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Interaction Between Phenolic Compounds and Lipase: The Influence of Solubility and Presence of Particles in the IC50 Value

Bustos, Atma‐Sol, Håkansson, Andreas, Linares‐Pastén, Javier A., Penarrieta, Jose M., Nilsson, Lars
Journal of food science 2018 v.83 no.8 pp. 2071-2076
aggregation behavior, aqueous solutions, beverages, caffeic acid, catechin, chlorogenic acid, cyanidin, enzyme inhibition, epigallocatechin gallate, false positive results, fruit juices, human health, in vitro studies, inhibitory concentration 50, lipid metabolism, myricetin, obesity, principal component analysis, quercetin, rutin, solubility, triacylglycerol lipase, vanillic acid
Obesity is one of the principal human health problems and one of the main treatments against it is the inhibition of pancreatic lipase, the main responsible enzyme of lipid digestion. For that purpose, previous studies have tested several phenolic compounds against lipase, without considering their aggregation behavior in aqueous solutions. Because of this, the present study focuses on understanding how the solubility and the presence of particles affect the IC₅₀ value of the interaction between lipase and phenolic compounds present in beverages like fruit juices and teas. Therefore, the inhibitory capacity against pancreatic lipase and the aggregate formation of 9 phenolic compounds (quercetin, rutin, myricetin, catechin, epigallocatechin gallate, cyanidin, caffeic acid, chlorogenic acid, and vanillic acid) were analyzed. The results obtained together with the solubility data from literature were treated by principal component analysis and indicate that the IC₅₀ value does not correlate with the solubility or aggregate formation of the phenolic compounds. However, the IC₅₀ values of phenolic compounds which aggregate during the assay conditions have low reproducibility. This study shows that the aggregate formation of phenolic compounds plays an important role during in vitro assays for pancreatic lipase inhibition and should be considered in future experiments as it can lead to false positive results. In terms of particle formation, the flavonoids investigated in this study are more prone to aggregation compared to the phenolic acids.