Antifertility Activities of Two Diphenyl-Dihydronaphthalene Derivatives

Duncan, Gary E.; Lyster, Stanley C.; Clark, John; Lednicer, Daniel

doi:10.3181/00379727-112-28070

Cited by 76 publications

(28 citation statements)

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“…It has been observed for many such compounds by Edgren & Calhoun (1960, for weak steroidal oestrogens by Huggins & Jensen (1955a), for weakly uterotrophic, non-steroidal aromatic substances by Lerner, Holthaus & Thompson (1958), Lerner, Turkheimer & Borman (1963) and Duncan, Lyster, Clark & Lednicer (1963), for androgens and progestins by Huggins & Jensen (19556) and Dorfman & Kind (1963),andforgluco-andmineralocorticoidsby Velardo & Sturgis (1955, 1956 and Velardo (1956). Many oestrogen antagonists have them¬ selves some positive hormonal activity although Dorfman & Kind (1963) (Hisaw, Velardo & Goolsby, 1954) and norethynodrel-oestrone (Edgren, 1958).…”

Section: Methodsmentioning

confidence: 99%

The Interaction in the Immature Mouse of Potent Oestrogens With Coumestrol, Genistein and Other Utero-Vaginotrophic Compounds of Low Potency

Folman¹,

Pope²

1966

Journal of Endocrinology

130

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SUMMARYInteraction in the immature mouse of potent oestrogens with the weak utero-vaginotrophic (UV) compounds, coumestrol, genistein, di methyl \x=req-\ stilboestrol, norethisterone acetate and megestrol acetate though sometimes additive at very low doses appeared to be essentially antagonistic at higher doses.In particular, the weak oestrogens coumestrol and genistein, found in certain plants, markedly inhibited the UV action of potent oestrogens, e.g. oestradiol-17\g=b\, oestrone and diethylstilboestrol and this effect may account in part for the anti-oestrogenic activity of extracts of these plants.Some differences in the ability of different oestrogens to promote uterine growth relative to vaginal growth were observed.

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Section: Methodsmentioning

confidence: 99%

The Interaction in the Immature Mouse of Potent Oestrogens With Coumestrol, Genistein and Other Utero-Vaginotrophic Compounds of Low Potency

Folman¹,

Pope²

1966

Journal of Endocrinology

130

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“…Antiestrogens like CI628 and nafoxidine usually have weak estrogenic (Duncan et al, 1963;Callantine et al, 1966) and progestational activity (Emmens and Martin, 1964). Nafoxidine administered for 6-12 wk produced in most rats a state of permanent diestrus (Heuson et al, 1972).…”

Section: Uterusmentioning

confidence: 99%

Endogenous peroxidase: specific marker enzyme for tissues displaying growth dependency on estrogen.

Anderson¹,

Kang²,

DeSombre³

1975

The Journal of Cell Biology

106

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Data derived from a correlated morphological and biochemical study suggest the following: (a) estradiol-17~, diethylstilbestrol, the estrogen antagonists nafoxidine (Upjohn 11,100), and Parke Davis CI628 induce synthesis of an endogenous peroxidase in the epithelium of target tissues like the vagina, the cervix, the uterus, and in the acinar cells of the estrogen-dependent rat mammary tumor; (b) peroxidase is a "specific" secretory protein of the estrogen-sensitized uterine endometrium; (c) peroxidase synthesis is not a nonspecific response to steroid hormone action, since progesterone and testosterone do not induce its synthesis; (d) endogenous peroxidase is a possible diagnostic protein for the detection of estrogen-dependent growing tissues, including breast cancer; (e) movement of exogenous horseradish peroxidase from the interstitium to the uterine lumina is restricted by tight junctions located at the apices of epithelial cells. Estrogen and antagonists do not appear to influence the transepithelial movement of exogenous peroxidase into the lumen.The uterus, cervix, vagina, and mammary gland of mammals require estrogen for their postpubertal trophic development and for the maintenance of their differentiated state. Indeed, the presence of estrogen-binding proteins (estrogen receptors or estrophiles, Jensen et al., 1966 a) in these tissues and of estrogen dependency of rat and human mammary carcinoma are well documented (Huggins et al., 1959; Jensen et al., 1966 b;Heuson et al., 1972).In the course of our investigation it was discovered that tissues displaying growth dependency on estrogen synthesize and secrete "specific marker proteins" into their lumina. These results show (a) that synthesis of peroxidase ~ (or a hemoprotein with peroxidatic activity) is a consistent marker for estrogen-dependent tissues (carcinogen-induced rat mammary carcinoma, cervix, vagina, and uterus), (b) estrogen antagonists (Upjohn 11,100; ~Throughout this paper, the DAB-positive reaction product will be referred to as peroxidase, since uterine peroxidase is a well-documented enzyme (see text) and since the histochemical medium employed is designed to demonstrate peroxidase activity. It is of course possible that what is being visualized in either a hemeprotein, which may possess peroxidase activity, or several substances with peroxidasic activity. The biochemical characterization of this enzyme as a peroxidase is still very limited.

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“…11,100) behaves in vivo as an anti-estrogen as well as a slight estrogenic compound on the rat uterus [1][2][3]. Its mechanism of action is unknown although it was suggested that it could act by competing with estradiol for binding to its receptor(s) in the target organ [4].…”

Section: Introductionmentioning

confidence: 99%

Binding properties of an anti‐estrogen to the estradiol receptor of uterine cytosol

Rochefort¹,

Capony²

1972

FEBS Letters

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Antifertility Activities of Two Diphenyl-Dihydronaphthalene Derivatives

Cited by 76 publications

References 0 publications

The Interaction in the Immature Mouse of Potent Oestrogens With Coumestrol, Genistein and Other Utero-Vaginotrophic Compounds of Low Potency

The Interaction in the Immature Mouse of Potent Oestrogens With Coumestrol, Genistein and Other Utero-Vaginotrophic Compounds of Low Potency

Endogenous peroxidase: specific marker enzyme for tissues displaying growth dependency on estrogen.

Binding properties of an anti‐estrogen to the estradiol receptor of uterine cytosol

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