Automated approach for the evaluation of glutathione-S-transferase P1-1 inhibition by organometallic anticancer compounds

• Tipo: Artigo em Revista Científica Internacional
• Data: 2022

Autores

Pereira, SAP (Autor) Outra; Baptista, LAC (Autor) Outra; Biancalana, L (Autor) Outra; Marchetti, F (Autor) Outra; Dyson, PJ (Autor) Outra; Lucia L M F S Saraiva (Autor) FFUP

Revista

Título: Journal of Enzyme Inhibition and Medicinal Chemistry

Vol. 37

Páginas: 1527-1536

ISSN: 1475-6366

Editora: Taylor & Francis

Indexação

ISI Web of Knowledge - 0 Citações

Outras Informações

ID Authenticus: P-00W-QK1

DOI: 10.1080/14756366.2022.2073443

Abstract (EN): A novel automated method based on sequential injection analysis (SIA), a non-segmented flow injection technique, was developed to evaluate glutathione S-transferase P1-1 (GST P1-1) activity in the presence of organometallic complexes with putative anticancer activity. The assay is based on the reaction of L-glutathione (GSH) and 1-chloro-2,4-dinitrobenzene (CDNB) in the presence of GST P1-1 to afford the GS-DNB conjugate and the reaction may be monitored by an increase in absorbance at 340 nm. A series of ruthenium, iron, osmium and iridium complexes were evaluated as GST P1-1 inhibitors by evaluating their half-maximal inhibitory concentration (IC50). An iridium compound displays the lowest IC50 value of 6.7 +/- 0.7 mu M and an iron compound displays the highest IC50 value of 275 +/- 9 mu M. The SIA method is simple to use, robust, reliable, and efficient and uses fewer reagents than batch methods and each analysis takes only 5 minutes.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 10