title: LTB4 as marker of 5-LO inhibitory activity of two new N-omega-ethoxycarbonyl-4-quinolones.
abstract: The supposed 5-LO inhibitory activity of two N-omega-ethoxycarbonyl-4-quinolones was tested determining leukotriene B4 (LTB4) in RBL-1 cell cultures, pretreated with the two compounds of interest. LTB4, obtained by solid-phase extraction (SPE) from cell cultures supernatants, was determined by micellar electrokinetic chromatography (MEKC). The analysis was performed using an uncoated capillary, filled with borate buffer at pH 8.3, containing 12.5 mM SDS as micelles generator. Therefore, following the decreasing of LTB4 it was possible to verify the 5-LO inhibitory activity of two quinolone derivatives. To asses the suitability of the use of LTB4 as marker of the activity of the new compounds, the analysis was repeated using quercetin, a well known 5-LO inhibitor.
authors.affiliation: Centro di Studio per la Chimica del Farmaco del CNR presso il Dip Studi Farmaceutici della Università La Sapienza, Rome, Italy.
authors.forename: E
authors.initials: E
authors.lastname: Bossù
authors.forename: A M
authors.initials: AM
authors.lastname: Aglianò
authors.forename: N
authors.initials: N
authors.lastname: Desideri
authors.forename: I
authors.initials: I
authors.lastname: Sestili
authors.forename: R
authors.initials: R
authors.lastname: Porrà
authors.forename: M
authors.initials: M
authors.lastname: Grandilone
authors.forename: M G
authors.initials: MG
authors.lastname: Quaglia
mesh_terms: D019377:12-Hydroxy-5,8,10,14-eicosatetraenoic Acid / Q000032:analysis; D000818:Animals; D001094:Arachidonate 5-Lipoxygenase / Q000378:metabolism; D015415:Biomarkers / Q000032:analysis; D000001:Calcimycin / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D020374:Chromatography, Micellar Electrokinetic Capillary; D017077:Culture Media, Conditioned / Q000737:chemistry; D019075:Electrophoresis, Capillary; D004789:Enzyme Activation / Q000187:drug effects; D005069:Evaluation Studies as Topic; D006893:Hydroxyeicosatetraenoic Acids / Q000032:analysis; D015471:Leukemia, Basophilic, Acute / Q000201:enzymology / Q000473:pathology; D007975:Leukotriene B4 / Q000032:analysis* / Q000378:metabolism; D016859:Lipoxygenase Inhibitors / Q000494:pharmacology*; D011456:Prostaglandins B / Q000032:analysis; D011794:Quercetin / Q000494:pharmacology; D015363:Quinolones / Q000494:pharmacology*; D051381:Rats; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry; D014407:Tumor Cells, Cultured
chemical_list: D015415:Biomarkers; D017077:Culture Media, Conditioned; D006893:Hydroxyeicosatetraenoic Acids; D016859:Lipoxygenase Inhibitors; D011456:Prostaglandins B; D015363:Quinolones; D007975:Leukotriene B4; D012967:Sodium Dodecyl Sulfate; D000001:Calcimycin; C022022:5-hydroxy-6,8,11,14-eicosatetraenoic acid; D019377:12-Hydroxy-5,8,10,14-eicosatetraenoic Acid; C025984:15-hydroxy-5,8,11,13-eicosatetraenoic acid; D011794:Quercetin; C042026:prostaglandin B2; D001094:Arachidonate 5-Lipoxygenase