Z-Guggulsterone - CAS 39025-23-5
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Z-Guggulsterone is a broad spectrum steroid receptor ligand that acts as a mineralocorticoid, progesterone and glucocorticoid receptor antagonist (Ki = 37, 224 and 252 nM, respectively) and weak androgen receptor agonist (Ki = 315 nM). Z-Guggulsterone is also a selective antagonist of farnesoid X receptor (FXR) exhibiting antilipidemic, antiseptic, antirheumatic and anti-inflammatory activity in vivo.
Brife Description:
steroid receptor ligand, FXR antagonist
≥98% by HPLC
Off-White Solid
Melting Point:
>191°C (dec.)
Canonical SMILES:
1.Effects of bile acids and the bile acid receptor FXR agonist on the respiratory rhythm in the in vitro brainstem medulla slice of neonatal Sprague-Dawley rats.
Zhao C1, Wang X1, Cong Y2, Deng Y1, Xu Y3, Chen A1, Yin Y3. PLoS One. 2014 Nov 18;9(11):e112212. doi: 10.1371/journal.pone.0112212. eCollection 2014.
Intrahepatic cholestasis of pregnancy is always accompanied by adverse fetal outcomes such as malfunctions of respiration. Farnesoid X receptor (FXR) plays a critical role in the homeostasis of bile acids. Thus, we are determined to explore the effects of farnesoid X receptor (FXR) and five bile acids on respiratory rhythm generation and modulation of neonatal rats. Spontaneous periodic respiratory-related rhythmical discharge activity (RRDA) was recorded from hypoglossal nerves during the perfusion of modified Krebs solution. Group 1-6 was each given GW4064 and five bile acids of chenodeoxycholic acid (CDCA), deoxycholic acid (DCA), lithocholic acid (LCA), cholic acid (CA) as well as ursodeoxycholic acid (UDCA) at different concentrations to identify their specific functions on respiratory rhythm modulations. Group 7 was applied to receive FXR blocker Z-guggulsterone and Z-guggulsterone with the above bile acids separately to explore the role of FXR in the respiratory rhythm modulation.
2.The appetite regulatory effect of guggulsterones in rats: a repertoire of plasma hormones and neurotransmitters.
Mithila MV1, Khanum F. J Diet Suppl. 2014 Sep;11(3):262-71. doi: 10.3109/19390211.2014.937045. Epub 2014 Jul 15.
Guggulsterone or guggulipid is a steroidal constituent present in the neutral fraction of gum resin of Commiphora mukul, commonly known as guggul. The traditional uses of guggul-resin extract are well documented in the Ayurveda-where it is prescribed to treat a variety of ailments including lipid-related disorders such as obesity and arteriosclerosis. The hypolipidemic activity of the extracts known since ancient times can be traced to the two closely related steroidal ketones, E-guggulsterone and Z-guggulsterone. In this study, we have investigated the dose dependent (100, 200, 400 mg/kg body weight) effect of guggulsterones on appetite regulating hormones [ghrelin, leptin, cholecystokinin (CCK)] and neurotransmitters (serotonin and dopamine), which play a major role in the energy homeostasis and thus influence obesity related factors. We have also studied its effect on food intake, body weight and plasma triglycerides and glucose in rats.
3.Regulation of P-glycoprotein efflux activity by Z-guggulsterone of Commiphora mukul at the blood-brain barrier.
Xu HB1, Yu J2, Xu LZ3, Fu J3. J Neurol Sci. 2016 Apr 15;363:147-52. doi: 10.1016/j.jns.2016.02.046. Epub 2016 Feb 20.
The present study was to investigate whether Z-guggulsterone had the regulatory effect on the activity and expression of P-glycoprotein in rat brain microvessel endothelial cells (rBMECs) and in rat brain. Inorganic phosphate liberation assay, high performance liquid chromatography, and western blot analysis were performed to assess the P-glycoprotein ATPase activity, the accumulation of NaF and rhodamine 123, and P-glycoprotein and MRP1 expression. The results showed that Z-guggulsterone (0-100μM) significantly enhanced basal P-glycoprotein ATPase activity in a concentration-dependent manner. Tetrandrine (0.1, 0.3, 1μM) or cyclosporine A (0.1, 0.3, 1μM) had non-competitively inhibitory manner on Z-guggulsterone-stimulated P-glycoprotein ATPase activity, suggesting that Z-guggulsterone might have unique binding site or regulating site on P-glycoprotein. However, Z-guggulsterone (30, 100μM) had almost no influence on MRP1 expression in rBMECs.
4.Assessment of in vitro metabolic stability, plasma protein binding, and pharmacokinetics of E- and Z-guggulsterone in rat.
Chhonker YS1,2, Chandasana H1,2, Mukkavilli R3,4, Prasad YD1, Laxman TS1,2, Vangala S3, Bhatta RS1,2. Drug Test Anal. 2015 Nov 26. doi: 10.1002/dta.1885. [Epub ahead of print]
Guggulsterone is a racemic mixture of two stereoisomers (E- and Z-), obtained from the gum resin of Commiphora mukul and it is marketed as an antihyperlipidemic drug. The aim of our study was to assess the in vitro and in vivo absorption, distribution, metabolism, and excretion (ADME) properties namely solubility, in vitro metabolism, plasma protein binding and oral pharmacokinetic studies of E- and Z-guggulsterone. In vitro metabolism experiments were performed by using rat liver and intestinal microsomes. In vitro intrinsic clearance (CLint ) was found to be 33.34 ± 0.51 and 39.23 ± 8.12 μL/min/mg protein in rat liver microsomes for E- and Z-isomers, respectively. Plasma protein binding was determined by equilibrium dialysis method and in vivo pharmacokinetic studies were performed in male Sprague Dawley (SD) rats. Both isomers were highly bound to rat plasma proteins (>95% bound). Plasma concentration of E- and Z-isomers decreased rapidly following oral administration and were eliminated from systemic circulation with a terminal half-life of 0.
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