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类异戊二烯磷脂共轭物作为潜在治疗剂:合成、表征及抗增殖研究。

Isoprenoid-phospholipid conjugates as potential therapeutic agents: Synthesis, characterization and antiproliferative studies.

作者信息

Gliszczyńska Anna, Niezgoda Natalia, Gładkowski Witold, Świtalska Marta, Wietrzyk Joanna

机构信息

Department of Chemistry, Wrocław University of Environmental and Life Sciences, Wrocław, Poland.

Ludwik Hirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Department of Experimental Oncology, Wrocław, Poland.

出版信息

PLoS One. 2017 Feb 14;12(2):e0172238. doi: 10.1371/journal.pone.0172238. eCollection 2017.

Abstract

The aim of this research was to extend application field of isoprenoid compounds by their introduction into phospholipid structure as the transport vehicle. The series of novel isoprenoid phospholipids were synthesized in high yields (24-97%), their structures were fully characterized and its anticancer activity was investigated in vitro towards several cell lines of different origin. Most of synthesized compounds showed a significantly higher antiproliferative effect on tested cell lines than free terpene acids. The most active phosphatidylcholine analogue, containing 2,3-dihydro-3-vinylfarnesoic acids instead of fatty acids in both sn-1 and sn-2 position, inhibits the proliferation of colon cancer cells at 13.6 μM.

摘要

本研究的目的是通过将类异戊二烯化合物引入磷脂结构作为运输载体来扩展其应用领域。一系列新型类异戊二烯磷脂以高产率(24 - 97%)合成,其结构得到充分表征,并在体外对几种不同来源的细胞系研究了其抗癌活性。大多数合成化合物对测试细胞系显示出比游离萜酸显著更高的抗增殖作用。最具活性的磷脂酰胆碱类似物,在sn-1和sn-2位均含有2,3-二氢-3-乙烯基法呢酸而非脂肪酸,在13.6 μM时抑制结肠癌细胞的增殖。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4bd/5308787/48ef9edf6750/pone.0172238.g001.jpg

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