Steroidal and Triterpenoidal Fungal Metabolites as Ligands of Liver X Receptors
| Autor: | Hiranthi Jayasuriya, Anne W. Dombrowski, Ziqiang Guan, John G. Ondeyka, Marvin D. Schulman, Sheo B. Singh, John G. Menke, Christine McCallum, Kithsiri Herath, Soojin S Kwon, Karen L. MacNaul, Javier Collado, Nancy S. Hayes, Neelam Sharma |
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| Rok vydání: | 2005 |
| Předmět: |
Agonist
Ergostane medicine.drug_class Receptors Cytoplasmic and Nuclear Pharmacology Biology Ligands digestive system Inhibitory Concentration 50 chemistry.chemical_compound Drug Discovery Coactivator polycyclic compounds medicine Liver X receptor IC50 Liver X Receptors Cholesterol Ligand binding assay Fungi Orphan Nuclear Receptors Triterpenes DNA-Binding Proteins Liver chemistry Biochemistry Steroids lipids (amino acids peptides and proteins) Efflux |
| Zdroj: | The Journal of Antibiotics. 58:559-565 |
| ISSN: | 1881-1469 0021-8820 |
| Popis: | Cholesterol homeostasis is tightly controlled process that involves a variety of regulators including liver X receptors (LXR). Agonists of LXR are expected to increase cholesterol efflux, lower LDL, and raise HDL levels. Screening of a natural product library of microbial extracts using a LXR-scintillation proximity assay (SPA) binding assay and bioassay-guided fractionation of a number of fungal extracts led to the isolation of five ergostane and a cycloartane derivative. These compounds exhibited IC50 value ranging 0.5 approximately 9 microM in the binding assay for a-receptor and a number of these showed in vitro agonist activity in the coactivator association assays but lacked the cell based LXR activation. The isolation and LXR activity of these compounds are described. |
| Databáze: | OpenAIRE |
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