Pharmacodynamics of cytochrome P450 2B induction by phenobarbital, 5-ethyl-5-phenylhydantoin, and 5-ethyl-5-phenyloxazolidinedione in the male rat liver or in cultured rat hepatocytes.

abstract：:NADPH in microsomes reduces the hydroxocob(III)alamin form of vitamin B12 to cob(II)alamin and the supernucleophilic cob(I)alamin, which are both highly reactive toward xenobiotic epoxides formed by mammalian metabolism of dienes such as the industrially important chemicals chloroprene and 1,3-butadiene. With styrene,...

journal_title：Chemical research in toxicology

authors： Watson WP,Munter T,Golding BT

更新日期：2004-12-01 00:00:00

abstract：:(R)-Thalidomide was oxidized to 5-hydroxythalidomide and 5'-hydroxythalidomide by NADPH-fortified liver microsomes from humans and monkeys. (R)-Thalidomide was hydroxylated more efficiently than (S)-thalidomide. Recombinant human P450s 3A4, 3A5, and 3A7 and monkey P450s 3A8 and 3A5 (coexpressed with NADPH-P450 reducta...

journal_title：Chemical research in toxicology

authors： Chowdhury G,Murayama N,Okada Y,Uno Y,Shimizu M,Shibata N,Guengerich FP,Yamazaki H

更新日期：2010-06-21 00:00:00

abstract：:Adverse effects of drugs (AEDs) continue to be a major cause of drug withdrawals in both development and postmarketing. While liver-related AEDs are a major concern for drug safety, there are few in silico models for predicting human liver toxicity for drug candidates. We have applied the quantitative structure-activi...

journal_title：Chemical research in toxicology

authors： Rodgers AD,Zhu H,Fourches D,Rusyn I,Tropsha A

更新日期：2010-04-19 00:00:00

abstract：:The measurement of metabolites constitutes a useful tool for detection of exposure and in pharmacokinetic studies. Epoxidation with subsequent glutathione conjugation and mercapturic acid formation is an important deactivation pathway for naphthalene, a toxin which presumably causes lung disease. The mercapturic acid ...

journal_title：Chemical research in toxicology

authors： Marco MP,Nasiri M,Kurth MJ,Hammock BD

更新日期：1993-05-01 00:00:00

abstract：:The current study examined the bioactivation potential of a nonpeptidyl thrombopoietin receptor agonist, 1-(3-chloro-5-((4-(4-fluoro-3-(trifluoromethyl)phenyl)thiazol-2-yl)carbamoyl)pyridine-2-yl)piperidine-4-carboxylic acid (1), containing a 2-carboxamido-4-arylthiazole moiety in the core structure. Toxicological ris...

journal_title：Chemical research in toxicology

authors： Kalgutkar AS,Driscoll J,Zhao SX,Walker GS,Shepard RM,Soglia JR,Atherton J,Yu L,Mutlib AE,Munchhof MJ,Reiter LA,Jones CS,Doty JL,Trevena KA,Shaffer CL,Ripp SL

更新日期：2007-12-01 00:00:00

abstract：:3-Methylindole (3MI) is a preferential pneumotoxicant found in cigarette smoke. A number of lung-expressed human cytochrome P450 enzymes, including 1A1, 2F1, and 2A13, catalyze the metabolism of 3MI to reactive intermediates that fragment DNA, measured with the Comet assay to assess DNA damage, in a cytochrome P450-de...

journal_title：Chemical research in toxicology

authors： Weems JM,Lamb JG,D'Agostino J,Ding X,Yost GS

更新日期：2010-11-15 00:00:00

abstract：:The Escherichia coli NarI restriction enzyme recognition site 5'G1G2C3G4C5C63' is a mutational hotspot for -2 deletions in E. coli plasmid pBR322, resulting in the sequence 5'GGCC3' when G4 is modified by the aromatic amine N-2-(acetyl)aminofluorene (AAF) [Burnouf, D., Koehl, P., and Fuchs, R. P. P. (1995) Proc. Natl....

journal_title：Chemical research in toxicology

authors： Roy D,Hingerty BE,Shapiro R,Broyde S

更新日期：1998-11-01 00:00:00

abstract：:Exposure to arsenic affects large human populations worldwide and has been associated with a long list of human diseases, including skin, bladder, lung, and liver cancers, diabetes, and cardiovascular disorders. In addition, there are large individual differences in susceptibility to arsenic-induced diseases, which ar...

journal_title：Chemical research in toxicology

authors： Lu K,Cable PH,Abo RP,Ru H,Graffam ME,Schlieper KA,Parry NM,Levine S,Bodnar WM,Wishnok JS,Styblo M,Swenberg JA,Fox JG,Tannenbaum SR

更新日期：2013-12-16 00:00:00

abstract：:Faithful replication of DNA is a critical aspect in maintaining genome integrity. DNA polymerases are responsible for replicating DNA, and high-fidelity polymerases do this rapidly and at low error rates. Upon exposure to exogenous or endogenous substances, DNA can become damaged and this can alter the speed and fidel...

journal_title：Chemical research in toxicology

authors： Gahlon HL,Romano LJ,Rueda D

更新日期：2017-11-20 00:00:00

abstract：:DNA nucleobases are the prime targets for chemical modifications by endogenous and exogenous electrophiles. Alkylation of the N7 position of guanine and adenine in DNA triggers base-catalyzed imidazole ring opening and the formation of N5-substituted formamidopyrimidine (N5-R-FAPy) lesions. Me-FAPy-dG adducts induced ...

journal_title：Chemical research in toxicology

authors： Pujari SS,Tretyakova N

更新日期：2017-01-17 00:00:00

abstract：:Unpredicted human safety events in clinical trials for new drugs are costly in terms of human health and money. The drug discovery industry attempts to minimize those events with diligent preclinical safety testing. Current standard practices are good at preventing toxic compounds from being tested in the clinic; howe...

journal_title：Chemical research in toxicology

authors： Cassar S,Adatto I,Freeman JL,Gamse JT,Iturria I,Lawrence C,Muriana A,Peterson RT,Van Cruchten S,Zon LI

更新日期：2020-01-21 00:00:00

abstract：:The diarrhetic shellfish toxin composition in the digestive glands of mussels collected in June 2001 from the Northern Adriatic sea was investigated by high-performance liquid chromatography coupled with electrospray ion trap mass spectrometry. Along with known yessotoxins (1, 3-6), identified by comparison of their r...

journal_title：Chemical research in toxicology

authors： Ciminiello P,Dell'Aversano C,Fattorusso E,Forino M,Magno S,Poletti R

更新日期：2002-07-01 00:00:00

abstract：:The nuclear receptor human pregnane X receptor (hPXR) is a ligand-regulated transcription factor that responds to a wide range of endogenous and xenobiotic molecules. Upon activation with ligands, hPXR can increase induction levels of metabolic enzymes. Therefore, hPXR plays a critical role in drug metabolism and excr...

journal_title：Chemical research in toxicology

authors： Chen CN,Shih YH,Ding YL,Leong MK

更新日期：2011-10-17 00:00:00

abstract：:Flavonols are potent naturally occurring antioxidants. Chemical oxidation reactions in combination with modern spectroscopic techniques have been employed to identify oxidized flavonoid products. Although many oxidized derivatives have been generated from commercially available starting materials, few studies have dev...

journal_title：Chemical research in toxicology

authors： Krishnamachari V,Levine LH,Zhou C,Paré PW

更新日期：2004-06-01 00:00:00

abstract：:Peroxynitrite (PN), a very reactive oxidant formed by the combination of superoxide and nitric oxide, appears to play a role in producing tissue damage in a number of inflammatory conditions. Pharmacological scavenging and decomposition of PN within these areas has therapeutic value in several tissue injury models. Re...

journal_title：Chemical research in toxicology

authors： Carroll RT,Galatsis P,Borosky S,Kopec KK,Kumar V,Althaus JS,Hall ED

更新日期：2000-04-01 00:00:00

abstract：:N,N-Bis(2-chloroethyl)-p-aminophenylbutyric acid (chlorambucil, 1) is an orally administrated drug widely used in the chemotherapy of chronic lymphocytic leukemia. We have recently described a new metabolic path for the decomposition of 1 in human gastric juice based on its reactions with saliva-derived thiocyanate io...

journal_title：Chemical research in toxicology

authors： Hovinen J,Pettersson-Fernholm T,Lahti M,Vilpo J

更新日期：1998-11-01 00:00:00

abstract：:We have reassigned relative and absolute configurations by unambiguous stereoselective syntheses of the cis- (13s and 13R) and trans-N6-deoxyadenosine (dAdo) adduct diastereomers (14S and 14R) derived from (+/-)-11beta,12alpha-dihydroxy-13alpha,14alpha-epoxy-11,12,13,14-tetrahydrodibenzo[a,l]pyrene (DB[a,l]P DE-2), pr...

journal_title：Chemical research in toxicology

authors： Yagi H,Frank H,Seidel A,Jerina DM

更新日期：2008-12-01 00:00:00

abstract：:In the present study, values of the binding energy (BE) were calculated for the rat androgen receptor on a data set of 25 steroidal and nonsteroidal compounds for which published values of the observed binding affinity (K(i)) are available. A correlation between BE and pK(i) was evident (r(2) = 0.50) for the entire da...

journal_title：Chemical research in toxicology

authors： Ai N,DeLisle RK,Yu SJ,Welsh WJ

更新日期：2003-12-01 00:00:00

abstract：:Docosahexaenoic acid (DHA) is a semiessential polyunsaturated fatty acid (PUFA) for eukaryotic cells that is found in natural sources such as fish and algal oils and widely used as an ingredient for omega-3 containing foods or supplements. DHA effects are connected to its natural structure with six cis double bonds, b...

journal_title：Chemical research in toxicology

authors： Menounou G,Giacometti G,Scanferlato R,Dambruoso P,Sansone A,Tueros I,Amézaga J,Chatgilialoglu C,Ferreri C

更新日期：2018-03-19 00:00:00

abstract：:Cyclic imides are known for their antitumor activity, especially the naphthalimide derivatives, such as Mitonafide and Amonafide. Recently, we have demonstrated the cytotoxic effect of a series of naphthalimide derivatives against B16F10 melanoma cells. On the basis of this fact, we have developed a study starting fro...

journal_title：Chemical research in toxicology

authors： Machado KE,de Oliveira KN,Andreossi HM,Bubniak Ldos S,de Moraes AC,Gaspar PC,Andrade Eda S,Nunes RJ,Santos-Silva MC

更新日期：2013-12-16 00:00:00

abstract：:The PI3K/Akt/mTOR pathway is considered to be an attractive target for the development of novel anticancer molecules. This paper reports for the first time that a small molecule, antrocin (MW = 234), from Antrodia camphorata was a potent antagonist in various cancer types, being highest in metastatic breast cancer MDA...

journal_title：Chemical research in toxicology

authors： Rao YK,Wu AT,Geethangili M,Huang MT,Chao WJ,Wu CH,Deng WP,Yeh CT,Tzeng YM

更新日期：2011-02-18 00:00:00

abstract：:The mechanisms underlying aryl hydrocarbon receptor (AHR) activation by agonists and circumstances that increase the sensitivity toward agonists and AHR inhibition by antagonists are diverse and still not fully understood. AHR antagonist, 2-methyl-2 H-pyrazole-3-carboxylic acid (2-methyl-4- o-tolylazo-phenyl)-amide, C...

journal_title：Chemical research in toxicology

authors： Mohammadi-Bardbori A,Omidi M,Arabnezhad MR

更新日期：2019-04-15 00:00:00

abstract：:Anxiolytic kava products have been associated with rare but severe hepatotoxicity in humans. This adverse potential has never been captured in animal models, and the responsible compound(s) remains to be determined. The lack of such knowledge greatly hinders the preparation of a safer kava product and limits its benef...

journal_title：Chemical research in toxicology

authors： Narayanapillai SC,Leitzman P,O'Sullivan MG,Xing C

更新日期：2014-10-20 00:00:00

abstract：:Alzheimer's disease (AD) is the most common neurodegenerative disorder in the elderly population, above 65 years of age. Multiple lines of evidence confirm the central role of 40-42 residue Abeta peptides in the pathogenesis of AD, but exact mechanisms of Abeta toxicity remain unclear. Recently, evidence has accumulat...

journal_title：Chemical research in toxicology

authors： Rózga M,Bal W

更新日期：2010-02-15 00:00:00

abstract：:Chloroprene (2-chloro-1,3-butadiene, 1) is an important industrial chemical, which is carcinogenic in experimental animals and possibly in humans. It is metabolized to the monoepoxides, 2-chloro-2-ethenyloxirane (2a,b) and (1-chloroethenyl)oxirane (3a,b), together with electrophilic chlorinated aldehydes and ketones. ...

journal_title：Chemical research in toxicology

authors： Munter T,Cottrell L,Golding BT,Watson WP

更新日期：2003-10-01 00:00:00

abstract：:The tumorigenic activity of manufactured gas plant residue (MGP) was evaluated in female A/J mice using a F0927 basal gel diet system. Adulterated diets containing MGP (0.10% or 0.25%) or benzo[a]pyrene (B[alpha]P; 16 or 98 ppm) were fed for 260 days. A negative control group was maintained on a nonadulterated basal g...

journal_title：Chemical research in toxicology

authors： Weyand EH,Chen YC,Wu Y,Koganti A,Dunsford HA,Rodriguez LV

更新日期：1995-10-01 00:00:00

abstract：:A method for the analysis of N-acetylcysteine conjugates of catechol estrogens [catechol estrogen mercapturates (CE SRs)], which are likely to be urinary markers of estrogen-induced tumors, was established in this study. The characteristics of the method that was established were (1) cleanup of urine using the immunoa...

journal_title：Chemical research in toxicology

authors： Nakagomi M,Suzuki E

更新日期：2000-12-01 00:00:00

abstract：:A newly developed recombinant yeast strain, in which the human estrogen receptor has been stably integrated into the genome of the yeast, was used to gain information on the estrogenic activity of a large series of dietary flavonoids. Among 23 flavonoids investigated, 8 were found to markedly stimulate the transcripti...

journal_title：Chemical research in toxicology

authors： Breinholt V,Larsen JC

更新日期：1998-06-01 00:00:00

abstract：:Chemical respiratory sensitization is an immunological process that manifests clinically mostly as occupational asthma and is responsible for 1 in 6 cases of adult asthma, although this may be an underestimate of the prevalence, as it is under-diagnosed. Occupational asthma results in unemployment for roughly one-thir...

journal_title：Chemical research in toxicology

authors： Golden E,Maertens M,Hartung T,Maertens A

更新日期：2020-12-15 00:00:00

abstract：:Allergic contact dermatitis (ACD) is a widespread cause of workers' disabilities. Although some substances found in the workplace are rigorously tested, the potential of the vast majority of chemicals to cause skin sensitization remains unknown. At the same time, exhaustive testing of all chemicals in workplaces is co...

journal_title：Chemical research in toxicology

authors： Fedorowicz A,Singh H,Soderholm S,Demchuk E

更新日期：2005-06-01 00:00:00