2. Academic Validation
  3. Pterosin Sesquiterpenoids from Pteris cretica as Hypolipidemic Agents via Activating Liver X Receptors

Pterosin Sesquiterpenoids from Pteris cretica as Hypolipidemic Agents via Activating Liver X Receptors

  • J Nat Prod. 2016 Dec 23;79(12):3014-3021. doi: 10.1021/acs.jnatprod.6b00558.
Xiangkun Luo 1,  Chanjuan Li 1,  Pan Luo 1,  Xin Lin 1,  Hang Ma 2,  Navindra P Seeram 2,  Ching Song 3,  Jun Xu 1,  Qiong Gu 1
Affiliations

Affiliations

  • 1 Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou 510006, People's Republic of China.
  • 2 Bioactive Botanical Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island , Kingston, Rhode Island 02881, United States.
  • 3 School of Chemistry and Biological Engineering, University of Science and Technology Beijing , Beijing 100083, People's Republic of China.
PMID: 28006909 DOI: 10.1021/acs.jnatprod.6b00558
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.

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