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	A fast screening model for drug permeability assessment based on native small intestinal extracellular matrix
	Li, Na1,2; Sui, Zhigang3; Liu, Yong4; Wang, Dandan1; Ge, Guangbo1; Yang, Ling1
刊名	Rsc advances
	2018
卷号	8期号:60页码:34514-34524
ISSN号	2046-2069
DOI	10.1039/c8ra05992f
通讯作者	Ge, guangbo(geguangbo@shutcm.edu.cn) ; Yang, ling(yling@dicp.ac.cn)
英文摘要	The caco-2 cell monolayer model is widely utilized to predict drug permeability across human intestinal epithelial cells. however, at least 21 days is required for the formation and maturation of a well-tight caco-2 cell monolayer, thereby restricting the throughput of the screening model during drug discovery. to address this challenge, a fast (7 days), and more physiologically relevant screening model integrating both the caco-2 cell model and a small intestinal submucosa (sis) hydrogel was developed in this study. the 7 day model exhibited desirable phenotype and functional similarity to the conventional 21 day caco-2 model with respect to paracellular resistance, alkaline phosphatase (alp) activities, and the mrna expression level of three transporters (pept1, oatp1a2, and p-gp) as well as their mediated influx or efflux. besides, the increased gene expression of two excretive transporters (bcrp, mrp2) and their enhanced functionality were observed in the current fast model compared to the traditional 21 day model. more importantly, a strong correlation (r(2) = 0.9458) was obtained between the absorptive p app values of 19 model compounds in the 7 day model and those in the conventional 21 day model. these results revealed the pivotal role of the native extracellular matrix (sis) in facilitating the differentiation of caco-2 cells, leading to the reconstruction of the accelerated 7 day model, which presents a promising tool for screening drug permeability in future drug discovery.
WOS关键词	CELL-ECM INTERACTIONS ; IN-VITRO ; CACO-2 CELL ; EPITHELIAL-CELLS ; GROWTH-FACTOR ; STEM-CELLS ; DIFFERENTIATION ; EXPRESSION ; SUBMUCOSA ; TRANSPORT
WOS研究方向	Chemistry
WOS类目	Chemistry, Multidisciplinary
语种	英语
出版者	ROYAL SOC CHEMISTRY
WOS记录号	WOS:000448423500039
内容类型	期刊论文
URI标识	http://www.corc.org.cn/handle/1471x/2373127
专题	大连化学物理研究所
通讯作者	Ge, Guangbo; Yang, Ling
作者单位	1.Shanghai Univ Tradit Chinese Med, Inst Interdisciplinary Integrat Med Res, Shanghai 201203, Peoples R China 2.Univ South Dakota, Dept Biomed Engn, Sioux Falls, SD 57107 USA 3.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China 4.Dalian Univ Technol, Sch Life Sci & Med, Panjin 124221, Peoples R China
推荐引用方式 GB/T 7714	Li, Na,Sui, Zhigang,Liu, Yong,et al. A fast screening model for drug permeability assessment based on native small intestinal extracellular matrix[J]. Rsc advances,2018,8(60):34514-34524.
APA	Li, Na,Sui, Zhigang,Liu, Yong,Wang, Dandan,Ge, Guangbo,&Yang, Ling.(2018).A fast screening model for drug permeability assessment based on native small intestinal extracellular matrix.Rsc advances,8(60),34514-34524.
MLA	Li, Na,et al."A fast screening model for drug permeability assessment based on native small intestinal extracellular matrix".Rsc advances 8.60(2018):34514-34524.

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