The role of the anticancer drug vinorelbine in lipid bilayers using differential scanning calorimetry and molecular modeling

被引：22
|
作者：
Koukoulitsa, C.
Kyrikou, I.
Demetzos, C.
Mavromoustakos, T.
机构：
[1] Inst Organ & Pharmaceut Chem, Athens 11635, Greece
[2] Univ Athens, Sch Pharm, Dept Pharmaceut Technol, GR-15771 Athens, Greece
来源：
CHEMISTRY AND PHYSICS OF LIPIDS | 2006年 / 144卷 / 01期
关键词：
cholesterol; docking; DPPC; DSC; interdigitation; vinorelbine;
D O I：
10.1016/j.chemphyslip.2006.07.002
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Differential scanning calorimetry (DSC) has been employed to investigate the thermal changes caused by the anticancer alkaloid drug vinorelbine in dipalmytoylphosphatidylcholine (DPPC) bilayers. The total enthalpy change was increased by the presence of the drug molecule, indicating a partial interdigitation of the lipid alkyl chains. The presence of cholesterol in DPPC bilayers including vinorelbine induced an obstruction of the interdigitation, since cholesterol interrupts the upraise of enthalpy change. Vinorelbine's interdigitation ability and stabilizing properties with the active site of the receptor have been compared with those of similar in structure amphipathic and bulky alkaloid vinblastine. The obtained results may in part explain their similar mechanism of action but different bioactivity. (c) 2006 Elsevier Ireland Ltd. All rights reserved.
引用
收藏
页码：85 / 95
页数：11
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