Pentasaccharide resin glycosides with multidrug resistance reversal activities from the seeds of Pharbitis nil

doi:10.1039/c7ra09026a

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 上海中药现代化研究中心

	Pentasaccharide resin glycosides with multidrug resistance reversal activities from the seeds of Pharbitis nil
	Li, Jun1,2 ; Wang, Wen-Qiong 1,2; Tang, Shuai 1,2; Song, Wei-Bin 1,2; Huang, Min1,2 ; Xuan, Li-Jiang1,2
刊名	RSC ADVANCES
	2017
卷号	7 期号:82 页码:52001-52009
ISSN号	2046-2069
DOI	10.1039/c7ra09026a
文献子类	Article
英文摘要	Resin glycosides are novel P-glycoprotein inhibitors. In order to evaluate their multidrug resistance (MDR) reversal activities, we isolated seven new resin glycosides, pharbitins A-G (1-7) from the seeds of Pharbitis nil. Their chemical structures were determined by extensive application of high resolution 2D NMR techniques, HRESIMS and chemical methods. Compounds 1-4 and 6 were evaluated for their MDR reversal activities in KB/VCR, A549/T and K562/ADR cells. Among them, compound 2 showed moderate MDR reversal activity in KB/VCR cells, and increased the cytotoxicity of vincristine by 2.2-fold when incorporated at 25 mu M. A structure-activity relationship study revealed that substituting Rha '' C-3 with a trans-cinnamoyl group improves the MDR reversal activity. Also, an intracellular Rh123 accumulation assay demonstrated that compound 2 could inhibit the function of P-gp.
资助项目	State Key Laboratory of Drug Research[SIMM1601ZZ-03] ; National Natural Science Foundation of China[81473111] ; China Postdoctoral Science Foundation[2016M600345]
WOS关键词	CELLS
WOS研究方向	Chemistry
语种	英语
出版者	ROYAL SOC CHEMISTRY
WOS记录号	WOS:000415116800033
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275695]
专题	上海中药现代化研究中心中科院受体结构与功能重点实验室新药研究国家重点实验室所领导
通讯作者	Xuan, Li-Jiang
作者单位	1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Meteria Med, 501 Haike Rd, Shanghai 201201, Peoples R China; 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
推荐引用方式 GB/T 7714	Li, Jun,Wang, Wen-Qiong,Tang, Shuai,et al. Pentasaccharide resin glycosides with multidrug resistance reversal activities from the seeds of Pharbitis nil[J]. RSC ADVANCES,2017,7(82):52001-52009.
APA	Li, Jun,Wang, Wen-Qiong,Tang, Shuai,Song, Wei-Bin,Huang, Min,&Xuan, Li-Jiang.(2017).Pentasaccharide resin glycosides with multidrug resistance reversal activities from the seeds of Pharbitis nil.RSC ADVANCES,7(82),52001-52009.
MLA	Li, Jun,et al."Pentasaccharide resin glycosides with multidrug resistance reversal activities from the seeds of Pharbitis nil".RSC ADVANCES 7.82(2017):52001-52009.