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安格敏能够有效地靶向哺乳动物以及细菌的 I 型和 II 型拓扑异构酶。

Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases.

机构信息

Dipartimento Farmaco Chimico Tecnologico, University of Cagliari, Cagliari, Italy.

出版信息

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7041-4. doi: 10.1016/j.bmcl.2011.09.097. Epub 2011 Oct 1.

DOI:10.1016/j.bmcl.2011.09.097
PMID:22014547
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4551395/
Abstract

From the methanol extract of the bulbs of Pancratium illyricum L., three phenanthridine type alkaloids, ungeremine (1), (-)-lycorine (2) and (+)-vittatine (3) were isolated. For the evaluation of their anticancer and antibacterial potential, compounds 1-3 were tested against human (I, IIα) and bacterial (IA, IV) topoisomerases. Our data demonstrated that ungeremine impairs the activity of both, human and bacterial topoisomerases. Remarkably, ungeremine was found to largely increments the DNA cleavage promoted by bacterial topoisomerase IA, a new target in antimicrobial chemotherapy.

摘要

从伊犁郁金香鳞茎的甲醇提取物中分离得到三种菲啶型生物碱

格尔明碱（1）、(-)-石蒜碱（2）和(+)-维替丁碱（3）。为了评估它们的抗癌和抗菌潜力，对化合物 1-3 进行了人（I、IIα）和细菌（IA、IV）拓扑异构酶的测试。我们的数据表明格尔明碱会损害人和细菌拓扑异构酶的活性。值得注意的是，格尔明碱被发现能大大增加细菌拓扑异构酶 IA 促进的 DNA 断裂，这是抗菌化疗的一个新靶点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d7d/4551395/2e3c38d21d05/nihms436173f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d7d/4551395/5292ad837f00/nihms436173f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d7d/4551395/8f4cae24d1ae/nihms436173f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d7d/4551395/915cde07b13f/nihms436173f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d7d/4551395/2e3c38d21d05/nihms436173f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d7d/4551395/5292ad837f00/nihms436173f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d7d/4551395/8f4cae24d1ae/nihms436173f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d7d/4551395/915cde07b13f/nihms436173f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d7d/4551395/2e3c38d21d05/nihms436173f4.jpg

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