الصفحة الرئيسية>>Signaling Pathways>> PI3K/Akt/mTOR Signaling>> Akt>>Z-Guggulsterone

Z-Guggulsterone

رقم الكتالوجGC10195

Z-guggulsterone ، أحد مكونات نبات الأيورفيدا الهندي الطبي Commiphora mukul ، يمنع نمو خلايا سرطان البروستاتا البشرية عن طريق التسبب في موت الخلايا المبرمج. يثبط Z-guggulsterone تكوين الأوعية عن طريق كبت محور إشارات VEGF – VEGF-R2 – Akt.

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Z-Guggulsterone التركيب الكيميائي

Cas No.: 39025-23-5

الحجم السعر المخزون الكميّة
10mg
140٫00
متوفر
50mg
558٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1]:

Cell lines

Bone marrow-derived macrophage (BMDM)

Preparation Method

Cells were incubated with Z-Guggulsterone at increasing concentrations (0, 0.5, 5, and 20 M) for 1 h and then simulated with LPS in the presence or absence of TREM-1 agonist antibody for the indicated time.

Reaction Conditions

0.5-20uM Z-Guggulsterone for 1h

Applications

Z-Guggulsterone attenuates TREM-1-mediated hyperactivation of macrophages through inhibition of TREM-1 expression and NF-κB and AP-1 activation.

Animal experiment [2]:

Animal models

IL-10, TLR4, and MyD88 deficient mice

Preparation Method

Z-Guggulsterone were administered orally at 100 mg/kg once daily after TNBS administration for 4 days or throughout the experiment. The mice were monitored for weight loss, fecal consistency, presence of crude blood in the feces or anus, and overall mortality

Dosage form

100 mg/kg Z-Guggulsterone orally administered once daily for 4 days

Applications

Z-Guggulsterone improves colitis in mice by regulating macrophage phenotype through IL-10 and TLR4/MyD88 pathways.

References:

[1]: Che X, Park KC, et,al. Protective effects of guggulsterone against colitis are associated with the suppression of TREM-1 and modulation of macrophages. Am J Physiol Gastrointest Liver Physiol. 2018 Jul 1;315(1):G128-G139. doi: 10.1152/ajpgi.00027.2018. Epub 2018 Mar 15. PMID: 29543509.

Background

Z-Guggulsterone, a component of the Ayurvedic medicinal plant Commiphora mukul, suppresses angiogenesis in vitro and in vivo with IC50 values of 1740, 1000, 220 and > 50000 nM for glucocorticoid, mineralocorticoid, androgen and farnesoid X receptors [1].

Bcl-2 protein expression was significantly decreased, and active caspase-3 and Bax protein expression was increased in SGC-7901 cells incubated with z-guggulsterone. The content of TNF-α was significantly increased, and the contents of VEGF and TGF-β1 were decreased in SGC-7901 cells incubated with z-guggulsterone[3]. In human umbilical vein endothelial cells (HUVEC) and DU145 cells, z-guggulsterone (5, 10 and 20 µM) significantly decrease cell migration in a concentration- and time-dependent manner, inhibiting capillary-like tube formation[4]. Z-guggulsterone (30 µM) simultaneously inhibited the expression of PXR and MDR1 at 24 h in human brain-derived microvessel endothelial cells (hBDMECs)[5].Z-guggulsterone attenuated TREM-1-mediated macrophage hyperactivation by suppressing TREM-1 expression and NF-κB and AP-1 activation[2].

Programmed death-ligand 1 (PD-L1) is an immune checkpoint molecule, that is overexpressed in non-small cell lung cancer (NSCLC) and has been associated with the response to anti-PD-1/PD-L1 immunotherapy.In vivo, Z-Guggulsterone treatment dose-dependently increased PD-L1 expression levels in mouse LLC tumor models[6]. Z-Guggulsterone significantly alleviated neurological deficits, infarct volume and histopathological damage in MCAO rats. Z-Guggulsterone successfully inhibited oxidative stress and inflammatory response in oxygen-glucose deprivation (OGD) treated neurons. Z-Guggulsterone exerted neuroprotective property through alleviated oxidative stress and inflammation via inhibiting the TXNIP/NLRP3 axis[7].

References:
[1]: Burris TP, Montrose C, et,al. The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand. Mol Pharmacol. 2005 Mar;67(3):948-54. doi: 10.1124/mol.104.007054. Epub 2004 Dec 15. PMID: 15602004.
[2]: Che X, Park KC, et,al.Protective effects of guggulsterone against colitis are associated with the suppression of TREM-1 and modulation of macrophages. Am J Physiol Gastrointest Liver Physiol. 2018 Jul 1;315(1):G128-G139. doi: 10.1152/ajpgi.00027.2018. Epub 2018 Mar 15. PMID: 29543509.
[3]: Lv R, Zhu M, et,al. Z-Guggulsterone Induces Apoptosis in Gastric Cancer Cells through the Intrinsic Mitochondria-Dependent Pathway. ScientificWorldJournal. 2021 Jan 4;2021:3152304. doi: 10.1155/2021/3152304. PMID: 33488300; PMCID: PMC7801056.
[4]: Xiao D, Singh SV. z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo. Mol Cancer Ther. 2008 Jan;7(1):171-80. doi: 10.1158/1535-7163.MCT-07-0491. PMID: 18202020.
[5]: Xu HB, Tang ZQ, et,al. Z-guggulsterone regulates MDR1 expression mainly through the pregnane X receptor-dependent manner in human brain microvessel endothelial cells. Eur J Pharmacol. 2020 May 5;874:173023. doi: 10.1016/j.ejphar.2020.173023. Epub 2020 Feb 19. PMID: 32087256.
[6]: Tian H, Gui Y, et,al. Z-guggulsterone induces PD-L1 upregulation partly mediated by FXR, Akt and Erk1/2 signaling pathways in non-small cell lung cancer. Int Immunopharmacol. 2021 Apr;93:107395. doi: 10.1016/j.intimp.2021.107395. Epub 2021 Jan 30. PMID: 33529916.
[7]: Liu T, Wang W, et,al. Z-Guggulsterone alleviated oxidative stress and inflammation through inhibiting the TXNIP/NLRP3 axis in ischemic stroke. Int Immunopharmacol. 2020 Dec;89(Pt B):107094. doi: 10.1016/j.intimp.2020.107094. Epub 2020 Oct 28. PMID: 33129097.

Chemical Properties

Cas No. 39025-23-5 SDF
Chemical Name (8S,9R,10R,13R,14S,Z)-17-ethylidene-10,13-dimethyl-7,8,9,10,11,12,13,14,15,17-decahydro-1H-cyclopenta[a]phenanthrene-3,16(2H,6H)-dione
Canonical SMILES O=C1C[C@H]([C@@](/C1=C/C)(C)CC2)[C@@H](CC3)[C@@H]2[C@](CC4)(C)C3=CC4=O
Formula C21H28O2 M.Wt 312.45
الذوبان ≥ 3.12mg/mL in DMSO with ultrasonic and warming Storage Store at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.2005 mL 16.0026 mL 32.0051 mL
5 mM 0.6401 mL 3.2005 mL 6.401 mL
10 mM 0.3201 mL 1.6003 mL 3.2005 mL
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