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Isolation and characterization of methyl esters and derivatives from Euphorbia kansui (Euphorbiaceae) and their inhibitory effects on the human SGC-7901 cells.大戟科大戟属甘遂中甲酯及其衍生物的分离、表征及其对人SGC - 7901细胞的抑制作用。
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Inhibition of cellular proliferation by diterpenes, topoisomerase II inhibitor.二萜类化合物(拓扑异构酶II抑制剂)对细胞增殖的抑制作用
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Ingenol derivatives inhibit proliferation and induce apoptosis in breast cancer cell lines.
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Inhibition of DNA decatenation, but not DNA damage, arrests cells at metaphase.抑制DNA解连环作用而非DNA损伤,会使细胞停滞在中期。
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Identification of decatenation G2 checkpoint impairment independently of DNA damage G2 checkpoint in human lung cancer cell lines.在人肺癌细胞系中鉴定与DNA损伤G2检查点无关的解连环G2检查点损伤。
Cancer Res. 2004 Jul 15;64(14):4826-32. doi: 10.1158/0008-5472.CAN-04-0871.
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Selective inhibition of the growth of cancer cells by diterpenes selected with embryonic cells of Xenopus.
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Ethanolic extracts of Euphorbia and other ethnobotanical species as inhibitors of human tumour cell growth.
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The human decatenation checkpoint.人类解连环检查点。
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9
Ingenol esters induce apoptosis in Jurkat cells through an AP-1 and NF-kappaB independent pathway.大戟醇酯通过一条独立于AP-1和核因子κB的途径诱导Jurkat细胞凋亡。
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依尼醇 EZ 对拓扑异构酶 IIalpha 的抑制作用及其对癌细胞增殖的影响分析。

Analysis of inhibition of topoisomerase IIalpha and cancer cell proliferation by ingenolEZ.

机构信息

Department of Chemistry, College of Humanities and Sciences, Nihon University, Tokyo, Japan.

出版信息

Cancer Sci. 2010 Feb;101(2):374-8. doi: 10.1111/j.1349-7006.2009.01408.x.

DOI:10.1111/j.1349-7006.2009.01408.x
PMID:20175785
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11158357/
Abstract

We previously reported that many ingenol compounds derived from Euphorbia kansui exhibit topoisomerase inhibitory activity and/or inhibitory activity of cell proliferation. The inhibitory effects of 20-O-(2'E,4'Z-decadienoyl) ingenol and 3-O-(2'E,4'Z-decadienoyl)-ingenol among these compounds on topoisomerase II activity and on the cell proliferative activity and arrest phase of the cell cycle were studied using a mouse breast cancer (MMT) cell line. Although 20-O-ingenolEZ exerted inhibitory effects on both topoisomerase II activity and cell proliferative activity, 3-O-ingenolEZ exerted inhibitory activity on neither. The 20-O-ingenolEZ-induced cell arrest of MMT-cell proliferation led to a cell cycle arrest in the G2/M phase. Topoisomerase II inhibition can be divided into the poison and catalytic inhibitor types. A checkpoint mechanism is activated when cells are treated with these topoisomerase II inhibitors. Poison-type inhibition occurs via induction of the DNA damage checkpoint and the catalytic-type inhibition occurs via induction of the DNA-decatenation checkpoint, suggestive of distinct checkpoint reactions. 20-O-ingenolEZ inhibited topoisomerase IIalpha activity through inhibition of ATPase, and induced DNA-decatenation checkpoint without signaling for phosphorylation of H2AX.

摘要

我们之前报道过,许多来源于大戟属植物甘遂的 ingenol 类化合物具有拓扑异构酶抑制活性和/或细胞增殖抑制活性。本研究选用小鼠乳腺癌(MMT)细胞系,研究了这些化合物中的 20-O-(2'E,4'Z-癸二烯酰基) ingenol 和 3-O-(2'E,4'Z-癸二烯酰基)-ingenol 对拓扑异构酶 II 活性、细胞增殖活性和细胞周期停滞期的抑制作用。虽然 20-O-ingenolEZ 对拓扑异构酶 II 活性和细胞增殖活性均具有抑制作用,但 3-O-ingenolEZ 则没有。20-O-ingenolEZ 诱导 MMT 细胞增殖停滞导致细胞周期停滞在 G2/M 期。拓扑异构酶 II 抑制剂可分为毒剂型和催化抑制剂型。当细胞用这些拓扑异构酶 II 抑制剂处理时,会激活检验点机制。毒剂型抑制通过诱导 DNA 损伤检验点发生,而催化型抑制则通过诱导 DNA 解链检验点发生,提示存在不同的检验点反应。20-O-ingenolEZ 通过抑制 ATPase 抑制拓扑异构酶 IIalpha 活性,并诱导 DNA 解链检验点发生,而不引发 H2AX 的磷酸化信号。