Inhibitory effect of astaxanthin on pancreatic lipase with inhibition kinetics integrating molecular docking simulation. (September 2018)

• Record Type: Journal Article
• Authors: Du, Xiping; Bai, Manli; Huang, Ying; Jiang, Zedong; Chen, Feng; Ni, Hui; Li, Qingbiao
• Is Part Of: Journal of functional foods. Volume 48(2018)
• Page Start: 551
• Page End: 557
• Publication Date: 2018-09
• Subjects: Astaxanthin -- Pancreatic lipase -- Inhibitory effect -- Kinetics -- Molecular interaction -- Docking simulation; HFFD High-fat-high-fructose diet -- p-NPG 4-nitrophenyl butyrate -- PNP p-nitrophenol -- MOPS 3-(N-morpholino) propane sulphonic acid -- DMSO dimethylsulfoxide -- HPLC high performance liquid chromatography -- FI fluorescence intensity -- CD spectroscopy circular Dichroism spectroscopy -- MD molecular docking; Functional foods -- Analysis -- Periodicals; Food -- Biotechnology -- Periodicals; Nutrition -- Periodicals; 613.2
• DOI: 10.1016/j.jff.2018.07.045
• Languages: English
• ISSNs: 1756-4646

Abstract

Graphical abstract: Highlights: Phaffia rhodozyma astaxanthin inhibited pancreatic lipase activity was first found. Astaxanthin reduced lipase activity through noncompetitive inhibition. Astaxanthin reduced enzyme activity by changing lipase's secondary conformation. Astaxanthin inhibited lipase by blocking the entrance channel of catalytic site. Abstract: Astaxanthin is a natural pigment that possesses benefit potentials to prevent obesity, however, its underlying mechanism is not clarified. In the current study, Phaffia rhodozyma astaxanthin was prepared and its inhibitory effect on pancreatic lipase was evaluated. The results showed that astaxanthin significantly inhibited the activity of pancreatic lipase in a dose-dependent manner within the tested concentration ranges. The kinetic analysis demonstrated that astaxanthin noncompetitively inhibited pancreatic lipase activity. In addition, astaxanthin induced secondary structure changes which resulted in decreased enzyme activities. Furthermore, the molecular docking analysis revealed that astaxanthin blocked the channel of catalytic site to delay substrate entrance or prevent product diffusion through changing the catalytic site conformation. These findings not only shed light on the underlying inhibitory mechanism of astaxanthin on pancreatic lipase, but also provide scientific evidence for extending the application of astaxanthin in functional food industries.