Abstract：
:The cholestatic effect of the newly developed oestradiol sulphamate (J995) was compared with that of the natural oestrogen oestradiol (E) and of the cholestatic standard oestrogen ethinyloestradiol (EE). Female ovariectomized rats were orally treated for 7 days with oestrogen doses molar equivalent to 0.01, 0.1, 1, and 10 mg E/kg body wt. Bile flow, biliary bile acid and glutathione excretion as well as liver glutathione status were determined after bile duct cannulation under the influence of ketamine anaesthesia. For systemic oestrogen activity, the increase of uterine weight was measured. J995 showed the highest oestrogenic activity followed by EE and E. Impairment of bile flow and biliary glutathione excretion (GSH, GSSG) were found to be in the order E < J995 < EE. As all three oestrogens did not influence bile acid excretion, we postulate that mainly the bile acid-independent fraction of bile flow was inhibited, caused at least partly by impairment of canalicular glutathione transport. Based on the results of these studies, we conclude that a tenfold higher dose of J995 exhibited the same cholestatic effect as EE. Together with higher systemic oestrogenic activity, J995 may be used as a prodrug with reduced hepatic side-effects to replace EE in contraception strategies.
journal_name
Arch Toxicoljournal_title
Archives of toxicologyauthors
Barth A,Elger W,Schneider B,Schwarz Sdoi
10.1007/s002040050409subject
Has Abstractpub_date
1997-01-01 00:00:00pages
443-9issue
7eissn
0340-5761issn
1432-0738journal_volume
71pub_type
杂志文章abstract：:To evaluate the developmental neurotoxicity of arsenic in offspring rats by transplacental and early life exposure to sodium arsenite in drinking water, the pregnant rats or lactating dams, and weaned pups were given free access to drinking water, which contained arsenic at concentrations of 0, 10, 50, 100 mg/L from G...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-009-0403-5
更新日期：2009-06-01 00:00:00
abstract：:Cadmium, copper and zinc have been determined in kidney cortex, kidney medulla and liver from 51 cadmium-polluted and 122 nonpolluted autopsied subjects. Liver cadmium and zinc were significantly higher in the cadmium-polluted subjects than in the nonpolluted subjects. Kidney cadmium, copper and zinc were lower in the...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00316211
更新日期：1987-04-01 00:00:00
abstract：:Pyrrolizidine alkaloids (PAs) are widely occurring phytotoxins which can induce severe liver damage in humans and other mammalian species by mechanisms that are not fully understood. Therefore, we investigated the development of PA hepatotoxicity in vivo, using an acutely toxic dose of the PA senecionine in mice, in c...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-019-02582-8
更新日期：2020-01-01 00:00:00
abstract：:In female rats dosed orally with 14C-hexachlorobenzene the extent of intestinal absorption of carbon-14 has been found to be dependent on the form of application. When the substance was given as a solution in oil about 80% of the dose administered was absorbed, but when given as an aqueous suspension only 6%. In anima...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00353283
更新日期：1975-11-20 00:00:00
abstract：:Contents of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and of 16 further congeners--polychlorinated dibenzodioxins and dibenzofuranes (PCDD/PCDF)--were determined in lipids of adipose tissue and of livers of 3 stillborns and of 17 infants (0.43-44 weeks old) who died from sudden infant death syndrome. International to...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s002040050402
更新日期：1997-01-01 00:00:00
abstract：:The effect of acetone pretreatment (5% in drinking water for 10 days on rat liver metabolism and toxicity of thiobenzamide (TB) was investigated. Hepatic microsomes from acetone-pretreated rats showed a significant increase of TB-S-oxidation rate which, on the basis of selective thermal inactivation of FAD-containing ...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF01974397
更新日期：1990-01-01 00:00:00
abstract：:Berberine, a main protoberberine component of Coptidis Rhizoma, was studied for the mechanism of its inhibitory effects on the tert-butyl hydroperoxide (t-BHP)-induced cytotoxicity and lipid peroxidation in rat liver. In the preliminary study, berberine expressed an antioxidant property by its capacity for quenching t...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-002-0351-9
更新日期：2002-11-01 00:00:00
abstract：:Sotalol [4-(2-isopropylamino-1-hydroxyethyl)-methane-sulfonanilide hydrochloride] is a beta-adrenergic blocking agent. Despite the widespread use of these drugs, poisonings are not frequent. In this report the authors describe the first recorded case of fatal sotalol overdosage to their knowledge. The results of toxic...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00297587
更新日期：1980-01-01 00:00:00
abstract：:The ability of 3,5-diethoxycarbonyl-1,4-dihydrocollidine (DDC), 3,5-diethoxycarbonyl-4-ethyl-1,4-dihydro-2,6-dimethylpyridine (EDDC) and griseofulvin to induce porphyria in primary cultures of mouse hepatocytes has been examined. Exposure of cultured mouse hepatocytes to DDC, EDDC or griseofulvin resulted in a marked ...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF01974011
更新日期：1992-01-01 00:00:00
abstract：:Previous studies indicate that benzanthrone, an anthraquinone dye intermediate, caused significant depletion of ascorbic acid (AsA). In this investigation the effect of benzanthrone on the status of different forms of AsA and other bio-antioxidants such as glutathione (GSH) was studied. Oral administration of benzanth...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s002040100222
更新日期：2001-06-01 00:00:00
abstract：:Since teratogenicity testing in mammals is a particular challenge from an animal welfare perspective, there is a great need for the development of alternative test systems. In this context, the zebrafish (Danio rerio) embryo has received increasing attention as a non-protected embryonic vertebrate in vivo model. The p...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-020-02928-7
更新日期：2020-10-27 00:00:00
abstract：:The effect of various hepatotoxicants on urinary taurine and urinary creatine has been studied in the rat. Several hepatotoxic agents, carbon tetrachloride, thioacetamide, galactosamine and allyl alcohol which all caused hepatic necrosis (sometimes accompanied by steatosis), resulted in a rise in urinary taurine and i...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF01974343
更新日期：1993-01-01 00:00:00
abstract：:Although carbon nanotubes (CNTs) are promising nanomaterials, their potential carcinogenicity is a major concern. We previously established a genetic method of analyzing genotoxicity of chemical compounds, where we evaluated their cytotoxic effect on the DT40 lymphoid cell line comparing DNA-repair-deficient isogenic ...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-013-1084-7
更新日期：2014-01-01 00:00:00
abstract：:Tacrolimus (FK506) and cyclosporin A (CsA) are two potent immunosuppressants mainly metabolized by hepatic cytochrome P-450 3A (CYP3A) monooxygenase. The aim of this study was to compare the toxic effects of the two drugs on hepatocytes in primary culture as a function of their metabolism and to explore the variations...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s002040050499
更新日期：1998-04-01 00:00:00
abstract：:The effects of six iv infusions of an emulsion containing the plasticizer di(2-ethylhexyl) phthalate (DEHP) on the liver and testes were investigated in 40-day-old rats. Groups of five to six animals received the emulsion every other day in doses of 0, 5, 50 or 500 mg DEHP/kg body weight. Liver effects were studied by...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00348313
更新日期：1985-12-01 00:00:00
abstract：:Reduced gluconeogenesis due to decreased activity of key gluconeogenic enzymes in liver, together with feed refusal, has been suggested to play an important role in 2,3,7, 8-tetrachlorodibenzo-p-dioxin (TCDD)-induced lethality in rats. This study was carried out to further analyse the toxicological significance of red...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s002040050626
更新日期：1999-08-01 00:00:00
abstract：:Bisphenol A (BPA) is a chemical in widespread use that is under scientific discussion due to its endocrine activity. Controversies exist about how to interpret reportedly high blood concentrations measured in uncontrolled situations. Physiologically based pharmaco-/toxicokinetic modelling resulted in 10-100-fold lower...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-013-1022-8
更新日期：2013-07-01 00:00:00
abstract：:This study was performed to assess the relation between occupational exposure to N,N-dimethylformamide after an 8 h work shift in the acrylic fibre industry and its three biological markers N-methylformamide (NMFtotal), N-acetyl-S-(N-methylcarbamoyl)cysteine (AMCC), and N-methylcarbamoyl adduct at haemoglobin (MCVal)....
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-018-2219-7
更新日期：2018-07-01 00:00:00
abstract：:A recent study reported that exposure of student embalmers in Cincinnati to high concentrations of formaldehyde (2 mg/m3) reduced the activity of the DNA repair protein O6-methylguanine DNA methyltransferase (MGMT). Reduction in a DNA repair enzyme may strongly increase the cancer risk not only with respect to the rep...
journal_title：Archives of toxicology
pub_type： 临床试验,杂志文章,多中心研究
doi：10.1007/s002040050581
更新日期：1999-02-01 00:00:00
abstract：:The hypothesis that methylmercury (MeHg) potently induces formation of reactive oxygen species (ROS) in the brain is supported by observations on the neuroprotective effects of various classes of antioxidants. Flavonoids have been reported to possess divalent metal chelating properties, antioxidant activities and to r...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-009-0482-3
更新日期：2010-02-01 00:00:00
abstract：:Standard treatment of poisoning by organophosphates (OP) includes the administration of an antimuscarinic agent, e.g. atropine, and of an acetylcholinesterase (AChE) reactivator (oxime). The presently available oximes, obidoxime and pralidoxime (2-PAM), are considered to be insufficient for highly toxic OPs, e.g. sari...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-002-0375-1
更新日期：2002-09-01 00:00:00
abstract：:Zearalenone, a cereal mycotoxin with mycoestrogen activity and effect on fertility, is known to trigger apoptosis of a variety of nucleated cell types including hematopoietic progenitor cells. In analogy to apoptosis of nucleated cells, eryptosis, the suicidal death of erythrocytes, leads to cell shrinkage and cell me...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-013-1037-1
更新日期：2013-10-01 00:00:00
abstract：:The effects of cadmium exposure during pregnancy (by means of daily subcutaneous injections of 4.4 mumol/kg to the mother) on the neonates were investigated. No effect was observed on fetal or neonatal body weights, nor on neonatal liver weights. These parameters were examined up to 5 weeks after birth. The weight of ...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00334632
更新日期：1989-01-01 00:00:00
abstract：:Organophosphate-induced delayed polyneuropathy (OPIDP) is initiated by inhibition/aging of more than 70-75% of neuropathy target esterase (NTE). Di-n-butyl-2,2-dichlorovinyl phosphate (DBDCVP) (1 mg/kg s.c.) inhibited 96%, 86% and 83% of NTE in brain, spinal cord and peripheral nerve, respectively, and induced a typic...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00316450
更新日期：1989-01-01 00:00:00
abstract：UNLABELLED:An overdose of acetaminophen (APAP) causes hepatotoxicity due to its metabolite, N-acetyl-p-benzoquinone imine. NAD(P)H:quinone oxidoreductase 1 (NQO1) is an important enzyme for detoxification, because it catabolizes endogenous/exogenous quinone to hydroquinone. Although various studies have suggested the ...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-014-1340-5
更新日期：2015-11-01 00:00:00
abstract：:A number of industrial chemicals and therapeutic agents cause liver tumors in rats and mice by activating the nuclear receptor peroxisome proliferator-activated receptor α (PPARα). The molecular and cellular events by which PPARα activators induce rodent hepatocarcinogenesis have been extensively studied elucidating a...
journal_title：Archives of toxicology
pub_type： 杂志文章,评审
doi：10.1007/s00204-017-2094-7
更新日期：2018-01-01 00:00:00
abstract：:The effect of ethanol on metabolism of 20 nitriles was studied in vivo and in vitro in mice. The hepatic microsomal metabolizing activity for nitriles was at a maximum 13 h after ethanol dosing (4.0 g/kg). Using microsomes from mice pretreated with ethanol under the above conditions, enhancement of the in vitro metabo...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00340977
更新日期：1986-02-01 00:00:00
abstract：:Perfluorocarboxylic acids (PFCAs) including perfluorooctanoic acid (PFOA) are environmental pollutants showing high accumulation, thermochemical stability and hepatocarcinogenicity. Peroxisome proliferator-activated receptor α is suggested to mediate their toxicities, but the precise mechanism remains unclear. Previou...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-016-1888-3
更新日期：2017-06-01 00:00:00
abstract：:The effect of duration of employment at a North American cadmium smelter on urinary metallothionein (MT), total protein, beta 2-microglobulin (beta 2-MG), glucose, cadmium, copper and zinc of 53 men was studied. The levels of all urinary parameters increased with the duration of employment. Smoking history did not aff...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00295090
更新日期：1987-02-01 00:00:00
abstract：:Chronic ethanol consumption is a strong risk factor for the development of liver disease. Multiple mechanisms are involved in ethanol-mediated liver injury; oxidative stress being pointed has an important factor. However, it should be noted that moderate consumption of red wine has been associated with hepatoprotectiv...
journal_title：Archives of toxicology
pub_type： 杂志文章,评审
doi：10.1007/s00204-015-1538-1
更新日期：2015-10-01 00:00:00
