Cinnamomum verum ingredient 2-methoxycinnamaldehyde: a new antiproliferative drug targeting topoisomerase I and II in human lung squamous cell carcinoma NCI-H520 cells
Cinnamomum verum ingredient 2-methoxycinnamaldehyde: a new antiproliferative drug targeting topoisomerase I and II in human lung squamous cell carcinoma NCI-H520 cells
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肉桂成分2-甲氧基肉桂醛：一种靶向人肺鳞状细胞癌NCI-H520细胞拓扑异构酶I和II的新型抗增殖药物
DOI：
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发表时间：
2017
影响因子：
2.4
通讯作者：
J. Cherng
中科院分区：
文献类型：
--
作者：
Yi;Kuen;Shu;Ho;Ta;J. Cherng;J. Cherng
肉桂已被用作中草药。我们研究了2-甲氧基肉桂醛（2-MCA）的抗增殖作用，该植物的皮质的成分，和与人肺鳞状细胞癌NCI-H520细胞中的肿瘤发生相关的分子生物标志物。本研究观察了2-MCA对人肺鳞癌NCI-H520细胞生长、细胞毒性、凋亡及拓扑异构酶I和II活性的影响。结果表明，2-MCA可通过线粒体膜电位（m）降低、caspase 3和caspase 9的激活以及细胞凋亡的形态学特征抑制细胞增殖并诱导细胞凋亡。此外，2-MCA还诱导溶酶体空泡化，增加酸性区室体积和细胞毒性，并抑制拓扑异构酶I和II活性。另外的研究显示了2-MCA在裸鼠模型中的抗增殖作用。总之，我们的数据表明，2-MCA在体外的抗增殖活性涉及下调细胞生长标志物，拓扑异构酶I和II，和上调促凋亡分子，与增加溶酶体空泡化。在体内，2-MCA减小了肿瘤大小，这可能具有显著的临床影响。我们的数据表明，2-MCA可能是一个潜在的化学预防剂，以及抗癌治疗。
Cinnamomum verum has been used as a Chinese herbal medication. We investigated the antiproliferative effect of 2-methoxycinnamaldehyde (2-MCA), a constituent of the cortex of the plant, and the molecular biomarkers associated with tumorigenesis in human lung squamous cell carcinoma NCI-H520 cells. The effects of 2-MCA on cell growth, cytotoxicity, apoptosis, and topoisomerase I and II activities in human lung squamous cell carcinoma NCI-H520 cells were evaluated in vitro and in vivo. The results showed that 2-MCA inhibited proliferation and induced apoptosis as implicated by mitochondrial membrane potential (&Dgr;&PSgr;m) loss, activation of both caspase 3 and caspase 9, as well as morphological characteristics of apoptosis. Furthermore, 2-MCA also induced lysosomal vacuolation with elevated volume of acidic compartment and cytotoxicity, and inhibited topoisomerase I as well as II activities. Additional study showed the antiproliferative effect of 2-MCA in a nude mice model. In short, our data imply that the antiproliferative activity of 2-MCA in vitro involved downregulation of cell growth markers, both topoisomerase I and II, and upregulation of proapoptotic molecules, associated with increased lysosomal vacuolation. In vivo, 2-MCA reduced the tumor size, which could have had a significant clinical impact. Our data imply that 2-MCA may be a potential agent for chemoprevention as well as anticancer therapy.
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癌症化学预防中选定的饮食植物化学物质的表观遗传学调节。
影响因子：
9.7
作者：
Shukla, Samriddhi;Meeran, Syed M.;Katiyar, Santosh K.
通讯作者：
Katiyar, Santosh K.
DOI：
10.2174/1568011054222364
发表时间：
2005-07-01
期刊：
Current Medicinal Chemistry - Anti-Cancer Agents
影响因子：
--
作者：
Baldwin, E. L.;Osheroff, N.
通讯作者：
Osheroff, N.
影响因子：
9.3
作者：
Yuan JM;Sun C;Butler LM
通讯作者：
Butler LM
影响因子：
4.1
作者：
Bandele, Omari J.;Clawson, Sara J.;Osheroff, Neil
通讯作者：
Osheroff, Neil