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)

Optimal conditions for prolonged in vitro synthesis of RNA in isolated chicken liver nuclei have been described. It is shown by incorporation of gamma32P-GTP into RNA, analysis of the product on sucrose density gradient, and digestion with alkaline phosphatase and ribonuclease A that there is reinitiation of RNA synthesis. Polynucleotide kinase activity has been ruled out as explanation for the incorporation of gamma32P-GTP. alpha-Amanitin inhibits RNA synthesis by about 50%. Nuclei prepared from estradiol-treated chicks have twice the RNA synthesis activity as the controls. RNA is synthesized in the presence of Hg-UTP and the mercurated product separated by affinity chromatography on sulfhydryl-Sepharose column under stringent conditions. Vitellogenin mRNA sequences are measured by hybridization with DNA complementary to vitellogenin mRNA. Estradiol treatment leads to a 10-fold increase in vitellogenin mRNA sequences.
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PMID:In vitro RNA synthesis and expression of vitellogenin gene in isolated chicken liver nuclei. 65 25

Ethinyl estradiol treatment to female rats resulted in increased levels of serum alkaline phosphatase, but was not associated with any other manifestation of toxicity such as increased serum transaminases or toxic lesions. Elevated serum alkaline phosphatase seen in rats treated with chloroform was associated with frank hepatotoxicity. Induction of hepatic drug metabolising enzymes in rats by phenobarbitone treatment did not result in raised serum alkaline phosphatase levels. Estradiol benzoate treatment to rats also did not increase serum alkaline phosphatase levels. Ethinyl estradiol also resulted in increased alkaline phosphatase content in the liver, intestine and bone. The raised intestinal alkaline phosphatase content of rats treated with phenobarbitone or estradiol benzoate was not associated with an increase in the serum levels. There was histochemical evidence of induction of canalicular alkaline phosphatase in the liver in Ethinyl Estradiol treatment. The study of the electrophoretic separation of serum alkaline phosphatase of ethinyl estradiol treated rats revealed the presence of a new fast moving fraction, similar to those seen in bile duct ligated rats. It is concluded that the serum alkaline phosphatase increase during ethinyl estradiol treatment at least in part is from the liver, due to new synthesis.
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PMID:Serum alkaline phosphatase elevation in female rats treated with ethinyl estradiol. 67 18

18 women were treated with Deposition (4th, 11th, and 18th cycle day each, 1 mg 17alpha-Ethynyl-3-isopropylsulfonyloxy-Estradiol; 25th cycle day, 10 mg norethisterone acetate). When these medicines were taken, the activities of aminotransferases, alkaline phosphatase and alpha-amylase, cholesterol, total bilirubin and proteins of the serum, TTT, and indocyanine green were measured. A little significant decrease of the activity of alaninamino transferase (GPT) was to be stated. Whereas at the end of the 6th cycle the TTT as well as the contents of total proteins and albumin, showed a little significant decrease and the contents of alpha-2-globulin, beta-globulin as well as cholesterol were statistically shown to grow. The indocyanine green elimation was longer at the end of the 6th cycle without any pathological worth from the clinical point of view being proved.
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PMID:[Liver function tests after a 6-month deposiston therapy]. 118 58

The effect of ipriflavone (IP) on the proliferation and differentiation of rat osteoblast-like (ROB) cells and human periodontal ligament fibroblasts (HPLF) was studied in the presence and absence of estrogen. ROB cells were isolated from newborn rat calvaria by sequential collagenase digestion and HPLF from the outgrowth of human periodontal ligament in culture. The alkaline phosphatase (ALP) activity, employed as a marker of bone cell differentiation, was significantly enhanced by IP in both cell types; however, the concentration at which IP had a maximal effect was lower in ROB cells than in HPLF (10(-10) versus 10(-7) M, respectively). Cell proliferation judged by DNA content was either constant (ROB cells) or slightly increased (HPLF) by IP up to 10(-10) M, and decreased significantly above that concentration. In addition, the dose-dependent effect of estrogen on the growth and differentiation of each cell type in the presence and absence of IP was also tested. At the concentrations of IP which showed maximum effects in the induction of ALP, 10(-10) M for ROB cells and 10(-7) M for HPLF, IP inhibited DNA increase in an estrogen-independent manner. Estradiol (10(-11)-10(-9) M) itself increased the growth rate of both cell types significantly in a dose-dependent manner. Regardless of the concentrations of estradiol tested, ALP activities of both ROB cells and HPLF were elevated by the addition of IP. The ratio of ALP in the presence and absence of IP was similar over the range of estradiol concentrations tested.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Effect of ipriflavone and estrogen on the differentiation and proliferation of osteogenic cells. 142 78

A 31-year old mother of a 3-year old child visited a rheumatologist complaining of pain in both wrists, nose bleeding, and headaches. Since her delivery her weight dropped 12 kg and she has taken Synthroid daily. Before her pregnancy, she took the combined oral contraceptive (OC) Norinyl for 7 years. After childbirth, she took the OC Ortho Novum 1/80. She did not smoke or abuse drugs or alcohol. She did not have a history of hepatic or gastrointestinal diseases. Her alkaline phosphatase and glutamyl transferase levels were higher than normal (632 IU/L and 142 IU/L vs. =or 110 IU/L and =or 55 IU/L, respectively). Other liver function tests, her electrolytes, and her complete blood cell count were not unusual. She underwent an abdominal computed tomography scan and ultrasonography which indicated a single right hepatic lobe lesion (9 cm in diameter). It was well vascularized and circumscribed (12 x 10.5 cm) with big arteries leading to the immediate subcapsular region. The veins and arteries of the other lobe and the spleen appeared normal. Based on these tests, surgeons removed a segment of the right liver. She recovered well. 18 months after surgery, she was in good health. Pathologic examination of the 748 gm segment revealed that endothelial cells lined the sinusoidal spaces indicating true sinusoidal ectasia. The segment also exhibited individual hepatocyte atrophy and necrosis and inflammatory reaction and early fibrosis. Bile ducts had proliferated many portal spaces. Hepatic sinusoidal ectasia may be a forerunner of focal nodular hyperplasia.
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PMID:Hepatic sinusoidal ectasia. 164 40

A human endometrial tumor (Ishikawa) cell line in culture responded to estradiol stimulation, as measured by growth and alkaline phosphatase activity. These effects were similar whether the medium was enriched with serum or was serum-free. Estradiol increased placental alkaline phosphatase activity 2-3-fold over control in these Ishikawa cells. The mechanism for this increase appeared to be at the level of transcription, at least in part, since there was an increase in the concentration of placental alkaline phosphatase mRNA. The administration of tamoxifen or 4-hydroxytamoxifen was unable to antagonize the estradiol-stimulated alkaline phosphatase enzyme activity or mRNA expression. The administration of tamoxifen alone had no effect on alkaline phosphatase enzyme activity, but tamoxifen did stimulate the steady state concentration of alkaline phosphatase mRNA. In contrast, a new antiestrogen, ICI 164,384, was able to antagonize both of these estradiol-stimulated effects.
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PMID:Estrogen regulation of placental alkaline phosphatase gene expression in a human endometrial adenocarcinoma cell line. 233 23

Aspartate aminotransferase, alanine aminotransferase, gamma-glutamyltransferase, and alkaline phosphatase activities in the blood serum of women taking the oral contraceptive preparation Microgynon through extended periods were raised; the activity of cholinesterase was simultaneously reduced. In rats liver homogenates ethynylestradiol, one of the active components of Microgynon, acted as an inducer of gamma-glutamyltransferase and alkaline phosphatase while leaving aspartate aminotransferase and alanine aminotransferase unaffected, but reduced the level of cholinesterase. Norgestrel, the other active component of the preparation, suppressed the biosynthesis of gamma-glutamyltransferase and alkaline phosphatase while leaving aspartate aminotransferase, alanine aminotransferase and cholinesterase levels unaffected. A mixture of ethynylestradiol plus norgestrel in the mass proportion occurring in Microgynon produced the same effects upon gamma-glutamyltransferase and alkaline phosphatase as ethynylestradiol alone. Estradiol, the parent hormone of ethynylestradiol, lacked the inducing capability of the latter while ethynylpropargyl chloride induced gamma-glutamyltransferase and alkaline phosphatase so it was concluded the inducing effect of ethynylestradiol must be ascribed to the ethynyl radical. Progesterone, the parent of norgestrel, shared the latter's suppressive activity for gamma-glutamyltransferase and alkaline phosphatase biosynthesis, and behaved like its derivative towards the other enzymes.
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PMID:Changes of activities of some transferases, alkaline phosphatase and cholinesterase in the blood of women using oral contraceptives and in vitro influence of these agents on tissular enzyme levels in rat liver. 260 59

In the introduction of the paper the authors explain that it is essential to adopt effective preventive provisions to prevent the loss of osseous tissue in women after the menopause and to prevent osteoporotic fractures. In Bohemia and Moravia during the last 20 years the incidence of these frequently fatal or invalidating fractures of the proximal femur has increased substantially and in view of the ageing of the population it may be assumed that this trend will proceed further. Among possible preventive provisions, in order to eliminate undesirable metabolic side-effects of long-term hormonal substitution treatment, it seems best to administer by the parenteral route natural oestradiol by using the transdermal therapeutic Estraderm TTS system. Its effectiveness in suppressing menopause-induced enhanced bone resorption was tested in 11 women where on average within three months after bilateral ovariectomy increased bone resorption was found. In all women in the course of four months treatment all biochemical indicators of bone remodelling became normal - urinary excretion of hydroxyproline, acid plasma phosphatase activity, serum alkaline phosphatase isoenzyme, and serum osteocalcin. The dynamics of indicators of osteoresorption were similar as in women treated with oral synthetic oestrogen, which may produce, however, serious metabolic side-effects. Substitution treatment with Estraderm improves significantly also other manifestations of the climacteric oestrogen deficiency syndrome. Its safety is further enhanced by combination with progesterone.
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PMID:[Transdermal estradiol in the prevention of the menopause-induced increase in osteoresorption]. 280 95

To investigate some biochemical changes during bovine follicle development, ovaries were obtained from cyclic heifers (7 to 11 heifers/d on each day of the 21-d estrous cycle; N = 152). Follicular fluid from the two largest follicles from both ovaries and a pool from small follicles (N = 30/cow) were collected from each animal and analyzed for ionic, enzymatic and endocrine changes in relation to day of the estrous cycle, follicle size, rank and atretic or growing status. Follicular fluid alkaline phosphatase activity and ascorbate concentrations were highest in all follicular sizes during the earlier portion of the estrous cycle (d 1 to 12; P less than .05), then decreased to the lowest levels (d 13 to 21). As follicular size (diameter) increased lactate dehydrogenase (LDH), acid and alkaline phosphatase activity was reduced in follicular fluid (P less than .05). Alkaline phosphatase and LDH activity tended to be increased in atretic follicles (P less than .10), and was correlated with increased progesterone and androgen concentrations of follicular fluid (r = .4, P less than .05). Both albumin and total protein concentrations decreased as follicular diameter increased (P less than .05). Sodium concentrations in follicular fluid were greater in growing-antral than atretic follicles, and increased with follicular enlargement (P less than .05). Follicular potassium concentrations increased as the estrous cycle progressed (P less than .05), and tended to be elevated in atretic follicles (nonsignificant). Both Ca and Mg concentrations increased with follicular enlargement (P less than .05). Dehydroepiandrosterone and testosterone were the predominant androgens in follicular fluid (androstenedione, the lowest concentration); their concentration decreased with follicle development (P less than .05), but were quite variable. Estradiol was increased in growing follicles (P less than .01). Estrone and estradiol concentrations increased as ovulation approached, particularly in small follicles (less than or equal to 4 mm diameter). Changes of biochemical components found in follicular fluid that relate to the growth and atresia process may provide a more sensitive and accurate method to classify follicle status, and thus aid in understanding the complexity of events associated with maturation of the bovine follicle and oocyte.
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PMID:Biochemical analysis of bovine follicular fluid: albumin, total protein, lysosomal enzymes, ions, steroids and ascorbic acid content in relation to follicular size, rank, atresia classification and day of estrous cycle. 357 Oct 24

Bone metastases of breast cancers produce not only osteolytic but also osteosclerotic lesions. The latter are often observed after androgenic treatment of the tumor. Potential production of osteoblast stimulating activity (ObSA) in breast cancer cell lines, and possible androgen control of this activity have been investigated. Conditioned media (CM) collected from 4 breast cancer cell lines (MCF-7, ZR75, MDA-MB 231, BT20) was tested in vitro on ROS 17/2,8 osteoblast-like cells and on osteoblasts derived from human bone biopsies. The parameters monitored in osteoblasts were [3H]thymidine incorporation, alkaline phosphatase activity, and osteocalcin secretion. Serum-free media conditioned during 24 h by MCF-7 cells presented the highest ObSA. CM decreased thymidine incorporation in DNA and increased alkaline phosphatase activity in a dose-dependent manner. Bone GLA protein (osteocalcin) secretion by human osteoblasts was not increased however in the presence of CM. MCF-7 cells were cultured in the presence of dihydrotestosterone (DHT) [1-100 nM] for 5 days. Serum-free, DHT-free CM collected after an additional 24 h, contained alkaline-phosphatase stimulating activity which was DHT dose-dependent. Estradiol and 1,25(OH)2D3 failed to elicit a comparable increase of the ObSA in the CM. In conclusion, MCF-7 cells product factor(s) that interfere with bone remodeling. The DHT modulation of ObSA parallels the estradiol control of MCF-7 cells osteolytic lesions in relation with Prostaglandin E secretion. Sex hormones at physiological and pharmacological levels might thus control both osteosclerotic and osteolytic lesions observed in bone deposits of hormone dependent cancers.
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PMID:Androgens increase osteoblast-stimulating activity of human breast cancer cells in vitro. 370 24


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