title: Dinapinones, novel inhibitors of triacylglycerol synthesis in mammalian cells, produced by Penicillium pinophilum FKI-3864.
abstract: Dinapinone A, a novel biaryl dihydronaphthopyranone, was isolated from the culture broth of Penicillium pinophilum FKI-3864 by solvent extraction, silica gel and ODS column chromatography and HPLC. Dinapinone A showed very potent inhibition of triacylglycerol (TG) synthesis in intact Chinese hamster ovary K1 (CHO-K1) cells with an IC(50) value of 0.097 μM. Dinapinone A was found to be a mixture of stereoisomers, resulting in its separation into dinapinones A1 and A2 by HPLC using a C30 reverse-phase column. Dinapinone A1 did not inhibit TG synthesis in CHO-K1 cells even at 12  μM, and dinapinone A2 showed less potent inhibition (IC(50); 0.65  μM) than dinapinone A; however, a mixture of isolated dinapinones A1 and A2 (a 1:1 ratio) recovered the potent TG inhibitory activity (IC(50); 0.054  μM). A similar effect of dinapinone on TG synthesis in intact Raji cells was also observed.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kitasato University, Minato-ku, Tokyo, Japan.
authors.forename: Satoshi
authors.initials: S
authors.lastname: Ohte
authors.forename: Daisuke
authors.initials: D
authors.lastname: Matsuda
authors.forename: Ryuji
authors.initials: R
authors.lastname: Uchida
authors.forename: Kenichi
authors.initials: K
authors.lastname: Nonaka
authors.forename: Rokuro
authors.initials: R
authors.lastname: Masuma
authors.forename: Satoshi
authors.initials: S
authors.lastname: Omura
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tomoda
mesh_terms: D000818:Animals; D016466:CHO Cells; D045744:Cell Line, Tumor; D002850:Chromatography, Gel; D002851:Chromatography, High Pressure Liquid; D003374:Coumarins / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D020128:Inhibitory Concentration 50; D010407:Penicillium / Q000378:metabolism*; D013237:Stereoisomerism; D014280:Triglycerides / Q000037:antagonists & inhibitors* / Q000096:biosynthesis
chemical_list: D003374:Coumarins; D014280:Triglycerides; C560368:dinapinone A