A natural product that lowers cholesterol as an antagonist ligand for FXR.

@article{Urizar2002ANP,
  title={A natural product that lowers cholesterol as an antagonist ligand for FXR.},
  author={Nancy L Urizar and Amy D B Liverman and D T Dodds and Frank Valentin Silva and Peter Ordentlich and Yingzhuo Yan and Frank J. Gonzalez and Richard A. Heyman and David J Mangelsdorf and David D. Moore},
  journal={Science},
  year={2002},
  volume={296 5573},
  pages={1703-6}
}
Extracts of the resin of the guggul tree (Commiphora mukul) lower LDL (low-density lipoprotein) cholesterol levels in humans. The plant sterol guggulsterone [4,17(20)-pregnadiene-3,16-dione] is the active agent in this extract. We show that guggulsterone is a highly efficacious antagonist of the farnesoid X receptor (FXR), a nuclear hormone receptor that is activated by bile acids. Guggulsterone treatment decreases hepatic cholesterol in wild-type mice fed a high-cholesterol diet but is not… CONTINUE READING
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