Antimycobacterial and cytotoxicity activity of synthetic and natural compounds. Secondary metabolites from Curvularia eragrostidis and Drechslera dematioidea, Clusia sp. floral resin, alkaloids from Pilocarpus alatus, salicylideneanilines, piperidine amides, the amine 1-cinnamylpiperazine and chiral pyridinium salts were assayed on Mycobacterium tuberculosis H37Rv. N-(salicylidene)-2-hydroxyaniline was the most effective compound with a minimal inhibitory concentration (MIC) of 8 µmol/L. Dihydrocurvularin was moderately effective with a MIC of 40 µmol/L. Clusia sp. floral resin and a gallocatechin-epigallocatechin mixture showed MIC of 0.02 g/L and 38 µmol/L, respectively. The cytotoxicity was evaluated for N-(salicylidene)-2-hydroxyaniline, curvularin, dihydrocurvularin and Clusia sp. floral resin, and the selectivity indexes were > 125, 0.47, 0.75 and 5, respectively.

The development of liquid chromatography-mass spectrometric (LC-MS) techniques in the last few decades has made possible the analysis of trace amounts of analytes from complex matrices. With LC, the analytes of interest can be separated from each other as well as from the interfering matrix, after which they can be reliably identified thanks to the sensitivity and specificity of MS. LC-MS has become an irreplaceable tool for many applications, ranging from the analysis of proteins or pharmaceuticals in biological fluids to the analysis of toxic substances in environmental samples. In different segments of Brazilian Industry mass spectrometry has an important role, e.g. in the pharmaceutical industry in the development of generic formulations, contributing to the growth of Industry and social inclusion. However, the Brazilian chemists until this moment don't have an effective role in this new segment of the analytical chemistry in Brazil. The present paper shows the actual scenario for mass spectrometry in the pharmaceutical industry, emphasizing the need of a revision of graduation courses to attend the needs of this growing market.

Reações de biocatálise foram realizadas em microplacas (200 µL) visando a utilização de substratos fluorogênicos (100 µmol L-1) para prospecção rápida de epóxido hidrolases (EHs) e Baeyer-Villiger monoxigenases (BVMOs) em microrganismos (células inteiras). Um protocolo final foi alcançado para EHs, com a detecção de 3 novas fontes enzimáticas (Agrobacterium tumefaciens, Pichia stipitis, Trichosporom cutaneum). O ensaio fluorogênico para BVMO não ocorreu como esperado. A abordagem de algumas variáveis envolvidas (aeração; pH) proporcionou a detecção inédita da atividade enzimática de BVM em T. cutaneum.

Biocatalysis reactions were performed on microtiter plates (200 µL) aiming at the utilization of fluorogenic substrates (100 µmol L-1) for rapid whole cell screening for epoxide hydrolases (EHs) and Baeyer-Villiger monoxygenases (BVMOs). A final protocol was achieved for EHs, with 3 new enzymatic sources being detected (Agrobacterium tumefaciens, Pichia stipitis, Trichosporom cutaneum). The fluorogenic assay for BVMO did not work as expected. However, an approach to possible variables involved (aeration; pH) provided the first detection of a BVMO activity in T. cutaneum.