Orally Active Oestrogens and Progestins in Prevention of Pregnancy in Rats

Banik, U. K.; Revesz, C.; Herr, Fiona

doi:10.1530/jrf.0.0180509

Cited by 15 publications

(4 citation statements)

References 7 publications

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“…The animals were injected daily for 14 days at alternate sites by the subcutaneous route. This dose was chosen because it is anovulatory for the rat (Yang et al, 1969;Banik et al, 1969).…”

Section: Animalsmentioning

confidence: 99%

Effects of ethynyloestradiol on the metabolism of [1-14C]-oleate by perfused livers and hepatocytes from female rats

Weinstein

Soler-Argilaga

Werner

et al. 1979

Biochemical Journal

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Normal female rats were given 15mug of ethynyloestradiol/kg body wt. for 14 days and were killed on day 15 after starvation for 12-14h. The livers were isolated and were perfused with a medium containing washed bovine erythrocytes, bovine serum albumin, glucose and [1-(14)C]oleic acid; 414mumol of oleate were infused/h during a 3h experimental period. The output of bile and the flow of perfusate/g of liver were decreased in livers from animals pretreated with ethynyloestradiol, whereas the liver weight was increased slightly. The rates of uptake and of utilization of [1-(14)C]oleate were measured when the concentration of unesterified fatty acid in the perfusate plasma was constant. The uptake of unesterified fatty acid was unaffected by pretreatment of the animal with oestrogen; however, the rate of incorporation of [1-(14)C]oleate into hepatic and perfusate triacylglycerol was stimulated, whereas the rate of conversion into ketone bodies was impaired by treatment of the rat with ethynyloestradiol. Pretreatment of the rat with ethynyloestradiol increased the output of very-low-density lipoprotein triacylglycerol, cholesterol, phospholipid and protein. The production of (14)CO(2) and the incorporation of radioactivity into phospholipid, cholesteryl ester and diacylglycerol was unaffected by treatment with the steroid. The net output of glucose by livers from oestrogen-treated rats was impaired despite the apparent increased quantities of glycogen in the liver. The overall effect of pretreatment with oestrogen on hepatic metabolism of fatty acids is the channeling of [1-(14)C]oleate into synthesis and increased output of triacylglycerol as a moiety of the very-low-density lipoprotein, whereas ketogenesis is decreased. The effect of ethynyloestradiol on the liver is apparently independent of the nutritional state of the animal from which the liver was obtained. It is pertinent that hepatocytes prepared from livers of fed rats that had been treated with ethynyloestradiol produced fewer ketone bodies and secreted more triacylglycerol than did hepatocytes prepared from control animals. In these respects, the effects of the steroid were similar in livers from fed or starved (12-14h) rats. Oestrogens may possibly inhibit hepatic oxidation of fatty acid, making more fatty acid available for the synthesis of triacylglycerol, or may stimulate the biosynthesis of triacylglycerol, or may be active on both metabolic pathways.

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“…The animals were injected daily for 14 days at alternate sites by the subcutaneous route. This dose was chosen because it is anovulatory for the rat (Yang et al, 1969;Banik et al, 1969).…”

Section: Animalsmentioning

confidence: 99%

Effects of ethynyloestradiol on the metabolism of [1-14C]-oleate by perfused livers and hepatocytes from female rats

Weinstein

Soler-Argilaga

Werner

et al. 1979

Biochemical Journal

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“…It is well known that continuous E or combined E + P administration prevents the ovulation. The modern contraceptive medication is based on these observations [26,39–41]. Nowdays high percent of girls around puberty uses contraceptive hormones [42], in some cases the steroids are used as medication of acne vulgaris in this early age [43].…”

Section: Discussionmentioning

confidence: 99%

Sexual dimorphism in the effect of concomitant progesterone administration on changes caused by long-term estrogen treatment in pituitary hormone immunoreactivities of rats

et al. 2011

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SummaryBackgroundSince in clinical practice long-term estrogen (E) treatment is frequently applied, our aim was to study the effect of concomitant progesterone (P) administration on changes caused by long-term estrogen treatment in the secretion of LH, FSH, PRL and GH.Material/MethodsDiethylstilbestrol (DES), P or both in silastic capsules were implanted under the skin of prepubertal Sprague-Dawley male and female rats. Animals survived for two or five months. We have also studied whether the changed hormone secretion caused by DES can return to normal level 1 or 2 months after removing DES capsule.Results1.) The males more rapidly responded than females with decreasing basal LH release upon treatments. The basal FSH release was decreased only in males. The effect of DES persisted in males; however, in females basal LH and FSH levels were upregulated after removal of DES capsule. 2.) The basal GH levels were low in each group. The body weight and length were depressed by DES in both genders and P little blunted this effect. The body weight and length in males remained low after removal of DES capsule, in females it was nearly similar to intact rats. 3.) There was no sexual dimorphism in the effect of steroids on PRL secretion. In both genders DES extremly enhanced the PRL levels, P prevented the effect of DES. PRL levels returned to intact value after removal of DES influence. 4.) Removal of DES capsule reversed the changes in the immunohisto-chemical appearance of hormone immunoreactivities.ConclusionsThere was sexual dimorphism in the change of basal gonadotropic hormone and GH secretion but not of PRL upon DES and DES+P treatments. P was basically protective and this role may be mediated by P receptors locally in the pituitary gland.

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“…By contrast, the uterotrophic assay in immature rats or mice is less specific for oestrogenicity since androgens, progestins and even desoxycorticosterone (Velardo, 1959) Since AY-11483 gave a shallow dose-response curve like oestriol in the utero¬ trophic assay in rats and mice, this compound could also be classified as an "impeded estrogen" (Huggins & Jensen, 1955). Like oestriol, AY-11483 also has anti-oestrogenic action (Revesz, 1969, unpublished data) which is another property of an impeded oestrogen.…”

Section: Discussionmentioning

confidence: 99%

“…Furthermore, Haskins, Moszkowski & Whitelock (1968) A series of seventeen substituted oestradiol derivatives was synthesized and tested (Lefebvre, Marshall, Revesz, Banik & Deghenghi, 1967) in our labora¬ tories, of which 3-acetoxy-17a-[3-furyl]-l,3,5(10)-7-oestratetraen-17-ol (AY-11483) was investigated in detail. The contraceptive effect of this compound in rats was reported in a previous communication (Banik, Revesz & Herr, 1969). The purpose of this paper is to describe some oestrogenic parameters of AY-11483 Vaginal cornification test (Allen-Doisy test) The method described by Allen & Doisy (1923) was used with a slight modification (Revesz & Chappel, 1966) 325 g) and mice (25 to 30 g).…”

Section: Introductionmentioning

confidence: 99%

Ay-11483, a New Type of Orally Active Oestrogen

Revesz¹,

Banik²,

Lefèbvre³

1970

Reproduction

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Summary. The oral oestrogenic activity of AY-11483 has been compared to that of oestriol and mestranol. The compound shows significant activity in the vaginal cornification test in rats and mice; however, it has a relatively weak effect in the uterotrophic assay in rats, mice and rabbits. Furthermore, like oestriol, it exerts a weak effect on the endometrium in rabbits. Based on our findings, AY-11483 should be classified as an impeded oestrogen with possible clinical application.

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Orally Active Oestrogens and Progestins in Prevention of Pregnancy in Rats

Cited by 15 publications

References 7 publications

Effects of ethynyloestradiol on the metabolism of [1-14C]-oleate by perfused livers and hepatocytes from female rats

Effects of ethynyloestradiol on the metabolism of [1-14C]-oleate by perfused livers and hepatocytes from female rats

Sexual dimorphism in the effect of concomitant progesterone administration on changes caused by long-term estrogen treatment in pituitary hormone immunoreactivities of rats

Ay-11483, a New Type of Orally Active Oestrogen

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