AIMTo observed the expression of estrogen receptor (ER alpha and ER beta) in the heart of Gekko swinhonis.

METHODSThe immunohistochemical technique for the estrogen receptor was used.

RESULTSThe positive ER alpha and beta cells existed in cardiac myocytes and fibroblasts of the atria and the ventricles of Gekko swinhonis and had no sexual difference. The difference of ER alpha between the atria (11.56 +/- 1.67) and ventricles (6.68 +/- 1.88) was observed in both sexes (P < 0.01).

CONCLUSIONThe atria are probably the main target tissue of estrogen through ER alpha pathway while some functions of whole heart will be regulated by estrogen through ER beta pathway. The sexual differences aren' t related to the content of ER. It may be involved in the state of activity and function of ER under the physiological conditions.

Animals ; Estrogen Receptor alpha ; metabolism ; Estrogen Receptor beta ; metabolism ; Female ; Immunohistochemistry ; Lizards ; physiology ; Male ; Myocardium ; metabolism

The coordination and unification of Yin and Yang are the basis of normal human life activities. Along with the age growth and aging of the body, women will suffer from menopausal syndrome during menopause. In addition to the significant changes in the genital system, there are also pathological manifestations in estrogen target points including bone, nerve and cardiovascular systems, due to the imbalance of Yin and Yang. Besides the insufficiency of estrogen, the main cause of menopausal syndrome is the changes in the response of target organs to estrogen. In other words, the biological effects mediated by estrogen receptor(ER) alpha and beta subtypes in target cells are often different or even opposite; the changes of expression level and ratio of ERα and ERβ are also important causes for the abnormal estrogenic effects in target organs and the imbalance of Yin and Yang of the body. Therefore, on one hand, the therapeutic mechanism of drugs is ER-mediated estrogenic effect. On the other hand, the drugs have a regulatory effect on ER subtype expression in target cells and Yin-Yang state in target organs and even organisms, so as to cause further changes in the response of target cells to estrogen or estrogenic components, and exert its therapeutic effects. This paper reviews the pharmacological mechanism of gynecological traditional Chinese medicine in harmonizing Yin and Yang in estrogen-positive target cells and the clinical efficacy in the following aspects, including estrogen and its mechanism, the estrogenic effect of ER in traditional Chinese medicine and the mechanism of ER subtype in balancing Yin and Yang and mediating and regulating the main target tissues in menopausal syndrome treatment.
Estrogen Receptor alpha ; Estrogen Receptor beta ; Estrogens ; Female ; Humans ; Medicine, Chinese Traditional ; Yin-Yang

OBJECTIVES: To study the effects of 17β-estradiol (E2) on the regulation of the proliferation of condylar chondrocytes and provide a preliminary discussion on the role of phosphorylate-mammalian target of rapamycin (p-mTOR) in this regulatory process. METHODS: Condylar chondrocytes were isolated from 6-week-old female rats for primary culture. Drug treatment with different concentrations of E2 and/or rapamycin (RAPA) was carried out on second-generation cells. Cell Counting Kit 8 was used to measure the cell viability of condylar chondrocytes after culture for 24, 48, or 72 h, and reverse transcription-polymerase chain reaction (RT-PCR) was applied to detect the relative gene expression of estrogen receptor alpha (ERα), estrogen receptor beta (ERβ), collagen type Ⅱ (COLⅡ), autophagy-related gene 6 (Beclin-1), and autophagy-related gene 5 (ATG-5). Western blot was employed to determine the relative protein expression of ERα, ERβ, Beclin-1, lipid-modified light chain 3B (LC3-Ⅱ), and p-mTOR. RESULTS: E2 could significantly promote the proliferation of chondrocytes cultured CONCLUSIONS At a concentration of 10
Animals ; Autophagy ; Cell Proliferation ; Chondrocytes ; Estradiol ; Estrogen Receptor alpha/metabolism* ; Estrogen Receptor beta ; Female ; Phosphorylation ; Rats

Estrogen plays an important role in the regulation of male reproduction. Through binding with the estrogen receptor (ER), estrogen produces genomic and non-genomic effects. Estrogen receptors include ERalpha and ERbeta which distribute in the male reproductive system including the testis, epididymis, prostate and penis. The spermatogenesis is impaired in mice with ERalpha gene knockout; however, it remains normal in mice with ERbeta gene knockout. This phenomenon suggests that the two subtypes of ER play different roles in spermatogenesis. Moreover, ERalpha or ERbeta may also act as a substitute of another.
Animals ; Estrogen Receptor alpha ; metabolism ; Estrogen Receptor beta ; metabolism ; Genitalia, Male ; metabolism ; Male ; Mice ; Receptors, Estrogen ; metabolism

One third of estrogens in the male are from the testis and the others from outside the testis. Aromatase P450 (CYP19) is an enzyme responsible for the conversion of androgens to estrogens. Estrogens regulate cell function via specific receptors--estrogen receptors (ER) which include ER alpha and ER beta. It has been found that the role of estrogens in male reproduction is complex and important, particularly during the neonatal life. Males lacking ER alpha are completely infertile because ER alpha-induced estrogens regulate the reabsorption of luminal fluid in the head of the epididymis and disruption of this essential function causes sperm to enter the epididymis diluted, rather than concentrated, resulting in infertility. Whereas males lacking aromatase or ER beta are fully fertile. Therefore, it is concluded that ER alpha, but not aromatase or ER beta, is essenitial for normal male fertility.
Animals ; Aromatase ; physiology ; Estrogen Receptor alpha ; Estrogen Receptor beta ; Estrogens ; physiology ; Humans ; Male ; Receptors, Estrogen ; physiology ; Reproduction ; physiology

Estrogen receptors (ERs) are members of nuclear receptors and related to several diseases such as cancer, inflammation and osteoporosis. ERs have two forms, ERα and ER&beta;, which have different functions and organism distributions. Compounds selectively targeting ER&beta; can regulate important physiological functions and avoid the side effects caused by targeting ERα. Therefore, selective ER&beta; ligands have received considerable research interest in recent years. In this article, different kinds of selective ER&beta; ligands were summarized and their structure-activity relationships were also analyzed.
Estrogen Receptor beta ; chemistry ; Humans ; Ligands ; Structure-Activity Relationship

OBJECTIVETo observe the statuses of estrogen receptor (ER) alpha and beta in the pelvic floor and its relation with stress urinary incontinence (SUI).

METHODSThe ERa and ERP in levator ani muscle and pelvic floor structure of premenopausal and postmenopausal SUI patients were detected by immunohistochemical staining and Western blot.

RESULTSThe positive biopsy rates in the premenopausal and postmenopausal SUI groups were 11% and 0, and the corresponding results in the control group were 35% and 33%. No ERalpha and ERbeta expression was detected in the levator ani muscle. ERalpha and ERbeta located in pelvic fasia tissue around the levator ani muscle. ERbeta was negatively stained in some segments of pelvic fasia tissue. The positive expression rates of ERbeta in the pelvic fasia tissue of premenopausal and postmenopausal SUI group were 57% and 33%, which were significantly lower than those in the control groups (P < 0.05). The positive expression rate of ERP in the pelvic fascia was significantly lower in postmenopausal group than in the premenopausal group (P < 0.05). The positive expression rates of ERa in the pelvic fasia tissue in the premenopausal and postmenopausal SUI groups were (4.43 +/- 2.64)% and (5.14 +/- 1.79)%, which were significantly lower than (9.61 +/- 5.48)% and (10.88 +/- 2.90)% in control group (P < 0.05). Western blot showed that ERbeta expression in pelvic fasia tissue was less than the expressions of ERalpha, ERalpha and ERbeta in the SUI group was also lower than that of the control group.

CONCLUSIONERalpha and ERbeta do not express in the levator ani muscle of women. Pathogenesis of premenopausal SUI correlates with lower serum estrodiol level and the expression of ER correlates SUI.

Estrogen Receptor alpha ; biosynthesis ; Estrogen Receptor beta ; biosynthesis ; Female ; Humans ; Pelvic Floor ; Postmenopause ; Premenopause ; Urinary Incontinence, Stress ; metabolism

PURPOSE: In our previous studies we showed that upregulating claudin-6 (CLDN6) expression may contribute to preventing breast cancer, and that 17beta-estradiol induces a concentration- and time-related effect on CLDN6 mRNA and protein expression in MCF-7 cells. However, the mechanisms of 17beta-estradiol regulation of CLDN6 are still unclear. We determined the role of estrogen receptors in the regulation of CLDN6 expression in human breast cancer tissues and a cell line. METHODS: CLDN6, estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta) expression in breast cancer tissues were examined using immunohistochemistry. The human breast cancer cell line, MCF-7, which expresses ERalpha but not ERbeta was used. CLDN6 and ERalpha expression were measured by reverse transcriptase-PCR, Western blotting and immunofluorescent staining. Treatments with propyl pyrazole triol (PPT) and ICI 182, 780 (ICI) were performed. RESULTS: The results revealed that CLDN6 expression was related to ERalpha in breast cancer tissues (p=0.033). PPT, an ERalpha-selective ligand, upregulated CLDN6 expression at 10-5 mol/L after 24 hours. The effect of PPT on regulating CLDN6 expression in MCF-7 cells was blocked by ICI. CONCLUSION: These findings suggest that Eralpha reulates CLDN6 expression in breast cancer tissues and that 17beta-estradiol induces CLDN6 expression through an ERalpha pathway in MCF-7 cells.
Blotting, Western ; Breast ; Breast Neoplasms ; Cell Line ; Claudins ; Estrogen Receptor alpha ; Estrogen Receptor beta ; Estrogens ; Humans ; Immunohistochemistry ; MCF-7 Cells ; Pyrazoles ; Receptors, Estrogen ; RNA, Messenger ; Tight Junctions

PURPOSE: To verify the difference of estrogen receptor beta (ER beta) expression between breast cancer and normal mammary tissue and the roles of ER beta in prognosis of breast cancer, its expression was investigated in normal mammary and breast cancer tissues METHODS: The ER beta expression of 89 normal mammary and 100 breast cancer tissues was examined using immunohistochemistry. The staining signal was scored by estimating the proportion (range, 0-5) and intensity scores (range, 0-3) of positive cells. The ER beta expression was considered as positive if the total score (IHC score; range, 0-8) was 3 or more. The ER beta expressions were compared between normal mammary and breast cancer tissues. The association of ER beta expression with other clinicopathological factors was also investigated. The distant relapse free survival (DRFS) and overall survival (OS) rates were compared according to the ER beta expression. RESULTS: Eighty-eight of the 89 (98.9%) cases of normal mammary tissues and 74 of the 89 (83.1%) counterpart breast cancer tissues showed positive staining with decreased ER beta expression in the breast cancer compared to the normal mammary tissue with statistical significance (p=0.026). In breast cancer, the ER beta expression was found to have a positive correlation with the ER expression but with only marginal significance (p=0.063). There was no correlation between the ER beta expression and other clinicopathological factors (age, tumor size, nodal status, histological grade, progesterone receptor status, and HER-2 expression). The 5 year DRFS and OS rates were found to be independent of ER beta expression. CONCLUSION: The ER beta expression was significantly decreased in cancer tissues. Further study with a sufficient number of patients is needed to verify the roles of ER beta during breast cancer carcinogenesis and clinical value.
Breast Neoplasms* ; Breast* ; Carcinogenesis ; Estrogen Receptor beta* ; Estrogens* ; Humans ; Immunohistochemistry ; Prognosis ; Receptors, Progesterone ; Recurrence

OBJECTIVETo investigate whether there is a association between estrogen receptor beta (ERb) gene polymorphism and primary hepatocellular carcinoma (HCC).

METHODS100 primary HCC patients and 100 controls from southwestern China were recruited in this study. The polymorphism of RsaI and AluI in ERb gene was analyzed by PCR- restriction fragment length polymorphism (RFLP).

RESULTSR allelic frequency was 35.0% and 51.0% in HCC patients and in control group, respectively, odds ratio (OR) was 0.517 [95% confidence intervals (CI) = 0.346-0.773], P less than 0.01. A allelic frequency was 20.5% and 11.0% in HCC patients and in control group, respectively, OR was 2.086 (95% CI = 1.191-3.654), P less than 0.01. Gene frequency of RsaI and AluI in the two groups was distributed with polymorphism.

CONCLUSIONERb gene polymorphism is associated with primary liver cancer. R allele may be the guard factor, and A allele may be its risk factor.

Carcinoma, Hepatocellular ; genetics ; Estrogen Receptor beta ; Gene Frequency ; Genetic Predisposition to Disease ; Humans ; Polymorphism, Genetic