Identification of metabolites and thermal transformation products of quinolones in raw cow milk by liquid chromatography coupled to high resolution mass spectrometry

The presence of residues of antibiotics, metabolites, and thermal transformation products (TPs), produced during thermal treatment to eliminate pathogenic microorganisms in milk, could represent a risk for people. Cow"s milk samples spiked with enrofloxacin (ENR), ciprofloxacin (CIP), difloxacin (DIF), and sarafloxacin (SAR) and milk samples from cows medicated with ENR were submitted to several thermal treatments. The milk samples were analyzed by liquid chromatography-mass spectrometry (LC-MS) to find and identify TPs and metabolites. In this work, 27 TPs of 4 quinolones and 24 metabolites of ENR were found. Some of these compounds had been reported previously, but others were characterized for the first time, including lactose-conjugated CIP, the formamidation reaction for CIP and SAR, and hydroxylation or ketone formation to produce three different isomers for all quinolones studied.

Síntese e atividade antibacteriana de imidas cíclicas: 3,4-dicloromaleimidas e 3-cloro-4-substituída-maleimidas

In the present study, new N-aryl and N-alkylarylcyclic imides were synthesized and their antibacterial properties against Escherichia coli and Staphylococcus aureus were evaluated by using the diffusion method. All compounds were obtained in good yield (54 - 95%) and characterized by spectral data (¹H-NMR, MS, IR) and elemental analysis (CHN). The biological results indicated that some compounds exert significative antibacterial effects, confirming previous studies on biological activities of cyclic imides.

Comparison of three analytical methods for the determination of quinolones in pig muscle samples

This work presents a comparison between three analytical methods developed for the simultaneous determination of eight quinolones regulated by the European Union (marbofloxacin, ciprofloxacin, danofloxacin, enrofloxacin, difloxacin, sarafloxacin, oxolinic acid and flumequine) in pig muscle, using liquid chromatography with fluorescence detection (LC-FD), liquid chromatography-mass spectrometry (LC-MS) and liquid chromatography-tandem mass spectrometry (LC-MS/MS). The procedures involve an extraction of the quinolones from the tissues, a step for clean-up and preconcentration of the analytes by solid-phase extraction and a subsequent liquid chromatographic analysis. The limits of detection of the methods ranged from 0.1 to 2.1 ng g−1 using LC-FD, from 0.3 to 1.8 using LC-MS and from 0.2 to 0.3 using LC-MS/MS, while inter- and intra-day variability was under 15 % in all cases. Most of those data are notably lower than the maximum residue limits established by the European Union for quinolones in pig tissues. The methods have been applied for the determination of quinolones in six different commercial pig muscle samples purchased in different supermarkets located in the city of Granada (south-east Spain).

Identification of metabolites and thermal transformation products of quinolones in raw cow milk by liquid chromatography coupled to high resolution mass spectrometry.

The presence of residues of antibiotics, metabolites, and thermal transformation products (TPs), produced during thermal treatment to eliminate pathogenic microorganisms in milk, could represent a risk for people. Cow"s milk samples spiked with enrofloxacin (ENR), ciprofloxacin (CIP), difloxacin (DIF), and sarafloxacin (SAR) and milk samples from cows medicated with ENR were submitted to several thermal treatments. The milk samples were analyzed by liquid chromatography-mass spectrometry (LC-MS) to find and identify TPs and metabolites. In this work, 27 TPs of 4 quinolones and 24 metabolites of ENR were found. Some of these compounds had been reported previously, but others were characterized for the first time, including lactose-conjugated CIP, the formamidation reaction for CIP and SAR, and hydroxylation or ketone formation to produce three different isomers for all quinolones studied.

Fármacos no combate à tuberculose: passado, presente e futuro

Approximately every minute, somewhere in the world four people die from tuberculosis (TB), an infection of Mycobacterium tuberculosis with about 3 million deaths per year. In spite of these problems, unfortunaly, it is about 40 years that a novel drug was last introduced on the market. Due to the rapid spread of multi-drug resistant TB strains, resistant against all major anti-tuberculosis drugs, and the recent resurgence of the incidence of tuberculosis in association with the human immunodeficiency virus (HIV) infection and AIDS, we need urgently the development of new drugs to fight tuberculosis. This is covered in the present article.

Constituintes químicos de Luehea divaricata Mart. (Tiliaceae)

Chemical studies of the leaves of L. divaricata afforded 3beta-p-hydroxybenzoyl-tormentic acid, a triterpene with an ursene-type skeleton, a mixture whose main compound was an oleanene derivative, the maslinic acid, a C-glycoside flavone, vitexin and glucopyranosylsitosterol. A flavonoid, characterized as (-)-epicatechin, which belongs to the flavan-3-ol class, was isolated from the stem's bark. The structures of the compounds were elucidated by spectroscopic analysis. The antibacterial, antifungal and antiproliferative activities of the crude methanolic extracts of leaves and bark were evaluated and the antibacterial properties of the fractions of the barks were also investigated.

Tiossemicarbazonas: métodos de obtenção, aplicações sintéticas e importância biológica

Thiosemicarbazones are a class of compounds known by their chemical and biological properties, such as antitumor, antibacterial, antiviral and antiprotozoal activity. Their ability to form chelates with metals has great importance in their biological activities. Their synthesis is very simple, versatile and clean, usually giving high yields. They are largely employed as intermediates, in the synthesis of others compounds. This article is a survey of some of these characteristics showing their great importance to organic and medicinal chemistry.

Fate of peat utilization

Peat is an organic substance with the maintenance of a mineral part, what shows it as interesting object for studying. Both organic and mineral parts of peat find application in various fields of activity of the people. Antibacterial properties of peat are known since an antiquity. Today people have expanded a spectrum of application of peat to use of by-products of its processing for reception of rather ecologically harmless fuel. The master theses are focused on peat, as on ambiguous raw materials for processing and fuel manufacture. The purpose of theses to show how much widely applied peat, technologies on its processing and its influence on environment at all stages of its working out.

Potencial antimicrobiano e alelopático das amidas isoladas do extrato das raízes de Ottonia martiana Miq.

Two amides, piperovatine and isopiperlonguminine, were isolated from the roots of Ottonia martiana Miq., a herbaceous shrub commonly used in folk medicine in the treatment of toothache. The crude extract (CE) and isolated compounds were submitted to bioautography and allelopathic assay. The bioautograms allowed the detection of compounds with antibacterial activity and the identification of the bioactive substance piperovatine. The CE and amides exhibited an allelopathic effect on Lactuca sativa (lettuce) seedling growth but did not affect the seeds' germinability.

Própolis do sudeste e nordeste do Brasil: influência da sazonalidade na atividade antibacteriana e composição fenólica

The composition and biological activities of propolis, a resinous hive product collected by honeybees from various plant sources, depends on various factors such as season and vegetation of the area. The aim of this study was to evaluate the influence of the seasonal effect on the ethanolic extracts of Brazilian propolis (EEP) type 6 and type 12, collected during 6 months in terms of antibacterial activity and phenolic composition. The antimicrobial properties were evaluated by MIC and MBC on S. mutans Ingbritt 1600 and the profile of chemical composition by UV-visible spectrophotometry, HPLC-RF and GC-MS. The results demonstrated that the season in which propolis is collected influences its chemical composition, resulting in modifications in its antibacterial activity.

Diversidade de policetídeos produzidos por espécies de Penicillium isoladas de Melia azedarach e murraya paniculata

Eight compounds comprising four groups of polyketides, the xanthone fusarindin, the mixed peptide alkaloid-polyketide GKK1032, the anthraquinones crisophanol, citreoveridin and janthinone, and the azaphylones dihydrocitrinone, citrinin and citrinin H-1, were identified in Penicillium species isolated as endophytic fungi from Melia azedarach and Murraya paniculata. The antibacterial activity of the azaphylones was tested and showed that citrinin H-1 is more active than citrinin.

Estudo comparativo de técnicas de screening para avaliação da atividade anti-bacteriana de extratos brutos de espécies vegetais e de substâncias puras

In this work, the effectiveness of four screening techniques (three techniques of the diffusion method and one microdilution broth method) were compared. Evaluated were the ethanolic and dichloromethanic extracts of Miconia rubiginosa (Melastomataceae) against six standard bacteria (ATCC). The results showed statistical disagreement among the three diffusion techniques. Among the diffusion techniques, the well technique displayed the best result. However the microdilution broth method demonstrated to be the most adequate method to evaluate the antibacterial activity of plant crude extracts and pure compounds when compared to the other methodologies.

Chaetoglobosinas produzidas por Chaetomium globosum, fungo endofítico associado a Viguiera robusta Gardn. (Asteraceae)

Endophytes live in association with host plants during all or part of their life cycle without causing any apparent disease. They are considered outstanding and underexploited sources of novel bioactive compounds. Chaetomium globosum was isolated as an endophytic fungus from the healthy leaves of Viguiera robusta. C.globosum is a remarkable producer of chaetoglobosins, which are typically cytotoxic. In this work, chaetoglobosins B (1), D (2) and E (3) have been produced by the endophytic C. globosum strain. Chaetoglobosin B was evaluated against Jurkat (leukemia) and B16F10 (melanoma) tumoral cells and showed 89.55% and 57.10% of inhibition at 0.1 mg mL-1, respectively. Chaetoglobosin B also showed weak antibacterial activity against Staphylococcus aureus (MIC 120 µg/mL) and Escherichia coli (MIC 189 µg/mL).

Ocorrência e diversidade estrutural de metabólitos fúngicos com atividade antibiótica

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.

Composição química e atividade biológica de extrato oleoso de própolis: uma alternativa ao extrato etanólico

Propolis is mostly used as hydroalcoholic extract. Recently there has been a growing number of patents dealing with new solvents for preparing propolis extracts. This study aimed to prepare edible oil propolis extracts and compare their chemical composition and biological activity with ethanolic propolis extracts. ESI-MS and spectrophotometric methods were used for qualitative and quantitative analyses, respectively. Antibacterial activity was evaluated by diffusion in agar. Cytotoxicity was tested by MTT assay using tumor cell lines. The oil is able to extract bioactive compounds from propolis. Further studies are needed to improve extraction efficiency and to characterize the active components.