包装 | 价格(元) |
50mg | 电议 |
10mg | 电议 |
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 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. |
产品描述 | 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: |