Artemether-loaded polymeric lipid-core nanocapsules reduce cell viability and alter the antioxidant status of U-87 MG cells.

Glioblastomas are tumors that present a high mortality rate. Artemether (ART) is a lactone with antitumor properties, demonstrating low bioavailability and water solubility. In the present study, we developed lipid-core nanocapsules (LNC) containing pequi oil (Caryocar brasiliense Cambess) as the oily core for ART-loaded LNCs (LNCART) and evaluated their effect on human glioblastoma cells (U-87 MG). LNCs were developed by interfacial deposition of a preformed polymer, followed by physicochemical characterization. LNCART revealed a diameter of 0.216 µm, polydispersity index of 0.161, zeta potential of -12.0 mV, and a pH of 5.53. Furthermore, mitochondrial viability, proliferation, total antioxidant status, and antioxidant enzyme activity were evaluated. ART reduced cell viability after 24 h and proliferation after 48 h of treatment at concentrations equal to or above 40 µg . mL-1. LNCART, at 1.25 µg . mL-1, reduced these parameters after 24 h of treatment. Furthermore, superoxide dismutase (SOD) activity was elevated, while glutathione reductase (GR) activity was reduced. These findings suggest that ART loaded into LNC may be a promising alternative to improve its pharmacological action and possible application as a therapeutic agent for glioblastoma.

Encapsulation in lipid-core nanocapsules improves topical treatment with the potent antileishmanial compound CH8.

Cutaneous leishmaniasis (CL) is a neglected parasitic disease conventionally treated by multiple injections with systemically toxic drugs. Aiming at a more acceptable therapy, we developed lipid-core nanocapsules (LNCs) entrapping the potent antileishmanial chalcone (CH8) for topical application. Rhodamine-labeled LNC (Rho-LNC-CH8) was produced for imaging studies. LNC-CH8 and Rho-LNC-CH8 had narrow size distributions (polydispersity index <0.10), with similar mean sizes (~180 nm) by dynamic light scattering. In vitro, Rho-LNC-CH8 was rapidly internalized by extracellular Leishmania amazonensis parasites macrophages in less than 15 min. LNC-CH8 activated macrophage oxidative mechanisms more efficiently than CH8, and was more selectively toxic against the intracellular parasites. In vivo, topically applied Rho-LNC-CH8 efficiently permeated mouse skin. In L. amazonensis-infected mice, LNC-CH8 reduced the parasite load by 86% after three weeks of daily topical treatment, while free CH8 was ineffective. In conclusion, LNC-CH8 has strong potential as a novel topical formulation for CL treatment.

Pequi (Caryocar brasiliense Cambess)-Loaded Nanoemulsion, Orally Delivered, Modulates Inflammation in LPS-Induced Acute Lung Injury in Mice.

Pequi is a Brazilian fruit used in folk medicine for pulmonary diseases treatment, but its oil presents bioavailability limitations. The use of nanocarriers can overcome this limitation. We developed nanoemulsions containing pequi oil (pequi-NE) and evaluated their effects in a lipopolysaccharide (LPS)-induced lung injury model. Free pequi oil or pequi-NE (20 mg/kg) was orally administered to A/J mice 16 and 4 h prior to intranasal LPS exposure, and the analyses were performed 24 h after LPS provocation. The physicochemical results revealed that pequi-NE comprised particles with mean diameter of 174-223 nm, low polydispersity index (0.11 ± 0.01), zeta potential of -7.13 ± 0.08 mV, and pH of 5.83 ± 0.12. In vivo evaluation showed that free pequi oil pretreatment reduced the influx of inflammatory cells into bronchoalveolar fluid (BALF), while pequi-NE completely abolished leukocyte accumulation. Moreover, pequi-NE, but not free pequi oil, reduced myeloperoxidase (MPO), TNF-α, IL-1ß, IL-6, MCP-1, and KC levels. Similar anti-inflammatory effects were observed when LPS-exposed animals were pre-treated with the nanoemulsion containing pequi or oleic acid. These results suggest that the use of nanoemulsions as carriers enhances the anti-inflammatory properties of oleic acid-containing pequi oil. Moreover, pequi's beneficial effect is likely due its high levels of oleic acid.

Healing of dermal wounds property of Caryocar brasiliense oil loaded polymeric lipid-core nanocapsules: formulation and in vivo evaluation.

Cutaneous lesions lead to complications in patients, since they may be recurrent and also represent risk of progression to infection and/or amputation. Therefore, effective, protective, and topical treatments of easy application and removal need to be developed to provide effective alternatives to patients. The Caryocar brasiliense Cambess (CBC) presents important pharmacological activities and proved in the healing process. This paper reports the improvement of the CBC nanostructured (LNCCBC and LNCCBC+) activity in dermal wounds in vivo. The oil was physico-chemically characterized and used in the development of lipid-core nanocapsules (LNCs), coated (LNCCBC+) or without chitosan (LNCCBC), in concentration of 1.0 mg mL-1. Hydrogel (HG) was tested in vivo on lesions in the back of male Wistar rats for 14 days. The oil presented appropriate physico-chemical characteristics for its use, such as moisture 0.76 %, acidity 0.85 % and oleic acid 25.90 %. The LNCs showed nanometric size (around 200 nm), monomodal distribution, slight acid pH and zeta potential of + 22.1 mV in accordance with the composition. The nanostructured oil induced dermal healing in vivo showing significantly better improvement than free oil. LNCCBC+ showed best results showing the higher increase of the production of type 1 collagen, an important protein to the healing repair. These results suggest that development of formulations LNCCBC and LNCCBC+ are promising and important alternative for the treatment of dermal wounds, avoiding complications related to cutaneous lesions.

Acaricidal activity of limonene, limonene oxide and beta-amino alcohol derivatives on Rhipicephalus (Boophilus) microplus.

Limonene, limonene oxide and eight beta-amino alcohol derivatives obtained by synthesis were investigated for the effect on egg hatchability and mortality rates of newly hatched larvae of the cattle tick Rhipicephalus (Boophilus) microplus. At the doses between 10 microg/ml and 2.5 microg/ml all the compounds were highly lethal to the larvae and some of them showed activity at lower concentrations. The effect on the eggs hatchability was observed in all the treatments.

Preparation and characterization of steam and CO2 activated carbon from Brazil nut shell

Comprehension of the bean responses of beans common under to water deficit is an important tool in agricultural planning, like sowing time, and deficit irrigation management strategies. The study aimed to understand the morpho-physiological responses and yield attributes of two common bean genotypes submitted to water stress at different phenological stages. The study was carried out in a greenhouse, in randomized block scheme with five repetitions. To achieve the objectives deficit irrigation of 25% of crop evapotranspiration was practiced during vegetative (DI-V), flowering (DI-F), and pod filling (DI-PF) stages. A non-deficit irrigated (NDI) and deficit irrigated through vegetative to pod filling stages (DI-VP) treatments were added for comparison. The following morphophysiological responses and yield attributes were evaluated: net assimilation of CO2, stomatal conductance, and leaf transpiration, chlorophyll index, number of trifoliate leaves, chlorophyll index, leaf area, number of grains per plant, number of grains per pod, number of pods per plant, the mass of thousand grains, harvest index, and water use efficiency. The beans genotype under DI-V exhibited acclimation, observed by the relative increment with NDI of 195%, 759%, and 231% of net assimilation of CO2, stomatal conductance, and leaf transpiration, respectively. Plants under treatment DI-PF experienced dis-stress and plastic responses as leaf losses and exhaustion of gas exchanges. Treatment DI-V received 11% less water than NDI and exhibited equal yield, resulting in higher water use efficiency. Yield attributes correlations indicated that yield penalty might be related to pods abortion, which not occurred to plants under DI-V.

Improved antimutagenic effect of Pyrostegia venusta (Ker Gawl. ) Miers nanostructured extract in liposome and polymeric nanoparticle

Abstract Pyrostegia venusta (Ker Gawl.) Miers, popularly known as "Cipó-de São-João", has been used in traditional medicine for its therapeutic properties. Nanotechnology is able to enhance the pharmacological activity of plant extracts. In this context, liposomes and polymeric nanoparticles containing P. venusta ethanolic extract were developed and then physico-chemically characterized to evaluate the mutagenic/antimutagenic effects of P. venusta. In addition, transaminases and serum creatinine were biochemically analyzed for liver and renal damage, respectively. The micronucleus test was performed with male Swiss mice treated orally for 15 consecutive days with free extracts and nanostructured with P. venusta, and then intraperitoneally with N-ethyl-N-nitrosurea (50 mg/kg) on the 15th day of treatment. Micronucleated polychromatic erythrocytes (MNPCE) were evaluated in bone marrow. There was a significant reduction in the frequency of MNPCE (LPEPV = 183% and NPEPV = 114%, p < 0.001), indicating antimutagenic potential of the nanostructured extracts with P. venusta. The groups treated with only nanostructured extract did not show an increase in MNPCE frequency, and biochemical analyzes showed no significant difference between treatments. The liposomes and polymeric nanoparticles containing Pyrostegia venusta ethanolic extract showed biological potential in preventing the first step of carcinogenesis under the experimental conditions

Atividade antimicrobiana in vitro de extratos metanólicos de secreções cutâneas de anfíbios amazônicos sobre fitopatógenos de interesse agrícola / n vitro antimicrobial activity of methanolic extracts from cutaneous secretions of Amazonian amphibians against phytopathogens of agricultural interest

Os mecanismos de defesa bioquímica dos anfíbios envolvem secreções cutâneas de moléculas bioativas com atividade antimicrobiana. Este estudo avaliou a atividade in vitro de extratos metanólicos da secreção cutânea de duas espécies de anfíbios da família Bufonidae, Rhaebo guttatus e Rhinella marina, no controle dos patógenos Fusarium udum, Fusarium solani, Colletotrichum truncatum, Aspergillus flavus, Rhizoctonia solani, Macrophomina phaseolina e Calonectria pseudometrosideri. O extrato de R. guttatus inibiu o crescimento micelial de F. udum, F. solani, A. flavus e M. phaseolina em algumas concentrações testadas. O extrato de R. marina inibiu o crescimento micelial de C. truncatum na concentração de 0,5 mg mL- ¹, e inibiu o crescimento micelial de A. flavus nas concentrações de 0,1 e 0,5 mg mL- ¹, que foi semelhante à inibição pelo controle positivo. O extrato de R. marina também diminuiu a produção de microescleródios de R. solani nas concentrações de 0,2 e 0,3 mg mL- ¹. Além disso, os extratos inibiram a esporulação e germinação de conídios em graus variados. A inibição da formação de apressórios em C. truncatum pelos extratos de R. guttatus e R. marina foi de 85%­99% e 63%­100%, respectivamente. Nossos resultados demonstraram que o tratamento com extratos da secreção cutânea de R. guttatus e R. marina apresentou atividade antifúngica sobre os fitopatógenos estudados.(AU)

Acaricidal activity of the hyacinthacine analogues derived from pyrrolizidine alkaloids on Rhipicephalus (Boophilus) microplus.

This study reports the effect of six hyacinthacine analogues derived from pyrrolizidine alkaloids on egg hatchability and mortality rates of newly hatched larvae of the cattle tick Rhipicephalus (Boophilus) microplus. All the compounds were toxic to the larvae of the ticks and inhibited the eggs hatchability in the higher concentration tested (5 microg/ml). Even in the lowest concentration (0.625 microg/ml), some effect in the eggs hatchability was observed.