A novel sulfonamide agent, MPSP-001, exhibits potent activity against human cancer cells in vitro through disruption of microtubule

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	A novel sulfonamide agent, MPSP-001, exhibits potent activity against human cancer cells in vitro through disruption of microtubule
其他题名	A novel sulfonamide agent, MPSP-001, exhibits potent activity against human cancer cells in vitro through disruption of microtubule
	Liu Zulong 1; Tian Wei 2; Wang Yong 1; Kuang Shan 1; Luo Xiaomin 1; Yu Qiang 1
	2012
发表期刊	ACTA PHARMACOLOGICA SINICA
ISSN	1671-4083
卷号	33 期号:2 页码:261-270
摘要	Aim: To evaluate the anti-cancer effects of a new sulfonamide derivative, 2-(N-(3-chlorophenyl)-4-methoxyphenylsulfonamido)-N-hydroxypropanamide (MPSP-001).
其他摘要	Aim: To evaluate the anti-cancer effects of a new sulfonamide derivative, 2-(N-(3-chlorophenyl)-4-methoxyphenylsulfonamido)-N-hydroxypropanamide (MPSP-001). Methods: Human cancer cell lines (HepG2, THP-1, K562, HGC-27, SKOV3, PANC-1, SW480, Kba, HeLa, A549, MDA-MB-453, and MCF-7) were examined. The cytotoxicity of MPSP-001 was evaluated using the WST-8 assay. Cell cycle distribution was examined with flow cytometry. Mitotic spindle formation was detected using immunofluorescence microscopy. Apoptosis-related proteins were examined with Western blot using specific phosphorylated protein antibodies. Competitive tubulin-binding assay was performed to test whether the compound competitively bound to the colchicine site. Molecular docking was performed to explore the possible binding conformation. Results: MPSP-001 potently inhibited the growth of the 12 different types of human cancer cells with the IC 50 values ranging from 1.9 to 15.7μmol 2 in vitro , and directly bound to the colchicine-site of β-tubulin. Molecular docking predicted that the compound may form two hydrogen bonds to the binding pocket. The compound showed synergistic effects with colchicine and taxol in blocking mitosis of HeLa cells. Conclusion: MPSP-001 shows a broad-spectrum of anti-tumor efficacy in vitro and represents a novel structure with anti-microtubule activity.
关键词	PHASE-I ANTITUMOR-ACTIVITY ANTICANCER AGENT BINDING APOPTOSIS E7070 COLCHICINE DISCOVERY HMN-214 CAMPTOTHECIN MPSP-001 sulfonamide anticancer drug microtubules tubulin mitotic spindle drug resistance drug synergism
收录类别	CSCD
语种	英语
资助项目	[National Natural Science Foundation of China] ; [Shanghai Science and Technology Research] ; [China Ministry of Science and Technology] ; [National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program", China]
CSCD记录号	CSCD:4437497
引用统计	被引频次：1[CSCD] [CSCD记录]
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/144913
专题	中国科学院金属研究所
作者单位	1.中国科学院 2.中国科学院金属研究所
推荐引用方式 GB/T 7714	Liu Zulong,Tian Wei,Wang Yong,et al. A novel sulfonamide agent, MPSP-001, exhibits potent activity against human cancer cells in vitro through disruption of microtubule[J]. ACTA PHARMACOLOGICA SINICA,2012,33(2):261-270.
APA	Liu Zulong,Tian Wei,Wang Yong,Kuang Shan,Luo Xiaomin,&Yu Qiang.(2012).A novel sulfonamide agent, MPSP-001, exhibits potent activity against human cancer cells in vitro through disruption of microtubule.ACTA PHARMACOLOGICA SINICA,33(2),261-270.
MLA	Liu Zulong,et al."A novel sulfonamide agent, MPSP-001, exhibits potent activity against human cancer cells in vitro through disruption of microtubule".ACTA PHARMACOLOGICA SINICA 33.2(2012):261-270.