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基于天然5,9-二十碳二烯酸的新型铜配合物的合成：有效的拓扑异构酶I抑制剂及对顺铂耐药细胞系的细胞毒素

Synthesis of New Cu Complex Based on Natural 5,9-Eicosadienoic Acid: Effective Topoisomerase I Inhibitor and Cytotoxin against the Cisplatin-Resistant Cell Line.

作者信息

Dzhemileva Lilya U, D'yakonov Vladimir A, Dil'mukhametova Leisan K, Dzhemilev Usein M

机构信息

Institute of Petrochemistry and Catalysis of RAS (IPC RAS), Prospect Octyabrya, 141, 450075 Ufa, Russian Federation.

出版信息

ACS Omega. 2019 Oct 11;4(17):17581-17587. doi: 10.1021/acsomega.9b02756. eCollection 2019 Oct 22.

DOI:10.1021/acsomega.9b02756
PMID:31656933
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6812112/
Abstract

The complex (bipy)Cu(5,9-eicd) was prepared by the reaction of Cu(OAc) with 5,9-eicosadienoic acid and 2,2'-bipyridine in methanol. The new copper complex showed high antitumor activity in vitro toward A2780cis, A2780, Hek293, K562, HL60, Jurkat, and U937 cell lines and efficiently inhibited human topoisomerase I. Using flow cytofluorometry, (bipy)Cu(5,9-eicd) was studied for the effect on the cell cycle and apoptosis-inducing activity in tumor cells.

摘要

通过在甲醇中使醋酸铜与5,9-二十碳二烯酸和2,2'-联吡啶反应制备了配合物(bipy)Cu(5,9-eicd)。这种新型铜配合物在体外对A2780cis、A2780、Hek293、K562、HL60、Jurkat和U937细胞系表现出高抗肿瘤活性，并能有效抑制人拓扑异构酶I。使用流式细胞荧光术研究了(bipy)Cu(5,9-eicd)对肿瘤细胞的细胞周期和凋亡诱导活性的影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/4b7ddedc85f3/ao9b02756_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/9cc6f3b752ca/ao9b02756_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/03ef33dbcbeb/ao9b02756_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/db1e9642a5c8/ao9b02756_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/32b6dd5b6f66/ao9b02756_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/2fbeef7da3d4/ao9b02756_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/4b7ddedc85f3/ao9b02756_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/9cc6f3b752ca/ao9b02756_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/03ef33dbcbeb/ao9b02756_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/db1e9642a5c8/ao9b02756_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/32b6dd5b6f66/ao9b02756_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/2fbeef7da3d4/ao9b02756_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/74c4/6812112/4b7ddedc85f3/ao9b02756_0006.jpg

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