Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: DrugBank:APRD00691 (EE2)
 7,802 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Immediate metabolic effects of Stediril and Eugynon, hormonal contraceptives containing 0.5 mg DL-norgestrel and 0.05 mg ethinyl estradiol, were studied in 39 women aged 18-43 years and 10 men aged 21-36 years. All subjects were volunteers who had taken no hormone preparations during the 3 months immediately preceding the study. Blood samples were taken at 9 and 11 AM and at 1 and 4 PM on 2 successive days; the contraceptive was administered immediately after the first sample was taken on the second day. From the measured values for arterial oxygen and carbon dioxide partial pressures, blood pH, and hemoglobin, values for oxygen saturation, standard bicarbonates, buffer abases, and base excess were calculated using the Thews nomogram. The primary effect of hormone administration was shown to be metabolic acidosis, which is partly compensated during the next 7 hours by the respiratory system. No signs of primary respiratory alkalosis were noted.
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PMID:[Acid-base balance immediately after administration of an oral contraceptive (author's transl)]. 2 17

17beta-[6,7-3H]Estradiol (E2) was incubated with slices and homogenates of adult human renal tissue. The metabolites formed were identified by chromatography on DEAE-Sephadex, thin layer chromatography and crystallization with carrier steroids or steroid derivatives. The major metabolites formed by slices were estradiol-17-glucuronide (E217G), estrone sulfate and estradiol-3-sulfate. This is the first report of in vitro synthesis of estrogen sulfates by adult renal tissue. Minor quantities of the 3-glucuronides of estrone and estradiol were also found. An oxygen atmosphere appeared to stimulate the production of E217G. A time study with tissue slices showed similarities between the in vitro pattern of glucuronide synthesis and the excretion pattern of these compounds seen in earlier in vivo studies. Homogenates fortified with uridine diphosphoglucuronic acid formed the same pattern of glucuronide products but in lesser amounts. No sulfates were formed under these conditions. Testosterone did not act as a substrate in the experimental conditions used.
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PMID:In vitro synthesis of estrogen glucuronides and sulfates by human renal tissue. 16 18

The role of coronary vasospasm in many heart attacks has been reported. The paper presents a quite different mechanism, overproduction of prostaglandins (PGs), as the major factor in producing both the spasm and disorders of the rhythm which often accompany it. Coronary vasodilatation is caused by a reduced oxygen supply to the heart. If the hypoxia is severe or prolonged, coronary vasospasm results, leading to a further reduction of myocardial oxygenation. Increased outflow of PG-like material is related with the spasm, which can be prevented or reversed by infusion of inhibitors of PG synthesis (e.g., indomethacin) or of antagonists of PG action (chloroquine). The mechanism of the spasm may be associated with loss of negative feedback control of PG pathway by TXA2 (thromboxane). Oxygen may stimulate TXA2 production and reduce formation of vasoconstrictor PGs; the opposite effect is achieved with smoking due to formation of carboxyhaemoglobin. Estradiol and testosterone have no effect on hypoxic spasms; progesterone at physiological concentration blocks it entirely. Increased susceptibility to myocardial infarction of women on oral contraceptives is associated with reduced formation of endogenous progesterone, possibly the protective female hormone.
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PMID:The mechanism of coronary artery spasm: roles of oxygen, prostaglandins, sex hormones and smoking. 45 92

The effect of estradiol-17beta (1 mug per kilogram) on regional blood flow and cardiac output was studied by means of radionuclide-labeled microspheres in 6 nonpregnant and 13 pregnant ewes five to seven days after operation. Estradiol caused vasodilation in myometrium, endometrium, and placental cotyledons throughout pregnancy, but these responses were significantly less than the fifteenfold increase seen in the nonpregnant uterine tissues. Significant vasodilation also occurred in the ovaries, cervix, vagina, uterine tubes, mammary gland, skin, and adrenal glands of pregnant ewes. Cardiac output increased by 14%. No significant change in uterine oxygen consumption was associated with the increase in blood flow to the pregnant uterus.
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PMID:Effect of estradiol-17beta on blood flow to reproductive and nonreproductive tissues in pregnant ewes. 125 14

Although the relationships among body composition, training, and physical characteristics and 17 B-estradiol (estradiol) have been described in active amenorrheic women, little is known about these relationships in eumenorrheic women. This study examined the relationship between selected body composition and training variables, physical characteristics, maximal oxygen consumption (VO2max), luteinizing hormone (LH) and estradiol in eumenorrheic runners. Fifteen women (25.8 +/- 0.8 years) running 19.8 +/- 1.8 miles per week were studied during the midluteal phase of the menstrual cycle. Estradiol and LH were determined by radioimmunoassay. Body composition was measured by hydrostatic weighing. Age, Ponderal Index, and menstrual cycle length (days) were inversely related to estradiol (r = -0.56, r = -0.55, r = -0.52, respectively, p less than 0.05). A significant relationship (R2 = 0.91; p less than 0.05) was found among age, menstrual cycle length, LH (mIU/ml), VO2max (ml/kg/min), weight training (hr/wk), miles run per week, height (cm), additional aerobic training (hr/wk), relative body fat (%), and Ponderal Index and estradiol (pg/ml). These data suggest the midluteal concentration of estradiol in moderately trained eumenorrheic runners is the result of a complex interaction of many factors.
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PMID:Relationship of selected body composition and training variables to 17 B-estradiol in eumenorrheic runners. 179 12

The antifungal effects of two commercially available spermicidal gels (Conceptrol, produced by Ortho Pharmaceutical, Raritan, N.J., and Koromex, produced by Schmid Laboratories, Little Falls, N.J.) as well as pure nonoxynol-9 and boric acid (both components of vaginal contraceptive products) were tested against 50 clinical yeast isolates by the agar dilution method. The formulated products exerted comparable dose-dependent inhibitory effects against all yeasts tested. A 3-fold dilution of the formulated spermicidal products inhibited 90% of the yeast strains tested. To determine if the antifungal effect was due to the spermicidal detergent nonoxynol-9, this compound was tested for antifungal activity but was completely ineffective against Candida albicans in concentrations up to 10%. Boric acid, present in at least one of the products (Koromex), inhibited representative yeasts at a concentration of 0.4%. The relationship of pH and oxygen tension to inhibition by the commercial spermicides was also investigated. The pH values tested ranged from 4 to 7 and had little effect on inhibition; anaerobiosis at pH 7 slightly reduced the inhibitory activity of Conceptrol gel.
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PMID:Growth inhibition of Candida albicans and other medically important yeasts by vaginal contraceptive products. 216 85

N-Acyl dehydroalanines have shown free radical scavenging activity. They react with and scavenge mainly oxygen-derived free radicals such as the superoxide anion (O2-.) and the hydroxyl radical (HO.). Ortho-methoxyphenylacetyl dehydroalanine (AD-20) protects total-body irradiated mice against the toxicity induced by X-rays when delivered as a single dose of 700 rads in a short period of time. This degree of protection was of the same order of magnitude as that obtained with the aminothiol S-2-(3-aminopropylamino)-ethylphosphorothioic acid (WR-2721). The radioprotection of AD-20 is extended to all other doses of X-rays tested (from 600 to 800 rads). Furthermore, AD-20 inhibits the development of thymic lymphomas in C57Bl/Ka mice undergoing a leukaemogenic course of irradiation (4 x 175 rads applied at weekly intervals). We postulate that AD-20 may act as a radioprotector and anticarcinogenic agent, most probably by inactivating the oxygen-derived free radicals formed during water radiolysis.
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PMID:N-acyl dehydroalanines protect from radiation toxicity and inhibit radiation carcinogenesis in mice. 254 51

Three patients underwent single left lung transplantation for end-stage pulmonary fibrosis between June and November 1987. Preoperatively all were housebound, receiving continuous, supplemental oxygen, and their pulmonary function had deteriorated despite corticosteroid and cyclophosphamide therapy. Pulmonary preservation was by means of pulmonary arterial perfusion with modified Euro-Collins solution, 60 ml/kg, at 4 degrees C with adjunctive iloprost (synthetic prostacyclin) infusion. The heart from each donor was used successfully for transplantation. Good early graft function enabled extubation 11, 46, and 96 hours after transplantation. An omental wrap was used around the bronchial anastomosis, and bronchial healing was satisfactory in all. All patients had episodes of pulmonary rejection diagnosed by a combination of symptoms, chest x-ray infiltrates, the exclusion of pneumonitis by bronchoalveolar lavage, and prompt response to "pulse" steroid therapy. Two of the three patients had three episodes of opportunistic pulmonary infections: Herpes simplex pneumonitis, Pneumocystis carinii infection, and Aspergillus pneumonitis. The three patients were discharged from the hospital after 5, 6, and 7 1/2 weeks, respectively. The first and third patients remain alive and well, living essentially normal lives 24 and 19 months after transplantation with no evidence of arterial desaturation on exercise testing while breathing room air. The second patient had symptoms of deteriorating lung function with a progressive decline in forced expiratory volume in 1 second, vital capacity, and diffusion capacity despite repeated "pulse" therapy with combinations of methylprednisolone, antithymocyte globulin, and OKT3 (Ortho Diagnostic Systems Inc., Raritan, N.J.). An open lung biopsy specimen showed obliterative bronchiolitis, and this patient underwent orthotopic lung retransplantation, on the right side. Despite excellent early graft function and early extubation, he died of uncontrolled rejection and general debility after 3 weeks. This early experience in our center with two of three patients surviving 19 to 24 months, respectively, confirms the restoration of good pulmonary function and near normal life-style in patients with end-stage pulmonary fibrosis after single lung transplantation, as first reported by the Toronto Lung Transplant Group. We have used an alternative method of lung preservation (cold crystalloid pulmonary perfusion as opposed to topical cooling, used by the Toronto group), which provided excellent pulmonary preservation up to and beyond 4 hours' storage.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Early results of single lung transplantation in patients with end-stage pulmonary fibrosis. 267 9

The murine colonic perfusion model allows for the examination of absorption, metabolism, and portal transfer by the colon under physiologic conditions. This model was characterized by the use of four radiolabeled compounds: estradiol and Vitamin D3, both physiologically active circulating steroid compounds, and benzo[a]pyrene and N-acetylaminofluorene, xenobiotic carcinogens of the aromatic hydrocarbon and aromatic amide classes, respectively. Hemodynamic parameters and oxygen consumption of the preparation were stable throughout perfusion. Estradiol and N-acetylaminofluorene entered the portal vein at a rate of 2% of the lumenal dose per hour. Benzo[a]pyrene crossed at 0.4% of the lumenal dose per hour. The rate of transfer of Vitamin D3 was negligible. Analysis of the lumenal label revealed only substrate. In all experiments less than 0.02% of the applied substrate remained in the tissue compartment. Analysis of the vascular perfusate demonstrated evidence for sulfates of estradiol and N-acetylaminofluorene. Three conjugate classes were found associated with benzo[a]pyrene, constituting 42% of the portal label. Hydrolysis data suggests the presence of double conjugates of benzo[a]pyrene involving glutathione. In the case of aromatic hydrocarbons, conjugation, particularly thioether formation, implies hydroxylation and epoxide formation. For sulfation an N-acetylamino-fluorene ring or N-hydroxylation is required. The latter process could allow for the delivery of highly carcinogenic N-O sulfates to the liver.
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PMID:An isolated perfused model for the study of colonic metabolism and transport. 282 86

In Experiment 1, highly significant changes were observed over the estrous cycle in body weight gain, but not in food intake, daytime resting oxygen consumption or brown fat thermogenesis in Syrian hamsters. In Experiments 2 and 3, body weight and composition, food intake, resting oxygen consumption, and brown fat thermogenesis were measured following estradiol or estradiol plus progesterone treatment in ovariectomized hamsters. The significant changes in body weight could not be explained by changes in food intake, and were not accompanied by significant alterations in daytime oxygen consumption or brown fat thermogenic activity. In Experiment 4, resting oxygen consumption and body weight were measured every 6 hours over the estrous cycle. There was a striking absence of the usual nocturnal peak in resting oxygen consumption on the night of estrus (the night of the largest body weight gain). However, brown fat thermogenic activity did not differ among groups of hamsters killed on different nights of the estrous cycle. Estradiol-induced changes in energy storage may be mediated by changes in the daily rhythm of energy expenditure which are not dependent on alterations in brown fat thermogenesis.
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PMID:Effects of estrous cycles and ovarian steroids on body weight and energy expenditure in Syrian hamsters. 302 92


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