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 e...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 eff ects 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 eff ectiveness of both methodologies in assessing the inhibition of PL catalytic activity.Some of the tested chalcones exhibited notable inhibitory eff ects on PL activity.Remarkably,the presence of hydroxy or chloro substituents appears to enhance the observed inhibitory activities of these compounds.展开更多
基金Open access funding provided by FCT|FCCN(b-on)financial support from Fundacao para a Ciência e Tecnologia and Ministério da Ciência,Tecnologia e Ensino Superior(FCT/MCTES)by projects UID/50006-Laboratório Associado para a Química Verde-Tecnologias e Processos Limpos,UIDB/04378/2020(UCIBIO),and LA/P/0140/2020(i4HB)through PT national funds,as well as by project EXPL/MED-QUI/0815/2021。
文摘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 eff ects 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 eff ectiveness of both methodologies in assessing the inhibition of PL catalytic activity.Some of the tested chalcones exhibited notable inhibitory eff ects on PL activity.Remarkably,the presence of hydroxy or chloro substituents appears to enhance the observed inhibitory activities of these compounds.
