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Steroidal and triterpenoidal fungal metabolites as ligands of liver X receptors.

Publication ,  Journal Article
Ondeyka, JG; Jayasuriya, H; Herath, KB; Guan, Z; Schulman, M; Collado, J; Dombrowski, AW; Kwon, SS; McCallum, C; Sharma, N; MacNaul, K ...
Published in: J Antibiot (Tokyo)
September 2005
Published version (DOI) Link to item

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.

Duke Scholars

Ziqiang Guan
Author Ziqiang Guan Biochemistry
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Published In

J Antibiot (Tokyo)

DOI

10.1038/ja.2005.76

ISSN

0021-8820

Publication Date

September 2005

Volume

58

Issue

9

Start / End Page

559 / 565

Location

England

Related Subject Headings

  • Triterpenes
  • Steroids
  • Receptors, Cytoplasmic and Nuclear
  • Orphan Nuclear Receptors
  • Microbiology
  • Medicinal & Biomolecular Chemistry
  • Liver X Receptors
  • Liver
  • Ligands
  • Inhibitory Concentration 50
 

Citation

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Ondeyka, J. G., Jayasuriya, H., Herath, K. B., Guan, Z., Schulman, M., Collado, J., … Singh, S. B. (2005). Steroidal and triterpenoidal fungal metabolites as ligands of liver X receptors. J Antibiot (Tokyo), 58(9), 559–565. https://doi.org/10.1038/ja.2005.76
Ondeyka, John G., Hiranthi Jayasuriya, Kithsiri B. Herath, Ziqiang Guan, Marvin Schulman, Javier Collado, Anne W. Dombrowski, et al. “Steroidal and triterpenoidal fungal metabolites as ligands of liver X receptors.” J Antibiot (Tokyo) 58, no. 9 (September 2005): 559–65. https://doi.org/10.1038/ja.2005.76.
Ondeyka JG, Jayasuriya H, Herath KB, Guan Z, Schulman M, Collado J, et al. Steroidal and triterpenoidal fungal metabolites as ligands of liver X receptors. J Antibiot (Tokyo). 2005 Sep;58(9):559–65.
Ondeyka, John G., et al. “Steroidal and triterpenoidal fungal metabolites as ligands of liver X receptors.” J Antibiot (Tokyo), vol. 58, no. 9, Sept. 2005, pp. 559–65. Pubmed, doi:10.1038/ja.2005.76.
Ondeyka JG, Jayasuriya H, Herath KB, Guan Z, Schulman M, Collado J, Dombrowski AW, Kwon SS, McCallum C, Sharma N, MacNaul K, Hayes N, Menke JG, Singh SB. Steroidal and triterpenoidal fungal metabolites as ligands of liver X receptors. J Antibiot (Tokyo). 2005 Sep;58(9):559–565.

Published In

J Antibiot (Tokyo)

DOI

10.1038/ja.2005.76

ISSN

0021-8820

Publication Date

September 2005

Volume

58

Issue

9

Start / End Page

559 / 565

Location

England

Related Subject Headings

  • Triterpenes
  • Steroids
  • Receptors, Cytoplasmic and Nuclear
  • Orphan Nuclear Receptors
  • Microbiology
  • Medicinal & Biomolecular Chemistry
  • Liver X Receptors
  • Liver
  • Ligands
  • Inhibitory Concentration 50