title: Isolation and structural determination of squalene synthase inhibitor from Prunus mume fruit.
abstract: Squalene synthase plays an important role in the cholesterol biosynthetic pathway. Inhibiting this enzyme in hypercholesterolemia can lower not only plasma cholesterol but also plasma triglyceride levels. A squalene synthase inhibitor was screened from Prunus mume fruit, and then purified via sequential processes of ethanol extraction, HP-20 column chromatography, ethyl acetate extraction, silica gel column chromatography, and crystallization. The squalene synthase inhibitor was identified as chlorogenic acid with a molecular mass of 354 Da and a molecular formula of C16H18O9 based on UV spectrophotometry, 1H and 13C NMRs, and mass spectrometry. Chlorogenic acid inhibited the squalene synthase of pig liver with an IC50 level of 100 nM. Since chlorogenic acid was an effective inhibitor against the squalene synthase of an animal source, it may be a potential therapeutic agent for hypercholesterolemia.
authors.affiliation: Department of Food and Culinary Art, Osan College, Osan 447-749, Korea.
authors.forename: Sung-Won
authors.initials: SW
authors.lastname: Choi
authors.forename: Nam-Yoon
authors.initials: NY
authors.lastname: Hur
authors.forename: Soon-Cheol
authors.initials: SC
authors.lastname: Ahn
authors.forename: Dong-Seob
authors.initials: DS
authors.lastname: Kim
authors.forename: Jae-Kwon
authors.initials: JK
authors.lastname: Lee
authors.forename: Dae-Ok
authors.initials: DO
authors.lastname: Kim
authors.forename: Seung-Kook
authors.initials: SK
authors.lastname: Park
authors.forename: Byung-Yong
authors.initials: BY
authors.lastname: Kim
authors.forename: Moo-Yeol
authors.initials: MY
authors.lastname: Baik
mesh_terms: D002726:Chlorogenic Acid / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D013186:Farnesyl-Diphosphate Farnesyltransferase / Q000037:antagonists & inhibitors*; D005638:Fruit / Q000737:chemistry; D020128:Inhibitory Concentration 50; D019906:Nuclear Magnetic Resonance, Biomolecular; D027861:Prunus / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet
chemical_list: D004791:Enzyme Inhibitors; D002726:Chlorogenic Acid; D013186:Farnesyl-Diphosphate Farnesyltransferase