同义名 :	Z-Guggulsterone
	CAS号 :	39025-23-5
	货号 :	A1144321
	分子式 :	C21H28O2
	纯度 :	98+%
	分子量 :	312.45
	MDL号 :	MFCD01310757
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Vascular Endothelial Growth Factors (VEGFs) and their receptors (VEGF-Rs) are important regulators for angiogenesis and lymphangiogenesis. VEGFs and VEGF-Rs are not only expressed on endothelial cells but also on various subtypes of solid tumors and leukemias contributing to the growth of the malignant cells[2]. VEGF rapidly induced tyrosine phosphorylation of type 1 and type 2 VEGF receptors. Physical association between VEGF-receptor 2 (VEGF-R2) and insulin receptor substrate (IRS-1) and phosphatidylinositol 3'-kinase (PI3K) was induced by VEGF, which augmented PI3K activity in VEGF-R2 immunoprecipitates[3]. In a human melanoma xenograft mouse model, blockade of both VEGF-R2 and Tie-2 pathways or the VEGF receptor pathway alone resulted in a significant inhibition of tumor growth and tumor angiogenesis (92.2 % and 74.4 %)[4]. (Z)-Guggulsterone inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the vascular endothelial growth factor (VEGF)-VEGF-R2–Akt signaling axis. In HUVEC, Z-guggulsterone (10, 20 μM; 24 or 48 hours) induces a reduction in the level of VEGF-R2 protein. In tumor volume and wet tumor weight, Z-guggulsterone (p.o.; 1 mg; 5 times/week) causes a statistically significant reduction[5].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	3.20mL 0.64mL 0.32mL	16.00mL 3.20mL 1.60mL	32.01mL 6.40mL 3.20mL

参考文献

[1]Meyer U, Costantino G, Macchiarulo A, Pellicciari R. Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. J Med Chem. 2005 Nov 3;48(22):6948-55. doi: 10.1021/jm0505056. PMID: 16250653. [2]Hilmar Quentmeier, DNA methylation regulates expression of VEGF-R2 (KDR) and VEGF-R3 (FLT4). BMC Cancer. 2012 Jan 17;12:19. [3]Denis Feliers,et al. VEGF regulation of endothelial nitric oxide synthase in glomerular endothelial cells. Kidney Int. 2005 Oct;68(4):1648-59. [4]N Jendreyko,et al. Simultaneous, phenotypic knockout of VEGF-R2 and Tie-2 with an intradiabody enhances antiangiogenic effects in vivo.Klin Padiatr. May-Jun 2006;218(3):143-51. [5]Xiao D, et al. 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.