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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 39025-23-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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.
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. |
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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