Aphadilactones A-D, Four Diterpenoid Dimers with DGAT Inhibitory and Antimalarial Activities from a Meliaceae Plant

doi:10.1021/jo402340h

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	Aphadilactones A-D, Four Diterpenoid Dimers with DGAT Inhibitory and Antimalarial Activities from a Meliaceae Plant
	Liu, Jia2 ; He, Xiu-Feng 2; Wang, Gai-Hong 2; Merino, Emilio F.3,4; Yang, Sheng-Ping 2; Zhu, Rong-Xiu 1; Gan, Li-She 6; Zhang, Hua 2; Cassera, Maria B.3,4; Wang, He-Yao2
刊名	JOURNAL OF ORGANIC CHEMISTRY
	2014-01-17
卷号	79 期号:2 页码:599-607
ISSN号	0022-3263
DOI	10.1021/jo402340h
文献子类	Article
英文摘要	Aphadilactones A D (1-4), four diaster. eoisomers possessing an unprecedented carbon skeleton, were isolated from the Meliaceae plant Aphanamixis grandifolia. Their challenging structures and absolute configurations were determined by a combination of spectroscopic data, chemical degradation, fragment synthesis, experimental CD spectra, and ECD calculations. Aphadilactone C (3) with the 5S,11S,5'S,11'S configuration showed potent and selective inhibition against the diacylglycerol O-acyltransferase-1 (DGAT-1) enzyme (IC50 = 0.46 +/- 0.09 mu M, selectivity index >217) and is the strongest natural DGAT-1 inhibitor discovered to date. In addition, compounds 1-4 showed significant antimalarial activities with IC50 values of 190 +/- 60, 1350 +/- 150, 170 +/- 10, and 120 +/- 50 nM, respectively.
资助项目	National Natural Science Foundation of China[81021062] ; National Natural Science Foundation of China[20902095] ; Foundation from the Ministry of Science and Technology of the People's Republic of China[2012CB721105] ; Jeffress Memorial Trust of Virginia[J-1058] ; Virginia Commonwealth Health Research Board[208-03-12]
WOS关键词	DIACYLGLYCEROL ACYLTRANSFERASE ; APHANAMIXIS-GRANDIFOLIA ; TRIACYLGLYCEROL BIOSYNTHESIS ; CHEMICAL-CONSTITUENTS ; STEM BARKS ; OBESITY ; POTENT ; AGENTS ; TRITERPENOIDS ; DERIVATIVES
WOS研究方向	Chemistry
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000330099000013
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277225]
专题	天然药物化学研究室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上海药物代谢研究中心
通讯作者	Yue, Jian-Min
作者单位	1.Shandong Univ, Sch Chem & Chem Engn, Jinan 250100, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Virginia Polytech Inst & State Univ, Dept Biochem, Blacksburg, VA 24061 USA; 4.Virginia Polytech Inst & State Univ, Virginia Tech Ctr Drug Discovery, Blacksburg, VA 24061 USA; 5.Virginia Polytech Inst & State Univ, Dept Chem, Blacksburg, VA 24061 USA; 6.Zhejiang Univ, Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China
推荐引用方式 GB/T 7714	Liu, Jia,He, Xiu-Feng,Wang, Gai-Hong,et al. Aphadilactones A-D, Four Diterpenoid Dimers with DGAT Inhibitory and Antimalarial Activities from a Meliaceae Plant[J]. JOURNAL OF ORGANIC CHEMISTRY,2014,79(2):599-607.
APA	Liu, Jia.,He, Xiu-Feng.,Wang, Gai-Hong.,Merino, Emilio F..,Yang, Sheng-Ping.,...&Yue, Jian-Min.(2014).Aphadilactones A-D, Four Diterpenoid Dimers with DGAT Inhibitory and Antimalarial Activities from a Meliaceae Plant.JOURNAL OF ORGANIC CHEMISTRY,79(2),599-607.
MLA	Liu, Jia,et al."Aphadilactones A-D, Four Diterpenoid Dimers with DGAT Inhibitory and Antimalarial Activities from a Meliaceae Plant".JOURNAL OF ORGANIC CHEMISTRY 79.2(2014):599-607.