Modulation of P-glycoprotein activity by acridones and coumarins from Citrus sinensis.
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.
Bayet
C
C
Université Claude Bernard Lyon 1, Laboratoire de Pharmacognosie, Faculté de Pharmacie, 8 avenue Rockefeller, 69373 Lyon Cedex 8, France.
Fazio
C
C
Darbour
N
N
Berger
O
O
Raad
I
I
Chaboud
A
A
Dumontet
C
C
Guilet
D
D
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
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000166:Acridines; D054831:Acridones; D003374:Coumarins; C041300:acridone