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At least 307 records · Page 17Linked to original sources

PubMed2002

Transepidermal water loss during halogen spotlight phototherapy in preterm infants.

Among preterm infants there is a relationship between skin blood flow and transepidermal water loss (TEWL). The aim of this study was to assess whether halogen spotlight phototherapy without significant heat stress increases TEWL and affects maintenance fluid requirements in preterm infants. TEWL was measured noninvasively before the start and after 1 h of halogen spotlight phototherapy in a group of preterm infants, nursed in double-walled incubators with moderately high relative humidity. Relative humidity and ambient temperature in the incubator were tightly controlled. Mean +/- SD birth weight of the 18 infants was 1412 +/- 256 g, gestational age 30.6 +/- 1.6 wk, and age at measurement 5 +/- 3 d. Nine infants received ventilatory assistance. Relative humidity was 40-80% (mean 52%). Average TEWL increased from 13.6 to 16.5 g/m(2)/h during phototherapy. These data show that TEWL increases by approximately 20% during phototherapy despite constant skin temperature and relative humidity. Maintenance fluids of preterm infants should be increased by 0.35 mL/kg/h during exposure to halogen spotlight phototherapy.

Fluid Therapy↗

PubMed1985

Mechanism of action of toxic halogenated aromatics.

2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) and related halogenated aromatic hydrocarbons are a highly toxic class of environmental contaminants, as evidenced by numerous cases of accidental poisonings of human and animal populations and their extreme toxic potency in laboratory animals. The proposed model for the mechanism of action of TCDD and related compounds is analogous to that of the steroid hormones, which modulate gene expression through a receptor mechanism. In the steroid receptor model, the compound enters the cell cytoplasm where it acts as a specific ligand, binding selectively to a high affinity receptor protein. Bound to the appropriate ligand, the receptor concentrates in the nucleus where its increased association with chromatin leads to altered gene expression. This model has been useful in characterizing the Ah receptor; however, it does not provide a unifying hypothesis for all biochemical and toxic effects associated with exposure to halogenated aromatic hydrocarbons. Several findings suggest that a primary factor in determining TCDD toxicity might be tissue and species specific factors that control the actions of Ah receptor(s) in target tissues. Furthermore, numerous mechanisms might be involved. Clarifying the mechanism(s) for TCDD toxicity would enhance our ability to predict human health consequences to toxic halogenated aromatic hydrocarbons and would provide a more rational basis for risk analysis.

Adipose Tissue↗

PubMed1985

The role of structure in the disposition of halogenated aromatic xenobiotics.

Halogenated aromatic xenobiotics such as the chlorinated and brominated biphenyls, naphthalenes, dibenzodioxins, and dibenzofurans are widespread environmental contaminants. The number, position, and nature of the halogen atoms as well as the structure of the aromatic rings influence the disposition of these chemicals in living systems. Absorption is governed primarily by the physical properties of lipophilicity and solubility. Distribution through the blood occurs by nonspecific binding to plasma proteins and cellular components. Liver and adipose tissue are the major depots. Metabolism is a prerequisite for excretion. The highly substituted isomers tend to be resistant to metabolism. The route of excretion shifts from urine to feces with increasing size and number of halogen atoms. Although pharmacokinetic modeling has allowed some predictions to be made from one compound to another or across species, more information on metabolism is required in order to improve the ability to predict the disposition in humans of this class of toxic environmental pollutants.

Absorption↗

PubMed1996

A QSAR evaluation of Ah receptor binding of halogenated aromatic xenobiotics.

Because of their widespread occurrence and substantial biological activity, halogenated aromatic hydrocarbons such as polychlorinated biphenyls (PCBs), polychlorinated dibenzofurans (PCDFs), and polychlorinated dibenzo-p-dioxins (PCDDs) comprise one of the more important classes of contaminants in the environment. Some chemicals in this class cause adverse biological effects after binding to an intracellular cytosolic protein called the aryl hydrocarbon receptor (AhR). Toxic responses such as thymic atrophy, weight loss, immunotoxicity, and acute lethality, as well as induction of cytochrome P4501A1, have been correlated with the relative affinity of PCBs, PCDFs, and PCDDs for the AhR. Therefore, an important step in predicting the effects of these chemicals is the estimation of their binding to the receptor. To date, however, the use of quantitative structure activity relationship (QSAR) models to estimate binding affinity across multiple chemical classes has shown only modest success possibly due, in part, to a focus on minimum energy chemical structures as the active molecules. In this study, we evaluated the use of structural conformations other than those of minimum energy for the purpose of developing a model for AhR binding affinity that encompasses more of the halogenated aromatic chemicals known to interact with the receptor. Resultant QSAR models were robust, showing good utility across multiple classes of halogenated aromatic compounds.

Benzofurans↗

PubMed1999

Synthesis of combinatorial libraries of 3,4,5-trisubstituted 2(5H)-furanones. Part One: Construction of a sub-library of halogenated 5-alkoxy-2(5H)-furanones.

Starting from furfural, 5-hydroxy-3,4-dihalo-2(5H)-furanones and 5-hydroxy-4 chloro-2(5H)-furanone were converted into 3 sublibraries of halogenated 5-alkoxy-2(5H)-furanones. The reactivity of 24 halogenated 5-alkoxy2(5H)-furanones was chemically evaluated by using 4 selected amines for subsequent reactions. The biological evaluation of the pseudo-muco halogen esters resulted in the discovery of a lead structure with potent anti-cancer activity.

Combinatorial Chemistry Techniques↗

PubMedDate not supplied

The effectiveness of cure of LED and halogen curing lights at varying cavity depths.

This study compared the effectiveness of cure of two LED (light-emitting diodes) lights (Elipar FreeLight [FL], 3M-ESPE and GC e-Light [EL], GC) to conventional (Max [MX] (control), Dentsply-Caulk), high intensity (Elipar TriLight [TL], 3M-ESPE) and very high intensity (Astralis 10 [AS], Ivoclar Vivadent) halogen lights at varying cavity depths. Ten light curing regimens were investigated. They include: FL1-400 mW/cm2 [40 seconds], FL2-0-400 mW/cm2 [12 seconds] --> 400 mW/cm2 [28 seconds], EL1-750 mW/cm2 [10 pulses x 2 seconds], EL2-350 mW/cm2 [40 seconds], EL3-600 mW/cm2 [20 seconds], EL4-0-600 mW/cm2 [20 seconds] --> 600 mW/cm2 [20 seconds], TL1-800 mW/cm2 [40 seconds], TL2-100-800 mW/cm2 [15 seconds] --> 800 mW/cm2 [25 seconds], AS1-1200 mW/cm2 [10 seconds], MX-400 mW/cm2 [40 seconds]. The effectiveness of cure of the different modes was determined by measuring the top and bottom surface hardness (KHN) of 2-mm, 3-mm and 4-mm thick composite (Z100, [3M-ESPE]) specimens using a digital microhardness tester (n = 5, load = 500 g; dwell time = 15 seconds). Results were analyzed using ANOVA/Scheffe's post-hoc test and Independent Samples t-Test (p < 0.05). For all lights, effectiveness of cure was found to decrease with increased cavity depths. The mean hardness ratio for all curing lights at a depth of 2 mm was found to be greater than 0.80 (the accepted minimum standard). At 3 mm, all halogen lights produced a hardness ratio greater than 0.80 but some LED light regimens did not; and at a depth of 4 mm, the mean hardness ratio observed with all curing lights was less than 0.80. Significant differences in top and bottom KHN values were observed among different curing regimens for the same light and between LED and halogen lights. While curing with most modes of EL resulted in significantly lower top and bottom KHN values than the control (MX) at all depths, the standard mode of FL resulted in significantly higher top and bottom KHN at a depth of 3 mm and 4 mm. The depth of composite cure with LED LCUs was, therefore, product and mode dependent.

Analysis of Variance↗

PubMedDate not supplied

Comparison of halogen, plasma and LED curing units.

This study evaluated the characteristics of two kinds of recently developed light-curing unit; plasma arc and blue light emitting diodes (LED), in comparison with a conventional tungsten-halogen light-curing unit. The light intensity and spectral distribution of light from these light-curing units, the temperature rise of the bovine enamel surface and the depth of cure of composites exposed to each unit were investigated. The light intensity and depth of cure were determined according to ISO standards. The spectral distributions of emitted light were measured using a spectro-radiometer. The temperature increase induced by irradiation was measured by using a thermocouple. Generally, light intensities in the range 400-515 nm emitted from the plasma arc were greater than those from other types. Light in the UV-A region was emitted from some plasma arc units. The required irradiation times were six to nine seconds for the plasma arc units and 40 to 60 seconds for the LED units to create a depth of cure equal to that produced by the tungsten-halogen light with 20 seconds of irradiation. The temperature increased by increasing the irradiation time for every light-curing unit. The temperature increases were 15 degrees C to 60 degrees C for plasma arc units, around 15 degrees C for a conventional halogen unit and under 10 degrees C for LED units. Both the plasma arc and LED units required longer irradiation times than those recommended by their respective manufacturers. Clinicians should be aware of potential thermal rise and UV-A hazard when using plasma arc units.

Animals↗

PubMed2004

Derivatisation of 4-nonylphenol and bisphenol A with halogenated anhydrides.

The aim of this work is to synthesize and characterise the halogenated derivatives of the endocrine disrupting compounds (EDCs) 4-nonylphenol (4-NP) and bisphenol A (BPA). Characterisation was performed after gas chromatographic (GC) separation on-line coupled to mass spectrometric (MS) detector and a Fourier Transform Infrared (FTIR) spectroscopic detector. Further structure elucidation was done applying Nuclear Magnetic Resonance spectroscopy (NMR). Two different approaches for the preparation of derivatives were evaluated. At first trifluoroacetyl derivatives were synthesized by the reaction of trifluoroacetic acid (TFA) anhydride and the EDCs in acetonitrile at a temperature of 50 degrees C for 30 minutes. In a second step the 4-NP was derivatised using trichloroacetic acid anhydride and triethylamine in diethyl ether at 20 degrees C for 30 minutes. After synthesis the halogenated NP and BPA derivatives were characterised applying GC/MS, GC/FTIR and NMR. Three indices for a successful derivatisation were observed: El-GC/MS proved a complete derivatisation presenting a characteristic fragmentation pattern for each derivative. The IR spectra obtained by GC/FTIR after derivatisation and separation confirmed the loss of the phenolic O-H stretching vibration at 3,600 cm(-1) while typical absorptions for halogenated compounds now were observed. The NMR-spectra contained the predicted resonance signals.

Acetic Anhydrides↗

PubMed2006

Effect of halogen light in fetal stimulation for fetal well-being assessment.

OBJECTIVE: To evaluate the shortening of the time of nonstress test (NST) by using transabdominal fetal stimulation with halogen light. STUDY DESIGN: Experimental research. MATERIAL AND METHOD: The authors enrolled 176 pregnant women between 32 and 42 weeks of gestation indicated for NST at the Division of Maternal Fetal Medicine, Siriraj Hospital, Mahidol University. They were randomly assigned to receive either NST (control) or halogen light stimulation test (LST). The stimulation was performed at the beginning of the test and repeated every 10 minutes until reassuring fetal heart rate (FHR) acceleration was achieved, or up to 3 times. All tracings were interpreted blindly by one investigator at the end of the tests. RESULTS: The mean (+/- SD) duration from starting the test to the first FHR acceleration was not significantly different between the control group and the LST group (5.6 +/- 7.2 and 5.4 +/- 5.2 minutes, respectively). The average testing time (+/- SD) to achieved reactivity was 10.5 +/- 8.8 minutes in the controls and 9.6 +/- 6.7 minutes in the LST group. This was not statistically different. The incidence of nonreactive tests was not significantly different between the LST and the controls (15.9% and 11.4%, respectively). Among the LST subjects, term fetuses and women with BMI < 27 kg/m2 required less time to reach reactivity, 2.4 and 2.3 minutes respectively. CONCLUSION: Transabdominal halogen light stimulation did not shorten the duration of NST in the presented population. However, the presented data suggests that the fetus at term could respond to visual stimulation, especially when the gestational age is more advanced.

Female↗

PubMed1987

Antiproliferative and cytotoxic effects of newly discovered halogenated coral prostanoids from the Japanese stolonifer Clavularia viridis on human myeloid leukemia cells in culture.

The antiproliferative and cytotoxic activities of newly discovered halogenated coral prostanoids (chlorovulone, bromovulone, and iodovulone) from the Japanese stolonifer Clavularia viridis and their related compounds were determined in HL-60 cells in culture. The order of antiproliferative and cytotoxic activities of naturally occurring marine prostanoids against HL-60 cells was chlorovulone I greater than bromovulone I = iodovulone I greater than clavulone I or II greater than prostaglandin A2. The IC50 (concentrations required to inhibit cell growth by 50%) value (0.03 microM (0.01 microgram/ml)) and cytotoxic effects (greater than 0.3 microM (0.1 microgram/ml)) of chlorovulone I were about 200 and 100 times stronger than those of prostaglandin A2, respectively, on the molar basis. From our data on the structure-activity relationship of the halogenated coral prostanoids and the related compounds, we elucidated that 1) the alkylidencyclopentenone structure in these prostanoids was essential for the antiproliferative and cytotoxic activities against HL-60 cells and the introduction of halogen function at C-10 position in the structure enhanced the activities (C1 = F greater than Br = I greater than H); 2) the stereospecificity of the 12-hydroxyl group in the chlorovulone molecule was not required for the activities; 3) the presence of dienone (C5-6 and C7-8) in the structure potentiated the activities. Bivariate DNA/bromodeoxyuridine analysis with a flow cytometer showed that chlorovulone I transiently arrested the cell cycle progression from G1 to S after 24-hr exposure to the nontoxic concentrations (0.03 and 0.09 microM) and caused the lasting blockade of leukemia cells in G1 at the cytotoxic concentration. These results suggest that these coral prostanoids and related compounds may be a promising antileukemic agent.

Animals↗

PubMed1987

In vitro and in vivo antiaggregant effects of magnesium halogenates.

The in vitro antiplatelet aggregating activity of magnesium and magnesium associated with soluble citroflavonoids (hesperidin and eriodictin, 1:1) is well-established. The degree of inhibition of in vitro platelet aggregation activity produced by different concentrations of magnesium halogenates was determined. ADP (4 microM) was used to induce aggregation following Cardinal and Flowers' (1) technique. Antithrombotic activity was studied in vivo. The difference in duration of ADP-induced respiratory dysfunction was compared between animals fed 25 mg/kg magnesium halogenates for 10 days before testing and controls. An increase in circulating platelets was observed in rats treated with magnesium halogenates.

Adenosine Diphosphate↗

PubMed1994

Potent carcinogenicity of uncovered halogen lamps in hairless mice.

Uncovered halogen quartz lamps, which are potently genotoxic both in prokaryotic and human cells due to the emission of far-UV radiation (UVB and UVC), were assayed for carcinogenicity in three strains of hairless mice (SKH-1, MF-1, and C3H) of both sexes. As assessed in 5 independent experiments, no spontaneous skin tumor was observed, even after more than 2 years, in 49 animals used as unexposed controls or in 29 animals exposed to halogen lamps equipped with a common glass cover. In contrast, almost all of the 185 mice exposed to the light emitted by low-voltage (12 V) and low-power (50 W) tungsten bulbs, equipped with dichroic diffusers, contracted multiple skin tumors of various histological type, both benign and malignant. Tumors were induced over a range of illuminance levels (1,000, 3,333, 5,000, and 10,000 lux) and daily exposure times (1.5, 3, 6, and 12 h). The tumor latency times were quite short and significantly correlated with the daily exposure times, as well as with the square of the distance (46-194 cm) from the illumination source. A carcinogenic effect was even observed when exposure was discontinued well before the appearance of skin lesions. Both in vitro genotoxicity data and animal carcinogenicity data support the view that the light emitted by uncovered halogen lamps, to which an enormous number of individuals are exposed, may pose carcinogenic risks to humans. Without renouncing the benefits of this modern illumination system, UV-blocking devices should be compulsory.

Animals↗

PubMed1997

[Involvement of enhanced glutamate release in halogenated volatile anesthetic-induced excitation in mouse brain].

The present experiments aimed to elucidate the mechanisms of excitatory effects of volatile anesthetics. In ddN mice, enflurane (2% in air), sevoflurane (2%) or isoflurane (1.2%) induced opisthotonus. In ddY mice, a halogenated ethane, tetrachlorodifluoroethane (CCl2FCCl2F:DF-112, 2%) induced tonic-clonic convulsion. These CNS excitatory effects were suppressed by pretreatment with an N-methyl-D-aspartate antagonist, MK-801 (0.5mg.kg-1). Halogenated volatile anesthetics (enflurane, sevoflurane, isoflurane and halothane) increased glutamate release from synaptosomes of the mouse cerebral cortex at concentrations corresponding to those used clinically. The convulsive gas, DF-112, released glutamate more potently than the anesthetics. These data suggest the involvement of enhanced glutamate release in the mechanisms of excitatory effects of halogenated volatile anesthetics.

Anesthetics, Inhalation↗

PubMed2000

On Neglecting the Polar Nature of Halogenated Hydrocarbons in the Surface Energy Determination of Polar Solids from Contact Angle Measurements.

The generally accepted strategy of neglecting the polar nature of halogenated liquids in the surface energy determination using the Lifshitz-van der Waals/Lewis acid-base (LW/AB) approach may lead to erroneous and inconsistent results for polar solids. This was demonstrated in a simulation study carried out on monopolar basic surfaces using water, glycerol, and hypothetical liquids whose surface energy characteristics (gamma(L)(LW)=50 mJ/m(2), gamma(L)(-)=0, and gamma(L)(+)=0-1 mJ/m(2)) were chosen to approximate halogenated hydrocarbons. Neglect of the liquid polarity overestimates the LW component and underestimates the basic parameter of the solid surface energy. This effect increases rapidly with an increase in the actual (nonzero) gamma(L)(+) value of supposedly apolar liquid. Consequently, results with an appropriate level of precision can be obtained only with liquids having gamma(L)(+)<0.02 mJ/m(2). For liquids having gamma(L)(+) approximately 0.5 mJ/m(2) (diiodomethane, s-tetrabromoethane, and, probably, other halogenated hydrocarbons), neglect of the liquid polarity causes errors up to 15% in the LW component and up to 100% in the basic parameter of the solid surface energy. The quantitative trends established in the simulation study were indeed observed in an experimental study performed on the surfaces of poly(methyl methacrylate) and polystyrene using water, glycerol, and diiodomethane or s-tetrabromoethane as the test liquids. Copyright 2000 Academic Press.

Journal Article↗

PubMed1996

Influence of the halogen-substituent pattern of fluoronitrobenzenes on their biotransformation and capacity to induce methemoglobinemia.

In the present study both the biotransformation patterns and the capacity to induce methemoglobinemia of a series of fluoronitrobenzenes were investigated. This was done to investigate to what extent variation in the number and position of the halogen substituents influence the metabolic fate of the fluoronitrobenzenes, thereby influencing their capacity to induce methemoglobinemia. The results obtained were compared to the effect of the fluorine substituent patterns on the calculated electronic characteristics and, thus, on the chemical reactivity of the fluoronitrobenzenes. Analysis of the in vivo metabolic profiles demonstrates a dependence of the extent of nitroreduction, of glutathione conjugation, and of aromatic hydroxylation with the pattern of halogen substitution. With an increasing number of fluorine substituents at electrophilic carbon centers, 24-hr urine recovery values decreased and fluoride anion elimination increased, due to increased reactivity of the fluoronitrobenzenes with cellular nucleophiles. In vitro studies even demonstrated a clear correlation between calculated parameters for the electrophilicity of the fluoronitrobenzenes and the natural logarithm of their rate of reaction with glutathione or with bovine serum albumin, taken as a model for cellular nucleophiles (r = 0.97 and r = 0.98, respectively). Increased possibilities for the conjugation of the fluoronitrobenzenes to cellular nucleophiles were accompanied by decreased contributions of nitroreduction and aromatic hydroxylation to the overall in vivo metabolite patterns, as well as by a decreased capacity of the fluoronitrobenzenes to induce methemoglobinemia. In vitro studies on the rates of nitroreduction of the various fluoronitrobenzenes by cecal microflora and rat liver microsomes revealed that the changes in the capacity of the fluoronitrobenzenes to induce methemoglobinemia were not due to differences in their intrinsic reactivity in the pathway of nitroreduction, leading to methemoglobinemia-inducing metabolites. Thus, the results of the present study clearly demonstrate that the number and position of fluorine substituents in the fluoronitrobenzenes influence the capacity of the fluoronitrobenzenes to induce methemoglobinemia, not because their intrinsic chemical reactivity for entering the nitroreduction pathway is influenced. The different methemoglobinemic capacity must rather result from differences in the inherent direct methemoglobinemic capacity and/or reactivity of the various toxic metabolites and/or from the fact that the halogen substituent pattern influences the electrophilic reactivity, thereby changing the possibilities for reactions of the nitrobenzenes with glutathione and, especially, other cellular nucleophiles. When the number of fluorine substituents increases, the electrophilicity of the fluoronitrobenzenes can become so high that glutathione conjugation is no longer able to compete efficiently with covalent binding of the fluoronitrobenzenes to cellular macromolecules. As a consequence, it can be suggested that with an increasing number of fluorine substituents at electrophilic carbon centers in a nitrobenzene derivative, a toxic end point of the nitrobenzene other than formation of methemoglobinemia can be foreseen.

Acetylcysteine↗

PubMed2004

Plasma versus halogen light: the effect of different light sources on the shear bond strength of brackets.

The aim of this study was to investigate differences between plasma and halogen light polymerization in relation to the attainable shear bond strength of brackets bonded with various adhesives. 720 brackets were divided into 72 different groups of n = 10. The brackets were bonded to 240 flat polished test specimens produced from bovine teeth, Pontor MPF alloy, and extra hard plaster (type III) respectively. Transbond XT, Kurasper F or Fuji Ortho LC served as adhesives to bond either ceramic (Transcend 6000) or stainless steel brackets (Mini Uni-Twin). 50% of all brackets were bonded with a minimum layer of adhesive, and the remaining 50% with an adhesive layer thickness of 1.0 mm. In 360 cases the adhesive was polymerized with a plasma light (PAC), and in a further 360 cases with a halogen light (Optilux 401). The light curing time was 10 s with plasma light and 40 s with halogen light. After 24 h of storage in deionized water at room temperature, all brackets were subjected to a shear bond strength test according to ISO standard 10477. The measured shear bond strength did not differ significantly between the two curing light sources. The 1 mm adhesive layer thickness group showed significantly higher shear bond strengths in comparison to the minimum layer thickness group.

Dental Bonding↗

PubMed2006

Halogen and LED light curing of composite: temperature increase and Knoop hardness.

This study assessed the Knoop hardness and temperature increase provided by three light curing units when using (1) the manufacturers' recommended times of photo-activation and (2) standardizing total energy density. One halogen--XL2500 (3M/ESPE)--and two light-emitting diode (LED) curing units--Freelight (3M/ESPE) and Ultrablue IS (DMC)--were used. A type-K thermocouple registered the temperature change produced by the composite photo-activation in a mold. Twenty-four hours after the photo-activation procedures, the composite specimens were submitted to a hardness test. Both temperature increase and hardness data were submitted to ANOVA and Tukey's test (5% significance). Using the first set of photo-activation conditions, the halogen unit produced a statistically higher temperature increase than did both LED units, and the Freelight LED resulted in a lower hardness than did the other curing units. When applying the second set of photo-activation conditions, the two LED units produced statistically greater temperature increase than did the halogen unit, whereas there were no statistical differences in hardness among the curing units.

Composite Resins↗

PubMed1978

Effects of halogenated antibacterials on the erythrocyte membrane.

The influence of halogenated antibacterials on membrane structure and function was investigated using the human erythrocyte membrane as a model. Measurements of hemolysis in isotonic solution, altered membrane permeability, and stabilization against hypotonic hemolysis resulting from exposure of erythrocytes to halogenated antibacterials served as criteria of membrane-related effects. The hemolytic potency of the compounds studied differed widely, decreasing in the order hexachlorophene (HCP) greater than 2,2'-methylenebis(3,5-dichlorophenol) (3,5-TCP) greater than 2,2'-methylenebis(3,4-dichlorophenol) (3,4-TCP) approximately equal to 2,2'-methylenebis(4,6-dichlorophenol) (4,6-TCP) greater than 2,2'-methylenebis(4-chlorophenol) (DCP) greater than 3,4'-tribromosalicylanilide (TBS) approximately equal to 3,3',4',5-tetrachlorosalicylanilide (TCSA). Each of the antibacterials tested stabilized the erythrocyte against hypotonic hemolysis, although there were marked differences in the concentrations required to afford maximum stabilization as well as in the extent of protection. The observed order of protective effectiveness was HCP greater than 3,4-TCP greater than 4,6-TCP greater than DCP approximately equal to TCS greater than TBS. As shown by measurements of the first-order rate constant for K+ efflux, the permeability of the erythrocyte membrane to K+ was increased upon exposure to the antibacterials, with the effect of HCP greater than 3,4-TCP greater than 4,6-TCP approximately equal to 3,4-TCP greater than DCP approximately equal to TCS greater than TBS. These results indicate that halogenated antibacterials are capable of perturbing mammalian membranes, a feature which may account in part for their mammalian toxicity.

Anti-Infective Agents↗