title: Lyngbyastatins 8-10, elastase inhibitors with cyclic depsipeptide scaffolds isolated from the marine cyanobacterium Lyngbya semiplena.
abstract: Investigation of an extract from the marine cyanobacterium Lyngbya semiplena, collected in Tumon Bay, Guam, led to the identification of three new cyclodepsipeptides, lyngbyastatins 8-10 (1-3). The structures of 1-3 were determined by NMR, MS, ESIMS fragmentation and chemical degradation. Compounds 1-3 are closely related to lyngbyastatins 4-7. Like the latter compounds, we found 1-3 to inhibit porcine pancreatic elastase, with IC(50) values of 123 nM, 210 nM and 120 nM, respectively.
authors.affiliation: Department of Medicinal Chemistry, University of Florida, 1600 SW Archer Road, Gainesville, FL 32610, USA. jkwan@ufl.edu
authors.forename: Jason C
authors.initials: JC
authors.lastname: Kwan
authors.forename: Kanchan
authors.initials: K
authors.lastname: Taori
authors.forename: Valerie J
authors.initials: VJ
authors.lastname: Paul
authors.forename: Hendrik
authors.initials: H
authors.lastname: Luesch
mesh_terms: D000818:Animals; D000458:Cyanobacteria / Q000737:chemistry*; D047630:Depsipeptides / Q000737:chemistry / Q000302:isolation & purification*; D004305:Dose-Response Relationship, Drug; D006141:Guam; D009682:Magnetic Resonance Spectroscopy; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D021241:Spectrometry, Mass, Electrospray Ionization; D013552:Swine
chemical_list: D047630:Depsipeptides; C550264:lyngbyastatin 10; C550262:lyngbyastatin 8; C550263:lyngbyastatin 9; D010196:Pancreatic Elastase