Pterodon emarginatus Vogel is a Brazilian species that belongs to the family Fabaceae, popularly known as sucupira. Its oil has several biological activities, including potent larvicidal property ...against Aedes aegypti. This insect is the vector of dengue, a tropical disease that has been considered a critical health problem in developing countries, such as Brazil. Most of dengue control methods involve larvicidal agents suspended or diluted in water and making active lipophilic natural products available is therefore considered a technological challenge. In this context, nanoemulsions appear as viable alternatives to solve this major problem. The present study describes the development of a novel nanoemulsion with larvicidal activity against A. aegypti along with the required Hydrophile Lipophile Balance determination of this oil. It was suggested that the mechanism of action might involve reversible inhibition of acetylcholinesterase and our results also suggest that the P. emarginatus nanoemulsion is not toxic for mammals. Thus, it contributes significantly to alternative integrative practices of dengue control, as well as to develop sucupira based nanoproducts for application in aqueous media.
•The main rosemary antioxidants were simultaneously extracted.•The experimental design included green solvents and low-diluted solution.•The extracted amount and the final product concentration were ...optimized.•After 55min, 89.8% of the total antioxidants assessed were extracted.•The final product was 4.75 times richer in antioxidants than the raw material.
A green solvent-based optimization for rosmarinic acid (RA), carnosol (COH), and carnosic acid (CA) extraction, the three main antioxidants from rosemary, was performed. The conventional solid-liquid extraction was optimized using a central composite design (CCD) followed by the desirability approach. In the CCD analysis the quantitative effects of extraction time (4.8–55.2min), liquid-to-solid ratio (4.6–21.4mLg−1), and ethanol content (44.8–95.2% v/v) were determined for the extracted amount of antioxidants, their concentrations in the extract, and the extraction yield. Samples were analyzed by HPLC and the antioxidants were identified by comparison with pure standard retention times and UV spectra. The desirability function that simultaneously maximizes the antioxidants extraction and their concentrations in the final product was validated. The extraction using a hydroalcoholic solution 70% v/v, at low liquid-to-solid ratio (5mLg−1), and after 55-min yielded an antioxidant recovery rate of 89.8%, and a final product 4.75 times richer in the main antioxidants than the raw material.
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•The Brazilian Sucupira tree oil has a wide range of biological properties.•SO-NE as a potential strategy for the cutaneous leishmaniasis treatment in vivo.•The formulation SO-NE was ...able to reduce lesions caused by L. (L.) amazonensis.•SO-NE and antimoniate combination altered cytokine levels related to leishmaniasis.
Cutaneous leishmaniasis (CL) is a neglected tropical skin disease caused by the protozoan genus Leishmania. The treatment is restricted to a handful number of drugs that exhibit toxic effects, limited efficacy, and drug resistance. Additionally, developing an effective topical treatment is still an enormous unmet medical challenge. Natural oils, e.g. the oleoresin from P. emarginatus fruits (SO), contain various bioactive molecules, especially terpenoid compounds such as diterpenes and sesquiterpenes. However, its use in topical formulations can be impaired due to the natural barrier of the skin for low water solubility compounds. Nanoemulsions (NE) are drug delivery systems able to increase penetration of lipophilic compounds throughout the skin, improving their topical effect. In this context, we propose the use of SO-containing NE (SO-NE) for CL treatment. The SO-NE was produced by a low energy method and presented suitable physicochemical characteristic: average diameter and polydispersity index lower than 180 nm and 0.2, respectively. Leishmania (Leishmania) amazonensis-infected BALB/c mice were given topical doses of SO or SO-NE. The topical use of a combination of SO-NE and intraperitoneal meglumine antimoniate reduced lesion size by 41 % and tissue regeneration was proven by histopathological analyses. In addition, a reduction in the parasitic load and decreased in the level of IFN-γ in the lesion may be associated, as well as a lower level of the cytokine IL-10 may be associated with a less intense inflammatory process. The present study suggests that SO-NE in combination meglumine antimoniate represents a promising alternative for the topical treatment of CL caused by L. (L.) amazonensis.
Preparation of nanoformulations using natural products as bioactive substances is considered very promising for innovative larvicidal agents. On this context, oil in water nanoemulsions develop a ...main role, since they satisfactorily disperse poor-water soluble substances, such as herbal oils, in aqueous media. Pterodon emarginatus, popularly known as sucupira, has a promising bioactive oleoresin. However, to our knowledge, no previous studies were carried out to evaluate its potential against Culex quinquefasciatus, the main vector of the tropical neglected disease called lymphatic filariasis or elephantiasis. Thus, we aimed to investigate influence of different pairs of surfactants in nanoemulsion formation and investigate if a sucupira oleoresin-based nanoemulsion has promising larvicidal activity against this C. quinquefasciatus. We also evaluated morphological alteration, possible mechanism of insecticidal action and ecotoxicity of the nanoemulsion against a non-target organism.
Among the different pairs of surfactants that were tested, nanoemulsions obtained with polysorbate 80/sorbitan monooleate and polysorbate 80/sorbitan trioleate presented smallest mean droplet size just afterwards preparation, respectively 151.0 ± 2.252 and 160.7 ± 1.493 nm. They presented high negative zeta potential values, low polydispersity index (<0.300) and did not present great alteration in mean droplet size and polydispersity index after 1 day of preparation. Overall, nanoemulsion prepared with polysorbate 80/sorbitan monooleate was considered more stable and was chosen for biological assays. It presented low LC
value against larvae (34.75; 7.31-51.86 mg/L) after 48 h of treatment and some morphological alteration was observed. The nanoemulsion did not inhibit acetylcholinesterase of C. quinquefasciatus larvae. It was not toxic to green algae Chlorella vulgaris at low concentration (25 mg/L).
Our results suggest that optimal nanoemulsions may be prepared with different surfactants using a low cost and low energy simple method. Moreover, this prototype proved to be effective against C. quinquefasciatus, being considered an ecofriendly novel nanoproduct that can be useful in integrated control programs of vector control.
Eugenia punicifolia (Kunth) DC, known as “pedra ume-caá” or “pitanguinha do cerrado”, is popularly used to treat infectious diseases like inflammation, and diabetes. Therefore, this study aimed to ...develop and validate an analytical method by high-performance liquid chromatography with diode array detector (HPLC-DAD) for the seasonal quantification of gallic acid (GA) and ellagic acid (EA), and to co-validate the method for quantification from the ethanol extract and fractions of the E. punicifolia leaves. Chromatographic separations were performed with a mobile phase gradient of acetonitrile/methanol/water acidified with 0.2% formic acid, a flow of 0.8 mL min‑1, detection at 254 nm, and a C18 column (250 × 4.6 mm, 5 μm). Method validation parameters were determined following Brazilian legislation. The HPLC-DAD analytical method developed for the quantification of GA and EA was validated and demonstrated to be selective, linear, precise, accurate, robust, and without matrix effect. Accordingly, it is helpful for the analysis of these tannins in crude ethanol extracts and fractions from E. punicifoila leaves. Thus, our results may be of great help for quality control assessment and standardization of raw materials containing Eugenia punicifolia.
Psoralen (PSO) and 5-methoxypsoralen (5-MOP) are widely used drugs in oral photochemotherapy against vitiligo and major bioactive components of root bark extract of Brosimum gaudichaudii Trécul ...(EBGT), previously standardized by LC-MS. However, the exceptionally low water solubility of these psoralens can cause incomplete and variable bioavailability limiting their applications and patient adherence to treatment. Therefore, the purpose of this work was to investigate the effects of 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex on the solubility and jejunal permeability of PSO and 5-MOP from EBGT. Characterization of inclusion complexes were evaluated by current methods in nuclear magnetic resonance studies on aqueous solution, Fourier transform infrared spectroscopy, thermal analysis, and scanning electron microscopy in solid state. Ex vivo rat jejunal permeability was also investigated and compared for both pure psoralens and plant extract formulation over a wide HP-β-CD concentration range (2.5 to 70 mM). Phase solubility studies of the PSO- and 5-MOP-HP-β-CD inclusion complex showed 1:1 inclusion complex formation with small stability constants (Kc < 500 M−1). PSO and 5-MOP permeability rate decreased after adding HP-β-CD by 6- and 4-fold for pure standards and EBGT markers, respectively. Nevertheless, the complexation with HP-β-CD significantly improved solubility of PSO (until 10-fold) and 5-MOP (until 31-fold). As a result, the permeability drop could be overcome by solubility augmentation, implying that the HP-β-CD inclusion complexes with PSO, 5-MOP, or EBGT can be a valuable tool for designing and developing novel oral drug product formulation containing these psoralens for the treatment of vitiligo.
Abstract Two experiments were conducted in order to evaluate the effect of dietary inclusion of guava extract on laying performance and lipid stability of egg of Japanese quails. For the first ...experiment, 384 Japanese quails with 42 days old were distributed in a completely randomized design with four treatments (0.0; 3.0; 6.0; 9.0 g.kg-1 guava extract), 6 replicates, and 16 birds/replicate. The experimental period lasted 84 days, divided into 4 cycles of 21 days. The parameters evaluated were: feed consumption, egg production, egg mass, feed conversion ratio, egg weight, and egg internal and external qualities. On the second experiment, 400 eggs from Japanese quails fed with diets containing four levels of guava extract were distributed in a completely randomized design with a 4x4 factorial arrangement (guava extract levels and storage time: 0, 9, 18, 27 days) with 5 replicates. Analysis of thiobarbituric acid reactive substances was performed on egg yolks. Data were submitted to regression analysis, using α=0.05. On the first experiment, the laying performance parameters were not influenced by the inclusion of guava extract in the feed, and eggshell thickness decreased linearly. On the second experiment an interaction was observed between the studied factors, affecting lipid oxidation in egg yolks. At nine days of storage, there was a quadratic effect of levels of dietary guava extract on lipid oxidation of yolk, being observed that using 4.8 g.kg-1 of guava extract on feed results in less lipid oxidation.
•Peel’s extract has antioxidant potential and high phenolic content.•It is possible to obtain nano-dispersed systems with this complex material by low energy methods.•Polysorbate 85 optimizes the ...development of the nanodispersions.•This novel nanobiotechnology product may decrease the economic costs of the process.•The green and ecofriendly method is in accordance with sustainable concepts.
Jaboticaba (Myrciaria cauliflora) is considered a “super fruit” due to its remarkable phenolic content and antioxidant capacity. Despite the great potential of its peels, to our knowledge the investigation of novel nanostructured systems with this natural raw material, still considered an industrial residue, is scarce. The present study aimed to obtain nanodispersions with its peel’s extract through a low energy method. Antioxidant assays were performed, showing positive results for DPPH (IC50 = 0.89 μg/mL) and FRAP (225.53 μmol equivalent ferrous sulphate/g). The chemical characterization in terms of flavonoids (2.56%) and total monomeric anthocyanins (0.80%) contents were also performed. Overall, the nanodispersion prepared with the non-ionic surfactant polysorbate 85 and the hydroalcoholic extract standardized in ellagic acid (129 µg/mL) presented the best properties regarding particle size distribution and zeta potential. Thus, it opens perspectives for the generation of novel food-grade nanodispersions through an ecofriendly approach that is in accordance to sustainable concepts.
Costus spiralis is a Brazilian native plant used in popular medicine, but the safety of this therapeutic use needs investigation. So, the aim of this study was to evaluate the cytogenotoxic and ...antigenotoxic effects of C. spiralis leaves or stems aqueous extracts on Allium cepa root cells. Moreover, a phytochemical screening and an antioxidant and antifungal activities evaluation were performed. C. spiralis aqueous extracts presented cytotoxicity, but no mutagenicity was observed. When the antigenotoxicity was evaluated, C. spiralis leaves aqueous extract presented preventive and modulatory effects on A. cepa root cells, reducing the sodium azide cytogenotoxic effects. In contrast, C. spiralis stems aqueous extract enhanced the sodium azide cytogenotoxicity in some conditions. The phytochemical screening revealed the presence of phenolic compounds in C. spiralis. When total phenolic content was determined, the leaves presented 73% more phenolic content than stems. Corroborating this data, C. spiralis leaves antioxidant potential was 30% higher than C. spiralis stems. However, these extracts did not present antifungal activity against Candida spp. In conclusion, empirical utilization of C. spiralis aqueous extracts should be avoided. Moreover, the cytotoxic effect of C. spiralis leaves and stems can play an important role in anticancer therapy and must be deeply studied.
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Obtaining artemisinin and its derivatives is very costly, which limits access to low-income people. Some hydroalcoholic extract of Artemisia annua L., Asteraceae, which has shown ...comparable antimalarial activity could be an alternative to the purified compound, especially if the cultivars have higher content of artemisinin. The objective of this study was to evaluate the effects of the extraction parameters (ethanol graduation, previous shaking time in an ultrasound bath and drug/solvent ratio) on the yield of artemisinin in the liquid extract obtained by percolation from A. annua and then optimize the extraction efficiency of this compound. The Box–Behnken (33) factorial design was used in association with response surface methodology. The derivatization reaction of artemisinin was used in an analytical method which was submitted to validation, after reaching the specification of the selectivity, linearity, precision, accuracy and robustness. Detection and quantification limits were 1.3 and 4.0μg/ml, respectively. The largest amount of this compound of interest was obtained without any ultrasound bath, with an ethanol graduation of 95% and a drug/solvent ratio of 2%. Drug/solvent ratio was the factor which most influenced extraction efficiency. The maximum range of artemisinin yield was 1.21%. Information obtained in this study can be used for future approaches to determining and extracting artemisinin from A. annua.
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