Phytoestrogens, which can bind with estrogen receptor and produce estrogen-like effects, are a kind of nonsteroidal compound in plant. Phytoestrogens chemically include isoflavones, coumarins, lignans and other compounds. Phytoestrogens are selective estrogen receptor modulator, and have therapeutical effects on breast cancer, prostate cancer, cardiovascular disease, menopausal symptoms, osteoporosis and other disease, however, do not produce stimulatory hyperplasia effects on uterus, mammary glands and other tissues and organs with positive estrogen receptor. Long-term exposure or excessive use of phytoestrogens maybe affects male reproductive system and hematopoietic function of fetus. Some questions need to be further studied, such as evaluation criteria on biological activity, adverse effects, and action mechanism of phytoestrogen. This review covers plant sources, chemical structure, pharmacological activity and safety of phytoestrogens. It will provide a useful reference for intensive research and rational utilization the phytoestrogens.
Animals ; Humans ; Phytoestrogens ; chemistry ; pharmacology ; Phytotherapy ; Plant Extracts ; chemistry ; pharmacology ; Plants, Medicinal ; chemistry

Phytoestrogens are bioactive substances existing in natural plants. They have similar molecular structure to those of estrogens. In this article we introduced their classification and sources, and elucidated their effects on heart from aspects involving cardiac function and myocardial electrophysiology. By regulating serum lipid metabolism, arterial vessels, cytokine levels, and coagulation/fibrinolysis system, phytoestrogens possess the effects of anti-atherosclerosis and may be used to prevent and treat cardiovascular diseases.
Arteriosclerosis ; prevention & control ; Cardiovascular Diseases ; prevention & control ; Humans ; Hyperlipidemias ; prevention & control ; Isoflavones ; pharmacology ; Phytoestrogens ; pharmacology ; Phytotherapy

Calycosin, which is a kind of typical phytoestrogen, can bind with estrogen receptor and produce estrogen-like effects. Calycosin were reported to have antioxidant, anti-osteoporosis, anti-tumor and immunomodulating activities. This review covers biological activities and its mechanism of calycosin. It will provide a useful reference for clinical research and rational utilization of monomericompound.
Animals ; Apoptosis ; drug effects ; Astragalus Plant ; chemistry ; Cell Proliferation ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Humans ; Isoflavones ; pharmacology ; Phytoestrogens ; pharmacology

Animals ; Apigenin ; pharmacology ; Female ; Follicle Stimulating Hormone ; blood ; Gonadotropin-Releasing Hormone ; blood ; Luteinizing Hormone ; blood ; Phytoestrogens ; pharmacology ; Rats

OBJECTIVETo observe effects of phytoestrogens quercetin (QC), Genistein (GEN), coumestrol (COM), and enterolactone (ENL) on gap junctional intercellular communication (GJIC) in HaCaT cells.

METHODSHaCaT cells were exposed to QC, GEN, COM, and ENL at 0.1, 1.0, 10.0 and 100.0 micromol/L for 24 hours. The effects of phytoestrogens on GJIC were determined by fluorescence redistribution after photobleaching (FRAP) technique of using a laser scanning confocal microscope (LSCM).

RESULTSQC did not affect the GJIC at 0.1-10.0 micromol/L, whereas, GEN, COM, and ENL exhibited inhibition on the GJIC in some extent at 0.1-10.0 micromol/L without showing significant cytotoxicity. The ratio of fluorescence recovery were between 31.77% to 37.06%, which were significantly decreased compared the vehicle control (44.74%).

CONCLUSIONThe phytoestrogens GEN, COM, and ENL, but not QC, could inhibit the GJIC function in HaCaT cells at concentrations could be reached in human serum in some instance, indicating they could, under certain conditions, be cancer promoters. Therefore, it should be prudent to use these chemicals as pharmaceuticals or dietary supplements.

Cell Communication ; drug effects ; physiology ; Cell Line ; Coumestrol ; pharmacology ; Dose-Response Relationship, Drug ; Gap Junctions ; drug effects ; physiology ; Genistein ; pharmacology ; Humans ; Microscopy, Confocal ; Phytoestrogens ; pharmacology ; Quercetin ; pharmacology

The purpose of this study was to investigate the effects of phytoestrogen genistein (GST) on delayed after depolarization (DAD) and triggered activity (TA) induced by ouabain in guinea pig papillary muscles. Action potentials (APs) were recorded from the guinea pig papillary muscles with standard glass microelectrode technique. The results are as follows: (1) DAD and TA induced by ouabain (1 micromol/L) were markedly inhibited by pretreatment with GST (10, 50, 100 micromol/L) in a concentration-dependent manner. (2) NG-nitro-L-arginine methyl ester (L-NAME, 1 mmol/L), an NO synthase inhibitor, failed to affect the above effects of GST. (3) 5 micromol/L 17beta-estradiol (E2) or 10 micromol/L GST alone showed no effects on DAD and TA, whereas GST combined with E(2) at the same doses exerted significant inhibitory effects on DAD and TA. Since GST is known to reduce the calcium influx, it is suggested that GST might have antiarrhythmic effects, possibly by reducing calcium influx. The antiarrhythmic effects of GST may contribute to its cardioprotective action.
Action Potentials ; drug effects ; Animals ; Genistein ; pharmacology ; Guinea Pigs ; Male ; Neuromuscular Depolarizing Agents ; pharmacology ; Ouabain ; pharmacology ; Papillary Muscles ; drug effects ; physiology ; Phytoestrogens ; pharmacology

OBJECTIVETo investigate the estrogen-like activities of icariin (ICA), icaritin (ICT) and desmethylicaritin (DICT) and their structure/activity relationships.

METHODSICT was hydrolyzed from ICA by cellulase and then DICT was demethylated from ICT in boron tribromide and dichloromethane system. Estrogen-sensitive MCF-7 cells and T47D cells were co-incubated with different concentrations of test compounds for 6 and 9 d respectively, and the cell proliferation was measured by MTT.

RESULTSICT and DICT both markedly enhanced cell proliferation. Compared with estradiol (10.(-9) mol/L), the proliferative effects of 10.-6 mol/L ICT and DICT on MCF-7 cells were 90.0% and 94.0% (P<0.01), respectively, and those of T47D cells were 65.6% and 50.0%. (P<0.01). But this phenomenon was not observed with ICA. Cell proliferation induced by ICT and DICT was completely antagonized by 10.(-7 )mol/L pure estrogen receptor antagonist, ICI182,780.

CONCLUSIONICT and DICT possess estrogen-like activity of enhancing proliferation in MCF-7 and T47D cells. However, ICA appears to have no estrogenicity on MCF-7 and T47D cell lines in vitro.

Breast Neoplasms ; pathology ; Cell Division ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Flavonoids ; chemistry ; pharmacology ; Humans ; Phytoestrogens ; isolation & purification ; pharmacology ; Tumor Cells, Cultured

OBJECTIVETo investigate the effects of phytoestrogens (daidzein and genistein) on the testosterone production of rat Leydig cells and the possible mechanisms.

METHODSPrimary Leydig cells were obtained from 3-month old male SD rats using discontinuous Percoll density gradient centrifugation. The effects of phytoestrogens at various concentrations were evaluated by ELISA, with hCG as the positive control. The mRNA expression of P450 side-chain cleavage enzyme (P450scc) was analyzed by semi-quantitative RT-PCR.

RESULTSGenistein at 0.1 micromol/L obviously promoted the secretion of testosterone and upregulated the mRNA level of P450scc. At a higher concentration of 5 micromol/L, however, both daidzein and genistein significantly inhibited the testosterone production of Leydig cells (P > 0.05).

CONCLUSIONGenistein can promote the testosterone production of Leydig cells at a low concentration (0.1 micromol/L), but both daidzein and genistein can inhibit it at a higher concentration ( >5 micromol/L).

Animals ; Cells, Cultured ; Genistein ; pharmacology ; Isoflavones ; pharmacology ; Leydig Cells ; drug effects ; secretion ; Male ; Phytoestrogens ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Testosterone ; biosynthesis

AIM: To evaluate the antifertility activity of Artemisia vulgaris leaves on female Wistar rats. METHOD: The plant extract was tested for its effect on implant formation at two dose levels, 300 and 600 mg·kg⁻¹, respectively. The effective methanolic plant extract was further studied for estrogenic potency on ovariectomised immature female Wistar rats. RESULTS: The data presented in this study demonstrate the antifertility potential of Artemisia vulgaris methanolic leaf extract, which shows a strong and significant decrease in implant formation (100%), and a strong estrogenic effect resulting in a significant increase in uterine weight in immature ovariectomised rats. These observations suggest that the methanolic extract of Artemisia vulgaris leaves has strong anti-implantation activity and estrogenic activity. CONCLUSION The methanolic plant extract of A. vulgaris has antifertility activity.
Animals ; Artemisia ; Contraceptive Agents ; pharmacology ; Embryo Implantation ; drug effects ; Female ; Fertility ; drug effects ; Organ Size ; Ovariectomy ; Phytoestrogens ; pharmacology ; Plant Extracts ; pharmacology ; Plant Leaves ; Rats, Wistar ; Uterus ; drug effects

OBJECTIVETo investigate the effect of genistein on the proliferation and lipid peroxidation of hepatic stellate cells (HSC) in vitro and its the protective effect against hepatic fibrosis.

METHODSRat hepatic stellate cells (HSC-T6 cells) were divided into 3 groups and incubated in the presence of 0.1 mol/L hydrogen dioxide followed by washing with PBS for 3 times. Genistein at different concentrations was added into the cell culture meclia, and after 48 h of incubation, the cell proliferation was assessed with MTT assay and the levels of superoxide dismutase (SOD), malonaldehyde (MDA), glutathione (GSH) and glutathione peroxidase (GSH-PX) in the supernatant of the cell culture were measured.

RESULTSGenistein at different concentrations inhibited the cell proliferation, showing a dose-effect relationship. Genistein significantly decreased the production of intracellular MDA and GSH and increased SOD and GSH PX activity.

CONCLUSIONGenistein can prevent the formation of hepatic fibrosis probably by decreasing HSC proliferation and lipid peroxidation.

Animals ; Cell Proliferation ; drug effects ; Cells, Cultured ; Genistein ; pharmacology ; Hepatocytes ; cytology ; Lipid Peroxidation ; drug effects ; Liver Cirrhosis ; prevention & control ; Phytoestrogens ; pharmacology ; Rats ; Rats, Sprague-Dawley