title: In vitro cytotoxicity of the LDE: daunorubicin complex in acute myelogenous leukemia blast cells.
abstract: Acute myelogenous leukemia (AML) blast cells show high-affinity degradation of low-density lipoprotein (LDL), suggesting an increased expression of cellular LDL receptors. LDE is a lipid microemulsion easily synthesized in vitro which is known to mimic the metabolic pathway of LDL. We used LDE as a carrier for daunorubicin and assayed the cytotoxicity of the complex using AML blast cells since RT-PCR analysis showed that AML cells express LDL receptor mRNA. The LDE:daunorubicin complex killed 46.7% of blast cells and 20.2% of normal bone marrow cells (P<0.001; Student t-test). Moreover, this complex destroyed AML blast cells as efficiently as free daunorubicin. Thus, LDE might be a suitable carrier of chemotherapeutic agents targeting these drugs to neoplastic cells and protecting normal tissues.
authors.affiliation: Departamento de Hematologia e Hemoterapia, Faculdade de Medicina, Universidade de São Paulo, São Paulo, SP, Brasil. llacer.ops@zaz.com.br
authors.forename: P E
authors.initials: PE
authors.lastname: Dorlhiac-Llacer
authors.forename: M V
authors.initials: MV
authors.lastname: Marquezini
authors.forename: O
authors.initials: O
authors.lastname: Toffoletto
authors.forename: R C
authors.initials: RC
authors.lastname: Carneiro
authors.forename: R C
authors.initials: RC
authors.lastname: Maranhão
authors.forename: D A
authors.initials: DA
authors.lastname: Chamone
mesh_terms: D000293:Adolescent; D000328:Adult; D000903:Antibiotics, Antineoplastic / Q000493:pharmacokinetics / Q000494:pharmacology*; D002648:Child; D003630:Daunorubicin / Q000493:pharmacokinetics / Q000494:pharmacology*; D004338:Drug Combinations; D004655:Emulsions; D005260:Female; D006801:Humans; D020014:K562 Cells / Q000187:drug effects; D015470:Leukemia, Myeloid, Acute / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D008077:Lipoproteins, LDL / Q000493:pharmacokinetics / Q000494:pharmacology*; D008297:Male; D011973:Receptors, LDL / Q000378:metabolism; D020133:Reverse Transcriptase Polymerase Chain Reaction; D014410:Tumor Stem Cell Assay
chemical_list: D000903:Antibiotics, Antineoplastic; D004338:Drug Combinations; D004655:Emulsions; D008077:Lipoproteins, LDL; D011973:Receptors, LDL; D003630:Daunorubicin