We describe here the extraction and identification of several classes of phenolic compounds from the lichens Parmotrema dilatatum (Vain.) Hale, Parmotrema tinctorum (Nyl.) Hale, Pseudoparmelia sphaerospora (Nyl.) Hale and Usnea subcavata (Motyka) and determined their anti-tubercular activity. The depsides (atranorin, diffractaic and lecanoric acids), depsidones (protocetraric, salazinic, hypostictic and norstictic acids), xanthones (lichexanthone and secalonic acid), and usnic acid, as well seven orsellinic acid esters, five salazinic acid 8',9'-O-alkyl derivatives and four lichexanthone derivatives, were evaluated for their activity against Mycobacterium tuberculosis. Diffractaic acid was the most active compound (MIC value 15.6mug/ml, 41.6 microM), followed by norstictic acid (MIC value 62.5 microg/ml, 168 microM) and usnic acid (MIC value 62.5 microg/ml, 182 microM). Hypostictic acid (MIC value 94.0 microg/ml, 251 microM) and protocetraric acid (MIC value 125 microg/ml, 334 microM) showed moderate inhibitory activity. The other compounds showed lower inhibitory activity on the growth of M. tuberculosis, varying from MIC values of 250 to 1370 microM.

Excessive body fat and obesity have adverse health effects and result in significant morbidity such as type 2 diabetes mellitus. The health burden of obesity can be reduced with the Roux-en-Y gastric bypass (RYGB) weight-loss bariatric surgery. Little is known on the molecular changes that occur at the metabolome level before and after bariatric surgery, with a view to clinical biomarker development. Hence, we employed a metabolomics approach in 10 obese diabetic patients who underwent bariatric surgery. Metabolomics data were obtained by T2- and diffusion-edited hydrogen nuclear magnetic resonance ((1)H NMR) spectra to monitor the metabolic and lipoprotein profiles, and gas chromatography-mass spectrometry (CG-MS) to access the fatty acid profile before and 12 months after RYGB. Using hierarchical partial least squares discriminant analysis, we found that RYGB induces several key metabolic alterations associated with glucose homeostasis, as well as fatty acid and amino acid metabolism. The levels of lactate (Krebs' intermediate cycle) decreased after RYGB. The leucine, isoleucine, valine, lactate, and glucose levels were higher in the samples before RYGB (p<0.05). Additionally, the levels of very low-density lipoprotein, unsaturated lipids, and N-acetyl-glycoprotein were higher before RYGB. By contrast, levels of the high-density lipoprotein and phosphatidylcholine were higher after bariatric surgery. These results collectively offer important holistic integrative biology data to develop future clinically relevant metabolomics biomarkers related to bariatric surgery in connection with obesity.

Lichens produce phenolic compounds, such as depsides, depsidones, dibenzofuranes, usnic acids, depsones and others. Many of them are exclusive of lichens.1) These substances, as well as their derivatives obtained by structural modification, have shown an ample variety of pharmacological activities: antibiotic, antimycobacterial, antiviral, antitumour, analgesic, antipyretic and enzyme inhibitory.2-5) Although these activities continue to be investigated, both in lichen extracts and with pure substances, a number of others have been attributed to the compounds produced by lichens, such as anti-human immunodeficiency virus (anti-HIV) 6) and anti-herpes simplex virus 1 (anti-HSV-1). 7)Numerous studies on the biological activities of phenols have indicated that these substances are also potent antioxidants and free radical scavengers. 8) Although the free radicals perform an important role in the organism, their cumulative effects can promote the initiation and/or progression of several diseases, including atherosclerosis, inflammation, cancer, cardiovascular diseases, ischaemia, aging and other degenerative diseases. [9][10][11] The antioxidants are of interest in the treatment of several cellular degenerations, and they inhibit or delay the oxidation process by blocking the initiation or propagation of oxidizing chain reactions. 12) They are also used to preserve food by retarding rancidity, discoloration, or deterioration due to autoxidation.13) Due to the importance of antioxidants, many researches have been carried out with plants of several families and with simple phenolic substances, like those of the hydroxycinnamates group and the gallic acid derivatives. [14][15][16][17] Although the lichens are an important source of phenolic substances, studies of antioxidant activity with this group are more recent, and they have been performed mainly with extracts of some species. 12,[18][19][20][21] We have investigated lichens from the "cerrado" of the Mato Grosso do Sul State, in Brazil, through the isolation, structural elucidation, structural modifications and evaluation of biological activities of phenolic substances. The lecanoric acid isolated from the lichen Parmotrema tinctorum, and the orsellinates obtained through reactions of this acid with alcohols were evaluated against Artemia salina and microorganisms. [22][23][24] In continuing our investigations, we are relating here the results of the antioxidant activity of the lecanoric acid (1), orsellinic acid (2) and the methyl (3), ethyl (4), n-propyl (5), n-butyl (6), iso-propyl (7), sec-butyl (8) and tert-butyl (9) orsellinates. With the aim of establishing a qualitative correlation structure-activity we have also included the antioxidant activity of orcinol (10), resorcinol (11) and gallic acid (12). Results and Discussion2,2-Diphenyl-1-picrylhydrazyl (DPPH) Radical-Scavenging Activity Antioxidants are closely related to their biofunctionalities, such as the reduction of chronic diseases like DNA damage, mutagenesis, carcinogenesis and inhibition of pathog...

The interactions of tetracycline (TC), oxytetracycline (OTC) and chlortetracycline (CTC) with ovalbumin (OVA), the main allergen protein of egg white, were investigated by molecular spectroscopy and electrophoresis at three pH conditions (1.5, 4.6 and 7.4). Molecular and synchronous fluorescence, UV-vis spectroscopy, electrophoresis and H NMR were used to study the interaction process. Tetracyclines interact with ovalbumin fluorescence by a static quenching mechanism with non-fluorescent complex formation changing the native protein structure. The binding constant (K) ranged from 2.11×10 to 58.4×10Lmol, and corresponding thermodynamic parameters were measured at different temperatures and pH values. The binding process was spontaneous (ΔG<0), and the magnitude of the interaction increased in the following order: TC

Roux-en-Y gastric bypass (RYGB) surgery goes beyond weight loss to induce early beneficial hormonal changes that favor glycemic control. In this prospective study, ten obese subjects diagnosed with type 2 diabetes underwent bariatric surgery. Mixed-meal tolerance test was performed before and 12 months after RYGB, and the outcomes were investigated by a time-resolved hydrogen nuclear magnetic resonance ( 1 H NMR)-based metabolomics. To the best of our knowledge, no previous omics-driven study has used time-resolved 1 H NMRbased metabolomics to investigate bariatric surgery outcomes. Our results presented here show a significant decrease in glucose levels after bariatric surgery (from 159.80 -61.43 to 100.00 -22.94 mg/dL), demonstrating type 2 diabetes remission ( p < 0.05). The metabolic profile indicated lower levels of lactate, alanine, and branched chain amino acids for the operated subject at fasting state after the surgery. However, soon after food ingestion, the levels of these metabolites increased faster in operated than in nonoperated subjects. The lipoprotein profile achieved before and after RYGB at fasting was also significantly different, but converging 180 min after food ingestion. For example, the very low-density lipoprotein, low-density lipoprotein, N-acetylglycoproteins, and unsaturated lipid levels decreased after RYGB, while phosphatidylcholine and high-density lipoprotein increased. This study provides important insights on RYGB surgery and attendant type 2 diabetes outcomes using an ''omics'' systems science approach. Further research on metabolomic correlates of RYGB surgery in larger study samples is called for.