High Molecular Weight Enzyme Inhibitors. IV. Polymeric Phosphates of Synthetic Estrogens.

Diczfalusy, E.; Fernö, O.; Fex, H.; Högberg, B.; Kneip, P.; Palmstierna, H.

doi:10.3891/acta.chem.scand.13-1011

Cited by 8 publications

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“…A prolonged oestrogenic effect results from a single dose of PSP (Diczfalusy et al 1959). From the results we have obtained, the prolonged effect can be considered to depend upon the injected polymer PSP being accumulated in reticuloendothelial tissue.…”

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confidence: 83%

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Autoradiographic Distribution Studies of Injected 32p-Labelled Polydiethylstilboestrol Phosphate

Bengtsson

1963

Acta Endocrinologica

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The autoradiographic distribution pattern of intravenously injected 32P\ x=r eq-\ polydiethylstilboestrol phosphate (32P-PSP), in which the diethylstilboestrol molecules are linked by 32P-phosphate bonds, has been studied in mice. In accordance with previous findings with a PSP-preparation labelled with 14C in the diethylstilboestrol molecules an accumulation was seen in tissues rich in reticuloendothelial cells which are a probable depot for the macromolecule. Contrary to 14C-PSP no specific uptake of 32P was observed in tissues presumed to be targets for oestrogens. This indicates that only the monomolecular diethylstilboestrol and not the polymer shows affinity to the target sites.

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Section: Fig 2 Detail Frommentioning

confidence: 83%

“…The technique of synthesis of non-radioactive PSP has been described by Diczfalusy et al (1959). On the day of injection the activity of the 32P-PSP was calculated to be 3 microcuries per mg.…”

Section: Methodsmentioning

confidence: 99%

Autoradiographic Distribution Studies of Injected 32p-Labelled Polydiethylstilboestrol Phosphate

Bengtsson

1963

Acta Endocrinologica

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“…In the present study four long-acting oestrogens were used. Three of these, phosphate polymers of oestradiol, diethylstilboestrol and oestriol, are strong phosphatase inhibitors in vitro (FERNO et al 1958;DICZFALUSY et al 1959;KONYVES 1965). It was therefore considered that these polymerized oestrogens might have an action on the phophatases in the ventral prostate due to both their oestrogenic and their enzyme-inhibiting properties.…”

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confidence: 99%

Effects of Oestrogen on Phosphatase Activity in the Ventral Prostate of Intact, Castrated, and Androgen‐treated Castrated, Adult Rats

Andersson

Müntzing

1971

Acta Pharmacologica et Toxicologica

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Male rats were subjected to the following treatment: 1. Castration or treatment with the oestrogens polyoestradiol phosphate (PEP) (estradurin®), polydiethylstilboestrol phosphate (PSP), polyoestriol phosphate (SEP) (triodurin®), oestradiol‐17‐undecylate (EU) (progynon®‐depot), oestradiol‐3‐N‐[bis(2‐chloroethyl)]‐carbamate‐17‐dihydrogenphosphate (E) (estracyt®) or diethylstilboestrol diphosphate (H) (honvan®). PEP, PSP, SEP and EU were given as a single injection intramuscularly in a dose of 8 mg/kg, whereas E and H were given orally as water solutions (8 mg/kg) every second day. 2. Castration and treatment with the oestrogens. 3. Castration and treatment with testosterone‐3‐(p‐hexyloxyphenyl)‐proprionate (A) (andradurin®) (60 mg/kg intramuscularly in a single injection) and the oestrogens. – After 20 days the weight of the ventral prostate in group 1 was reduced to 85% by SEP, to 20% by E and to 10% by castration and the administration of other oestrogens. In group 2 the prostatic weight was reduced to 10%. In 3, A alone or combined with PEP, SEP, EU or E restored the prostatic weight. PSP reduced the prostatic weight to 75% and H to 65%. The alkaline phosphatase activity in group 1 was reduced to 55% by castration and increased to 135% by EU; in group 2 PEP, PSP, EU and E restored the activity; in group 3, A given alone restored the activity and A + PEP, PSP, EU or H increased the activity to 175–350%. The acid phosphatase activity in group 1 was reduced to 45% by castration, to 55% by H and to 70% by PSP. In group 2 PEP, PSP and E partly reversed the decrease brought about by castration; in 3, A given alone restored the activity, which was increased to 115–155% after A + PEP, PSP, H or E. Secretion from the ventral prostate of intact rats or castrated rats treated with A or A + PEP was squeezed out. The alkaline and acid phosphatase activities after A + PEP were approximately doubled. The findings indicate that oestrogen can affect the rat ventral prostate in ways other than by reducing the secretion of testicular androgens.

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Determination of β‐Glucuronidases

Fishman

1967

Methods of Biochemical Analysis

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High Molecular Weight Enzyme Inhibitors. IV. Polymeric Phosphates of Synthetic Estrogens.

Cited by 8 publications

References 0 publications

Autoradiographic Distribution Studies of Injected 32p-Labelled Polydiethylstilboestrol Phosphate

Autoradiographic Distribution Studies of Injected 32p-Labelled Polydiethylstilboestrol Phosphate

Effects of Oestrogen on Phosphatase Activity in the Ventral Prostate of Intact, Castrated, and Androgen‐treated Castrated, Adult Rats

Determination of β‐Glucuronidases

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