Salacia crassifolia traditionally known as “Bacupari-do-Cerrado” is used to treat kidney problems, and as a healing agent for coughs and malaria. The phytochemical study of the S. crassifolia roots led to the isolation of thirteen compounds: abruslactone-A (1), urs-12-ene-3β,25,30-triol (2), carioprystimerin (3), β-sitosterol (4), pristimerin (5), dispermoquinone (6), netzahualcoyonol (7), 20-hydroxy-20-epi-tingenone (8), 6-oxo-pristimerol (9), 9β,10β-epoxi-3β-hydroxy-1βH,4βH,5βH,7βH,11αH-guaian-12,8β-olide (10), 3-O-b-D-glucosyl-b-sitosterol (11), 4`-O-methylepigalocatechin (12) and cerebroside (13). The chemical structures of 1-13 were determined by IR, 1D/2D NMR together with X-ray diffractometry. Compounds 2 and 10 are herein described for the first time. Extracts of S. crassifolia and compounds 3, 5, 8 and 9 were evaluated on acetylcholinesterase inhibition, in vitro cytotoxic activity and in vivo toxicity tests using Caenorhabditis elegans model. All tested compounds inhibited acetylcholinesterase, and compounds 3, 8 and 9 demonstrated a greater potential when compared to the standard eserine. The tested compounds showed low cytotoxicity against the THP-1, K562 and MDA-MB-231 cancer cell lines. None of the tested compounds and extracts were toxic against C. elegans since the larvae survival rate in L1 stage was higher than 90%.

The objective of this work was to determine the chemical composition, total phenolic compounds content, antioxidant capacity through the ABTS (2,20-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) method, as well as to evaluate the use of paper spray ionization mass spectrometry (PS-MS) to obtain fingerprints in different brands of mixed industrialized beverage based on fruits and vegetables with “detox” denomination. The carbohydrate contents ranged from 4.17% (sample D) to 12.72% (sample G). The differences may be related to the composition and proportion of the ingredients present in each formulation. The contents of total phenolic compounds varied between 26.75 mg GAE (gallic acid equivalents) g-1 (sample F) to 48.61 mg GAE g-1 (sample D). The samples A, B and C contain cabbage, spinach and parsley and presented significantly higher phenolic compounds content than the other samples. The antioxidant activity values varied between 1.76 µmol L-1 Trolox g-1 (sample B) to 18.95 µmol L-1 Trolox g-1 (sample E). The brands E, F, and G, that presented higher antioxidant potential, have ingredients pineapple, apple, cabbage, and ginger as common. The analysis of PS-MS allowed for the identification of a number of substances, including organic acids, sugars, and phenolic acids. PS-MS is a relatively simple method, fast and efficient to obtain fingerprints of mixed beverages.

ABSTRACT Major health challenges as the increasing number of cases of infections by antibiotic multiresistant microorganisms and cases of Alzheimer's disease have led to searching new control drugs. The present study aims to verify a new way of obtaining bioactive extracts from filamentous fungi with potential antimicrobial and acetylcholinesterase inhibitory activities, using epigenetic modulation to promote the expression of genes commonly silenced. For such finality, five filamentous fungal species (Talaromyces funiculosus, Talaromyces islandicus, Talaromyces minioluteus, Talaromyces pinophilus, Penicillium janthinellum) were grown or not with DNA methyltransferases inhibitors (procainamide or hydralazine) and/or a histone deacetylase inhibitor (suberohydroxamic acid). Extracts from T. islandicus cultured or not with hydralazine inhibited Listeria monocytogenes growth in 57.66 ± 5.98% and 15.38 ± 1.99%, respectively. Increment in inhibition of acetylcholinesterase activity was observed for the extract from P. janthinellum grown with procainamide (100%), when compared to the control extract (39.62 ± 3.76%). Similarly, inhibition of acetylcholinesterase activity increased from 20.91 ± 3.90% (control) to 92.20 ± 3.72% when the tested extract was obtained from T. pinophilus under a combination of suberohydroxamic acid and procainamide. Concluding, increases in antimicrobial activity and acetylcholinesterase inhibition were observed when fungal extracts in the presence of DNA methyltransferases and/or histone deacetylase modulators were tested.

RESUMO: O desperdício na cadeia produtiva de frutos, incluindo as indústrias de suco e polpa, produz grandes quantidades de resíduos, como cascas, sementes e bagaços. Esse volume de resíduos gera impacto ambiental e econômico. O objetivo deste trabalho foi determinar o potencial de aproveitamento de resíduos de maracujá (Passiflora edulis) e de variedades de maçã (Malus domestica) na produção de farinhas funcionais. A farinha de maracujá apresentou maior redução de radicais DPPH (EC50%: 50,4μg/mL), demonstrando potencial antioxidante, maior inibição de Staphylococcus aureus (71,3±1,2μg/mL) e da acetilcolinesterase (10%). Todas as farinhas de maçã foram boas antioxidantes e a fuji destacou-se inibindo Pseudomonas aeruginosa (78,6±3,1μg/mL). Todos os resíduos mostraram potencial para aproveitamento como produto funcional, seja como fonte de antioxidantes, conservante natural (antimicrobiano) para alimentos secos ou uso suplementar no tratamento de Alzheimer.

ABSTRACT: The waste in the fruit production chain, including the juice and pulp industries, produces large quantities of leftover husks, seeds and bagasse. This volume of waste generates huge environmental and economic impact. The objective of this research was to determine the potential of using residues from passion fruit (Passiflora edulis) and apple (Malus domestica) varieties in the production of functional flours. Passion fruit flour showed greater reduction of DPPH (EC50%: 50.4μg/mL) radicals, showing antioxidant potential, as well as a more efficient inhibition of Staphylococcus aureus (71.3±1.2μg/mL), with a modest; however efficient, inhibition of acetylcholinesterase (10%). All Apple flours were good antioxidants and the fuji apple flour stood out inhibiting Pseudomonas aeruginosa (78.6±3.1μg/mL). All the residues showed potential for use as a functional product either as a source of antioxidants, a natural (antimicrobial) preservative for dry foods or supplementary use by patients with Alzheimer’s disease.

Introdução: o uso de plantas para fins medicinais vem crescendo a cada dia. A partir de métodos extrativos, podem-se obter extratos com diferentes atividades terapêuticas, dentre elas ação antifúngica, anticolinesterásica, antitussígena e antibacteriana, esta última, por sua vez, de grande importância comercial em vista do crescimento gradativo de casos de infecções por bactérias resistentes aos tratamentos convencionais. Objetivos: caracterizar químicamente os extratos foliares de B. anisandra, uma vez que não há relatos sobre a mesma na literatura e verificar as atividades anticolinesterásica e antibacteriana destes frente às bactérias patogênicas. Métodos: os extratos obtidos a partir de hexano, clorofórmio, acetato de etila e metanol tiveram as classes fitoquímicas presentes identificadas através de métodos de identificação clássica, testados frente a bactérias patogênicas Staphylococcus aureus, Streptococcus mutans, Bacillus cereus, Klebsiella pneumoniae, Shigella flexneri, Pseudomonas aeruginosa e avaliados quanto à capacidade de degradação da enzima acetilcolinesterase. Resultados: os resultados encontrados revelaram a diversificação química encontrada em B. anisandra e o potencial farmacotecnológico de seus extratos, especialmente em relação a alcalóides presentes e à sua atividade anticolinesterásica. Conclusão: conclui-se que os extratos de B. anisandra podem ser utilizados para fins farmacotecnológico e que necessita-se de mais estudos fitoquímicos em relação a esta espécie.

Introducción: el uso de plantas con fines medicinales está creciendo cada día. De los métodos de extracción, se pueden obtener extractos con diferentes actividades terapéuticas, entre ellas, antifúngicas, anticolinesterasa, antitusivas y antibacterianas; esta última, a su vez, de gran importancia comercial en vista al aumento gradual de los casos de infecciones por bacterias resistentes a los tratamientos convencionales. Objetivos: caracterizar químicamente los extractos de hojas de B. anisandra, porque no hay reportes en la literatura y verificar las actividades de la acetilcolinesterasa y la actividad antibacteriana frente a bacterias patógenas. Métodos: los extractos obtenidos a partir de la partición con hexano, cloroformo, acetato de etilo y metanol fueron identificados y las clases de fitoquímicos presentes en los extractos mediante métodos de identificación clásica, los cuales fueron probados contra bacterias patógenas de Staphylococcus aureus, Streptococcus mutans, Bacillus cereus, Klebsiella pneumoniae, Shigella flexneri, Pseudomonas aeruginosa, y evaluados por la capacidad de degradación de la enzima acetilcolinesterasa. Resultados: se mostró la diversidad química encontrada en B. anisandra y el potencial farmacotecnológico, especialmente en relación con los alcaloides encontrados y su actividad anticolinesterasa. Conclusiones: los exctratos de B. anisandra se pueden utilizar para fines farmacotecnológicos y se necesitan más estudios fitoquímicos en relación con esta especie.

Several reasons motivated the development of new generations of antibiotics, such as their high ability to develop resistance to virtually all kinds of anti-infective agents and the crescent market demand for new drugs to treat special demanding patients. After penicillin discovery, several antibiotics were developed from fungal metabolites, since antibacterial secondary metabolites consists on a fungal endogenous protective mechanism against natural competitors. The aim of this review is to present the structural diversity of antibacterial and antifungal metabolites produced by fungi, mentioning sources of fungal isolates, cultivation process and details on the scope of their antibiotic activity.

Condições otimizadas para a biotransformação de compostos diterpênicos pelo fungo Cephalosporium aphidicola foram determinadas, realizando-se incubações em microescala nas quais variaram-se parâmetros como o tempo de incubação e a quantidade de substrato adicionado. A velocidade (índice) de bioconversão foi monitorada analisando-se os extratos de cultivo através de cromatografia em camada delgada e cromatografia gasosa. Os resultados obtidos mostraram que, para melhores rendimentos, o substrato deve ser adicionado em solução etanólica, na concentração de 15-30 mg por 100 mL de meio de cultura. A extração de produtos deve ser realizada com acetato de etila, a partir da fase aquosa e do micélio, no sexto dia após a adição do substrato. Estes resultados podem ser utilizados como um roteiro para incubações de compostos estruturalmente semelhantes com o fungo Cephalosporium aphidicola.

Parameters for a more efficient biotransformation of diterpene-like compounds by the fungus Cephalosporium aphidicola were established by carrying out microscale feedings at several conditions. Experiments were guided by thin layer chromatography and gas chromatography analysis. It was observed that the substrate should be added in ethanol at concentrations between 15 to 30 mg per 100 ml of medium. The extraction of the product showed to be more efficient when carried out from both mycelia and broth and using ethylacetate as the extracting solvent. The experiment should be stopped six days after feeding the substrate to the fungus for the best product yield.