title: Natural anionic polymer acts as highly efficient trypsin inhibitor based on an electrostatic interaction mechanism.
abstract: Sodium alginate (SA), acting as a trypsin inhibitor by means of electrostatic interaction, is studied. The half-maximal inhibitory concentration (IC50 = 0.05 μg mL(-1) ) of this natural anionic polymer is about 400 times lower than that of commercial soybean trypsin inhibitor (STI). Unlike the Ca(2+) -deprivation mechanisms, its inhibition may be attributed to preventing the trypsin active site (TAS) from accessing the macromolecular substrates instead of denaturing it. SA is an efficient, innocuous, and cost-effective inhibitory excipient that can be conveniently used in many peptide and protein dosage formulations.
authors.affiliation: Laboratory of Biomedical Material Engineering, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, 457 Zhongshan Road, Dalian, 116023, PR China; University of the Chinese Academy of Sciences, 19 Yuquan Road, Beijing, 100049, PR China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Lv
authors.forename: Jianbin
authors.initials: J
authors.lastname: Zhang
authors.forename: Yizhe
authors.initials: Y
authors.lastname: Song
authors.forename: Bing
authors.initials: B
authors.lastname: Wang
authors.forename: Shujun
authors.initials: S
authors.lastname: Wang
authors.forename: Shan
authors.initials: S
authors.lastname: Zhao
authors.forename: Guojun
authors.initials: G
authors.lastname: Lv
authors.forename: Xiaojun
authors.initials: X
authors.lastname: Ma
mesh_terms: D000464:Alginates / Q000737:chemistry*; D000838:Anions / Q000737:chemistry; D001688:Biological Products / Q000737:chemistry; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D007328:Insulin / Q000737:chemistry / Q000378:metabolism; D007700:Kinetics; D046529:Microscopy, Electron, Transmission; D011108:Polymers / Q000737:chemistry*; D055672:Static Electricity; D014357:Trypsin / Q000737:chemistry / Q000378:metabolism; D014361:Trypsin Inhibitors / Q000737:chemistry* / Q000378:metabolism
chemical_list: D000464:Alginates; D000838:Anions; D001688:Biological Products; D006603:Hexuronic Acids; D007328:Insulin; D011108:Polymers; D014361:Trypsin Inhibitors; D020723:Glucuronic Acid; D014357:Trypsin
keywords: alginate; biological applications of polymers; drug delivery systems; insulin; trypsin inhibitors