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Synthesis and Evaluation of Pancreatic Lipase Inhibitory Effects Halogenated Polyunsaturated Lipids from Marine Natural Products: Methyl Xestospongoate and Analogs
Author(s) -
Gong JingXu,
He WenFei,
Liu HaiLi,
Jiang ChengShi,
Wang Ting,
Wang HeYao,
Guo YueWei
Publication year - 2016
Publication title -
helvetica chimica acta
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.74
H-Index - 82
eISSN - 1522-2675
pISSN - 0018-019X
DOI - 10.1002/hlca.201500229
Subject(s) - chemistry , pancreatic lipase , lipase , inhibitory postsynaptic potential , bioassay , in vitro , polyunsaturated fatty acid , biochemistry , stereochemistry , biological activity , enzyme , fatty acid , genetics , neuroscience , biology
Methyl xestospongoate (MXS), a brominated polyunsaturalted lipid recently isolated from the Chinese marine sponge Xestospongia testudinaria , showed strong in vitro pancreatic lipase (PL) inhibitory activity. Inspired by its promising activity and potential clinical application, a series of shorter or longer‐chain and chlorinated analogs of MXS was prepared and evaluated for PL inhibitory activity. The result of a bioassay indicated that the terminal brominated ones are better than the chlorinated ones on their bioactivity, and 16–20 C‐atoms in the structures of MXS analogs might be optimal for their PL inhibitory activity. The results obtained in the present work are useful for the design of novel pancreatic lipase inhibitors.