Damage of Egg Phosphatidylcholine Liposomes by DNA-Binding Cytotoxic Agents
Damage of Egg Phosphatidylcholine Liposomes by DNA-Binding Cytotoxic Agents
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DNA 结合细胞毒剂对卵磷脂酰胆碱脂质体的损伤
DOI：
10.1246/bcsj.64.1364
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发表时间：
1991
期刊：
影响因子：
--
通讯作者：
J. Sunamoto
中科院分区：
文献类型：
--
作者：
C. O'Connor;W. Denny;D. Emery;H. Tank;Toshinori Sato;J. Sunamoto
在四种 DNA 嵌入药物（吖啶、蒽、苯基喹啉和苯基苯并咪唑的甲酰胺）存在下，研究了由鸡蛋磷脂酰胆碱形成的小单层囊泡 (SUV) 的稳定性。囊泡膜的物理化学稳定性随着总药物浓度的增加而变化，在所研究的四种药物中，苯基喹啉甲酰胺最具破坏性。脂质体双层中胆固醇的存在增加了对除蒽甲酰胺之外的药物引起的物理化学损伤的抵抗力。在所有情况下，用多糖涂覆脂质体使脂质体表面更加疏水，并导致细胞毒性剂导致囊泡破裂。细胞毒性的 9-苯胺基吖啶衍生物安吖啶和 9-[2-甲氧基-4-(甲基磺酰氨基)苯胺基]-5-甲基吖啶-4-N-甲基甲酰胺 (CI-921) 太难溶，无法封装在脂质体的水性核心内，但 CI-921 的中性形式被嵌入......
The stability of small unilamellar vesicles (SUV) formed by egg phosphatidylcholine has been examined in the presence of four DNA-intercalating drugs—carboxamides of acridine, anthracene, phenylquinoline, and phenylbenzimidazole. The physicochemical stability of the vesicle-membrane changed as the total drug concentration increased and, of the four drugs investigated, the phenylquinolinecarboxamide was the most destructive. The presence of cholesterol in the liposomal bilayer increased resistance to physicochemically induced damage by the drugs except the anthracenecarboxamide. In all cases, coating the liposomes with a polysaccharide made the liposomal surface more hydrophobic and led to the vesicle rupture by the cytotoxic agents. The cytotoxic 9-anilinoacridine derivatives, amsacrine and 9-[2-methoxy-4-(methylsulfonylamino)anilino]-5-methylacridine-4-N-methylcarboxamide (CI-921), were too insoluble to be encapsulated within the aqueous core of liposomes, but the neutral form of CI-921 was intercalated ...