Plasma prolactin and growth hormone levels as well as mRNA expression levels of pituitary estrogen-regulated genes, such as estrogen receptor (ER) subtypes alpha (ERα) and beta (ERβ), truncated ER product-1 (TERP-1) and -2 (TERP-2) and gonadotropin alpha subunit, were examined using radioimmunoassay and TaqMan® real-time PCR, respectively. The effects were compared with the potent ER agonist, 17β-estradiol-3-benzoate (E2B), and both substances were supplemented at low and high doses, i.e., 0.6 or 3 g puerarin and 0.0043 or 0.0173 g E2B per kilogram of phytoestrogens-free rat chow, and applied to ovariectomized rats (five groups; 11–12 rats per group) for 12 weeks.
Puerarin possessed weak E2B-like activities on pituitary function by acting as ERβ and TERP-1/-2 agonists, which resulted in the downregulation and upregulation of ERβ and TERP-1/-2 mRNA expressions, respectively, and elevation of growth hormone levels. There were trends of decreased levels of alpha subunit mRNA transcripts and increased levels of prolactin in puerarin-treated rats as observed in E2B-treated animals.
This is the first report in ovariectomized rats the effects of puerarin on somatotropes and pituitary estrogen-responsive mRNA expressions, which are very weakly estrogenic by acting through ERβ- and TERP-1/-2 mediated pathways.