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Free Linoleic Acid and Oleic Acid Reduce Fat Digestion and Absorption In Vivo as Potent Pancreatic Lipase Inhibitors Derived from Sesame Meal
Authors:Xuan Li  Sayo Morita  Hiroaki Yamada  Keita Koga  Wakana Ota  Toma Furuta  Atsushi Yamatsu  Mujo Kim
Affiliation:1.Pharma Foods International Co., Ltd., Kyoto 615-8245, Japan; (S.M.); (H.Y.); (K.K.); (M.K.);2.Mitsui Sugar Co., Ltd., Tokyo 103-8423, Japan; (W.O.); (T.F.)
Abstract:
Pancreatic lipase catalyzes the cleavage of triacylglycerols at the oil–water interface, and is known as the dominant determiner of dietary fat digestion. Reducing dietary fat digestion and absorption by modulating the activity of pancreatic lipase has become a favorable strategy to tackle obesity. Orlistat is, at present, the only pancreatic lipase inhibitor approved for the treatment of obesity; however, an array of gastrointestinal adverse effects associated with orlistat limits its tolerability. As a safe alternative to orlistat, a number of natural product-derived compounds with varying degrees of pancreatic lipase inhibitory activity have been reported. We herein reported that bioactivity-guided fractionation of sesame meal led to the identification of free linoleic acid and oleic acid as potent inhibitors of porcine pancreatic lipase in vitro with an IC50 of 23.1 µg/mL (82.4 µM) and 11.7 µg/mL (41.4 µM), respectively. In rats, a single oral dose of the mixture of these fatty acids significantly suppressed the elevation of blood triacylglycerol level following fat intake. These results substantiate the role of free linoleic acid and oleic acid as a novel class of natural product-derived functional molecules that act as pancreatic lipase inhibitors, and their potential for healthy, routine-based weight management.
Keywords:pancreatic lipase inhibitor   functional molecule   free fatty acids   oleic acid   linoleic acid   sesame   obesity   fat digestion and absorption   dietary supplement
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