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At least 109 records · Page 6Linked to original sources
PubMed1976

Studies on drug-induced lipidosis: VII. Effects of bis-beta-diethyl-aminoethylether of hexestrol, chloroquine, homochlorocyclizine, prenylamine, and diazacholesterol on the lipid composition of rat liver and kidney.

4,4'-Bis (beta-diethylaminoethoxy)-alpha, beta-diethyldiphenylethane (DH), which had been shown to induce a type of lipidosis resembling Niemann-Pick disease, was given to rats at a dose of 20, 50, 100, and 150 mg/kg body weight per day for 1 or 2 weeks. An enlargement of the liver with marked increases in free cholesterol, total phospholipids, and phosphatidylinositol took place by administration of a larger dose. The increase in bis (monoacylglyceryl) phosphate (BMGP), which is peculiar to this kind of drug-induced lipidosis, was dependent upon the dose of the drug as well as the length of time. Similar changes were also observed in kidney. Among several other drugs tested, chloroquine and diazacholesterol brought on as much increase in BMGP as treatment with DH.

Animals↗
PubMed1987

Inhibition of microtubule polymerization by synthetic estrogens: formation of a ribbon structure.

Dienestrol, meso-hexestrol, and dl-hexestrol, synthetic nonsteroidal estrogens, were shown to be inhibitors of microtubule assembly in vitro using microtubule proteins isolated from porcine brains. The order of activity of the synthetic estrogens as inhibitors of microtubule assembly is: dienestrol greater than diethylstilbestrol greater than meso-hexestrol greater than dl-hexestrol greater than isodienestrol. The activity of dienestrol as an inhibitor was of the same order as that of (+)-griseofulvin, as determined by turbidity measurement. Electron microscopic observation revealed that twisted ribbon structures are formed from microtubule proteins in the presence of some synthetic estrogens (dienestrol, meso-hexestrol, and dl-hexestrol).

Animals↗
PubMed1994

Bivalent ligands as probes of estrogen receptor action.

The estrogen receptor (ER) is a hormone-regulated transcription factor which is thought to bind to specific DNA sequences as a homodimer. In order to better understand structural requirements for dimerization and its functional role in ER action, we synthesized a series of bivalent ligands based on the non-steroidal estrogen hexestrol. These molecular probes join two hexestrol molecules of the erythro (E, active) configuration with either 4 or 8 carbon linkers (designated E-4-E and E-8-E series, respectively), or with longer linkers comprised of ethylene glycol units (E-eg-E series). Several other bi- and monovalent control compounds were prepared. The bivalent ligands bind to ER with a relative affinity 1-7% that of estradiol. While most of the ligands demonstrated normal monophasic displacement curves in competitive binding assays with [3H]estradiol, uncharacteristic biphasic competitive binding curves were seen for some of the ligands, indicating possible structure-specific, negative site-site interaction. In ER-deficient Chinese hamster ovary (CHO) cells transfected with an expression vector encoding ER, one series of bivalent ligands (E-4-E) had little stimulatory activity and inhibited transcription stimulated by hexestrol, as determined by a transient transfection assay using an estrogen-responsive reporter gene construct [(ERE)2-TATA-CAT, containing two estrogen response elements linked to a TATA promoter and the chloramphenicol acetyl transferase reporter gene]. Monovalent or control bivalent ligands failed to antagonize hexestrol-stimulated activity and were as fully active as hexestrol itself. Studies performed in MCF-7 human breast cancer cells, which contain endogenous ER, yielded similar bioactivity profiles for the E-4-E bivalent inhibitory ligands, showing them to be effective estrogen antagonists, when using either induction of progesterone receptor or (ERE)2-TATA-CAT transcriptional activation as the endpoint. The E-8-E ligand, however, acted as a partial agonist/antagonist of ERE-reporter gene transactivation and a full agonist of progesterone receptor induction in MCF-7 cells, thus showing cell- and response-specific differences in the effects of this bivalent ligand. These bivalent ligands for ER do not show enhanced potency or receptor binding affinity; however, some of them display binding properties that suggest the possibility of structure-specific negative site-site interaction, and some of them function as quite effective estrogen antagonists.

Animals↗
PubMed1984

Effect of high doses of synthetic estrogen on lipid metabolism in castrated male rats.

The mechanism by which high doses of estrogen influences lipid metabolism was studied with a microtubular blocking agent. Castrated male rats received oral injection daily for 14 days of 3 mg hexestrol in olive oil, or oil alone as controls. About half of the animals in each group were injected intraperitoneally with 4 mg/100 g body weight colchicine 3 hr before they were killed. Hexestrol treatment caused an accumulation of esterified cholesterol in the liver while it decreased those in serum. Triglyceride concentrations slightly decreased in the liver but were unaffected in serum. On polyacrylamide-gel disc electrophoresis, the peaks of high density lipoproteins (HDL) and low density lipoproteins (LDL) were decreased remarkably. Electron microscopic examination of hepatocytes revealed electron-lucent lipid droplets in the cytoplasm. After a colchicine treatment of the control animals, concentrations of esterified cholesterol and triglycerides markedly increased in the liver, while those in serum decreased. Electron microscopic examination of hepatocytes revealed numerous secretory vesicles filled with nascent VLDL. In hexestrol-treated animals, the colchicine treatment was associated with marked decreases in serum-esterified cholesterol and triglyceride as seen in the controls. However, there were no further increases of esterified cholesterol in the liver, and the increase of triglycerides was slight. Electron microscopic examination showed less secretory droplets than in the controls. These data suggest that very low density lipoproteins (VLDL) synthesis in the liver of hexestrol treated rats was inhibited. An accumulation of esterified cholesterol with a marked decrease in serum could not be accounted for by the inhibition of lipoproteins secretion, but rather by their enhanced entry into the liver.

Animals↗
PubMed1984

[Effectiveness of 5-fluorouracil combined with hormones in low dose as a basal treatment for prostatic carcinoma].

In the treatment of prostatic carcinoma, administration of some therapeutic agents, e.g. hormones, continuously as a basal treatment, and other proper treatment, e.g. irradiation or chemotherapy or both, were combined for occasional recurrence of the disease as additional treatment. Effectiveness of 5-fluorouracil in combination with hormones (estrogen or gestagen) in low doses, as a basal treatment, was compared with that of hormones alone in high doses. 5-Fluorouracil at 200 mg/day doses combined with gestagen (allylestrenol or chloromadinone acetate) at 50 mg/day doses was compared with estrogen (hexestrol) at 60 mg/day doses in 30 randomized patients with previously untreated prostatic carcinoma. On the other hand, 5-fluorouracil at 200 mg/day doses combined with hexestrol at 30 mg/day doses was compared with hexestrol at 60 mg/day doses also in 26 randomized patients with carcinoma already well controlled by hexestrol at 60 mg/day doses for more than two years. In patients of the former group treated with 5-fluorouracil and gestagen the rate of recurrence was 20%, mean effective period of therapy was 69 months and 5-year survival rate was 73%, although, in patients treated with high dose estrogen, the rate of recurrence was 60%, mean effective period was 43 months and 5-year survival rate was 55%. At occasional recurrence of the disease, in nearly half the patients in both groups, the disease responded to additional treatments and remission was obtained again. In patients of the latter group with already well controlled disease, no significant difference in prognosis was observed between patients treated with 5-fluorouracil plus low dose estrogen and those treated with high dose estrogen alone.(ABSTRACT TRUNCATED AT 250 WORDS)

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