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Author Lin, Hsiang-Ru
Source World Health Organization (WHO)-Global Index Medicus
Content type Text
Publisher Taylor & Francis
File Format HTM / HTML
Language English
Difficulty Level Medium
Subject Domain (in DDC) Natural sciences & mathematics ♦ Chemistry & allied sciences ♦ Life sciences; biology ♦ Physiology & related subjects ♦ Biochemistry ♦ Natural history of organisms ♦ Technology ♦ Medicine & health ♦ Human physiology ♦ Pharmacology and therapeutics ♦ Diseases ♦ Manufacture for specific uses ♦ Precision instruments & other devices
Subject Domain (in MeSH) Eukaryota ♦ Organisms ♦ Organic Chemicals ♦ Enzymes and Coenzymes ♦ Amino Acids, Peptides, and Proteins ♦ Chemicals and Drugs ♦ Investigative Techniques ♦ Analytical, Diagnostic and Therapeutic Techniques and Equipment ♦ Chemical Phenomena ♦ Biological Sciences
Subject Keyword Discipline Chemistry ♦ Discipline Pharmacology ♦ Hepatophyta ♦ Chemistry ♦ Receptors, Cytoplasmic And Nuclear ♦ Agonists ♦ Sesquiterpenes ♦ Isolation & Purification ♦ Pharmacology ♦ Animals ♦ Cholesterol 7-alpha-hydroxylase ♦ Metabolism ♦ Humans ♦ Molecular Structure ♦ Phospholipid Transfer Proteins ♦ Genetics ♦ Promoter Regions, Genetic ♦ Transfection ♦ Journal Article
Abstract Lepidozenolide is a sesquiterpenoid isolated from the liverwort Lepidozia fauriana and its possible bioactivity is unclear. The farnesoid X receptor (FXR) is a member of nuclear receptor superfamily that has been widely targeted for developing treatments for chronic liver disease and hyperglycemia. In this study, whether lepidozenolide may act as a FXR agonist was determined. Indeed, in mammalian one-hybrid and transient transfection reporter assays, lepidozenolide transactivated FXR to modulate promoter action including GAL4, CYP7A1, and PLTP promoters in a dose-dependent manner, while it exhibited slightly less agonistic activity than chenodeoxycholic acid, an endogenous FXR agonist. Through the molecular modeling docking studies lepidozenolide was shown to bind to FXR ligand binding pocket fairly well. All these results indicate that lepidozenolide acts as a FXR agonist.
Description Country affiliation: Taiwan
Author Affiliation: Lin HR ( a Department of Chemistry , College of Science, National Kaohsiung Normal University , Kaohsiung 82446 , Taiwan.)
ISSN 10286020
Educational Role Student ♦ Teacher
Age Range above 22 year
Educational Use Reading ♦ Research ♦ Self Learning
Interactivity Type Expositive
Education Level UG and PG
Learning Resource Type Article
Publisher Date 2015-01-01
Publisher Place Great Britain (UK)
e-ISSN 14772213
Journal Journal of Asian Natural Products Research
Volume Number 17
Issue Number 2

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Source: WHO-Global Index Medicus