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Microbial proteases, especially aspartic proteases, are an essential group of enzymes produced from different microorganisms. Microbial proteases have several applications, mainly in the food, beverage, cosmetic, and pharmaceutical industries, due to their efficiency in the processing and in the manufacturing stages. The yeast Rhodotorula mucilaginosa CBMAI 1528 was isolated from the Antarctic environment and was previously reported to have higher extracellular aspartic protease production. In addition, advances in the operational conditions of bioreactors for enzyme production are important to reduce the gap associated with scaling-up processes. This is the first study that evaluates the influence of oxygen transference (kLa) on the protease production of R. mucilaginosa yeast. To that end, batch cultures were created in a stirred tank bioreactor using Sabouraud dextrose broth at 25 °C for 72 h under kLa values from 18 to 135 h-1. The results show that kLa (121 h-1) obtained at 500 rpm and 1.5 vvm plays an important role in protease production (124.9 U/mL) and productivity (6.784 U/L.h) as well as biomass (10.4 g/L), µmax (0.14 h-1) and Yx/s (0.484 g/g). In conclusion, R. mucilaginosa showed high yield production in aerobic culture with the efficiency of protease expression and secretion influenced by kLa. In this sense, our results could be used for further industrial investment.

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Cucurbitacins are a wide group of natural products found in several plant families, especially in the Cucurbitaceae family. In the last decade, there has been a significant increase in studies aimed at identifying new biological activities of cucurbitacins and describing their mechanisms of action. The most researched pharmacological activities are antineoplastic and anti-inflammatory activity, the first being recently reviewed. The present review explains the anti-inflammatory, antioxidant, and immunomodulatory potential of cucurbitacins, identifying the most studied compounds in this area and exploring their mechanisms of action already studied. A brief report was made about the main structural characteristics of cucurbitacins, in addition to an update on the biological activities attributed to this class in the last 5 years. Cucurbitacin B and cucurbitacin E have been identified as the most investigated when it comes to the immune response, playing roles in both innate and adaptive immunity. The most cited mechanisms were inhibition of COX-2 and NOS, reduction of oxidative stress, suppression of proinflammatory cytokines and modulation of acquired immunity proteins. It was found that cucurbitacins are promising molecules in the search for therapeutic innovation and have wide versatility in the immune response.

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Bacterial resistance refers to the ability of bacteria to resist the action of some antibiotics due to the development of adaptation and resistance mechanisms. It is a serious public health problem, especially for diseases caused by opportunistic bacteria. In this context, the search for new drugs, used alone or in combination, appears as an alternative for the treatment of microbial infections, and natural products, such as essential oils, are important in this process due to their structural diversity, which increases the probability for antimicrobial action. The objective of this study was to extract and identify the chemical components of the essential oil from Croton conduplicatus (EOCC), to evaluate the antimicrobial activity, to investigate the effect of the interaction between the EOCC and different antibiotics and to evaluate its antibiofilm potential. The EOCC was obtained by hydrodistillation. Based on chemical characterisation, 70 compounds were identified, with 1.8 cineole (13.15%), p-cymene (10.68%), caryophyllene (9.73%) and spathulenol (6.36%) being the major constituents. The minimum inhibitory concentration (MIC) values of EOCC were 256 and 512 µg mL-1 for methicillin-sensitive and -resistant Staphylococcus aureus strains (MSSA and MRSA), respectively. The combinations of EOCC with the antibiotics oxacillin and ampicillin were synergistic (OXA/EOCC and AMP/EOCC combined decreased the OXA MIC and AMP MIC to 0.5 and 0.25 for MSSA, respectively, and OXA/EOCC and AMP/EOCC combined decreased the OXA MIC and the AMP MIC to 1 and 0.5 for MRSA, respectively) and could modify the resistance profile of MSSA and MRSA strains. The results indicated that EOCC was also able to partially inhibit biofilm formation. Our study presents important information about the chemical composition of EOCC and its antimicrobial potential and provides a reference to determine the mechanisms of action of EOCC and its use in pharmaceutical formulations.

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Aspidosperma pyrifolium is used in traditional medicine to treat inflammatory disorders. The aim of the study was to perform phytochemical characterization and evaluate the anti-inflammatory, anti-nociceptive and acute toxicity effects of the total alkaloid fraction (TAF-Ap) from stem barks. Two monoterpenic indole alkaloids were isolated by high performance liquid chromatography coupled with mass spectrometry (HPLC-MS) and the structural elucidation was performed using 1D and 2D NMR analysis. As for toxicity, no animals died at 50 mg kg-1 and this concentration presented mild sedation and forced breathing within the first 24 h. The lethal dose capable of killing 50% of the animals (LD50) was estimated to be 160 mg kg-1. In the pharmacological tests, the models used were 1% carrageenan-induced paw edema and peritonitis, 1% formalin-induced nociception and 1% acetic acid-induced abdominal writhing in Swiss mice. The study made it possible to isolate 15-methoxyaspidospermine and 15-methoxypyrifolidine, corroborating the results of pharmacological assays, which showed anti-inflammatory and analgesic potential, especially at 30 mg kg-1 (p < 0.001). Thus, the species was shown to be a promising source of active substances, with special attention paid to its toxicological potential.

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This work aimed to carry out a study of Apodanthera congestiflora by investigating its chemical composition and pharmacological potential. From the dichloromethane phase (Dic-Ac) of the A. congestiflora stems, three compounds were identified: cayaponoside C5b (Ac-1), cabenoside C (Ac-2) and fevicordin C2 glucoside (Ac-3), being last identified for the first time as a natural product. These compounds were obtained by chromatographic methods and their structures were elucidated by means of spectroscopic analysis of IR, MS and NMR. In the quantification of Dic-Ac, it was possible to observe the presence of 7% of cayaponoside C5b. Dic-Ac showed significant toxicity for in vivo tests, with macroscopic and biochemical changes. The anti-inflammatory activity of Dic-Ac was investigated using the paw edema model. A decrease in inflammatory signs was observed in the first 5 h and the most effective dose in reducing edema with was 7.5 mg kg-1 (66.6%). Anti-tumor activity of Dic-Ac was evaluated by Ehrlich's carcinoma model, which showed inhibition rate of 78.46% at 15 mg kg-1 dosage. The phytochemical investigation, together with the biological tests carried out in this study, demonstrated that A. congestiflora is a promising species in the search for therapeutics, since it contains substances with high pharmacological potential in its composition.

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Aiming the valorisation of the fruit of Cereus jamacaru D.C. (mandacaru), from the Caatinga biome, the physicochemical and nutritional parameters, total phenolic content and antioxidant capacity of its raw pulp and skin were evaluated. Extracts of the lyophilised pulp (PE) and skin (SE) of this fruit were also characterised for their antioxidant capacity parameters, phenolic compounds and for the semi-quantitative elemental analysis of minerals. From the total carbohydrates of the pulp (13.43 g/100 g, in the fresh basis), 79% was composed by total dietary fibre and, from this fraction, 89% was insoluble dietary fibre. The total antioxidant capacity of the raw skin was about 1.5-fold higher than that of the raw pulp, while the improvement of phenolic content in the lyophilised PE and SE was by 5- and 36-folds, respectively, compared with their respective raw samples (fresh basis). The lyophilised SE had the higher antioxidant capacity, requiring only 3.79 g to scavenge 1 g of DPPH radicals. Frequencies of functional groups assessed through the FT-IR spectrum corroborates with the presence of phenolic compounds in the samples. Potassium was the predominant mineral in both PE and SE. These results indicate that mandacaru, currently consumed only locally, can be an important source of nutrients and antioxidants for the general population and also for industrial use.

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Cnidoscolus quercifolius is an Euphorbiaceae endemic to the northeast region of Brazil, which is used in folk medicine as anti-inflammatory, analgesic and antibiotic. An ethanolic extract was prepared with the leaves from C. quercifolius, and also partitioned and chromatographed leading to the isolation of cyanoglucoside linamarin (1), cinnamic acid (2), as well as a mixture of steroids and terpenoids (3-6). Structural elucidation of the compounds was done by IR, MS and NMR analysis. For the cyanoglucoside (1) were also evaluated its antimicrobial and antileishmanial viabilities by plaque microdilution and MTT test, respectively. Both tests showed from moderate to zero activity against the organisms evaluated. In addition, the antiproliferative activity of compounds 1 and 5-6 were tested against tumor cells, which did not show statistically significant growth inhibition 50% (GI50). The obtained results suggested that further pharmacological studies should prove the folk medicinal uses.

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Anadenanthera colubrina var cebil (Griseb.) Altschul is a medicinal plant found throughout the Brazilian semi-arid area. This work performed a bioguided purification of active substances present in ethyl acetate extract from A. colubrina leaves. The anti-Staphylococcus aureus and antioxidant actions were used as markers of bioactivity. The extract was subjected to flash chromatography resulting in five fractions (F1, F2, F3, F4, and F5). The fractions F2 and F4 presented the highest antimicrobial action, with a dose able to inhibit 50% of bacteria growth (IN50) of 19.53 µg/mL for S. aureus UFPEDA 02; whereas F4 showed higher inhibitory action towards DPPH radical (2,2-diphenyl-1-picryl-hydrazyl-hydrate) [dose able to inhibit 50% of the radical (IC50) = 133 ± 9 µg/mL]. F2 and F4 were then subjected to preparative high-performance liquid chromatography (HPLC) and nuclear magnetic resonance (NMR), resulting in the identification of p-hydroxybenzoic acid and hyperoside as the major compounds in F2 and F4, respectively. Hyperoside and p-hydroxybenzoic acid presented IN50 values of 250 µg/mL and 500 µg/mL against S. aureus UFPEDA 02, respectively. However, the hyperoside had an IN50 of 62.5 µg/mL against S. aureus UFPEDA 705, a clinical isolate with multidrug resistant phenotype. Among the purified compounds, the proanthocyanidins obtained from F2 exhibited the higher antioxidant potentials. Taken together, these results highlight the potential of A. colubrina leaves as an alternative source of biomolecules of interest for the pharmaceutical, food, and cosmetic industries.

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Cellulose is among the top 5 excipients used in the pharmaceutical industry. It has been considered one of the main diluents used in conventional and modern dosage forms. Therefore, different raw materials of plant origin have been evaluated as potential alternative sources of cellulose. In this context, Opuntia ficus-indica L. Miller (palma forrageira), a plant of the cactus family that has physiological mechanisms that provide greater productivity with reduced water requirements, is an interesting and unexplored alternative for extracting cellulose. By using this source, we aim to decrease the extraction stages and increase the yields, which might result in a decreased cost for the industry and consequently for the consumer. The aim of this work was to investigate the use of Opuntia ficus-indica L. Miller as a new source for cellulose extraction, therefore providing an efficient, straight forward and low-cost method of cellulose II production. The extraction method is based on the oxidation of the lignins. The obtained cellulose was identified and characterized by spectroscopic methods (FTIR and NMR), X-ray diffraction, thermal analysis (TGA-DTG and DSC) and scanning electron microscopy. The results confirmed the identity of cellulose and its fibrous nature, which are promising characteristics for its use in the industry and a reasonable substrate for chemical modifications for the synthesis of cellulose II derivatives with different physicochemical properties that might be used in the production of drug delivery systems and biomaterials.

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The adherence to therapy associated with the socio-demographic variables and the habits of patients with hypertension and/or diabetes mellitus were investigated in this study. The registration forms of 105 patients in the Hiperdia program in the municipality of Campina Grande-PB were used as a data collection instrument, applying the Morisky-Green test (MGT) and Batalla test (BT) to assess compliance treatment. For the MGT, there was a prevalence of non-adherent individuals (76.2%) and the type of predominant behavior was unintentional. The internal consistency of the responses obtained through the MGT presented good reliability, according to the value of 0.69 obtained by Cronbach's alpha. For the BT, there was a predominance of adherence (68.6%) and the alpha value was 0.80, showing a high reliability level. It was found that a diet lacking in salt is a strong impact variable for determining the adherence to the BT. Given the representativity of the tests, there is a need to amend the interferences that facilitate the low adherence to drug treatment. The results of this study can be used to construct strategies that will address these difficulties and optimize the adherence level and quality of life of patients.

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ABSTRACT Harrisia adscendens (Gürke) Britton & Rose is a species of the family Cactaceae found in the northeastern semi-arid and popularly known as foxtail. In folk medicine, the roots of this species are used for the treatment of toothache and heartburn. The objective of this study was to perform the isolation and identification of the secondary metabolites obtained from the vegetal drug by chromatographic and spectroscopic techniques and to evaluate the antimicrobial activity of the extract. The qualitative phytochemical analysis of the extract showed suggestive results for the presence of alkaloids. Two compounds were isolated and identified: 2-methyl-9H-β-carboline-2-ion, a β-carboline alkaloid obtained for the first time as a natural product and 2',6'-dihydroxy-4'-methoxyacetophenone-2'-O-β-glucoside. In the antimicrobial tests, it was possible to observe activity against Pseudomonas aeruginosa. The results obtained by spectroscopic techniques allowed to characterize the phytochemical properties of the vegetal drug and may be useful in future studies for production of herbal medicines.

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Four new compounds were isolated from the branches of Piper montealegreanum Yuncker, a shrub found in the Amazon rainforest, including two new dihydrochalcones named claricine (1) and maisine (2), a cinnamic acid derivative 3 and a phenylalkanoid 4, along with a porphyrin identified as the known compound phaeophytin a (5). The structures were established using spectroscopic experiments, including 1D and 2D NMR and HRESIMS experiments, performed on the two monoterpene dihydrochalcones and their monoacetyl derivatives. The structural diversity of these substances is very important for the Piper genus chemotaxonomy.

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Introdução: espécies do gênero Piper são encontradas nas regiões tropicais do globo e possuem inúmeras indicações terapêuticas. Objetivos: avaliar a atividade antimicrobiana de extratos e frações de quatro espécies de Piper, além de dois flavonoides isolados de Piper montealegreanum e determinar a concentração inibitória mínima dos produtos ativos. Métodos: o material vegetal foi coletado em diferentes regiões do estado da Paraíba e na cidade de Belém (Pará) submetido à extração com etanol e partição com solventes em grau crescente de polaridade. Os flavonoides foram isolados por meio de técnicas cromatográficas. A avaliação da atividade antimicrobiana foi realizada pelo método de disco-difusão frente a três espécies bacterianas: Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 e três espécies fúngicas: Candida albicans ATCC 76645, Candida tropicalis ATCC 13803 e Candida glabrata ATCC 15545. Resultados: quase metade dos produtos testados foi capaz de inibir o crescimento de S. aureus com halos de inibição variando entre 8-16 mm. O extrato etanólico bruto e as frações hexânica e CHCl3 das folhas de P. mollicomum mostraram atividade antibacteriana frente as três linhagens testadas. As frações hexânicas de P. arboreum, de P. caldense e de P. mollicomum apresentaram atividade antifúngica, enfatizando a formação do halo de inibição de 28 mm para a fração de P. mollicomum. Os dois flavonoides isolados de P. montealegreanum não apresentaram atividade antimicrobiana. Conclusões: os resultados preliminares deste estudo sugerem que alguns dos produtos obtidos das espécies de Piper são uma fonte promissora de compostos com atividade antimicrobiana(AU)

Introducción: el género Piper se encuentra en las regiones tropicales del mundo y numerosas indicaciones terapéuticas. Objetivos: evaluar la actividad antimicrobiana de extractos y fracciones de cuatro especies de Piper, además de dos flavonoides aislados de Piper montealegreanum y determinar la concentración inhibitoria mínima de los productos activos. Métodos: el material vegetal fue recolectado en diferentes regiones del estado de Paraíba y en Belém (Pará) y sometido a extracción con etanol y partición com disolventes en grado creciente de polaridad. Los flavonoides fueron aislados por medio de técnicas cromatográficas. La evaluación de la actividad antimicrobiana se realizó por el método de difusión en disco frente a tres especies bacterianas:Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 y três especies de hongos: Candida albicans ATCC 76645, Candida tropicalis ATCC 13803 y Candida glabrata ATCC 15545. Resultados: casi la mitad de los productos ensayados fueron capaces de inhibir el crecimiento de S. aureus con zonas de inhibición entre 8-16 mm. Los extractos etanolicos crudo y fracciones hexano y CHCl3 de las hojas de P. mollicomum mostraron actividad antibacteriana contra todas las cepas probadas. Las fracciones hexano de P. arboreum, P. caldense y P. mollicomum mostraron actividad antifúngica, con énfasis en la zona de inhibición de 28 mm para la fracción de P. mollicomum. Los dos flavonoides aislados de P. montealegreanum no mostraron actividad antimicrobiana. Conclusiones: los resultados preliminares de este estudio sugieren que algunos de los productos obtenidos de especies de Piper son una fuente prometedora de compuestos con actividad antimicrobiana(AU)

Introduction: The species of the genus Piper are widely found in the tropical regions of the globe and have numerous therapeutic indications. Objective: To evaluate the antimicrobial activity of extracts and fractions of four species of Piper and two flavonoids isolated from Piper montealegreanum and determine the minimum inhibitory concentration of the active products. Methods: The plant material was collected in different regions of the state of Paraíba and in Belém (Pará) and subjected to extraction with ethanol and partition with solvents in increasing degree of polarity. Flavonoids were isolated through chromatographic techniques. The evaluation of antimicrobial activity was performed by disk diffusion method front the three bacterial species: Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 and three fungi species: Candida albicans ATCC 76645, Candida tropicalis ATCC 13803 and Candida glabrata ATCC 15545. Results: Almost half of the products tested were able to inhibit the growth of S. aureus with inhibition zones between 8-16 mm. The crude ethanolic extract and hexane fractions and CHCl3 of P. mollicomum leaves showed antibacterial activity against all the tested strains. The hexane fractions of P. arboreum, P. caldense and P. mollicomum showed antifungal activity, emphasizing the formation of 28 mm inhibition zone for the fraction of P. mollicomum. The two flavonoids isolated from P. montealegreanum showed no antimicrobial activity. Conclusions: preliminary results suggest that some the products obtained from Piper species are a promising source of compounds with antimicrobial activity(AU)

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Os flavonóides 5,3’,4’-triidroxi-7-metoxiflavona, 5,3’-diidroxi-7-4’-dimetoxiflavona, 5,4’-diidroxi-7-metoxiflavona e uma mistura de esteróides (β-sitosterol e estigmasterol) foram isoladas das partes aιreas de Piper carniconnectivumC.DC, Piperaceae. As estruturas desses compostos foram estabelecidas por análises espectroscópicas de UV, IV e RMN de ¹H e 13C, incluindo técnicas uni e bidimensionais.

The flavonoids 5,3’,4’-trihydroxy-7-methoxyflavone, 5,3’-dihydroxy-7-4’-dimethoxyflavone, 5,4’-dihydroxy-7-methoxyflavone and steroids mixture (β-sitosterol and stigmasterol) were isolated from the dried aerials parts of Piper carniconnectivumC.DC. Their structures were established by spectroscopic analyses (UV, IV and ¹H, 13C NMR, including 1D and 2D NMR).