The worldwide emergence of viral diseases such as Zika, Dengue, Chikungunya, West Nile and Yellow Fever urge the search for solutions to eliminate their common vector, the Aedes aegypti mosquito. This paper describes the quantitative structure-activity relationship (QSAR) and docking studies of a series of nine 3-(3-aryl-1,2,4-oxadiazol-5-yl)propionic acids (AOPA), 1-9, previously published by our group. Additionally, three new 1,2,4-oxadiazoles, 10-12, have also been synthesized, characterized and studied. The QSAR and docking studies of all compounds, 1-12, clearly indicate that larger hydrophobic substituents such as biphenyl groups attached on position 3 in 1,2,4-oxadiazoles improve the larvicidal activity. It is worthwhile to mention that nanocapsulation of compounds 10-12 were necessary to help their dissolution in water and these three new 1,2,4-oxadiazoles also exhibited approximately equal or higher larvicidal activities compared to the former prototypes at stage L4.

ABSTRACT The effects of different nitrogen doses on dry weight yield, stevioside and rebaudioside A contents, and yields were evaluated in stevia (Stevia rebaudiana Bertoni). This study was carried out at the Instituto Federal Catarinense, Rio do Sul (SC), Brazil, under decreasing photoperiods. A randomized complete block design with four blocks and five treatments (0, 65, 135, 200 and 270 kg ha-1 N) was used. Variables related to dry weight yield (total dry weight, leaf dry weight, stem dry weight, number of secondary branches and tertiary branches, and main stem length), growth rates (total leaf area, leaf area index, specific leaf area, leaf area ratio, leaf weight ratio), and stevioside and rebaudioside A contents and yields were evaluated. The doses of nitrogen fertilization did not affect the variables related to dry weight yield, stevioside and rebaudioside A contents and yields, or rebaudioside A:stevioside ratio in stevia genotype 8 (G8), grown under decreasing photoperiods.

RESUMEN El efecto de diferentes tasas de nitrógeno en la producción de biomasa, el contenido y rendimiento de esteviósido y rebaudiósido A en el cultivo de estevia se evaluaron en un experimento de campo en el Instituto Federal Catarinense, Rio do Sul (SC), Brasil, en condiciones de fotoperíodo decreciente. Se utilizó un diseño de bloques completos al azar con cuatro bloques y cinco tratamientos (0, 65, 135, 200 y 270 kg ha-1 N). Se evaluaron las variables relacionadas con la producción de biomasa (DM total, tallo MS, hojas MS, número de ramas secundarias, número de ramas terciarias y longitud de rama más grande), variables relacionadas con los índices de crecimiento (AFT, IAF, AFE, RAF y RPF) y también variables relacionadas con el contenido y el rendimiento de esteviósido y rebaudiósido A. Las diferentes dosis de fertilización nitrogenada no afectaron las variables relacionadas con la acumulación de materia seca en el genotipo G8 cultivado en condiciones de fotoperíodo decreciente en las condiciones de campo. Los niveles de fertilización nitrogenada no afectaron los niveles de esteviósido y rebaudiósido A, la productividad de esteviósido y rebaudiósido A y la proporción de rebaudiósido A / esteviósido en el G8 cultivado en condiciones de fotoperíodo de disminución de campo.

Abstract The therapeutic effects from Citrus reticulata on painful inflammatory ailments are associated to its flavonoids constituent and phytochemical studies with Citrus genus affirm that the peels have important amounts of it. These bioactive compounds have been a considerable therapeutic source and evaluate potential application of the peel extract is significant. This research aims to investigate the influence of ethanolic crude extract from the peels of Citrus reticulata and its possible mechanism of action in different animal models of pain. The extract reduced hyperalgesia in the second phase of formalin test (vehicle: 501.5 ± 40.0 s; C. reticulata extract 300 mg/kg: 161.8 ± 41.1 s), in the carrageenan model (vehicle at 4th h: 82.5 ± 9.6 %; C. reticulata extract 300 mg/kg at 4th h: 47.5 ± 6.5 %) and in Complete Freund’s Adjuvant model (vehicle: 501.5 ± 40.0 s; C. reticulata extract 300 mg/kg: 161.8 ± 41.1 s). The possible contribution of opioidergic and adenosinergic systems in the anti-hyperalgesic effect of C. reticulata extract was observed after treatment, with non-selective antagonists for both systems, which produced reversal effects. In conclusion, these properties of C. reticulata extract suggest a potential therapeutic benefit in treating painful conditions.

Poly(ethylene-co-methyl acrylate) (EMA) and poly (caprolactone) triol (PCL-T) blends, a biodegradable aliphatic polyester with low molecular weight and moderate water solubility containing diltiazem hydrochloride (DZ) were studied in terms of the thermal and morphological properties, and drug release mechanism. An increase in the PCL-T content in the EMA/PCL-T/DZ films decreased the degree of DZ crystallinity. Drug release from these films is temperature-dependent, and it is possible to modify the drug release rate by adjusting the EMA/PCL-T composition of the blends. The mechanism of drug release is governed by PCL-T melting and PCL-T leaching from EMA matrix.

Este trabalho teve como objetivo desenvolver uma metodologia analítica por espectroscopia UV, para doseamento de cumarina em xaropes de Mikania glomerata. A técnica foi baseada na extração da cumarina utilizando solventes como o clorofórmio e hexano. Após a seleção do solvente, o comprimento de onda foi definido através da sobreposição dos espectros da cumarina, metil parabeno, diluição do xarope e solução extrativa do xarope. Foram preparadas curvas analíticas de cinco soluções de cumarina com concentração variando de 0,002 a 0,03 mg/mL. Para análise da exatidão do método, foram preparados três lotes de xarope de Mikania glomerata Sprengel e o teor de cumarina determinado pela técnica espectrofotométrica foi comparado a técnica por cromatografia líquida de alta eficiência. O solvente selecionado para extração foi o clorofórmio, o comprimento de onda 320 nm. A curva analítica apresentou R² de 0,99978, demonstrando linearidade. A comparação estatística do doseamento da cumarina pela técnica espectrofotométrica estudada com a técnica cromatográfica desenvolvida por Celeghini et al. (2001) demonstrou não existir diferenças significativas, indicativo de exatidão da técnica.

A spectrophotometric procedure for coumarin determination in Mikania glomerata Sprengel (guaco) syrup is described in this work. Due to the high number of constituents in guaco syrups, the coumarin was extracted with apolar extractors (chloroform and hexane), in which chloroform was selected, because of its higher capacity of extraction. After the solvent choice, the wavelength at 320 nm, region where there is the lower interference of syrup constituents, was selected. The calibration curve showed linearity, R² of 0.99978. The spectrophotometric assay of coumarin in three samples of Mikania glomerata Sprengel syrup showed accuracy compared with the HPLC method. The results presented suggest that the spectrophotometric method may be useful for the quantitative analysis of coumarin in Mikania glomerata Sprengel syrup.