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OBJECTIVE To screen the active ingredient with estrogenic effect from total flavonoids of Cuscutae Semen. METHODS The estrogenic effect of total flavonoids from 10 batches of Cuscutae Semen was evaluated with mouse uterus coefficient and endometrial thickness as evaluation indexes， establish its fingerprint and calibrate the common peak. Common peak and spectrum-effect relationship of the above two indicators were analyzed by bivariate relationship analysis and grey correlation analysis to screen active components with estrogenic effect. UPLC-Q-TOF-MS technology was used to characterize the active components. RESULTS The estrogenic effect of total flavonoids from 10 batches of Cuscutae Semen was good. Twenty-eight and thirty-three common peaks of total flavonoids in Cuscutae Semen were obtained in the positive and negative ion modes respectively. The constituents represented by peaks 7，10，12-16，26 in positive ion mode and peaks 2，5，8，9，12，16，19，22-26 in negative ion mode were highly correlated with the estrogenic effect of total flavonoids from Cuscutae Semen. Further identification showed that the active substances with estrogenic effect from the total flavonoids of Cuscutae Semen were 5，7，3′， 4′-tetramethoxyflavone， 6- O-（trans） p-coumarin-furanfructose-（2→1）-glucopyranoside， rutin， kaempferol-3，7-diglucoside， apigenin-7-O-glucoside， hyperoside， baicalin， quercitin， quercetin， apigenin， kaempferol， isorhamnetin， rhododendron， isoquercetin， kaempferol-3-furan arabinoside， 2，6-octadecanediacetylic acid. CONCLUSIONS A total of 16 chemical components with estrogenic effect are screened from total flavonoids of Cuscutae Semen in the study， which can provide reference for the development of phytoestrogens.
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Epimedii folium is a commonly used Traditional Chinese Medicine (TCM) for warming the kidney and strengthening the yang qi. It has androgen-estrogen-like effect. It can not only directly act on sexual organs to regulate hormone levels, but also exert sex-hormone-like effect through hypothalamus-pituitary-gonadal axis. Its regulation of hormone levels is similar to that of plant hormones. At present, Epimedii folium is commonly used with other TCMs to treat diseases caused by sex-hormone deficiency, such as male spermatopenia, asthenospermia, benign prostatic hyperplasia, functional erectile dysfunction, female premature ovarian failure, perimenopausal syndrome, dysfunctional infertility during ovulation, hyperandrogenemia of PCOS patients, etc.
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OBJECTIVE: To identify the metabolites of Cuscuta chinensis in the serum and feces of rats with estrogenic estrogen, and to provide the basis for elucidating the pharmacological basis of its efficacy. METHODS: Using the HPLC-ESI-MS/MS technique, the molecular weight and molecular formula of the compounds were preliminarily estimated by the first-order mass spectrometry, and the chemical constituents of serum and feces were characterized by the retention time of the standard, the fragment ion information, the fragmentation law of mass spectrometry and the reference data. RESULTS: Five prototypic components and 4 metabolites were identified in the serum. A total of 11 chemical constituents were identified in the feces after administration, including 5 prototype components and 6 metabolites. CONCLUSION: Through the comparative analysis between serum and feces, the main metabolic pathways of Cuscuta chinensis compound are deduced, which provides reference for the basic research on the estrogenic substance of Cuscuta chinensis.
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Objective To qualitatively analyze the chemical constituents in rats after intragastric administration of estrogenically active ethanol extract of Cuscuta chinensis. Methods The high performance liquid chromatography quadrupole time-of-flight mass spectrometry (HPLC-Q/TOF MS/MS) was used to identify the prototypes and metabolites in rat urine. Results Twelve chemical constituents were identified in the drug-containing urine, including six prototypes and six metabolites. The prototypes are kaemoferol-3-β-D-glucuronide, 6-O-(E)-p-coumaroyl-β-D-fructofuranosyl-(2→1)-α-D-glucopyranoside, aempferol-7-rhamnoside, chlorogenic acid, and apigenin. The metabolites are p-hydroxycinnamic acid, p-hydroxyphenylpropionic acid, isorhamnetin, kaempferol-3-O-glucoside, acetyl caffeic acid, and quercetin sulfate. Conclusion The method of HPLC-Q/TOF MS/MS is simple and rapid for the analysis of prototype components and metabolites in rats urine after oral administration of ethanol extract of C. chinensis, providing the basis for further clarification of the estrogen material basis of C. chinensis.
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Objective: To investigate the estrogenic effect of (8,9)-furanyl-pterocarpan-3-ol (FPC) on growth of human breast cancer T47D cells and the interactions between the FPC and tamoxifen (TAM), on the growth of estrogen receptor-dependent breast cancer T47D cells.Methods:T47D cells were treated with FPC alone (0.01-200 μmol/L) or in combination with TAM 20 nmol/L. The proliferation effect of FPC were conducted on T47D cells in vitro by MTT test. Furthermore, the expression of ERα or c-Myc were also determined by immunohistochemistry.Results:inhibitory effect on T47D cells, wheraes co-administered with low concentration (less than 1μmol/L) of FPC attenuated to promote cell proliferation. In contrast, the combination of TAM with higher doses (more than 20 μmol/L) of FPC showed growth inhibitory. This result was supported by immunocytochemistry studies that the administration of 20 nmol/L TAM down-regulated ER-αand c-Myc, but the combination of 20 nmol/L TAM and 1 μmol/L FPC robustly up-regulated expression of ER-α. Thus, the reduced growth inhibition of TAM 20 nmol/L by FPC 1 μmol/L on T47D cells may act via the modulation of ER-α.Conclusions:The findings indicate and suggest that FPC had estrogenic activity at low The results indicated that administration of an anti-estrogen TAM showed growth concentrations and anti-estrogenic effect that are likely to be regulated by c-Myc and estrogen receptors. We also confirm that low concentration of FPC attenuated the growth-inhibitory effects of TAM on mammary tumor prevention. Therefore, the present study suggests that caution is warranted regarding the consumption of dietary FPC by breast cancer patients while on TMA therapy.
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The estrogenic activity of petroleum ether extract of Citrus medica L. leaves as well as the chemical constituents responsible for the biological activity was studied. The petroleum ether extract proved to retain high estrogenic activity in immature female rats. The extract was saponified and its components (saponifiable part 23% and the unsaponifiable matter 77%) were identified using GC/MS technique. The extract proved to be safe (LD50< 2g/kg.bw). Oral administration of petroleum ether extract of C. medica in ovariectomized immature female Wistar rats for 7 days in a dose of 400 mg/kg resulted in significant increase in the uterine weight (g) (1.7±0.11) when compared with ovariectomized control rats (1.3±0.07). GC/MS analysis of both saponifiable and unsaponifiable matters revealed the presence of thirty three components (28 hydrocarbons and 5 sterols) in the unsaponifiable fraction, the major hydrocarbon was n- Heneicosane (16.7%) while the major sterol was β-sitosterol (4.03%) and 15 components in the saponifiable matter it's major component was hexadecanoic acid (19.93%). As a conclusion petroleum ether extract of Citrus medica L. leaves possess a significant estrogenic activity.
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Estetrol es un esferoide estrogénico sintetizado exclusivamente por el hígado fetal, que traspasa a la circulación materna por la placenta. Descrito por primera vez por Diczfalusy en 1965. Desde esa fecha se han realizado diversas investigaciones preclínicas. En los últimos años, el interés por el estetrol ha aumentado, dado el logro de su síntesis en el laboratorio y la demostración de su buena biodisponibilidad y larga vida media al administrarlo por vía oral a mujeres. Se presenta una revisión de su síntesis, metabolismo y de la información científica existente de sus diferentes efectos en los tejidos estrógeno sensibles en distintos modelos animales.
Estetrol is an estrogenic steroid synthesized exclusively by the fetal liver. It crosses over from the placenta to the maternal circulation. It was first described in 1965 by Diczfalusy and from this date onwards, several preclinical investigations have been carried out. In recent years, the interest for estetrol has been growing due to its laboratory synthesis and the demonstration of its good bioavailability together with its long half life, when administered orally to women. A review of its synthesis, metabolism and existing scientific information on its different effects on estrogen sensitive tissues, in a variety of animal models, is here presented.
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Humans , Female , Menopause/drug effects , Estetrol/pharmacologyABSTRACT
Objective To study the estrogenic effect of organic extracts of effluent samples from different treatment stages in Tianjin reclaimed water treatment plant. Methods Reverse phase C-18 solid-phase extraction (RP-C18SPE) was used for the extraction of target compounds from water samples. Then, a simplified proliferation test with human estrogen receptor-positive MCF-7 breast cancer cell and recombined yeast assay were applied to assess the estrogenic effect in effluent samples from different treatment stages in Tianjin reclaimed water treatment plant. Results The amount of extracts of reclaimed water inducing the maximum effect in cell proliferation assay was equal to that from 1.00 ml primary water. In recombined yeast assay, the amount of extracts of reclaimed water inducing maximum ?-galactosidase activity was equal to that from 20.00 ml primary water. Conclusion The effluent of reclaimed water treatment plant still shows estrogenic effect though slightly reduced.