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《Natural modulators of liver X receptors.》.pdf

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《Natural modulators of liver X receptors.》.pdf

JournalHomepage: www.jcimjourna1.corn/jim www.elsevier.com /locate/issn Availablealsoonlineatwww.sciencedirect.com. Copyright@2014.JournalofIntegrativeMedicineEditorialoffice. E.editionpublishedby曰sevier(Singapore)PteLtd.Allrightsrese~ed NaturalmodulatorsofliverX receptors ChengHuang SchoolofPharmacy,ShanghaiUniversityofTraditionalChineseMedicine,Shanghai201203,China ABSTRACT:Nuclearreceptortranscriptionfactorsare ligand-activatedproteinsthatcontroI variousbiologicaleventsfrOm cellgrowth anddevelopmentto lipidmetaboIIsm,and energy andglucosehomeostasis.Nuclearreceptorsareimpo~antdrugtargetsformetabolicdiseases. LiverX receptors(LXRs)arenuclearreceptortranscriptionfactorsthatplayessentiaIrolesin regulationofcholesterol,triglyceride,fattyacid,and glucosehomeostasis.LXR-deficientmice haveshowntheassociationofLXR.signalingpathwaydysfunctionwithseveralhumanpathologies includingatherOsclerOsis,hyperlipidemia,AIzheimersdiseaseandcancer.Thus,LXRsare promisingpharmacologicaltargetsforthesediseases.SyntheticLXR agonistsmaylowercholesterol, butincreasetriglycerideandinducefattyliver.ThenaturallyoccurringLXR ligands,withmoderate activity,mayserveasnutraceuticalsforpreventionortreatmentofthedisorders,whilem inimIzIng potentiaIsideeffects.Inthisreview.recentadvancesinnaturaILXRmodulatorsare summarized includingagonist.antagonistandthemodulatorofLXR pathway. KEYWORDS:LiverX receptors;agonist;antagonist;atherosclerosis;steatosis;hyperlipidemia: hypercholesterolem ia;hypertriglyceridem ia;nutraceuticaIs:reviews http://dx.doi.org/10.1016/S2095—4964(14)60013-3 HuangC.NaturalmodulatorsofliverXreceptors.JIntegerMed.2014;12(2):76—85. ReceivedJanuary 11,2014:acceptedFebruary24,2014. Correspondence:Prof.ChengHuang;Tel:+86—21E—mail:chuang(shutcm.edu.

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