OBJECTIVETo study 17β-estradiol (E2), ethinylestradiol (EE2), estriol (E3), estrone (E1) on MCF-7 proliferation effects, and compare the effects of independent action (IA) model with concentration addition (CA) model in assessing the combined effects of estrogen.

METHODSThe combinations of E2 + EE2, E2 + E3 and E2 + E1 were chosen and the cellular proliferation effects were examined by MTT assay.

RESULTSThe maximum proliferation effects at dose of 10⁻⁹ mol/L was 325.48% for E2, 330.34% for EE2, 255.22% for E3, and 199.61% for E1. In the E2 + EE2, E2 + E3, E2 + E1 groups, the results of IA model analysis were very close to the experimental results. The IA model tend to overestimated the experimental results, while the CA model often underestimated the experimental results. In the EC (E2, 30) + C (EE2, 70) group, the results exceed the maximum estrogen effects of E2, while in other groups, the results were lower.

CONCLUSIONSThe estrogenic effects of the four tested substances from high to low efficiency were that: EE2 > E2 > E3 > E1. The effect of IA model in predicting the combined effects of binary mixture was better than CA model. A small proportion of binary mixture showed synergy.

Cell Line, Tumor ; Cell Proliferation ; drug effects ; Estradiol ; pharmacology ; Estriol ; pharmacology ; Estrogens ; pharmacology ; Estrone ; pharmacology ; Ethinyl Estradiol ; pharmacology ; Female ; Humans

OBJECTIVETo study the effect of purariae isoflavone on estrogen level in ovariectomized rats.

METHOD80 rats were divided into four groups randomly, every group with 20 rats: 1. Control group; 2. Normal + purariae isoflavone group; 3. Ovariectomized group; 4. Ovariectomized + purariae isoflavone group. Estrogen level and gonadotropin-releasing hormone level of all rats were measured.

RESULTThirty days after being ovariectomized, E2, E3 level was significantly lower than that of the first group(P < 0.05). But Testerone, FSH, LH, PRL and GH increased(P < 0.05). After being gastrogavaged with purariae-isolfavone for thirty days, Estrogen level and gonadotropin-relasing hormone level of the second group were significantly lower in various degree than those of normal control group (P < 0.05). But in ovariectomized rats, the estrogen level was recovered (P > 0.05). The gonadotropin-releasing hormone level was increased (P < 0.05).

CONCLUSIONPurariae-isoflavone can increase estrogen level to normal in ovariectomized rats by way of increasing the level of gonadotropin-releasing hormone. In normal rats, it has anti-estrogen effect.

Animals ; Estradiol ; blood ; Estriol ; blood ; Estrogen Antagonists ; pharmacology ; Female ; Gonadotropin-Releasing Hormone ; blood ; Isoflavones ; isolation & purification ; pharmacology ; Ovariectomy ; Plants, Medicinal ; chemistry ; Pueraria ; chemistry ; Rats ; Rats, Sprague-Dawley

The effects of estriol on oxygen uptake, glucose release, lactate and pyruvate production, beta-hydroxybutyrate and acetoacetate production in perfused rat liver as well as, carbon uptake in rat liver and intracellular calcium in isolated Kupffer cells were investigated. Basal oxygen consumption of perfused liver increased significantly in estriol or ethanol-treated rats. But these increased effects were blocked by gadolinium chloride pretreatment. In a metabolic study, pretreatment with estriol resulted in a decrease in glucose production and in glycolysis while an increase in ketogenesis. A more oxidized redox state of the mitochondria was indicated by increased ratios of perfusate [lactate]/[pyruvate] and decreased ratios of perfusate [beta-hydroxybutyrate]/[acetoacetate]. Carbon uptake of Kupffer-cell increased significantly in estriol-treated rats. But these increased uptake were not shown in rats pre-treated by gadolinium chloride blocking phagocytosis. In isolated Kupffer cells from estriol-treated rats, intracellular calcium was more significantly increased after addition of lipopolysaccharide (LPS) than in controls. These findings suggest that the metabolic effects of estriol (two mg per 100 mg body wt) can be summarized to be highly toxic in rat liver, and these findings suggest that oral administration of estrogens may induce hepatic dysfunctions and play a role in the development of liver disease.
3-Hydroxybutyric Acid/metabolism ; Acetoacetates/metabolism ; Animal ; Calcium/metabolism ; Carbohydrates/metabolism ; Carbon/metabolism ; Cells, Cultured ; Colloids/metabolism ; Estriol/pharmacology* ; Estriol/metabolism ; Ethanol/pharmacology ; Female ; Gadolinium/pharmacology ; Glucose/biosynthesis ; Intracellular Fluid/metabolism ; Kupffer Cells/metabolism ; Kupffer Cells/cytology ; Lactates/metabolism ; Lipids/metabolism ; Liver/metabolism ; Liver/drug effects* ; Oxygen Consumption ; Phagocytosis ; Pyruvic Acid/metabolism ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo study effects of soy extract on lipid metabolims in ovariectomized rats.

METHOD90 Wistar rats were randomly divided into 9 groups: control group, sham group, model group, estrogen group, soy isoflavone group of high dose, soy isoflavone group of low dose, soy extract of high dose, soy extract of low dose, and soy polysaccharde group, 10 rats in each group. Except fer of control and sham groups, the test rats were ovariectomized. One week after operation, the rats were treated with different drugs. Six weeks after operation, the rats were killed, with serum and liver taken, and serumglycerol(sGT), cholesterol(sGC), LDL, HDL and liver homogenate hGT, hGC, measured.

RESULTThe level of sGC, LDL in ovariectmized rats increased significantly, compared with that in control and sham groups. In liver both the level of hGT and hGC were higher than that in liver from control and sham groups. Administration of estrogen or soy extract or soy isoflavone could attenuate these in ovariectomized rats, but soy polysacchardes did not have any effects.

CONCLUSIONOvariectomized rats have an imbalance of lipid metabolism, the level of hGT and hGC were increased, and administration of estrogen, soy extracts or soy isoflavone could decrease these changes induced by ovariectomizing.

Animals ; Cholesterol ; blood ; metabolism ; Estriol ; analogs & derivatives ; pharmacology ; Female ; Isoflavones ; isolation & purification ; pharmacology ; Lipoproteins, LDL ; blood ; Liver ; metabolism ; pathology ; Ovariectomy ; Plant Extracts ; isolation & purification ; pharmacology ; Quinestrol ; analogs & derivatives ; Random Allocation ; Rats ; Rats, Wistar ; Soybeans ; chemistry ; Triglycerides ; blood ; metabolism

OBJECTIVETo observe the effect of Gengnianchun Recipe (GNC) on bone mineral density (BMD), bone biomechanical parameters and serum lipid level in the bilaterally ovariectomized (OVX) rats and to explore the prophylactic and therapeutic action of GNC on ovariectomy induced osteoporosis and hyperlipidemia.

METHODSOVX SD rats, 10 - 12 months old, were divided into different groups and fed with GNC 2 g/d, GNC 1 g/d and Nilestriol 0.125 mg/week, respectively for 4 months to observe the change of BMD and bone biomechanical parameters of the lumbar vertebrae, and the serum levels of total cholesterol (TC), triglyceride (TG), high-density lipoprotein cholesterol (HDL-C) and low-density lipoprotein cholesterol (LDL-C), and to compare the effect of the two drugs on the morphology of the uterus.

RESULTSThere was marked reduction in BMD and biomechanical parameters in lumbar vertebrae (P < 0.01) and increase of serum TC and LDL-C levels (P < 0.01) in rats after OVX. GNC or Nilestriol significantly improved the decreased BMD and biomechanical parameters of the lumbar vertebrae (P < 0.05 or P < 0.01), and reduced the serum TC and LDL-C levels (P < 0.01). In the Nilestriol group, the wet weight of uterus got increased obviously (P < 0.01), the number of uterine glands increased, uterine columnar epithelium thickened, and the mitotic figures in the epithelial stroma and myointimal cells augmented. But no such effect in wet weight and morphology of uterus was found in the GNC group.

CONCLUSIONGNC could increase the BMD and biomechanical parameters of the lumbar vertebrae, reduce the serum TC and LDL-C levels, yet produce no adverse reaction in stimulating proliferation and hypertrophy of uterus.

Animals ; Biomechanical Phenomena ; Bone Density ; drug effects ; Bone and Bones ; drug effects ; Cholesterol ; blood ; Cholesterol, HDL ; blood ; Cholesterol, LDL ; blood ; Drugs, Chinese Herbal ; pharmacology ; Estriol ; analogs & derivatives ; pharmacology ; Female ; Lipids ; blood ; Ovariectomy ; Quinestrol ; analogs & derivatives ; Rats ; Rats, Sprague-Dawley ; Triglycerides ; blood ; Uterus ; cytology ; drug effects