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游离型和脂质体型烷基磷胆碱的体外抗肿瘤活性

Antineoplastic activity in vitro of free and liposomal alkylphosphocholines.

作者信息

Zeisig R, Jungmann S, Arndt D, Schütt A, Nissen E

机构信息

Max Delbrück Center for Molecular Medicine, Berlin-Buch, Germany.

出版信息

Anticancer Drugs. 1993 Feb;4(1):57-64. doi: 10.1097/00001813-199302000-00008.

DOI:10.1097/00001813-199302000-00008
PMID:8457716
Abstract

We investigated the liposome forming properties of three homologues of alkylphosphocholines: hexadecylphosphocholine (HPC), octadecylphosphocholine (OPC) and eicosanylphosphocholine (EPC). In the presence of cholesterol and dicetylphosphate, alkylphosphocholines form liposomes with slow permeability for entrapped carboxyfluorescein. We studied the direct cytotoxicity of alkylphosphocholine vesicles and their ability to attack MethA sarcoma cells, human skin and muscle fibroblasts (M22, GUS, Moscow), and human mouth epidermoid carcinoma cells (KB, ATCC, CCL 17). All alkylphosphocholines show cytotoxic activity against the investigated cells, the degree of which depends on the number of carbon atoms in the alkyl chain, concentration and incubation time. Whereas the etherlipid liposomes are less toxic to MethA cells than the free compounds, the liposomal alkylphosphocholines are more toxic toward KB and M22 cells than the corresponding free lipids.

摘要

我们研究了三种烷基磷胆碱同系物的脂质体形成特性

十六烷基磷胆碱(HPC)、十八烷基磷胆碱(OPC)和二十烷基磷胆碱(EPC)。在胆固醇和十六烷基磷酸存在的情况下,烷基磷胆碱形成对包封的羧基荧光素具有缓慢渗透性的脂质体。我们研究了烷基磷胆碱囊泡的直接细胞毒性及其攻击MethA肉瘤细胞、人皮肤和肌肉成纤维细胞(M22、GUS、莫斯科)以及人口腔表皮样癌细胞(KB、ATCC、CCL 17)的能力。所有烷基磷胆碱对所研究的细胞均表现出细胞毒性活性,其程度取决于烷基链中的碳原子数、浓度和孵育时间。虽然醚脂质体对MethA细胞的毒性低于游离化合物,但脂质体烷基磷胆碱对KB和M22细胞的毒性高于相应的游离脂质。

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Antineoplastic activity in vitro of free and liposomal alkylphosphocholines.游离型和脂质体型烷基磷胆碱的体外抗肿瘤活性
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引用本文的文献

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Testing the hypothesis that amphiphilic antineoplastic lipid analogues act through reduction of membrane curvature elastic stress.验证两亲性抗肿瘤脂质类似物通过降低膜曲率弹性应力发挥作用这一假说。
J R Soc Interface. 2008 Nov 6;5(28):1371-86. doi: 10.1098/rsif.2008.0041.
2
Influence of hexadecylphosphocholine on the release of tumor necrosis factor and nitroxide from peritoneal macrophages in vitro.十六烷基磷胆碱对体外培养的腹膜巨噬细胞释放肿瘤坏死因子和氮氧化物的影响。
J Cancer Res Clin Oncol. 1995;121(2):69-75. doi: 10.1007/BF01202215.
3
Antineoplastic activity of alkylphosphocholines (APC) in human breast carcinomas in vivo and in vitro; use of liposomes.
Breast Cancer Res Treat. 1994;32(3):269-79. doi: 10.1007/BF00666004.
4
Alkylphosphocholine-induced production of nitric oxide and tumor necrosis factor alpha by U 937 cells.烷基磷胆碱诱导U 937细胞产生一氧化氮和肿瘤坏死因子α 。
J Cancer Res Clin Oncol. 1995;121(6):350-6. doi: 10.1007/BF01225687.