Dysoxylactam A: A Macrocyclolipopeptide Reverses P-Glycoprotein-Mediated Multidrug Resistance in Cancer Cells

doi:10.1021/jacs.9b02259

	Dysoxylactam A: A Macrocyclolipopeptide Reverses P-Glycoprotein-Mediated Multidrug Resistance in Cancer Cells
	Liu, Cui-Ping 3; Xie, Cheng-Ying 3; Zhao, Jin-Xin 3; Ji, Kai-Long 3; Lei, Xin-Xiang 1; Sun, Han 2; Lou, Li-Guang 3; Yue, Jian-Min 3
刊名	JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
	2019-05-01
卷号	141 期号:17 页码:6812-6816
ISSN号	0002-7863
DOI	10.1021/jacs.9b02259
通讯作者	Sun, Han(HSun@fmp-berlin.de) ; Lou, Li-Guang(lglou@mail.shcnc.ac.cn) ; Yue, Jian-Min(jmyue@simm.ac.cn)
英文摘要	A 17-membered macrocyclolipopeptide, named dysoxylactam A (1) comprising an unprecedented branched C19 fatty acid and an L-valine, was isolated from the plants of Dysoxylum hongkongense. The challenging relative configuration of 1 was established by means of residual dipolar coupling-based NMR analysis. The absolute configuration of 1 was determined by singlecrystal X-ray diffraction on its p-bromobenzoate derivative (2). Compound 1 dramatically reversed multidrug resistance in cancer cells with the fold-reversals ranging from 28.4 to 1039.7 at the noncytotoxic concentration of 10 mu M. The mode-of-action study of 1 revealed that it inhibited the function of P-glycoprotein (P-gp), a key mediator in multidrug resistance.
资助项目	National Natural Science Foundation of the People's Republic of China[21532007] ; Drug Innovation Major Project of China[2018ZX09711001-001-005] ; Biological Resources Programme of Chinese Academy of Sciences[KFJ-BRP-008] ; Sino-German Center for Research Promotion[GZ1289]
WOS研究方向	Chemistry
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000466987900006
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/289886]
专题	中国科学院上海药物研究所
通讯作者	Sun, Han; Lou, Li-Guang; Yue, Jian-Min
作者单位	1.South Cent Univ Nationalities, Sch Pharmaceut Sci, Wuhan 430074, Peoples R China 2.Leibniz Forschungsinst Mol Pharmakol, Sect Struct Biol, D-13125 Berlin, Germany 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Liu, Cui-Ping,Xie, Cheng-Ying,Zhao, Jin-Xin,et al. Dysoxylactam A: A Macrocyclolipopeptide Reverses P-Glycoprotein-Mediated Multidrug Resistance in Cancer Cells[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,2019,141(17):6812-6816.
APA	Liu, Cui-Ping.,Xie, Cheng-Ying.,Zhao, Jin-Xin.,Ji, Kai-Long.,Lei, Xin-Xiang.,...&Yue, Jian-Min.(2019).Dysoxylactam A: A Macrocyclolipopeptide Reverses P-Glycoprotein-Mediated Multidrug Resistance in Cancer Cells.JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,141(17),6812-6816.
MLA	Liu, Cui-Ping,et al."Dysoxylactam A: A Macrocyclolipopeptide Reverses P-Glycoprotein-Mediated Multidrug Resistance in Cancer Cells".JOURNAL OF THE AMERICAN CHEMICAL SOCIETY 141.17(2019):6812-6816.