<p>This study aimed to identify new compounds capable of decreasing pancreatic lipase (PL) catalytic activity. A panel of structurally related chalcones with hydroxy and chloro substituents was chosen, and their inhibitory effects on the targeted enzyme were assessed. This work also optimized the conditions for UV/Vis spectrophotometric and fluorimetric microanalysis systems and, whenever possible, a structure–activity relationship analysis was performed. The obtained results showed the effectiveness of both methodologies in assessing the inhibition of PL catalytic activity. Some of the tested chalcones exhibited notable inhibitory effects on PL activity. Remarkably, the presence of hydroxy or chloro substituents appears to enhance the observed inhibitory activities of these compounds.</p>

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Optimization and Implementation of Spectrophotometric and Fluorimetric Methodologies to Evaluate Pancreatic Lipase Inhibitory Using Chalcones: A Comparative Study

  • Sílvia Rocha,
  • Maria C. Lobo,
  • Carina Proença,
  • Ana T. Rufino,
  • Félix Carvalho,
  • Eduarda Fernandes

摘要

This study aimed to identify new compounds capable of decreasing pancreatic lipase (PL) catalytic activity. A panel of structurally related chalcones with hydroxy and chloro substituents was chosen, and their inhibitory effects on the targeted enzyme were assessed. This work also optimized the conditions for UV/Vis spectrophotometric and fluorimetric microanalysis systems and, whenever possible, a structure–activity relationship analysis was performed. The obtained results showed the effectiveness of both methodologies in assessing the inhibition of PL catalytic activity. Some of the tested chalcones exhibited notable inhibitory effects on PL activity. Remarkably, the presence of hydroxy or chloro substituents appears to enhance the observed inhibitory activities of these compounds.