title: Modulation of P-glycoprotein activity by acridones and coumarins from Citrus sinensis.
abstract: Bioguided fractionation of the roots of Citrus sinensis (Rutaceae) led to the isolation and identification of five coumarins, namely, clausarin, suberosin, poncitrin, xanthyletin and thamnosmonin, seven acridones, namely, acrimarine B, 2-methoxycitpressine I, citpressine I, buntanine, acrimarine E, honyumine and acrimarine C, and one terpenoid, namely, limonin. Among these compounds, clausarin, 2-methoxycitpressine I and acrimarine E inhibited P-glycoprotein-mediated drug efflux in K562/R7 human leukemic cells over-expressing P-glycoprotein.
authors.affiliation: Université Claude Bernard Lyon 1, Laboratoire de Pharmacognosie, Faculté de Pharmacie, 8 avenue Rockefeller, 69373 Lyon Cedex 8, France.
authors.forename: C
authors.initials: C
authors.lastname: Bayet
authors.forename: C
authors.initials: C
authors.lastname: Fazio
authors.forename: N
authors.initials: N
authors.lastname: Darbour
authors.forename: O
authors.initials: O
authors.lastname: Berger
authors.forename: I
authors.initials: I
authors.lastname: Raad
authors.forename: A
authors.initials: A
authors.lastname: Chaboud
authors.forename: C
authors.initials: C
authors.lastname: Dumontet
authors.forename: D
authors.initials: D
authors.lastname: Guilet
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors*; D000166:Acridines / Q000302:isolation & purification* / Q000494:pharmacology*; D054831:Acridones; D045744:Cell Line, Tumor; D032084:Citrus sinensis / Q000737:chemistry*; D003374:Coumarins / Q000302:isolation & purification* / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D018517:Plant Roots / Q000737:chemistry
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000166:Acridines; D054831:Acridones; D003374:Coumarins; C041300:acridone