Abstract:
:It has been postulated that reversible, high-affinity binding of 3-methylcholanthrene(MC)-type inducers to a receptor protein (the Ah receptor) in hepatic cytosol is essential for induction of aryl hydrocarbon hydroxylase (AHH) enzymic activity. To test this postulate, the binding affinities of 16 highly-purified, synthetic chlorinated biphenyl (PCB) congeners, which have been categorized either as phenobarbitone(PB)-, MC- or mixed (PB + MC)-type inducers of cytochrome P-450-dependent monooxygenase have been examined. The affinity of individual biphenyl congeners for the receptor was determined by their competition with 2,3,7,8-[3H]tetrachlorodibenzo-p-dioxin ([3H]TCDD) for specific cytosolic binding sites as measured by sucrose density gradient analysis following dextran-charcoal treatment. This assay demonstrates (a) that the receptor binds with highest affinity to 3,3', 4,4',5-pentachlorobiphenyl and 3,3',4,4'-tetrachlorobiphenyl ('pure MC-like' inducers); (b) mixed-type PCB inducers also bind to the receptor but with an affinity (average EC50-value of 8.6 microM) lower than that for 3,3',4,4',5-pentachlorobiphenyl; this corresponds with their relatively lower potencies as AHH inducers; (c) the receptor binds 2,2',4,4'-tetra-, 2,3,4,5-tetra-, 2,2',4,4',5,5'-hexa- and 2,3',4,4',5',6-hexachlorobiphenyl at high concentrations (0.1 mM), whereas PB fails to bind, even at a concentration of 10 mM. All PCBs tested competed with [3H]TCDD for Ah receptor, but there was a great variation in their relative binding affinities. The fact that two chlorinated biphenyls classed as 'PB-like' inducers and two chlorinated biphenyls which are neither 'PB- nor MC-type' inducers competed, coupled with the fact that PB did not bind to the receptor suggest that chemicals other than "pure MC-type' inducers can bind to the cytosolic receptor. Affinity of the binding dictates the relative potency of given PCB congeners as inducers of cytochrome P-448.
journal_name
Chem Biol Interactjournal_title
Chemico-biological interactionsauthors
Bandiera S,Safe S,Okey ABdoi
10.1016/0009-2797(82)90045-xsubject
Has Abstractpub_date
1982-04-01 00:00:00pages
259-77issue
3eissn
0009-2797issn
1872-7786pii
0009-2797(82)90045-Xjournal_volume
39pub_type
杂志文章abstract::NADPH:quinone oxidoreductase 1 (NQO1) may perform multiple functions within the cell. It is known to detoxify benzene-derived quinones and generate antioxidant forms of ubiquinone and Vitamin E. Recently suggested roles for NQO1 which may have relevance for mechanisms underlying benzene toxicity include modulation of ...
journal_title:Chemico-biological interactions
pub_type: 杂志文章,评审
doi:10.1016/j.cbi.2005.03.018
更新日期:2005-05-30 00:00:00
abstract::The most common non-communicable diseases (NCD) are obesity, cardiovascular disease, diabetes, cancer, chronic respiratory diseases, and neurological diseases. Together, they constitute the commonest cause of death and disability worldwide. Mitochondrial alterations, oxidative stress and inflammation underpin NCD and ...
journal_title:Chemico-biological interactions
pub_type: 杂志文章,评审
doi:10.1016/j.cbi.2016.04.005
更新日期:2016-11-25 00:00:00
abstract::Chrysophanol, a major anthraquinone component occurring in many traditional Chinese herbs, is accepted as important active component with various pharmacological actions such as antibacterial and anticancer activity. Previous studies demonstrated that exposure to chrysophanol induced cytotoxicity, but the mechanisms o...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/j.cbi.2018.04.015
更新日期:2018-06-01 00:00:00
abstract::Liquid-holding recovery and rejoining of gamma-radiation-induced DNA single-strand scissions in Escherichia coli could be effectively inhibited by procaine hydrochloride at the concentration of 20 mM. At this concentration, the drug also reversibly altered cellular permeability barrier as evidenced from the uptake of ...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/0009-2797(75)90097-6
更新日期:1975-09-01 00:00:00
abstract::A variety of substances of diverse structure have been shown to affect the activity of protein kinase C. Many of the agents which affect protein kinase C activity also markedly shift the bilayer to hexagonal phase transition temperature of phosphatidylethanolamines. Although one of the more potent activators of protei...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/0009-2797(87)90044-5
更新日期:1987-01-01 00:00:00
abstract::4-Methylcyclophosphamide, an analogue of the antitumour agent cyclophosphamide, exists in cis and trans forms, each of which comprises a pair of optical isomers. The extents of metabolism by rat liver microsomes during 20 min were compared for the four steroisomers incubated separately, and for the racemic cis and tra...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/0009-2797(77)90140-5
更新日期:1977-07-01 00:00:00
abstract:OBJECTIVES:Oxidative stress is one component of alcoholic liver disease (ALD) that is manifested in the peroxidation of cellular lipids producing the electrophile, 4-hydroxynonenal (4-HNE). This electrophile is proposed to modify essential cellular proteins resulting in loss of protein function and cellular homeostasis...
journal_title:Chemico-biological interactions
pub_type: 杂志文章,评审
doi:10.1016/j.cbi.2011.02.021
更新日期:2011-06-30 00:00:00
abstract::Prostate (CaP) cancer is the second-leading cause of cancer-related mortality in men in Western societies. Androgen receptor (AR) signaling is a critical survival pathway for prostate cancer cells, and androgen-deprivation therapy (ADT) remains the principal treatment for patients with locally advanced and metastatic ...
journal_title:Chemico-biological interactions
pub_type: 杂志文章,评审
doi:10.1016/j.cbi.2016.10.002
更新日期:2016-12-25 00:00:00
abstract::The anticancer prodrug CPT-11 is a highly effective camptothecin analog that has been approved for the treatment of colon cancer. The 2.6 angstroms resolution crystal structure of its complex with Torpedo californica acetylcholinesterase (TcAChE) demonstrates that CPT-11 binds to TcAChE and spans its gorge similarly t...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/j.cbi.2005.10.016
更新日期:2005-12-15 00:00:00
abstract::Due to its antiviral effects and its importance for all immunological functions, the administration of selenium is suggested as a supportive measure in early as well as in advanced stages of HIV-induced disease. Initial observations on the effects of selenium supplementation in HIV-infected patients indicate that sele...
journal_title:Chemico-biological interactions
pub_type: 杂志文章,评审
doi:10.1016/0009-2797(94)90040-x
更新日期:1994-06-01 00:00:00
abstract::Known spectroscopic and kinetic data are used to formulate pathways of the physiological and transfer reactions and the substrate inhibition of phenol sulfotransferase. Kinetic mechanisms indicate that release of PAP from enzyme complex is required for the physiological reaction but not for the transfer reaction. The ...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/s0009-2797(97)00127-0
更新日期:1998-02-20 00:00:00
abstract::Human foreskin cell cultures in scheduled DNA synthesis (S phase) of the cell cycle were exposed to UV irradiation at a dose of 10 J . m-1 in the presence of insulin. These treated cell populations, when selectively passaged in a high amino acid supplemented complete growth medium (CM) after 20 Dulbecco's phosphate bu...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/0009-2797(81)90028-4
更新日期:1981-07-01 00:00:00
abstract::Administration of a single oral dose of dieldrin (20 mg/kg body wt.) to rhesus monkeys considerably elevated the uptake of glucose and the activities of brush border sucrase, lactase, maltase and alkaline phosphatase in intestine compared to control animals. Leucine uptake and leucine amino peptidase activity was sign...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/0009-2797(81)90173-3
更新日期:1981-10-01 00:00:00
abstract::Oxidative stress induced by Reactive Oxygen Species (ROS) was shown to be involved in the pathogenesis of chronic diseases such as cardiovascular pathologies. Particularly, oxidative stress has proved to mediate abnormal platelet function and dysfunctional endothelium-dependent vasodilatation representing a key factor...
journal_title:Chemico-biological interactions
pub_type: 杂志文章,评审
doi:10.1016/j.cbi.2017.11.012
更新日期:2018-01-05 00:00:00
abstract::The secretion of digoxin and digitoxin into in situ perfused jejunal and colonic segments of normal or quinidine treated guinea pigs was studied. Quinidine was administered intravenously by constant rate infusion resulting in a quinidine plasma concentration of about 6 micrograms/ml. After 2 h digoxin or digitoxin was...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/s0009-2797(85)80128-9
更新日期:1985-10-01 00:00:00
abstract::Oxidative stress and oxidative damage to tissues are common end points of chronic diseases such as atherosclerosis, diabetes, and rheumatoid arthritis. Oxidative stress in diabetes coexists with a reduction in the antioxidant status, which can further increase the deleterious effects of free radicals. The aim of the p...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/j.cbi.2006.10.014
更新日期:2007-01-30 00:00:00
abstract::The metabolism of [3H]benzo[a]pyrene (BP) and (-)-trans-[14C]7,8-dihydroxy-7,8-dihydrobenzo[a]pyrene (BP-7,8-diol) was studied in freshly isolated hepatocytes of the wild benthic fish, brown bullhead (Ictalurus nebulosus). Bullhead hepatocytes incubated with 40 microM [3H]BP for 1 h metabolized BP to water soluble met...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/0009-2797(90)90063-s
更新日期:1990-01-01 00:00:00
abstract::Intracellular calcium (Ca(2+)i) overload induced by chronic hypoxia alters Ca(2+)i homeostasis, which plays an important role on mediating myocardial injury. We tested the hypothesis that treatment with trimetazidine (TMZ) would improve Ca(2+)i handling in hypoxic myocardial injury. Cardiomyocytes isolated from neonat...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/j.cbi.2015.04.022
更新日期:2015-07-05 00:00:00
abstract::Susceptibility to drug toxicity is influenced by a variety of factors, both genetic and environmental. The focus of this article is the evidence addressing the hypothesis that inflammation is both a result of and a susceptibility factor for drug toxicity, with an emphasis on liver as a target organ. Results of studies...
journal_title:Chemico-biological interactions
pub_type: 杂志文章,评审
doi:10.1016/j.cbi.2004.09.002
更新日期:2004-11-01 00:00:00
abstract::Penicillamine increases the levels of metallothionein (MT) mRNA in a time and concentration dependent manner without altering either the rate of copper uptake or the amount of copper within the cell. The effect is dependent on the presence of intracellular copper, however, since depletion of copper by chelators blocks...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/0009-2797(90)90074-w
更新日期:1990-01-01 00:00:00
abstract::Five mouse anti-human butyrylcholinesterase (BChE) monoclonal antibodies bind tightly to native human BChE with nanomolar dissociation constants. Pairing analysis in the Octet system identified the monoclonal antibodies that bind to overlapping and independent epitopes on human BChE. The nucleotide and amino acid sequ...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/j.cbi.2015.11.011
更新日期:2016-01-05 00:00:00
abstract::The interactions of benzo(a)pyrene (B(a)P) with the cell surface membrane were studied by measuring B(a)P uptake into intact mammalian cells and by determining B(a)P fluorescence in the presence of isolated cell surface membranes. It was found that 0.19 mu-g B(a)P were taken up by 10-6 Chinese hamster ovary (CHO) cell...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/0009-2797(75)90061-7
更新日期:1975-07-01 00:00:00
abstract::Since skin cancer incidence and prevalence is constantly rising up the charts despite all efforts, search for newer, better agents for protection and treatment is required. Ginger (Zingiber officinale Roscoe), a monocotyledonous herb, is widely used as a herbal medicine, given the presence of homologous phenolic keton...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/j.cbi.2009.05.012
更新日期:2009-09-14 00:00:00
abstract::Pelargonidin (PEL) is a well-known red pigment found in plants, and has been reported as having important biological activities that are potentially beneficial for human health. Here, we tested the possible use of PEL in the treatment of lipopolysaccharide (LPS)-mediated vascular inflammatory responses. The anti-infla...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/j.cbi.2019.02.007
更新日期:2019-04-01 00:00:00
abstract::Epidermal growth factor receptor (EGFR) is conventionally known to play a crucial role in hepatocyte proliferation, liver regeneration and is also associated with hepatocellular carcinogenesis. In addition to these proliferative roles, EGFR has also implicated in apoptotic cell death signaling in various hepatic cells...
journal_title:Chemico-biological interactions
pub_type: 杂志文章,评审
doi:10.1016/j.cbi.2020.109090
更新日期:2020-06-01 00:00:00
abstract::Fosfomycin is clinically recognized to reduce the aminoglycoside antibiotics-induced nephrotoxicity. However, little has been clarified why fosfomycin protects the kidney from the aminoglycosides-induced nephrotoxicity. Gentamicin, a typical aminoglycoside, is reported to cause lipid peroxidation. We focused on lipid ...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/j.cbi.2004.05.005
更新日期:2004-07-20 00:00:00
abstract::Genistein (4', 5, 7-trihydroxyisoflavone), a naturally occurring flavonoid characteristic of Leguminoseae plants, is a phyto-oestrogen exerting oestrogenic activity as both an agonist and an antagonist substance. A large body of evidence suggests that genistein possesses many physiological and pharmacological properti...
journal_title:Chemico-biological interactions
pub_type: 杂志文章,评审
doi:10.1016/j.cbi.2017.02.012
更新日期:2017-04-25 00:00:00
abstract::Recombinant (r) and native butyrylcholinesterse (BChE) are potent bioscavengers of organophosphates (OPs) such as nerve agents and pesticides and are undergoing development as antidotal treatments for OP-induced toxicity. Because of the lethal properties of such agents, regulatory approval will require extensive testi...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/j.cbi.2015.09.021
更新日期:2015-12-05 00:00:00
abstract::The cytochrome P450 isoforms responsible for the regio-selective metabolism of benz[a]anthracene (BA) are poorly defined but as with other polycyclic aromatic hydrocarbons (PAHs) may include members of the CYP2C sub-family. Since the expression of some of these is regulated in a gender-specific manner and may be alter...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/s0009-2797(00)00147-2
更新日期:2000-03-15 00:00:00
abstract::Formic acid is a common organic acid used in many industrial processes. There is a paucity of research on the direct toxicity of formic acid and how it might affect the cardiovascular system. This study aimed to understand the effect of formic acid on vascular tension in an animal model and the underlying mechanism. R...
journal_title:Chemico-biological interactions
pub_type: 杂志文章
doi:10.1016/j.cbi.2019.06.023
更新日期:2019-08-25 00:00:00