title: Screening of lipase inhibitors from marine algae.
abstract: The possible presence of an inhibitor of pancreatic lipase (triacylglycerol acylhydrolase, EC 3.1.1.3) was screened in 54 marine algae. An active inhibitor, caulerpenyne, was purified from an extract of Caulerpa taxifolia, using ethyl acetate extraction, followed by successive chromatographies on ODS and silica gel columns. The purified inhibitor was identified by thin-layer chromatography, infrared and nuclear magnetic resonance spectroscopy. Caulerpenyne competitively inhibited lipase activities using emulsified triolein and dispersed 4-methylumbelliferyl oleate (4-MU oleate) as substrates. The concentrations producing 50% inhibition against triolein and 4-MU oleate hydrolysis were 2 mM and 13 microM, respectively. In vivo, oral administration of corn oil with or without caulerpenyne to rats demonstrated a reduced and delayed peak plasma triacylglycerol concentration with caulerpenyne.
authors.affiliation: Marine Greens Laboratory Co., Ltd., Iyo-city, Ehime, Japan.
authors.forename: N
authors.initials: N
authors.lastname: Bitou
authors.forename: M
authors.initials: M
authors.lastname: Ninomiya
authors.forename: T
authors.initials: T
authors.lastname: Tsujita
authors.forename: H
authors.initials: H
authors.lastname: Okuda
mesh_terms: D000284:Administration, Oral; D000818:Animals; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D056890:Eukaryota / Q000737:chemistry*; D006923:Hymecromone / Q000031:analogs & derivatives / Q000378:metabolism; D008049:Lipase / Q000037:antagonists & inhibitors*; D008297:Male; D010179:Pancreas / Q000201:enzymology; D051381:Rats; D017208:Rats, Wistar; D012717:Sesquiterpenes / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D013379:Substrate Specificity; D013552:Swine; D014280:Triglycerides / Q000097:blood; D014304:Triolein / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D012717:Sesquiterpenes; D014280:Triglycerides; D014304:Triolein; C023520:4-methylumbelliferyl oleate; D006923:Hymecromone; C097889:caulerpenyne; D008049:Lipase