Cytotoxic Activity of Lysophosphatidylcholine Analogues on Human Lymphoma Raji Cells
作者:
E.A. M. Fleer,
D.-J. Kim,
G.A. Nagel,
H. Eibl,
C. Unger,
期刊:
Onkologie
(Karger Available online 1990)
卷期:
Volume 13,
issue 4
页码: 295-300
ISSN:0378-584X
年代: 1990
DOI:10.1159/000216779
出版商: S. Karger GmbH
关键词: Etherlipid analogues;Cytotoxicity;Raji cells;Alkylphosphocholines;Growth inhibition
数据来源: Karger
摘要:
The cytotoxic activity of 21 lysophosphocholine analogues was tested on human lymphoma Raji cells. Structure-activity investigations revealed a more than 50-fold difference in the cytotoxicity between the different compounds. Whereas acyllysophosphocholines showed only borderline effects, the most pronounced toxic activity was observed with compounds which have an etherbond in the sn-1 position and a hydrogen, a methoxy or a methoxymethylgroup in position sn-2. Elongation of the phosphorous-nitrogen distance in the choline group markedly reduced the cytotoxicity of the compounds. From the results obtained it was concluded that a long chain fatty alcohol adjacent to a phosphocholine headgroup represents the minimal requirement for antineoplastic activity. Thus, a new group of antineoplastic compounds, the alkylphosphocholines, was developed in our laboratory, with in vitro cytotoxic activities just as effective as the most toxic alkyllysophosphocholines.
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