Cytotoxic effect of a lipophilic alkylating agent after incorporation into low density lipoprotein or emulsions: Studies in human leukemic cells

被引:19
作者
Masquelier, M [1 ]
Lundberg, B
Peterson, C
Vitols, S
机构
[1] Karolinska Univ Hosp, Karolinska Inst, Div Clin Pharmacol, Dept Med, S-17176 Stockholm, Sweden
[2] Abo Akad Univ, Dept Biochem & Pharm, FIN-20520 Turku, Finland
[3] Linkoping Univ, Fac Hlth Sci, Dept Med & Care, Div Clin Pharmacol, SE-58185 Linkoping, Sweden
关键词
LDL; lipid emulsion; acute myeloid leukemia; DNR; melphalan;
D O I
10.1016/j.leukres.2005.06.012
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
The use of low density lipoprotein (LDL) as drug carrier in acute myeloblastic leukemia chemotherapy is attractive due to high LDL uptake by leukemic cells. Lipid-based formulations, such as liposomes or microemulsions are promising alternatives. In the current study, we incorporated N-trifluoroacelyl-adriamycin-14-valerate (AD32), a lipophilic derivative of daunorubicin (DNR), and WB4291, a lipophilic alkylating agent, into LDL or lipid microemulsions and evaluated their cytotoxic activities towards leukemic cell lines using as references DNR and melphalan. The incorporation of AD32 into LDL or emulsion resulted in complexes with poor cytotoxicity. WB4291-LDL and WB4291-emulsion exerted, on the other hand, promising cytotoxic effects towards parental and resistant K562 and HL60 cell lines. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:136 / 144
页数:9
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