Guggulsterones Fig 5205

The molecular basis for the lipid-lowering action of guggulsterones has been suggested to be an antagonism of the farnesoid X receptor, a member of the nuclear receptor super family of ligand-activated transcription factors. Guggulsterones activate the estrogen receptor, progesterone receptor, and pregnane X receptor with EC50 values in low micromolar range. Guggulsterone-mediated activation of pregnane X receptor induces the expression of CYP3A genes both in rodent and human hepatocytes. Pregnane X receptor activation is known to cause herb-drug interactions and it has been suggested that guggulipid therapy should be used cautiously in patients taking prescription medications that are metabolized by the CYP3A family members.

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