Background:

Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.

Alpha-Estradiol (17 alpha-Estradiol) is a 5α-reductase inhibitor, and inhibits testosterone metabolism catalyzed by 5 alpha-reductase[1]. Alpha-Estradiol (17 Alpha-estradiol, 10 μM) attenuates LPS-induced inflammatory markers in both C57BL/6J male and female mouse embryonic fibroblast (MEF) cells, primary pre-adipocytes and differentiated 3T3-L1 adipocytes in an ERα-dependent manner, and such effects are through decreased NFκB-p65 and increased ERα protein expression[2].

Alpha-Estradiol (17-alpha-estradiol, 0.01, 0.1, 1 μg) significantly reduces the percentage of central avascular/total retina area of the mouse pups. Alpha-Estradiol (1 μg) markedly decreasesmalondialdehyde (MDA) levels on postnatal days (PND) 9, 13, and 17 in retinas of hyperoxia-exposed pups. Alpha-Estradiol (1 μg) also decreases the number of NADPH-oxidase-positive cells, NADPH oxidase concentration and activity in retinas of the pups. In the 1.0-μg Alpha-Estradiol-treated pups, VEGF retinal concentrations are high on PND 9 but lower on PND 14 and 17. The best effect in retinas of 1.0-μg Alpha-Estradiol-treated pups is partly reversed by ICI182780 on PND 14 and 17[3].

参考文献:
[1]. Schriefers H, et al. Inhibition of testosterone metabolism by 17-alpha-estradiol in rat liver slices. Arzneimittelforschung. 1991 Nov;41(11):1186-9.
[2]. Santos RS, et al. The effects of 17 alpha-estradiol to inhibit inflammation in vitro. Biol Sex Differ. 2017 Sep 6;8:30.
[3]. Zhang HB, et al. 17-Alpha-estradiol ameliorating oxygen-induced retinopathy in a murine model. Jpn J Ophthalmol. 2012 Jul;56(4):407-15.