Mesalamine (5-aminosalicylic acid, 5-ASA) is used because of its local effects in the treatment
. do Café, s/n, 14040-903 Ribeirão Preto -SP, BrasilRecebido em 7/8/08; aceito em 11/3/09; publicado na web em 4/8/09This study validated a high performance liquid chromatography (HPLC) method for the quantitative evaluation of quercetin in topical emulsions. The method was linear within 0.05 -200 µg/mL range with a correlation coefficient of 0.9997, and without interference in the quercetin peak. The detection and quantitation limits were 18 and 29 ng/mL, respectively. The intra-and inter-assay precisions presented R.S.D. values lower than 2%. An average of 93% and 94% of quercetin was recovered for non-ionic and anionic emulsions, respectively. The raw material and anionic emulsion, but not non-ionic emulsion, were stable in all storage conditions for one year. The method reported is a fast and reliable HPLC technique useful for quercetin determination in topical emulsions.
Kaurenoic acid (KA), a kaurane-type diterpene extracted from leaves of Mikania hirsutissima, was previously reported as an inhibitor of vascular contractility mainly by blocking extracellular Ca 2+ influx. The compound is known for several other biological activities such as antiparasitic, antispasmodic and antibacterial activity. The aim of the present study was to investigate the effect of KA on Aspergillus nidulans. KA (0.3 mM) showed fungistatic activity against A. nidulans with visible hyphal elongation and morphology damage. These effects were reverted by CaCl 2 addition showing that KA interferes with intracellular Ca 2+ gradient in A. nidulans. This is the first report on the mechanism of action of KA involving calcium levels by altering the elongation of fungi hyphae.
: The goal of the biotransformation process is to develop structural changes and generate new chemical compounds, which can occur naturally in mammalian and microbial organisms, such as filamentous fungi, and represent a tool to achieve enhanced bioactive compounds. Cunninghamella spp is among the fungal models most widely used in biotransformation processes at phase I and II reactions, mimicking the metabolism of drugs and xenobiotics in mammals and generating new molecules based on substances of natural and synthetic origin. Therefore, the goal of this review is to highlight the studies involving the biotransformation of Cunninghamella species between January 2015 and March 2021, in addition to updating existing studies to identify the similarities between the human metabolite and Cunninghamella patterns of active compounds, with related advantages and challenges, and providing new tools for further studies in this scope.
Research background. Extracts from grape pomace, including the wine, showed many biological effects such as antioxidant and anti-inflammatory activities. Unfortunately winemakers discard the bagasse and the waste is less useful, however it contains bioactive compounds which result in antioxidant and anti-inflammatory properties. The work aimed to analyze the hydroethanolic extract of peels from agro-industrial waste from Vitis labrusca and to evaluate its antinociceptive and anti-inflammatory assays. This study is relevant for reusing a residue and adding value to the grape economic chain. Experimental approach. A representative sample of pomace was obtained and the peels were applied to produce the extract. The phenolic compounds were determined by multiple reaction monitoring mode of mass spectrometry methods and Folin-Ciocalteu, using gallic acid as standard. The biological analyzes were carried out using mice orally treated with crude extract at doses (30, 100, and 300 mg/kg). We evaluated mechanical hyperalgesia by the von Frey method, thermal heat hyperalgesia using a hot plate at 55 °C, paw edema using a pachymeter, and neutrophil recruitment by measurement of myeloperoxidase enzyme activity. The nephrotoxicity and hepatotoxicity were evaluated by biochemical analyses using blood samples that were collected after the Vitis labrusca administration. Results and conclusions. The peels correspond to 75 % of all wet winemaking residue and 59 % on a dry basis. We identified nine anthocyanins (3-O-glucoside: peonidin, delphinidin, petunidin, and malvidin; 3-p-coumaroyl-glucoside: cyanidin, peonidin, petunidin, and malvidin, and malvidin-3,5-diglucoside), five flavonoids (apigenin-7-glucoside, luteolin-7-glucoside, quercetin-3-galactoside, isorhamnetin-3-glucoside, and myricetin-3-rutinoside), and 26.62 mg GAE/g of phenolic compounds. In vivo assays, showed that Vitis labrusca extract at concentrations 100 and 300 mg/kg reduced carrageenan-induced mechanical and thermal hyperalgesia, 50 % of the paw edema, and neutrophil recruitment. In addition, there were no nephrotoxicity and hepatotoxicity. Our extract obtained from winemaking residue has analgesic and anti-inflammatory action, related at least in part to the presence of phenolic compounds, and it has no toxicity to renal and hepatic tissues. Novelty and scientific contribution. We demonstrated that this waste can be used for the production of antioxidant and anti-inflammatory products (pharmaceutical and cosmetics) without toxicity, contributing to the environmental economy.
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