海参鞘素衍生物对胶质母细胞瘤模型的体外抗肿瘤活性

Antitumor Activity of Fascaplysin Derivatives on Glioblastoma Model In Vitro.

作者信息

Lyakhova I A, Bryukhovetsky I S, Kudryavtsev I V, Khotimchenko Yu S, Zhidkov M E, Kantemirov A V

机构信息

Biomedicine School, Far-Eastern Federal University, Vladivostok, Russia.

A. V. Zhirmunsky Institute of Marine Biology, Far-Eastern Division of the Russian Academy of Sciences, Vladivostok, Russia.

出版信息

Bull Exp Biol Med. 2018 Mar;164(5):666-672. doi: 10.1007/s10517-018-4055-4. Epub 2018 Mar 26.

DOI:10.1007/s10517-018-4055-4

PMID:29577186

Abstract

Antitumor efficiency of fascaplysin synthetic derivatives (7-phenylfascaplysin, 3-chlorofascaplysin, 3-bromofascaplysin, and 10-bromofascaplysin) was compared out in vitro on C6 glioma cells. The cytotoxic efficiency of all tested compounds was higher than that of unsubstituted fascaplysin; 3-bromofascaplysin and 7-phenylfascaplysin exhibited the best capacity to kill glioma C6 cells. Apoptosis was the main mechanism of glioma cell death. The cytotoxic activity of these compounds increased with prolongation of exposure to the substance and increase of its concentration. Fascaplysin derivatives modified all phases of glioma cell vital cycle. The count of viable tumor cell in G0 phase remained minimum by the end of experiment under the effects of 3-bromofascaplysin and 7-phenylfascaplysin.

摘要

在体外对C6胶质瘤细胞比较了法卡普利辛合成衍生物（7-苯基法卡普利辛、3-氯法卡普利辛、3-溴法卡普利辛和10-溴法卡普利辛）的抗肿瘤效率。所有测试化合物的细胞毒性效率均高于未取代的法卡普利辛；3-溴法卡普利辛和7-苯基法卡普利辛表现出杀死胶质瘤C6细胞的最佳能力。凋亡是胶质瘤细胞死亡的主要机制。这些化合物的细胞毒性活性随着接触该物质时间的延长及其浓度的增加而增强。法卡普利辛衍生物改变了胶质瘤细胞生命周期的所有阶段。在3-溴法卡普利辛和7-苯基法卡普利辛的作用下，实验结束时G0期活肿瘤细胞数量保持最低。