DAT-230, a Novel Microtubule Inhibitor, Induced Aberrant Mitosis and Apoptosis in SGC-7901 Cells
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- Qiao Foxiao
- Department of Pharmacology, Shenyang Pharmaceutical University
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- Zuo Daiying
- Department of Pharmacology, Shenyang Pharmaceutical University
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- Wang Haifeng
- Department of Pharmacology, Shenyang Pharmaceutical University
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- Li Zengqiang
- Department of Pharmacology, Shenyang Pharmaceutical University
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- Qi Huan
- Department of Pharmacology, Shenyang Pharmaceutical University
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- Zhang Weige
- Key Laboratory of Structure-Based Drug Design & Discovery belong to Ministry of Education, Shenyang Pharmaceutical University
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- Wu Yingliang
- Department of Pharmacology, Shenyang Pharmaceutical University
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抄録
2-Methoxy-5-(2-(3,4,5-trimethoxyphenyl)thiophen-3-yl) aniline (DAT-230) is a novel synthesized compound of combretastatin-A-4 derivative with more stability. The present study is to investigate its anti-tumor activity and molecular mechanisms in human gastric adenocarcinoma SGC-7901 cells. DAT-230 inhibited SGC-7901 cells growth. The treatment of DAT-230 resulted in microtubule de-polymerization and G2/M phase arrest. Besides the accumulation and translocation of Cyclin B1, reduction of p-14/15-cdc2 and mitosis delay denoted the Cyclin B1-cdc2 complex active and M phase arrest in SGC-7901 cells treated with DAT-230. Mitochondria pathway participated in apoptosis after G2/M arrest in SGC-7901 cells treated with DAT-230, which was characterized by DNA fragmentation, cleavage of poly(ADP-ribose) polymerase (PARP), activation of caspase-3 and caspase-9, changes of Bcl-2 and Bax expression, decrease of mitochondrial membrane potential and release of cytochrome c from mitochondria. In vivo, DAT-230 delayed tumor growth in BALB/c nude mice with human gastric adenocarcinoma xenografts. Besides apoptosis was detected with terminal deoxynucleotidyl transferase mediated deoxyuridine triphosphate nick-end labeling (TUNEL) assay in tumor tissue. In conclusion, DAT-230 is a promising microtubule inhibitor with great anti-tumor activity to SGC-7901, in vitro and in vivo. Its potential to be a candidate of anti-cancer agent is worth of being further investigated.
収録刊行物
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- Biological & Pharmaceutical Bulletin
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Biological & Pharmaceutical Bulletin 36 (2), 193-201, 2013
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204633365248
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- NII論文ID
- 130003361365
- 40019558376
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- NII書誌ID
- AA10885497
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- COI
- 1:STN:280:DC%2BC3szksVGisw%3D%3D
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- ISSN
- 13475215
- 09186158
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- NDL書誌ID
- 024219921
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- PubMed
- 23370351
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 使用不可