Abstract：
:The activity of 18 vitamin D analogs on soft tissue calcification and growth impairment in neonatal rats and their effect on bone calcium mobilization, intestinal calcium absorption and binding to intestinal 1,25-dihydroxyvitamin D3 receptors in adult rats were compared. Depending on the chemical modification of the vitamin D parent compounds, they could be separated into active and inactive analogs. Cholecalciferol and ergocalciferol were similarly active, but epimerization of ergocalciferol at carbon 23 caused loss of activity. Hexafluorination at carbon 26 and 27 and the introduction of a double bond at carbon 22 or 23 had no or little effect on the activity. The loss of activity was caused by the introduction of a triple bond at carbon 23 and by hydroxylation at carbon 23, 26 or 28. The differentiation of human promyelocytic leukemia cells (HL-60) induced by these derivatives was used as a parameter for antitumour activity. All six analogs, which markedly affected calcium metabolism, were highly active in HL-60 cells. However, at least three derivatives were highly active in the antitumour test but failed to induce hypercalcemia. Thus, these results indicate that it could be possible to develop medically useful vitamin D derivatives devoid of hypercalcemic side-effects.
journal_name
Arch Toxicoljournal_title
Archives of toxicologyauthors
Kistler A,Galli B,Horst R,Truitt GA,Uskoković MRdoi
10.1007/BF00303129subject
Has Abstractpub_date
1989-01-01 00:00:00pages
394-400issue
5eissn
0340-5761issn
1432-0738journal_volume
63pub_type
杂志文章abstract：:Platinum coordination complexes (PtCx) are potent against several types of cancer but are often nephrotoxic. With a view to developing a PtCx nephrotoxicity model, the toxicity of cisplatin (cDDP), transplatin (tDDP) and carboplatin (CBDCA) was studied in primary cultures of rabbit proximal tubule (RPT) cells and in t...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF01973705
更新日期：1993-01-01 00:00:00
abstract：:The covalent binding of 14C-1,1,2-trichloroethylene (14C-TRI) metabolites to calf thymus DNA in vitro and to RNA and DNA of mouse brain, lung, liver, kidney, spleen, pancreas, and testis after repeated i.p. injections has been studied. Hydrolysates of DNA reacted with 14C-TRI in vitro and hydrolysates of RNA and DNA f...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF01239202
更新日期：1983-11-01 00:00:00
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：:Degradation of neurofilament (NF) proteins by Ca2+-activated neutral protease (CANP) was studied in the nervous system of rats treated with neurotoxic or non-neurotoxic compounds. In the tibial nerve, the degradation of NF 68K was depressed by five neurotoxic compounds: acrylamide, N-hydroxymetylacrylamide, N-isopropy...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00316261
更新日期：1988-08-01 00:00:00
abstract：:Second order rate constants for the initial reaction of 12 mammalian oxyhemoglobins (Hb) with equimolar phenylhydrazine (PHZ), a compound inducing Heinz body hemolytic anemia, were determined by recording continuous changes in absorbance with time at 577 nm. The rate constants were varied in a range from 43 m-1.s-1 wi...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s002040050161
更新日期：1995-01-01 00:00:00
abstract：:Female Wistar rats were treated with various doses of progesterone orally via the diet or via the SC route. Oral treatment resulted in enhanced progesterone levels in the liver as measured by radioimmunoassay. There were up to 3-fold increases in activity of ethylmorphine demethylation by isolated microsomes; metaboli...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00316323
更新日期：1986-10-01 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：:Mouse liver tumors that harbor activating mutations in Ctnnb1, encoding β-catenin, express high levels of various cytochromes P450 (CYP), including CYP2E1 and CYP1A2. Acetaminophen (AAP) is metabolized in hepatocytes by these CYPs to the reactive intermediate N-acetyl-p-benzoquinone-imine, which is toxic to hepatocyte...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-013-1030-8
更新日期：2013-08-01 00:00:00
abstract：:5-Hydroxymethylfurfural (HMF) and furfuryl alcohol (FFA) are moderately potent rodent carcinogens that are present in thermally processed foodstuffs. The carcinogenic effects were hypothesized to originate from sulfotransferase (SULT)-mediated bioactivation yielding DNA-reactive and mutagenic sulfate esters, a confirm...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-014-1392-6
更新日期：2016-01-01 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：:Manufactured nanomaterials (MNMs) selected from a library of over 120 different MNMs with varied compositions, sizes, and surface coatings were tested by four different laboratories for toxicity by high-throughput/-content (HT/C) techniques. The selected particles comprise 14 MNMs composed of CeO2, Ag, TiO2, ZnO and S...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-017-2106-7
更新日期：2018-02-01 00:00:00
abstract：:In his Nobel Prize Lecture of December 12, 1946, Hermann J. Muller argued that the dose-response for radiation-induced germ cell mutations was linear and that there was "no escape from the conclusion that there is no threshold". However, assessment of correspondence between Muller and Curt Stern 1 month prior to his N...
journal_title：Archives of toxicology
pub_type： 历史文章,杂志文章
doi：10.1007/s00204-011-0728-8
更新日期：2011-12-01 00:00:00
abstract：:pp'DDT (600 mg/kg, orally) produced an increase in the level of free ammonia and a decrease of acetylcholine in the corpus striatum of rats. These effects were maximal 5 h after the administration of pp'DDT. The animals showed tremors after 2 h, mild or moderate convulsions after 3.5 h and severe convulsions 5 h after...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00303292
更新日期：1980-05-01 00:00:00
abstract：:Carbromal is metabolized extensively in humans. The major metabolites known to date are bromoethylbutyramide, ethylbutyrylurea and inorganic bromide. After ingestion of a therapeutic dose of 1.0 g carbromal (4.2 mmoles) by four healthy volunteers highest concentrations in serum were found to be for carbromal 30 mumole...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00364653
更新日期：1978-06-16 00:00:00
abstract：:Recent work concerned with the mechanism underlying the development of organophosphorous compound-induced delayed neurotoxicity (OPIDN) is reviewed. Topics covered include the prophylaxis of OPIDN by phenylmethylsulfonyl fluoride and other agents, neurotoxic esterase (NTE) as measured using either labelled di-isopropy...
journal_title：Archives of toxicology
pub_type： 杂志文章,评审
doi：10.1007/BF00316365
更新日期：1989-01-01 00:00:00
abstract：:Using the rat liver foci bioassay a dose-response relationship was evaluated for the promoting activity of the ubiquitous and persistent environmental pollutants polychlorinated biphenyls (PCBs) and chloroform. Initiation of liver foci was performed by oral administration of a single dose of 8 mg/kg body wt of diethyl...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00296982
更新日期：1987-01-01 00:00:00
abstract：:False-negative judgment due to poor chemical solubility is a problem with in vitro skin sensitisation tests. Water-insoluble chemicals are typically dissolved in DMSO in most sensitisation tests but precipitate when diluted with medium beyond their solubility in water. Such tests lack procedures to rule out false-nega...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-020-02934-9
更新日期：2020-10-17 00:00:00
abstract：:The protective effects of various chelating agents such as D-penicillamine (D-PEN), 2,3-dimercaptosuccinic acid (DMSA), 2,3-dimercaptopropane sulphonate (DMPS), and N-(2-mercapto-2-methylpropanoyl)-L-cysteine (bucillamine), on the renal damage induced by gold sodium thiomalate (AuTM) in rats were studied. Rats were in...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF01973712
更新日期：1991-01-01 00:00:00
abstract：:In vitro assays are often used for the hazard characterisation of compounds, but their application for quantitative risk assessment purposes is limited. This is because in vitro assays cannot provide a complete in vivo dose-response curve from which a point of departure (PoD) for risk assessment can be derived, like t...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-013-1107-4
更新日期：2013-09-01 00:00:00
abstract：:Darbepoetin (DPO), an erythropoietin (EPO) derivative, was licensed in 2002 to treat patients with solid tumors suffering from chemotherapy-dependent anemia, although various tumors express EPO to improve vascularization, thus favoring tumor growth and spreading. Therefore, we wanted to investigate direct effects of D...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-013-1094-5
更新日期：2014-01-01 00:00:00
abstract：:Lead (Pb) exposure of consumers and the environment has been reduced over the past decades. Despite all measures taken, immission of Pb onto agricultural soils still occurs, with fertilizer application, lead shot from hunting activities, and Pb from air deposition representing major sources. Little is known about the ...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-020-02762-x
更新日期：2020-07-01 00:00:00
abstract：:The genotoxicity of the sensory irritant 2-chlorobenzylidene malonitrile (CS) to V79 Chinese hamster cells was investigated using the induction of gene mutations, micronuclei and DNA repair synthesis as biological endpoints. CS efficiently induced micronuclei and mutants resistant to 6-thioguanine in these cells, but ...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00278645
更新日期：1989-01-01 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：:Ochratoxin A (OTA) is a toxin produced by fungi such as Aspergillus spp. and Penicillium spp. The key target organ of OTA toxicity is the kidney, and it is known that epithelial-to-mesenchymal transition (EMT) leading to fibrosis is enhanced after long-term exposure of the kidney to OTA. However, the mechanisms respon...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-020-02829-9
更新日期：2020-09-01 00:00:00
abstract：:Cats were given vincristine sulfate (50 micrograms/kg i.v. every 4 days) and studied after 7-29 injections when neurological deficits became evident. The conduction velocity spectrum of individual afferent nerves from soleus muscles was shifted toward slower velocities. Relatively few functional muscle spindles or oth...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00319653
更新日期：1981-11-01 00:00:00
abstract：:Sulfur dioxide (SO2) is a common air pollutant, and inhaled SO2 in airway epithelium easily forms its soluble derivatives in vivo (bisulfite and sulfite), which are toxic to the respiratory system and related to the exacerbation of asthma. To investigate the effects of SO2 derivatives on the expressions of asthma rela...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-007-0212-7
更新日期：2007-12-01 00:00:00
abstract：:Many in the welding industry suffer from bronchitis, lung function changes, metal fume fever, and diseases related to respiratory damage. These phenomena are associated with welding fumes; however, the mechanism behind these findings remains to be elucidated. In this study, the lungs of cynomolgus monkeys were exposed...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-009-0486-z
更新日期：2010-03-01 00:00:00
abstract：:The present study was designed to evaluate the effects of chronic fluorosis on the dynamics (including fusion and fission proteins), fragmentation, and distribution of mitochondria in the cortical neurons of the rat brain in an attempt to elucidate molecular mechanisms underlying the brain damage associated with exces...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-012-0942-z
更新日期：2013-03-01 00:00:00
abstract：:The first withdrawal of certain polybrominated diphenyl ethers flame retardants from the US market occurred in 2004. Since then, use of brominated non-PBDE compounds such as bis(2-ethylhexyl)-2,3,4,5-tetrabromophthalate (BEH-TEBP) and 2-ethylhexyl-2,3,4,5-tetrabromobenzoate (EH-TBB) in commercial formulations has incr...
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/s00204-015-1489-6
更新日期：2016-03-01 00:00:00
abstract：:A pharmacokinetic profile of [14C] leptophos was determined in laying hens following a single oral dose of 400 mg/kg (0.58 muCi). Most of the radioactivity was excreted into the urine and feces. After 15 days, the total radioactivity recovered in the combined urinary-fecal excretion was 73.5% of the administered dose....
journal_title：Archives of toxicology
pub_type： 杂志文章
doi：10.1007/BF00351968
更新日期：1976-10-28 00:00:00
