title: Pterosin Sesquiterpenoids from Pteris cretica as Hypolipidemic Agents via Activating Liver X Receptors.
abstract: Four new pterosin sesquiterpenoids (1-4), a new ent-kaurane diterpenoid (17), and 18 known compounds were isolated from the aerial parts of Pteris cretica L. The structures of the isolates were elucidated based on spectroscopic data analysis, and their absolute configurations were determined by comparison of experimental and calculated electronic circular dichroism spectra. The compounds were evaluated for lipid-lowering effects in 3T3-L1 adipocytes. Compounds 4, 8, 17, and 22 were more potent than the positive control, berberine, in decreasing triglycerides activity, with compound 4 exerting the most potent activity. Compound 4 activated LXRα/β in a HEK 293T cell-based reporter gene assay. Molecular dynamic simulations revealed that compound 4 activates liver X receptors (LXRs) through hydrogen bonding with the residues of LXRα/β, suggesting that compound 4 reduces total triglycerides through the regulation of LXRα/β.
authors.affiliation: Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou 510006, People's Republic of China.
authors.forename: Xiangkun
authors.initials: X
authors.lastname: Luo
authors.affiliation: Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou 510006, People's Republic of China.
authors.forename: Chanjuan
authors.initials: C
authors.lastname: Li
authors.affiliation: Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou 510006, People's Republic of China.
authors.forename: Pan
authors.initials: P
authors.lastname: Luo
authors.affiliation: Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou 510006, People's Republic of China.
authors.forename: Xin
authors.initials: X
authors.lastname: Lin
authors.affiliation: Bioactive Botanical Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island , Kingston, Rhode Island 02881, United States.
authors.forename: Hang
authors.initials: H
authors.lastname: Ma
authors.affiliation: Bioactive Botanical Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island , Kingston, Rhode Island 02881, United States.
authors.forename: Navindra P
authors.initials: NP
authors.lastname: Seeram
authors.affiliation: School of Chemistry and Biological Engineering, University of Science and Technology Beijing , Beijing 100083, People's Republic of China.
authors.forename: Ching
authors.initials: C
authors.lastname: Song
authors.affiliation: Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou 510006, People's Republic of China.
authors.forename: Jun
authors.identifier: http://orcid.org/0000-0002-1075-0337
authors.initials: J
authors.lastname: Xu
authors.affiliation: Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou 510006, People's Republic of China.
authors.forename: Qiong
authors.identifier: http://orcid.org/0000-0001-6011-3697
authors.initials: Q
authors.lastname: Gu
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry; D045786:Diterpenes, Kaurane / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D000960:Hypolipidemic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D007189:Indans / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D000071518:Liver X Receptors / Q000187:drug effects*; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D035261:Plant Components, Aerial / Q000737:chemistry*; D032495:Pteris / Q000737:chemistry*; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D045786:Diterpenes, Kaurane; D004365:Drugs, Chinese Herbal; D000960:Hypolipidemic Agents; D007189:Indans; D000071518:Liver X Receptors; D012717:Sesquiterpenes; C010772:pterosin