Interaction Between Phenolic Compounds and Lipase: The Influence of Solubility and Presence of Particles in the IC50 Value
Abstract
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.
Citing Literature
Number of times cited according to CrossRef: 9
- Riccardo Trentin, Luísa Custódio, Maria João Rodrigues, Emanuela Moschin, Katia Sciuto, José Paulo da Silva, Isabella Moro, Exploring Ulva australis Areschoug for possible biotechnological applications: In vitro antioxidant and enzymatic inhibitory properties, and fatty acids contents, Algal Research, 10.1016/j.algal.2020.101980, 50, (101980), (2020).
- Qingfeng Zhou, Jiexin Zhou, Xiaojing Liu, Yan-Bing Zhang, Shengbao Cai, Digestive Enzyme Inhibition of Different Phenolic Fractions and Main Phenolic Compounds of Ultra-High-Pressure-Treated Palm Fruits: Interaction and Molecular Docking Analyses, Journal of Food Quality, 10.1155/2020/8811597, 2020, (1-10), (2020).
- Atma-Sol Bustos, Andreas Håkansson, Javier A. Linares-Pastén, J. Mauricio. Peñarrieta, Lars Nilsson, Interaction of quercetin and epigallocatechin gallate (EGCG) aggregates with pancreatic lipase under simplified intestinal conditions, PLOS ONE, 10.1371/journal.pone.0224853, 15, 4, (e0224853), (2020).
- Pedro H. S. Cesar, Marcus V. Trento, Thais A. Sales, Anderson A. Simão, Teodorico C. Ramalho, Silvana Marcussi, Vanillic acid as phospholipase A2 and proteases inhibitor: In vitro and computational analyses, Biotechnology and Applied Biochemistry, 10.1002/bab.1943, 0, 0, (2020).
- Atma-Sol Bustos, Andreas Håkansson, Javier A. Linares-Pastén, Lars Nilsson, Interaction between Myricetin Aggregates and Lipase under Simplified Intestinal Conditions, Foods, 10.3390/foods9060777, 9, 6, (777), (2020).
- Hao Zhang, Zhao-Yu Wu, Yin-Zhen Wang, Dong-Dong Zhou, Feng-Qing Yang, De-Qiang Li, On-line immobilized trypsin microreactor for evaluating inhibitory activity of phenolic acids by capillary electrophoresis and molecular docking, Food Chemistry, 10.1016/j.foodchem.2019.125823, (125823), (2019).
- Ruyi Li, Taotao Dai, Yunbing Tan, Guiming Fu, Yin Wan, Chengmei Liu, David Julian McClements, Fabrication of pea protein-tannic acid complexes: Impact on formation, stability, and digestion of flaxseed oil emulsions, Food Chemistry, 10.1016/j.foodchem.2019.125828, (125828), (2019).
- Shiqi Luo, Harsharn Gill, Daniel Anthony Dias, Mingdi Li, Andrew Hung, Linh Toan Nguyen, George Binh Lenon, The inhibitory effects of an eight-herb formula (RCM-107) on pancreatic lipase: enzymatic, HPTLC profiling and in silico approaches, Heliyon, 10.1016/j.heliyon.2019.e02453, 5, 9, (e02453), (2019).
- Chunfang Gu, Michael A. Stashko, Ana Puhl-Rubio, Molee Chakraborty, Anutosh Chakraborty, Stephen V. Frye, Kenneth H. Pearce, Xiaodong Wang, Stephen B. Shears, Huanchen Wang, Inhibition of Inositol Polyphosphate Kinases by Quercetin and Related Flavonoids: A Structure/Activity Analysis., Journal of Medicinal Chemistry, 10.1021/acs.jmedchem.8b01593, (2019).




