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1.
J Pharm Biomed Anal ; 181: 113097, 2020 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-31931446

RESUMO

The screening of compounds is the initial step in research for the development of new drugs. For this reason, the availability of fast and reliable tools for the screening of a large number of compounds becomes essential. Among the therapeutic targets, the enzyme xanthine oxidase (XO) is of great interest for its importance as a biological source of superoxide radicals, which contribute to the oxidative stress on organisms and are involved in many pathological processes. In the present study, we validated a new method using an immobilized capillary enzyme reactor in an LC system directly coupled to triple quadrupole mass spectrometry to screen for XO ligands. The use of mass spectrometry provided selectivity and speed to the system, eliminating the analytical separation step. The Michaelis-Menten constant (KM) value determined for the immobilized enzyme was 14.5 ±â€¯0.4 µmol L-1, which is consistent with the value previously reported for the XO-ICER with UV detection in a 2D LC method. The on-line approach was successfully applied to assay the XO inhibitory activities of thirty isolated compounds from different classes of natural products and provided greater productivity (288 analysis/day) than 2D LC method (84 analysis/day) of screened samples.


Assuntos
Descoberta de Drogas/métodos , Inibidores Enzimáticos/farmacologia , Ensaios de Triagem em Larga Escala , Xantina Oxidase/antagonistas & inibidores , Artemisininas/farmacologia , Cromatografia Líquida de Alta Pressão , Glicosídeos/farmacologia , Piranos/farmacologia , Succinatos/farmacologia , Espectrometria de Massas em Tandem
2.
An Acad Bras Cienc ; 88(3 Suppl): 1899-1907, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27901194

RESUMO

Aldama arenaria and A. robusta are morphologically similar aromatic species that have seasonal development. The yield and chemical composition of essential oils from aerial and underground vegetative organs of these species were compared to verify the production of volatile metabolites in flowering and dormant phases of development and to identify if there are unique compounds for either species. The major compound in the essential oils from A. arenaria leaves was palustrol (16.22%) and for aerial stems was limonene (15.3%), whereas limonene (11.16%) and α-pinene (19.64%) were the major compounds for leaves and aerial stems from A. robusta, respectively. The major compound for the underground organs was α-pinene, in both species and phenological stages. High amounts of diterpenes were found especially for A. arenaria essential oils. Each analyzed species presented unique compounds, which can provide a characteristic chemical profile for both species helping to solve their taxonomic problems. This study characterized for the first time the yield and essential oil composition of A. arenaria and A. robusta, which have medicinal potential, and some of the compounds in their essential oils are unique to each one and may be useful in helping the correct identification of them.


Assuntos
Asteraceae/química , Óleos Voláteis/química , Óleos Vegetais/química , Estações do Ano , Monoterpenos Bicíclicos , Brasil , Cicloexenos/análise , Cromatografia Gasosa-Espectrometria de Massas , Limoneno , Monoterpenos/análise , Folhas de Planta/química , Raízes de Plantas/química , Caules de Planta/química , Terpenos/análise
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