Anticancer properties of lamellarins.

Anticancer properties of lamellarins.
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DOI:
10.3390/md13031105
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发表时间:
2015-02-19
期刊:
影响因子:
5.4
通讯作者:
Bailly C
Bailly C
中科院分区:
医学2区
文献类型:
--
作者:
Bailly C

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1985年,第一个片螺蛋白从一种小型海洋蜗牛中分离出来。今天,已经有超过50种片螺素被列入清单,许多衍生物被合成并作为抗病毒或抗癌剂进行测试。该家族中的先导化合物是片螺素D,其特征在于作为核和线粒体拓扑异构酶I的有效抑制剂,但也能够直接干扰线粒体以引发癌细胞死亡。在这里讨论了片螺素的药理学和化学,并详细介绍了片螺素D的机理。片螺素经常作为抗癌化合物设计的起点。大量的工作致力于创造新的结构以及改进合成方法,导致片螺素和相关的吡咯衍生的海洋生物碱。
In 1985 the first lamellarins were isolated from a small oceanic sea snail. Today, more than 50 lamellarins have been inventoried and numerous derivatives synthesized and tested as antiviral or anticancer agents. The lead compound in the family is lamellarin D, characterized as a potent inhibitor of both nuclear and mitochondrial topoisomerase I but also capable of directly interfering with mitochondria to trigger cancer cell death. The pharmacology and chemistry of lamellarins are discussed here and the mechanistic portrait of lamellarin D is detailed. Lamellarins frequently serve as a starting point in the design of anticancer compounds. Extensive efforts have been devoted to create novel structures as well as to improve synthetic methods, leading to lamellarins and related pyrrole-derived marine alkaloids.
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