Details der Publikation - Synthesis, Spectral Characterization, and In Vitro Cellular Activities of Metapristone, a Potential Cancer Metastatic Chemopreventive Agent Derived from Mifepristone (RU486)

Synthesis, Spectral Characterization, and In Vitro Cellular Activities of Metapristone, a Potential Cancer Metastatic Chemopreventive Agent Derived from Mifepristone (RU486)

Abstract Mifepristone (RU486) is marketed and used widely by women as an abortifacient, and experimentally for psychotic depression and anticancer treatments. After administration, metapristone is found to be the most predominant metabolite of mifepristone. We hypothesized that adhesion of circulating tumor cells (CTCs) to vascular endothelial bed is a crucial starting point in metastatic cascade, and that metapristone can serve as a cancer metastatic chemopreventive agent that can interrupt adhesion and invasion of CTCs to the intima of microvasculature. In the present study, we modified the synthesis procedure to produce grams of metapristone, fully characterized its spectral properties and in vitro cellular activities, including its cytostatic effects, cell cycle arrest, mitochondrial membrane potential, and apoptosis on human colorectal cancer HT-29 cells. Metapristone concentration dependently interrupted adhesion of HT-29 cells to endothelial cells. Metapristone may potentially be a useful agent to interrupt metastatic initiation..

Medienart:	E-Artikel

Erscheinungsjahr:	2014
Erschienen:	2014

Enthalten in:	Zur Gesamtaufnahme - volume:16
Enthalten in:	The AAPS journal - 16(2014), 2 vom: 18. Jan., Seite 289-298

Sprache:	Englisch

Beteiligte Personen:	Wang, Jichuang [VerfasserIn] Chen, Jianzhong [VerfasserIn] Wan, Liyuan [VerfasserIn] Shao, Jingwei [VerfasserIn] Lu, Yusheng [VerfasserIn] Zhu, Yewei [VerfasserIn] Ou, Minrui [VerfasserIn] Yu, Suhong [VerfasserIn] Chen, Haijun [VerfasserIn] Jia, Lee [VerfasserIn]

Links:	Volltext [lizenzpflichtig]

BKL:	44.40$jPharmazie$jPharmazeutika

Anmerkungen:	© American Association of Pharmaceutical Scientists 2014

doi:	10.1208/s12248-013-9559-2

funding:
Förderinstitution / Projekttitel:

PPN (Katalog-ID):	OLC2101952084

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520			\|a Abstract Mifepristone (RU486) is marketed and used widely by women as an abortifacient, and experimentally for psychotic depression and anticancer treatments. After administration, metapristone is found to be the most predominant metabolite of mifepristone. We hypothesized that adhesion of circulating tumor cells (CTCs) to vascular endothelial bed is a crucial starting point in metastatic cascade, and that metapristone can serve as a cancer metastatic chemopreventive agent that can interrupt adhesion and invasion of CTCs to the intima of microvasculature. In the present study, we modified the synthesis procedure to produce grams of metapristone, fully characterized its spectral properties and in vitro cellular activities, including its cytostatic effects, cell cycle arrest, mitochondrial membrane potential, and apoptosis on human colorectal cancer HT-29 cells. Metapristone concentration dependently interrupted adhesion of HT-29 cells to endothelial cells. Metapristone may potentially be a useful agent to interrupt metastatic initiation.
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700	1		\|a Ou, Minrui \|4 aut
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700	1		\|a Jia, Lee \|4 aut
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Synthesis, Spectral Characterization, and In Vitro Cellular Activities of Metapristone, a Potential Cancer Metastatic Chemopreventive Agent Derived from Mifepristone (RU486)

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