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Brominated polyunsaturated lipids from the Chinese sponge Xestospongia testudinaria as a new class of pancreatic lipase inhibitors

文献类型：期刊论文

作者Liang, Lin-Fu1,2; Wang, Ting1; Cai, You-Sheng1,3,4; He, Wen-Fei1; Sun, Peng1; Li, Yu-Fen1; Huang, Qi1; Taglialatela-Scafati, Orazio5; Wang, He-Yao1; Guo, Yue-Wei1
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2014-05-22
卷号79页码:290-297
关键词Brominated polyunsaturated lipids Marine sponge Xestospongia testudinaria Pancreatic lipase inhibitory activity SAR
ISSN号0223-5234
DOI10.1016/j.ejmech.2014.04.003
文献子类Article
英文摘要Chemical analysis of the Chinese marine sponge Xestospongia testudinaria afforded a library of brominated polyunsaturated lipids including eight new compounds, named xestonarienes A-H (3-10) and thirteen known analogues (11-23). The structures of the new compounds were elucidated by detailed spectroscopic analysis and by comparison with literature data. The isolated lipids were evaluated for their inhibitory activity against pancreatic lipase (PL), an essential enzyme for efficient fat digestion and the major metabolite, 14, exhibited a marked inhibitory activity (IC50 = 3.11 mu M), similar to that of the positive control Orlistat (IC50 = 0.78 mu M). The preliminary structure activity relationships on the series of compounds clearly evidenced that a terminal (E)-enyne functionality, a diyne within the chain, and methyl ester group are all key functional groups for the activity of this class of PL inhibitors. Further biological investigation on compound 14 revealed a significant decrease in the plasma triglyceride level following an oral lipid challenge in C57BLKS/J male mice. Acute toxicology study demonstrated that compound 14 was non-toxic up to 1600 mg/kg p.o in mice. This is the first report of the PL inhibitory activity for brominated polyunsaturated lipids and the obtained results qualify compound 14 as a potent and bioavailable drug candidate for a mild and safe treatment to prevent and reduce obesity. (c) 2014 Elsevier Masson SAS. All rights reserved.
WOS关键词MARINE SPONGE ; ACETYLENIC ACIDS ; IN-VITRO ; ANTIOBESITY ; OBESITY ; CONSTITUENTS ; METABOLITES ; ESTERASE ; ORLISTAT ; EXTRACTS
资助项目Natural Science Foundation of China[81273430] ; Natural Science Foundation of China[41306130] ; National Marine '863' Project[2011AA09070102] ; National Marine '863' Project[2013AA092902] ; China Posdoc Foundation[2012M520956] ; SKLDR/SIMM Project[SIMM1203ZZ-03]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000336700600030
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/277069]  
专题药理学第三研究室
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
天然药物化学研究室
通讯作者Taglialatela-Scafati, Orazio
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
2.Cent South Univ Forestry & Technol, Coll Mat Sci & Engn, Changsha 410004, Hunan, Peoples R China;
3.Wuhan Univ, Sch Pharmaceut Sci, Minist Educ, Key Lab Combinatorial Biosynth & Drug Discov, Wuhan 430071, Peoples R China;
4.Wuhan Univ, Sch Pharmaceut Sci, Inst TCM & Nat Prod, Wuhan 430071, Peoples R China;
5.Univ Naples Federico II, Dipartimento Farm, I-80131 Naples, Italy
推荐引用方式
GB/T 7714		 Liang, Lin-Fu,Wang, Ting,Cai, You-Sheng,et al. Brominated polyunsaturated lipids from the Chinese sponge Xestospongia testudinaria as a new class of pancreatic lipase inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,79:290-297.
APA Liang, Lin-Fu.,Wang, Ting.,Cai, You-Sheng.,He, Wen-Fei.,Sun, Peng.,...&Guo, Yue-Wei.(2014).Brominated polyunsaturated lipids from the Chinese sponge Xestospongia testudinaria as a new class of pancreatic lipase inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,79,290-297.
MLA Liang, Lin-Fu,et al."Brominated polyunsaturated lipids from the Chinese sponge Xestospongia testudinaria as a new class of pancreatic lipase inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 79(2014):290-297.

入库方式： OAI收割

来源：上海药物研究所

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