Description
Droloxifene is an anti-estrogen triphenylthylene selective estrogen receptor modulator (SERM); it is an analog of tamoxifen. Droloxifene acts as an estrogen receptor agonist in bone and as an estrogen receptor antagonist in breast tissue. As a result of these actions, this compound exhibits anticancer chemotherapeutic, chemopreventive, anti-osteoporotic, and anti-resorptive benefits. In breast cancer cells, droloxifene decreases production of NO and increases levels of pro-apoptotic TGF-β. Droloxifene increases apoptosis in luteal cells in vivo, increasing levels of c-myc and increasing the Bax/Bcl-2 ratio. In ovariectomized rats that act as a post-menopausal animal model, droloxifene inhibits bone resorption and turnover as well as estrogen-related bone loss. This compound also decreases levels of E-selectin and increases levels if vascular cellular adhesion molecule 1 (VCAM-1) in clinical settings.
References
Shelly W, Draper MW, Krishnan V, et al. Selective estrogen receptor modulators: an update on recent clinical findings. Obstet Gynecol Surv. 2008 Mar;63(3):163-81. PMID: 18279543.
Martin JH, Symonds A, Chohan S. Down-regulation of nitric oxide production by droloxifene and toremifene in human breast cancer cells. Oncol Rep. 2003 Jul-Aug;10(4):979-84. PMID: 12792756
Herrington DM, Brosnihan KB, Pusser BE, et al. Differential effects of E and droloxifene on C-reactive protein and other markers of inflammation in healthy postmenopausal women. J Clin Endocrinol Metab. 2001 Sep;86(9):4216-22. PMID: 11549652.
Leng Y, Feng Y, Cao L, et al. Effects of droloxifene on apoptosis and Bax, Bcl-2 protein expression of luteal cells in pseudopregnant rats. Acta Pharmacol Sin. 2001 Feb;22(2):155-62. PMID: 11741521.
Leng Y, Gu ZP, Cao L. Apoptosis induced by droloxifene and c-myc, bax and bcl-2 mRNA expression in cultured luteal cells of rats. Eur J Pharmacol. 2000 Dec 8;409(2):123-31. PMID: 11104825.
Knabbe C, Zugmaier G, Schmahl M, et al. Induction of transforming growth factor beta by the antiestrogens droloxifene, tamoxifen, and toremifene in MCF-7 cells. Am J Clin Oncol. 1991;14 Suppl 2:S15-20. PMID: 1835818.
ABOUT LKT LABS
LKT Laboratories is a biochemical supply company focused on the synthesis, purification, and isolation of small molecules for research applications. Its range of products exhibit known biological activities that have found uses in a wide array of research fields, especially cancer and neuroscience. These products include protein kinase inhibitors, ion channel modulators, and activators. LKT serves the global research community by supplying the highest purity products for use in cell culture models, animal studies, or as reference materials or analytical standards.
