Suramin is a polyanionic compound currently used under evaluation for antineoplastic activity. One of the main problems encountered during clinical trials was an adverse neurotoxic effect, probably due to a direct cytotoxic effect on neural cells. Suramin is also known to trigger differentiation of human colon cancer cells, yet a chronic treatment induces a lysosomal storage disorder. The aim of this study was to evaluate suramin analogs for their effect: (i) on the lysosomal system of the human colon cancer cell clone HT29-D4; and (ii) on C6 glioma cell growth and morphology. One of the derivatives tested, NF036, induced terminal differentiation of HT29-D4 cells without any impairment of the lysosomal system. Furthermore, in contrast to suramin, NF036 did not alter C6 cell growth and morphology. We conclude that there is a relationship between the ability of a suramin derivative to induce a lysosomal storage disorder in human colon cancer cells and its neurotoxic effect. A double screening of suramin analogs on HT29-D4 and C6 cells allowed us to identify a new candidate antineoplastic drug: NF036.

译文

:Suramin是目前正在评估抗肿瘤活性的聚阴离子化合物。临床试验期间遇到的主要问题之一是不良的神经毒性作用,这可能是由于对神经细胞的直接细胞毒性作用所致。还已知苏拉明会触发人结肠癌细胞的分化,然而长期治疗会引起溶酶体贮积症。这项研究的目的是评估苏拉明类似物的作用:(i)对人结肠癌细胞克隆HT29-D4的溶酶体系统; (ii)C6胶质瘤细胞的生长和形态。测试的衍生物之一NF036诱导了HT29-D4细胞的终末分化,而对溶酶体系统没有任何损害。此外,与苏拉明相反,NF036不会改变C6细胞的生长和形态。我们得出结论,苏拉明衍生物在人结肠癌细胞中诱导溶酶体贮积病的能力与其神经毒性作用之间存在关联。在HT29-D4和C6细胞上对苏拉明类似物的双重筛选使我们能够鉴定出新的候选抗肿瘤药NF036。

+1
+2
100研值 100研值 ¥99课程
检索文献一次
下载文献一次

去下载>

成功解锁2个技能,为你点赞

《SCI写作十大必备语法》
解决你的SCI语法难题!

技能熟练度+1

视频课《玩转文献检索》
让你成为检索达人!

恭喜完成新手挑战

手机微信扫一扫,添加好友领取

免费领《Endnote文献管理工具+教程》

微信扫码, 免费领取

手机登录

获取验证码
登录