書誌： Steroids , 2012
Steroids 77 (2012) 845–849
Mayumi Okamoto, Shun Kobayashi, Hiroshi Ikeuchi, Shunji Yamada, Korehito Yamanouchi,Kazumichi Nagasawa, Shun Maekawa, Takashi Kato, Isao Shimizu
C7a-substituted estradiols bind to estrogen receptors in cell nuclei, yet these derivatives remain little used in bioimaging. Here, we describe a fluorescent derivative of estradiol (E2) with a boron-dipyrromethene (BODIPY) moiety attached to C7a, synthesized by olefin metathesis reaction of 7a-allylestradiol and 9-decenyl-BODIPY. In ovariectomized rats and non-ovariectomized mice, E2-BODIPY promoted the growth of uterine tissue similar to the effect of estradiol. Twenty-four hours after subcutaneous injection of E2-BODIPY in non-ovariectomized mice, we observed fluorescence of E2-BODIPY in the nuclei of uterine epithelial cells. Our findings suggest that fluorescence microscopy can localize this derivative in E2- responsive cells during normal development and tumorigenesis in vivo.