Quantitative comparison of the inhibitory effects of GW5638 and tamoxifen on angiogenesis in the cornea pocket assay

Angiogenesis
Sheng TongFan Yuan

Abstract

GW5638 is a novel tissue-selective estrogen receptor (ER) modulator. Structurally, it is a derivative of tamoxifen that is known for its inhibitory effects on angiogenesis in an ER-independent manner. Therefore, it is possible that GW5638 has the same effects as tamoxifen on angiogenesis. To test this hypothesis, we used the rat cornea pocket assay and developed a new method that could precisely determine the total projected area of microvessels induced by basic fibroblast growth factor (bFGF) in the cornea. Animals in the study were treated with corn oil (control group), tamoxifen, or GW5638. After treatment, we observed that both GW5638 and tamoxifen could inhibit angiogenesis in the cornea (P<0.05) and that the inhibitory effects were not mediated by blocking functions of estrogen. Meanwhile, GW5638 had minimal effects on the body weight of animals whereas tamoxifen significantly reduced the body weight. Based on these observations, we concluded that GW5638 was as effective as tamoxifen in antiangiogenic treatment but less toxic than tamoxifen.

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Citations

Oct 19, 2010·Graefe's Archive for Clinical and Experimental Ophthalmology = Albrecht Von Graefes Archiv Für Klinische Und Experimentelle Ophthalmologie·Wenru SuDan Liang
Aug 27, 2013·Drug Design, Development and Therapy·Stephanie L GrilloPeter Koulen
Apr 30, 2014·Journal of Ophthalmology·Deli KrizovaPavel Studeny
Sep 15, 2018·Oncology Letters·Yanzhen ZuoYuhong Li
Apr 16, 2016·Molecular Medicine Reports·Changying LiuBo Li

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