Selected natural products as inhibitors of pancreatic lipase

Lipids are important components in human nutrition. Human pancreatic lipase (triacylglycerol acylhydrolase, EC 3.1.1.3) is the main enzyme that breaks down dietary fats in the human digestive system. It is released from the human pancreas and hydrolyzes 40% to 70% of triacylglycerides [1, 2]. However, an excessive fat intake can have serious consequences for health. Overweight and obesity are the fifth leading risk for global deaths. At least 2.8 million adults die each year as a result of being overweight or obese (WHO 2013). An important target for the treatment of obesity includes the development of inhibitors of nutrient digestion and absorption. Inhibition of pancreatic lipase and the associated reduction of lipid absorption is one attractive approach [3]. For finding new potent agents, an enzymatic in vitro assay based on the hydrolysis kinetic of an oleate ester of 4-methylumbelliferone by porcine pancreatic lipase was used to screen the inhibitory potential of various secondary plant products. From the compounds tested, quinic acid (IC₅₀: 13µM) and the flavonoid fisetin (IC₅₀: 20µM) showed the best pancreatic lipase inhibiting effects. The results suggest that selected secondary plant products can have a lipase inhibitory effect. For developing effective anti-obesity agents, further identification and characterization of natural compounds with anti-lipase action is necessary.

References:

[1] Winkler, F.K. et al. (1990) Nature 343: 771 – 774.

[2] Kimura, H. et al. (1982)J Biochem 92(1): 243 – 251.

[3] Foster-Schubert, K.E. et al. (2006) Endocr. Rev 27: 779 – 793.