Z-Guggulsterone

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Background

Z-Guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, a broad-spectrum ligand of steroid hormone receptors, with IC50 values of 1740, 1000, 220 and > 50000 nM for glucocorticoid, mineralocorticoid, androgen and farnesoid X receptors, respectively, as well as EC50 values of 1200 and > 5000 nM for progesterone and estrogen receptors, correspondingly [1].
Steroid hormone receptors, found in the nucleus, cytosol, and also on the plasma membrane of target cells, transcribe genes that lead to important biological processes, including normal organ development and function, tissue differentiation, and promotion of oncogenic transformation [2].
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 [3].
Oral gavage of z-guggulsterone (1 mg per day, five times per week) to male nude mice inhibited in vivo angiogenesis in DU145-Matrigel plug assay as evidenced by a statistically significant decrease in tumor burden, microvessel area, and vascular endothelial growth factor receptor 2 (VEGF-R2) protein expression [3].

[1]. Burris T P, Montrose C, Houck K A, et al. The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand. Molecular Pharmacology, 2005, 67(3): 948-954.
[2]. Levin E R. Rapid signaling by steroid receptors. American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, 2008, 295(5): R1425-R1430.
[3]. Xiao D, Singh S V. z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo. Molecular Cancer Therapeutics, 2008, 7(1): 171-180.