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trans-guggulsterone
- Development stage
- Unknown
- Modality
- Small Molecules
- Administration
- Oral, Topical
01
Overview
trans-Guggulsterone (also known as E-guggulsterone) is a naturally occurring phytosteroid and stereoisomer of guggulsterone, isolated from the oleo-gum resin of the guggul tree (*Commiphora mukul* or *Commiphora wightii*). It acts as an antagonist of the farnesoid X receptor (FXR) and has been investigated for its potential hypolipidemic, anti-inflammatory, and anticancer properties. Unlike its cis-isomer (Z-guggulsterone), which primarily inhibits the IKK/NF-κB pathway, trans-guggulsterone has been shown to inhibit the MAPK/AP-1 signaling pathway, leading to the downregulation of matrix metalloproteinase-9 (MMP-9) expression and the suppression of cancer cell invasion, particularly in breast cancer models. It is widely used as a research reagent and is also found as a component of guggul-based dietary supplements.
- Other names
- (E)-guggulsteroneE-guggulsteroneguggulsterone Etrans-guggulsterone
02
Targets
PXR (Pregnane X receptor)PR (Progesterone receptor)FXR (Farnesoid x-activated receptor)ESR1 (ERα)GR (Glucocorticoid receptor)AR (Adrenergic receptors)MR (Mineralocorticoid receptor)
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