Description
Guggulsterone-(Z) (39025-23-5) is a natural steroid fromCommiphora mukulextract (guggulipid) which lowers cholesterol and acts as an FXR antagonist.1Attenuates astrocyte-mediated neuroinflammation.2 Induces differentiation of pluripotent stem cells to dopaminergic neurons.3 Produces antidepressant-like effects via activation of the BDNF signaling pathway in mouse models.4
Uses
Z-Guggulsterone acts as an α-glucosidase inhibitor also known as a hypolipidemic agent.
Uses
(Z)-Guggulsterone acts as an α-glucosidase inhibitor also known as a hypolipidemic agent.
Definition
ChEBI: Guggulsterone is a 3-hydroxy steroid. It has a role as an androgen.
Biological Activity
Broad spectrum steroid receptor ligand; mineralocorticoid, progesterone and glucocorticoid receptor antagonist (K i values are 37, 224 and 252 nM respectively) and weak androgen receptor agonist (K i = 315 nM). Induces apoptosis in prostate cancer cells and inhibits angiogenesis via suppression of the VEGF-VEGFR2-Akt signalling pathway. Exhibits antilipidemic activity via antagonism of the farnesoid X receptor (FXR) and displays antiseptic, antirheumatic and anti-inflammatory activity in vivo . More active isomer of Guggulsterone (Pregna-4,17(20)-diene-3,16-dione ).
Biochem/physiol Actions
(Z)-Guggulsterone is a natural product that lowers cholesterol due to its function as an antagonist ligand for the bile acid receptor. (Z)-Guggulsterone is a nuclear hormone receptor that regulates the transcription of several genes involved in cholesterol metabolism and plays a role in cholesterol level regulation. (Z)-Guggulsterone is also a selective farnesoid X receptor (FXR) modulator.
References
[1] NANCY L. URIZAR. A Natural Product That Lowers Cholesterol As an Antagonist Ligand for FXR[J]. Science, 2002, 296 5573. DOI:
10.1126/science.1072891[2] TIANLONG LIU. Z-Guggulsterone attenuates astrocytes-mediated neuroinflammation after ischemia by inhibiting toll-like receptor 4 pathway[J]. Journal of Neurochemistry, 2018, 147 6: 803-815. DOI:
10.1111/jnc.14583[3] ANDREW AGBAY. Guggulsterone-releasing microspheres direct the differentiation of human induced pluripotent stem cells into neural phenotypes.[J]. Biomedical materials (Bristol, England), 2018, 13 3: 034104. DOI:
10.1088/1748-605x/aaaa77[4] FENG-GUO LIU. Z-Guggulsterone Produces Antidepressant-Like Effects in Mice through Activation of the BDNF Signaling Pathway.[J]. International Journal of Neuropsychopharmacology, 2017, 20 6: 485-497. DOI:
10.1093/ijnp/pyx009
