Improvement in Solubility-Permeability Interplay of Psoralens from Brosimum gaudichaudii Plant Extract upon Complexation with Hydroxypropyl-ß-cyclodextrin.

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-ß-cyclodextrin (HP-ß-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-ß-CD concentration range (2.5 to 70 mM). Phase solubility studies of the PSO- and 5-MOP-HP-ß-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-ß-CD by 6- and 4-fold for pure standards and EBGT markers, respectively. Nevertheless, the complexation with HP-ß-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-ß-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.

Lipid stability of egg and laying performance of Japanese quail feed with extract of guava (Psidium guajava L.).

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.

Effects of plant extracts from Stryphnodendron adstringens (mart.) coville, Lafoensia pacari a. st.-hil, copaifera spp., and Pterodon emarginatus Vogel on in vitro rumen fermentation.

The effects of doses CTL (0 mg), 30, 300 and 3000 mg/L of extracts from Stryphnodendron adstringens (Mart.) Coville (SA), Lafoensia pacari A. St.-Hil (LP), Copaifera spp. (CO) and Pterodon emarginatus Vogel (PE) on ruminal fermentation were investigated in eight experiments conducted in randomized complete block designs. The in vitro system contained four fermentation vessels. Each treatment was allocated in one vessel in each run. Incubation was run four and five times with diets 50:50 and 10:90 (roughage to concentrate ratio) respectively. Incubation vessel was the experimental unit, and each incubation run was a block. All plant extracts negatively affected DM degradation at 3000 mg/L. In diet 50:50, SA-3000 increased the molar proportion of propionate (p < 0.05), yet it decreased the concentration of fermentation products (p < 0.05); LP-300 reduced ruminal ammonia nitrogen (NH3 -N; 98 vs. 120 mg/dl for LP-300 and average of CTL and LP-30, respectively) and isobutyrate (p < 0.05); CO-300 reduced (p < 0.05) NH3 -N (98 vs. 123 mg/dl for CO-300 and average of CTL and CO-30, respectively); and P. emarginatus had no positive effects on rumen fermentation (p > 0.05). In diet 10:90, SA-300 reduced (p < 0.001) NH3 -N and total volatile fatty acids (VFA); LP-30 increased (p < 0.05) total VFA (85 vs. 63 mM for LP-30 and CTL, respectively), molar proportions of acetate and propionate, and had lower C2 :C3 than CTL (3.6 vs. 4.3, respectively); CO-300 decreased acetate and increased propionate, reducing C2 :C3 (p < 0.001; 2.8 vs. 3.6 for CO-300 and average of other doses, respectively); PE-30 and PE-300 reduced NH3 -N by 14% and increased total VFA by 29% compared with CTL (p < 0.05). Further in vivo investigations may consider L. pacari (LP-30), Copaifera spp. (CO-300) oleoresin and P. emarginatus oleoresin (PE-30 and PE-300) in diets with high inclusion of concentrate.

Efficacy of nanoemulsion with Pterodon emarginatus Vogel oleoresin for topical treatment of cutaneous 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.

Hancornia speciosa serum fraction latex stimulates the angiogenesis and extracellular matrix remodeling processes.

The Hancornia speciosa latex reveals angiogenic, osteogenic, and anti-inflammatory properties, which present its potential for developing of wound healing drugs; however, the latex compounds responsible for angiogenesis remain unknown. One strategy to screen these active compounds is evaluation of latex fractions. This study aimed to obtain different fractions of latex and evaluate its angiogenic activity separately using the chick chorioallantoic membrane (CAM) assay. The serum (SE) fraction was responsible for angiogenesis, which was subject to biochemical characterization and computational simulations in order to understand the contribution of H. speciosa latex in wound healing process. Our results revealed weak antioxidant potential and absence of antimicrobial activity in the SE fraction. Phytochemical analysis identified chlorogenic acids (CGA) as the main compound of SE fraction. CGA bioactivity predictions identify different molecules associated with extracellular matrix (ECM) remodeling, such as metalloproteinases, which also are overexpressed in our CAM assay experiment. Docking simulations revealed the interactions between CGA and matrix metalloproteinase 2. In conclusion, SE latex fraction stimulates angiogenesis and may influence ECM remodeling. These properties may contribute to the wound healing process, and also confirm the widespread use of this plant.

Is it possible to obtain nanodispersions with jaboticaba peel's extract using low energy methods and absence of any high cost equipment?

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.

In vivo assessment of cyto/genotoxic, antigenotoxic and antifungal potential of Costus spiralis (Jacq.) Roscoe leaves and stems.

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.

Novel Approaches to Extraction Methods in Recovery of Capsaicin from Habanero Pepper (CNPH 15.192).

INTRODUCTION: The objective of this study was to compare three capsaicin extraction methods: Shoxlet, Ultrasound-assisted Extraction (UAE), and Shaker-assisted Extraction (SAE) from Habanero pepper, CNPH 15.192. MATERIALS AND METHODS: The different parameters evaluated were alcohol degree, time extraction, and solid-solvent ratio using response surface methodology (RSM). RESULTS: The three parameters found significant (p < 0.05) were for UAE and solvent concentration and extraction time for SAE. The optimum conditions for the capsaicin UAE and SAE were similar 95% alcohol degree, 30 minutes and solid-liquid ratio 2 mg/mL. The Soxhlet increased the extraction in 10-25%; however, long extraction times (45 minutes) degraded 2% capsaicin. CONCLUSION: The extraction of capsaicin was influenced by extraction method and by the operating conditions chosen. The optimized conditions provided savings of time, solvent, and herbal material. Prudent choice of the extraction method is essential to ensure optimal yield of extract, thereby making the study relevant and the knowledge gained useful for further exploitation and application of this resource. SUMMARY: Habanero pepper, line CNPH 15.192, possess capsaicin in higher levels when compared with others speciesHigher levels of ethanolic strength are more suitable to obtain a higher levels of capsaicinBox-Behnken design indicates to be useful to explore the best conditions of ultrasound assisted extraction of capsaicin. Abbreviations used: Nomenclature UAE: Ultrasound-assisted Extraction; SAE: Shaker-assisted Extraction.

Box-Behnken experimental design for extraction of artemisinin from Artemisia annua and validation of the assay method

ABSTRACT 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 4.0 µg/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.

Ação do extrato etanólico da casca do pequi (Caryocar brasiliense) na cardiotoxicidade crônica induzida por doxorrubicina em ratos / Caryocar brasiliense shell ethanol extract in chronic cardiotoxicity induced by doxorubicin in rats

A doxorrubicina (DOX) é um quimioterápico utilizado no tratamento de neoplasias malignas, porém possui a cardiotoxicidade como efeito colateral. O objetivo deste trabalho foi verificar quanto à ação do extrato etanólico da casca do pequi (Caryocar brasiliense) (EECP) por meio de avaliação morfológica (macroscópica, microscópica e ultramicroscópica), bem como avaliar a expressão de metaloproteinases (MMP2 e MMP9) e seus inibidores teciduais (TIMP1 e TIMP2) no miocárdio de ratos submetidos à cardiotoxicidade crônica pela DOX, tratados ou não com o EECP. O experimento teve duração de três meses e foram utilizados 30 ratos da raça Wistar, distribuídos em seis grupos de cinco animais. G1 e G2 receberam como pré-tratamento 300mg/kg e 600mg/kg de EECP, respectivamente, por gavagem, durante sete dias e mantiveram o tratamento durante os 21 dias de aplicação da DOX. Em G1, G2, G3, G4 e GC, a cardiotoxicidade foi induzida com aplicações semanais de 2mg/kg de DOX, via intraperitoneal, totalizando quatro aplicações (8mg/kg) e, nos ratos do grupo Sham (GS), foi aplicado 1ml de solução fisiológica. Os animais do G3 receberam diariamente 300mg/kg e os do G4 600mg/kg de EECP, por gavagem, durante os 21 dias de aplicação da DOX. Os do GC e GS receberam 1 ml de água, diariamente, também por gavagem. Após o término das aplicações, os animais foram mantidos por dois meses, totalizando três meses de experimento. A avaliação macroscópica foi realizada após 90 dias, momento em que foram colhidas amostras para análise em microscopia eletrônica, histopatologia e imunoistoquímica. Ao exame necroscópico foi observada ascite nos animais que receberam DOX. Houve baixo índice de mortalidade (3,33%), representado pela morte de um rato que desenvolveu pneumonia por falsa via. Não foi observada alteração no peso e nas medidas do coração dos ratos. Nas doses de 300 e 600mg/kg, o EECP atenuou a degeneração vacuolar miocítica. Na dose de 600mg/kg, o EECP reduziu a quantidade de células de Anitschkow e a fragmentação das miofibrilas. Não houve resultado significativo quanto à imunomarcação das MMP e, quanto a seus inibidores (TIMP), houve maior imunomarcação de TIMP2 no GC, grupo que recebeu apenas DOX. Concluiu-se que o extrato etanólico da casca do pequi (EECP) é eficiente em minimizar os efeitos da cardiotoxicidade crônica induzida pela DOX no miocárdio de ratos, considerando que nas doses de 300 e 600mg/kg o EECP atenua a degeneração vacuolar miocítica e, na dose de 600mg/kg, o EECP reduz a quantidade de células de Anitschkow e a fragmentação das miofibrilas.(AU)

Doxorubicin (DOX) is a chemotherapic drug used in the treatment of malignancies, but has the cardiotoxicity as collateral effect. The objective of this study was to evaluate the action of pequi shell etanolic extract (Caryocar brasiliense) (PSEE) through morphological evaluation (macroscopic, microscopic and ultramicroscopic), and to evaluate the expression of metalloproteinases (MMP2 and MMP9) and its tissue inhibitors (TIMP1 and TIMP2) in the myocardium of rats with chronic cardiotoxicity by DOX and treated or not with PSEE. The experiment lasted three months and 30 Wistar rats were divided into six groups of five animals. G1 and G2 received 300mg/kg and 600mg/kg of PSEE, respectively, as pretreatment, by gavage for seven days and continued treatment for 21 days of application of DOX. In G1, G2, G3, G4 and GC, cardiotoxicity was induced with weekly applications of 2mg/kg DOX, intraperitoneally, totaling four applications (8 mg/kg), and in the Sham group (GS) 1ml of saline solution was applied. G3 animals received daily 300mg/kg of PSEE, and G4, 600mg/kg, by gavage, for 21 days of application of DOX. The GC and GS received 1ml of water daily by gavage also. After the completion of the application, the animals were kept for two months, with three months of experiment. Macroscopic evaluation was performed after 90 days, at which time samples were taken for analysis in electron microscopy, histopathology and immunohistochemistry. At necropsy, ascites was observed in animals that received DOX. There was a low mortality rate (3.33%), being one mouse that developed false road pneumonia. There was no change in weights and measures of the rat hearts. At doses of 300 and 600mg/kg, the PSEE attenuates myocyte vacuolar degeneration. At a dose of 600mg/kg, PSEE reduces amount Anitschkow cells. There was no significant result on the immunostaining of MMP, but considering their inhibitors (TIMP) there was a greater immunostaining of TIMP2 in GC, the group that received only DOX. It was concluded that PSEE is effective in minimizing effects of chronic cardiotoxicity induced by DOX in the myocardium of rats, whereas at doses of 300 and 600mg/kg, PSEE attenuates vacuolar degeneration in myocytes and at the dose of 600mg/kg the PSEE reduces the amount of Anitschkow cells and myofibrils fragmentation.(AU)

Engineering spray-dried rosemary extracts with improved physicomechanical properties: a design of experiments issue

ABSTRACT A 33 Box–Behnken design and Response Surface Methodology were performed to evaluate the influence of extract feed rate, drying air inlet temperature and spray nozzle airflow rate on the process yield, stability parameters (moisture content and water activity) and on several physicomechanical properties of spray-dried rosemary extracts. Powder yield ranged from 17.1 to 74.96%. The spray-dried rosemary extracts showed moisture content and water activity below 5% and 0.5%, respectively, which indicate their chemical and microbiological stabilities. Even without using drying aids, some sets of experimental conditions rendered dried products with suitable flowability and compressibility characteristics for direct preparation of solid dosage forms. Analysis of variance and Response Surface Methodology proved that studied factors significantly affected most of the spray-dried rosemary extract quality indicators at different levels. The main processing parameter affecting the spray-dried rosemary extract characteristics was inlet temperature. The best combination of parameters used to obtain a reasonable yield of stable dry rosemary extracts with adequate technological properties for pharmaceutical purpose involves an extract feed rate of 2 ml/min, 80 °C inlet temperature and 40 l/min SA. The design of experiments approach is an interesting strategy for engineering spray-dried rosemary extracts with improved characteristics for pharmaceutical industrial purpose.

Pterodon emarginatus oleoresin-based nanoemulsion as a promising tool for Culex quinquefasciatus (Diptera: Culicidae) control.

BACKGROUND: 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. RESULTS: 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 LC50 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). CONCLUSIONS: 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.

Multiresponse optimization of an extraction procedure of carnosol and rosmarinic and carnosic acids from rosemary.

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.

Development of a Larvicidal Nanoemulsion with Pterodon emarginatus Vogel Oil.

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.

Eugenia calycina Cambess extracts and their fractions: Their antimicrobial activity and the identification of major polar compounds using electrospray ionization FT-ICR mass spectrometry.

Eugenia calycina, which is described as "red pitanga or pitanga cherry of cerrado," is widely distributed in the Cerrado area of Brazil. Its leaf and bark extracts are used in folk medicine for many applications. In this study, the compositions of the major polar compounds of the bark and leaf extracts and their fractions were obtained from a liquid-liquid extraction using hexane, dichloromethane, ethyl acetate, and water. They were then evaluated using electrospray ionization negative FT-ICR mass spectrometry (ESI(-) FT-ICR MS), which revealed a large number of oxygen-containing compounds, such as flavonoids, terpenes, tanins, steroids, and fat acids. The biological activity of these extracts towards several bacterial and fungal strains was then evaluated. The highest activity was found using aqueous fractions, in which the ESI(-) FT-ICR MS analysis revealed compounds with a high content of oxygen (e.g., glycosed flavonoids, tannins, and polyphenolic compounds) against Cryptococcus sp. D (minimum inhibitory concentration [MIC]=15.62µg/mL). Strong activity was also found using the hexanic fractions-in which the ESI(-) FT-ICR MS analysis revealed that the compounds contained a decreased amount of oxygen (e.g., fat acids and steroids)-towards Cryptococcus gatti L48, Cryptococcus neoformans L3 (MIC=31.2µg/mL), and Cryptococcus sp. D (MIC=62.5µg/mL). Therefore, antimicrobial assays using the bark/leaf extracts of E. calycina present prospects for the research of active substances that may be used for the treatment of cryptococcosis, a disease that is common in immunosuppressed patients.

Influence of environmental factors on the composition of essential oils from leaves of Myrcia tomentosa (Aubl) DC / Influencia de los factores ambientales sobre la composición de los aceites esenciales de hojas de Myrcia tomentosa (Aubl) DC

The leaves of Myrcia tomentosa were collected from five sites and four different months in the Brazilian Cerrado and their essential oils were obtained by hidrodistillation and analyzed by GC/MS. The aim of this work was to evaluate the influence of environmental factors on essential oils composition in the leaves of M. tomentosa. The results were submitted to stepwise Multiple Regression and Canonical Correlation Analysis that indicated a relationship between compounds in essential oils and some environmental factors (foliar nutrients, soil nutrients and climatic data). Cluster Analysis indicated a high chemovariability in the essential oils from different sites, also showed that the collection time had a minor effect on oil composition.

Las hojas de Myrcia tomentosa se obtuvieron de cinco sitios diferentes y cuatro meses en el Cerrado brasileño y sus aceites esenciales fueron obtenidos por hidrodistillation y analizados por GC/MS. El objetivo de este trabajo fue evaluar la influencia de los factores ambientales sobre la composición de los aceites esenciales en las hojas de M. tomentosa. Los resultados fueron sometidos a múltiples etapas de regresión y análisis de correlación canónica indicó que la relación entre los compuestos en los aceites esenciales y algunos factores ambientales (nutrientes foliares, fertilizantes y datos climáticos). El análisis de agrupamiento indicó chemovariability un alto en los aceites esenciales de diferentes sitios, también mostró que el equipo de recolección tuvo un efecto menor sobre la composición del aceite.

Dissolution test of herbal medicines containing Passiflora sp.

The dissolution test is an essential tool to assess the quality of herbal medicines in the solid dosage form for oral use. This work aimed to evaluate the dissolution behavior of three herbal medicines in the form of capsules and tablet containing Passiflora, produced with powder or dried extract. Assay of total flavonoids and dissolution methods were validated and obtained results allowed the quantification of flavonoids with precision, accuracy and selectivity. The percentage of total flavonoids found was 2 percent for capsule A (containing only powder), 0.97 percent for capsule B (containing only dried extract) and 5.5 percent for tablet. Although the content was lower, the release of flavonoids present in the capsule containing dried extract was 12 percent higher over 30 min, with dissolved percentage values of 87 and 75, for the capsules containing extract and powder, respectively. The tablet containing dried extract presented dissolution of 76 percent, despite the higher content of flavonoids, which may be due to pharmacotechnical problems. Obtained data demonstrated the need to implement these tests in the quality control of herbal medicines, confirming the release of the active ingredients that underlie the pharmacological action of these medicines.