e 4º estágios de Aedes aegypti, após 24 e 48 horas de exposição aos produtos. Embora estudos prévios tenham demonstrado a ação de sementes e frutos de Melia azedarach em larvas de diferentes populações de Aedes aegypti, o presente estudo é o primeiro a reportar o efeito larvicida de folhas verdes e secas desta planta.

Leaf extracts of Melia azedarach Linnaeus (Sapindales: Meliaceae) act as larvicide against Aedes aegypti (Linnaeus, 1762) (Diptera: Culicidae).

The objective of this study was to compare the larvicidal effect of hydroethanolic extracts of fresh and dry leaves of Melia azedarach Linnaeus (Sapindales: Meliaceae) on Aedes aegypti (Linnaeus, 1762) (Diptera: Culicidae). All the extracts evaluated induced mortality among the third and fourth instar larvae of Aedes aegypti after 24 and 48 hours of exposure to the products. Although previous studies had demonstrated the action of seeds and fruits of Melia azedarach against the larvae of different Aedes aegypti populations, the present report is the first to show the larvicidal effect of the fresh and dry leaves of this plant.