title: Paeoniflorin acts as a liver X receptor agonist.
abstract: Paeoniflorin is one of the active ingredients of Paeonia lactiflora Pall., a novel traditional herbal medicine exerting pharmacological effects including antihyperlipidemic, neuroprotective, and anti-hepatofibrosis effects. Liver X receptor (LXR) acts as a ligand-activated transcription factor to exhibit antihyperlipidemic and neuroprotective effects. In this study, the activity of paeoniflorin against LXR was evaluated by the mammalian one-hybrid and transient transfection reporter assays. The results showed that paeoniflorin transactivated GAL4, rat cholesterol 7 α-hydroxylase, phospholipid transfer protein, and ATP-binding cassette A1 gene promoters in dose-dependent manner. Furthermore, the docking study demonstrated that paeoniflorin resided in the LXR ligand-binding pocket in the similar manner as GSK 3987, a novel LXR agonist. These results indicated that paeoniflorin might exert pharmacological effects through LXR pathway.
authors.affiliation: Department of Chemistry, College of Science, National Kaohsiung Normal University, Taiwan. t3136@nknucc.nknu.edu.tw
authors.forename: Hsiang-Ru
authors.initials: HR
authors.lastname: Lin
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000187:drug effects / Q000378:metabolism; D000818:Animals; D001189:Aryl Hydrocarbon Hydroxylases / Q000378:metabolism; D001565:Benzoates / Q000737:chemistry / Q000494:pharmacology*; D001952:Bridged-Ring Compounds / Q000737:chemistry / Q000494:pharmacology*; D002790:Cholesterol 7-alpha-Hydroxylase / Q000378:metabolism; D005960:Glucosides / Q000737:chemistry / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D008099:Liver / Q000187:drug effects; D000071518:Liver X Receptors; D008156:Luciferases / Q000378:metabolism; D015394:Molecular Structure; D039821:Monoterpenes; D057093:Orphan Nuclear Receptors / Q000819:agonists*; D029596:Paeonia / Q000737:chemistry; D051381:Rats; D013250:Steroid Hydroxylases / Q000378:metabolism; D014157:Transcription Factors / Q000378:metabolism; D006027:Glycosides
chemical_list: D018528:ATP-Binding Cassette Transporters; D001189:Aryl Hydrocarbon Hydroxylases; D001565:Benzoates; D001952:Bridged-Ring Compounds; D002790:Cholesterol 7-alpha-Hydroxylase; D005960:Glucosides; D000071518:Liver X Receptors; D008156:Luciferases; D039821:Monoterpenes; D057093:Orphan Nuclear Receptors; D013250:Steroid Hydroxylases; D014157:Transcription Factors; C015423:peoniflorin; D006027:Glycosides; C029009:steroid hormone 7-alpha-hydroxylase; C553219:CYP7A1 protein, human