[Effects of Yi-Fu Ning soft gelatin capsules on estrogen receptor expression in bone of postmenopausal osteoporosis rats].

OBJECTIVE: To investigate the effects of Yi-Fu Ning Soft Gelatin Capsules on estrogen receptor expression in bone of postmenopausal osteoporosis rats. METHOD: 60 female Sprague-Dawley rats in 3-month were used, 50 of them were ovariectomized and randomly divided into 5 groups:ovariectomy (OVX), OVX with diethylstilbestrol tables (DT), OVX with YFN (high dose, middle dose and low dose), the others were sham-operated group. The rats were administrated initially in the fifth week after the operation. After 12 weeks the rats were killed. The blood and bones were collected to inspect. The content of Estrogen (E2) in serum was detected by radioimmunoassay method. The expression of estrogen receptor in bones was studied with Western blotting. RESULT: After using the drugs, the content of E2, the estrogen receptor expression in bone increased significantly. CONCLUSION: Yi-Fu Ning Soft Gelatin Capsules has a good effect on postmenopausal osteoporosis by increasing E2 and ER expression in bones.

[Effect of the Yifuning soft gelatin capsules on estrogen receptor and nitric oxide levels in ovariectomized rats].

OBJECTIVE: To investigate the effects of the Yifuning soft gelatin capsules(YFN)on estrogen receptor (ER) and nitric oxide (NO) levels in ovariectomized rats. METHOD: Fifty female mature sprague-dawley rats were randomly divided into 5 groups: normal control; model control; diethylstilbestrol tablets (DT); YFN (high dose and low dose). After 4 weeks' treatment, the serum E2 levels were detected by radioimmunoassay. The estrogen receptor (ER) levels of uterus and artery were detected with method of radioligand binding assay of receptor (RBAR). The uterus pathologic changes were investigated with light microscope. NO and NOS levels of the artery and the uterus index were detected too. RESULT: YFN can obviously improve serum E2, increase index and ER of uterus (P < 0.01 or P < 0.05), and ameliorate the uterus' pathologic changes in OVX rats. It also can increase the artery' ER, NO and NOS levels. CONCLUSION: YFN can cure the climacteric syndrome and prevent the cardiovascular disease after post-menopause.

[Effects of the mixture of Rhizoma Curcumae and Oviducts Ranae on estrogen and its receptor expressions in ovariectomized rats].

OBJECTIVE: To study the effect of the mixture of Rhizoma Curcumae (YFN) and Oviducts Ranae on serum estrogen and spleen estrogen receptor expressions and its effect on reproductive endocrine-immune network in ovariectomized (OVX) rats. METHODS: Female SD rat models of climacteric syndrome (CS) were established by ovariectomy. After administration of YFN in the rats for 12 consecutive weeks, the serum estrogen levels (E2, FSH, LH, T, and P) and interleukin-2 were determined using radioimmunoassay, and the expression levels of estrogen receptor in the spleen were detected with immunofluorescence assay. RESULTS: The serum E2, T, P, and interleukin-2 levels (P<0.01) and spleen estrogen receptor expression (P<0.05) were significantly increased after high-dose YFN administration in the OVX rats as compared with the levels in the untreated OVX rats. YFN also resulted in lowered serum FSH and LH levels, but the changes were not statistically significant. CONCLUSION: YFN can increase the serum estrogen levels and estrogen receptor expression in the spleen of OVX rats, suggesting its clinical potential for relieving CS.

In vitro evaluation of estrogenic, estrogen antagonistic and progestagenic effects of a steroidal drug (Org OD-14) and its metabolites on human endometrium.

The human endometrial model for in vitro evaluation of estrogenic, estrogen antagonistic, and progestagenic effects of endogenous steroids, natural products or synthetic drugs was applied to the study of Org OD-14, an analog of norethynodrel developed by Organon International, Oss, The Netherlands, and some of its metabolites. Estrogen antagonistic actions of Org OD-14 and its 4-ene isomer were evident from their ability to suppress the enhancement of PGF2 alpha output elicited by estradiol on fragments of secretory endometrium and to decrease the rate of output of the prostaglandin by proliferative tissue, already stimulated by endogenous estrogens. These inhibitory effects were similar to those obtained with progesterone and do not appear to involve competition for the estrogen receptor since the antiestrogen 4-hydroxyamoxifen was not active in parallel incubations of proliferative endometrium. The progestagenic effects of Org OD-14 and its 4-ene isomer were also evident from their capability to enhance estradiol 17 beta-dehydrogenase activity and glycogen accumulation in specimens of proliferative endometrium. Estrogenic effects of the 3 alpha- and 3 beta-hydroxy metabolites of Org OD-14 were demonstrated by their stimulatory actions on PGF2 alpha output during incubations of secretory endometrium. The estrogenic and progestagenic actions of these compounds are in general agreement with their relative affinity for binding to the estradiol and progesterone receptors, although their actions may be influenced by intracellular metabolism in the endometrial tissue. For instance, the similarity in progestagenic activity of Org OD-14 and the 4-ene isomer, contrasting with their different affinities for the progesterone receptor, may result from in situ isomerization of Org OD-14 to the 4-ene metabolite.

Generation of C127-derived cell lines expressing estrogen or progesterone receptors for studying gene regulation on bovine papilloma virus minichromosomes.

To study regulation of transcription by multiple steroid hormones we have stably introduced expression vectors for human estrogen and rabbit progesterone receptors into the genome of the murine fibroblast cell line C127. These cells express functional endogenous glucocorticoid receptor and support bovine papilloma virus minichromosomes, a useful system for studying the role of chromatin structure on gene expression. Three clones containing progesterone receptor integrates and six containing estrogen receptors integrates were selected and characterized. All three progesterone and four of the estrogen receptors containing cell lines expressed functional receptors that were able to transactivate transcription from a mouse mammary tumor virus and Xenopus vitellogenin promoter, respectively, in steroid-specific manner. Levels of steroid binding varied between 38 and 890 fmol/mg protein for progesterone receptor, and between 22 and 94 fmol/mg protein for estrogen receptor. The observed dissociation constants of 1.8-2.5 nM (Organon.2058) and 0.75-2.8 nM (17 beta-Estradiol) are consistent with previously reported values for wild type rabbit progesterone receptor and the estrogen receptor derivative employed. Finally, we demonstrate that transcription of a mouse mammary tumor virus construct in a novel nontransforming bovine papilloma virus vector is regulated by both progestin and glucocorticoid agonists in line C127PR9.