title: A new P-glycoprotein inhibitor from the caper spurge (Euphorbia lathyris).
abstract: The macrocyclic lathyrane polyester Euphorbia factor L10 (1a) has been obtained from the seeds of the caper spurge (E. lathyris). The interaction of L10 (1a) and its acetyl derivative (1b) with P-glycoprotein, a multidrug transporter overexpressed in cancer cells and responsible for resistance to chemotherapy, was investigated. The results established lathyrane diterpenoids as a novel chemotype for P-glycoprotein inhibitors.
authors.affiliation: Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche, Viale Ferrucci 33, 28100 Novara, Italy. appendino@pharm.unipmn.it
authors.forename: Giovanni
authors.initials: G
authors.lastname: Appendino
authors.forename: Carla
authors.initials: C
authors.lastname: Della Porta
authors.forename: Gwenaëlle
authors.initials: G
authors.lastname: Conseil
authors.forename: Olov
authors.initials: O
authors.lastname: Sterner
authors.forename: Enrico
authors.initials: E
authors.lastname: Mercalli
authors.forename: Charles
authors.initials: C
authors.lastname: Dumontet
authors.forename: Attilio
authors.initials: A
authors.lastname: Di Pietro
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors*; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D028481:Euphorbia / Q000737:chemistry*; D005858:Germany; D006801:Humans; D020014:K562 Cells / Q000187:drug effects; D007938:Leukemia; D015394:Molecular Structure; D010946:Plants, Medicinal / Q000737:chemistry*; D012639:Seeds / Q000737:chemistry; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D004224:Diterpenes; C474529:Euphorbia factor L10; C474530:Euphorbia factor L10, acetyl derivative