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PubMed1983

Surfactants selectively ablate enteric neurons of the rat jejunum.

Surfactants, a group of nonspecific membrane perturbating substances, can cause nerve damage. Various concentrations of the cationic surfactants benzalkonium chloride (BAC) and benzethonium chloride, the anionic surfactants sodium ricinoleate, dioctyl sodium sulfosuccinate and sodium lauryl sulfate and the nonionic surfactant Triton X-100 were applied to the serosal surface of the rat jejunum every 5 min for 0.5 hr and then rinsed off with saline. Thirty days after surfactant application, the treated and an untreated segment of jejunum were removed and examined histologically. All surfactants which were tested significantly reduced the number of ganglion cells in the myenteric plexus. In addition, sodium ricinoleate significantly reduced the number of ganglion cells in the submucosal plexus. Higher concentrations of the cationic agents BAC and benzethonium chloride caused a generalized tissue damage including disruption of the smooth muscle, lymphocytic infiltration, intestinal perforation and death. Using BAC as a prototype surfactant, peptidergic neuron distribution and gut electrical activity were examined. BAC treatment markedly reduced the immunoreactivity of somatostatin, substance P, met-enkephalin and vasoactive intestinal peptide in the myenteric plexus. In addition, the electric properties of the smooth muscle were altered. BAC treatment resulted in an erratic, markedly distorted basic electric rhythm and an alteration in spike potential generation. These studies demonstrate that surfactants in appropriate concentrations selectively ablate the myenteric neurons and alter peptidergic neuron distribution and gut electrical parameters in the rat jejunum.

Animals↗
PubMed1984

Direct quantitation of antiseptic quaternary ammonium compounds by fast atom bombardment mass spectrometry.

The medicinally important quaternary ammonium salts benzyldimethyltetradecylammonium chloride (BDTA), cetylpyridinium chloride and benzethonium chloride, all afford, under fast atom bombardment (FAB) mass spectrometric conditions, abundant and persistent [M-Cl]+ species usefully amenable to quantitative analysis with the aid of thioglycerol as a liquid FAB matrix. The use of BDTA as an internal standard allowed a direct, precise and accurate determination of cetylpyridinium and benzethonium chlorides, either as pure samples or in dosage forms, in the concentration range 0.05-2 mg/ml.

Journal Article↗
PubMed2006

Development and validation of an HPLC/UV/MS method for simultaneous determination of 18 preservatives in grapefruit seed extract.

Grapefruit seed extracts are used in cosmetics, food supplements, and pesticides because of their antimicrobial properties, but suspicions about the true nature of the active compounds arose when synthetic disinfectants such as benzethonium or benzalkonium chloride were found in commercial products. The HPLC method presented herein allows the quality assessment (qualitative and quantitative) of these products for the first time. On the basis of a standard mixture of 18 preservatives most relevant for food and grapefruit products, a method was developed allowing the baseline separation of all compounds within 40 min. Optimum results were obtained with a C-8 stationary phase and a solvent system comprising aqueous trifluoroacetic acid, acetonitrile, and 2-propanol. The assay was fully validated and shown to be sensitive (LOD < or= 12.1 ng on-column), accurate (recovery rates > or = 96.1%), repeatable (sigma(rel) < or = 3.5%), precise (intra-day variation < or = 4.5%, interday variation < or = 4.1%), and rugged. Without any modifications the method could be adopted for LC-MS experiments, where the compounds of interest were directly assignable in positive ESI mode. The quantitative results of several products for ecofarming confirmed previous studies, as seven out of nine specimens were adulterated with preservatives in varying composition. The samples either contained benzethonium chloride (2.5-176.9 mg/mL) or benzalkonium chloride (138.2-236.3 mg/mL), together with smaller amounts of 4-hydroxybenzoic acid esters, benzoic acid, and salicylic acid.

Chromatography, High Pressure Liquid↗
PubMed2001

Effect of concentration and biochemical assay on the accuracy of urine dipsticks in hypertensive pregnancies.

OBJECTIVE: To assess how urine concentration and biochemical assay influence the assessment of proteinuria. METHODS: This was a prospective study to assess the accuracy of detection and quantification of proteinuria within the day assessment unit and antenatal ward of a teaching hospital in Leicester, United Kingdom. We studied hypertensive pregnancies (of mixed parity) referred to day care assessment or attending the antenatal hypertension clinic after 20 completed weeks of gestation (n = 197). Aliquots of a well-mixed 24-h urine collection were tested by routine dipstick urinalysis and then assayed for protein using the Benzethonium Chloride and the Bradford assays (n = 197). MAIN OUTCOME MEASURES: Total protein excretion in 24 h and protein concentration per liter of urine for both biochemical assays were compared to semiquantitative dipstick protein measurement. RESULTS: The prevalence of proteinuria in the study group varied according to the method used for testing. Dipstick urinalysis recorded the lowest prevalence (16.2%) and the Benzethonium Chloride assay measuring total protein excretion in 24 h recorded the highest (70.1%). When the positive and negative predictive values for dipstick urinalysis were calculated, performance was found to be dependent on both the units of measurement compared and the type of assay used as the "gold standard." Positive predictive values ranged from 87.5% to 96.9% and negative predictive values ranged from 35.2% to 92.1%. CONCLUSIONS: The prevalence of proteinuria in hypertensive pregnancies is dependent on the method used to detect it. The amount of protein assessed quantitatively is further dependent on the biochemical assay employed. However, regardless of the quantitative assessment, dipstick urinalysis has a significant false-negative rate. This first reporting of a variation in performance between dipstick urinalysis and two different biochemical assays in pregnancy may be explained in relation to protein assay specificity and the observed protein compositions of the samples on electrophoretic analysis. The significance of proteinuria should be considered in light of the method used to detect it, but, ultimately, it must be related to clinical outcome.

Adolescent↗
PubMed1985

Three turbidimetric methods for determining total protein compared.

We used human serum protein fractions to evaluate the sensitivity and bias of three turbidimetric methods for determining concentrations of proteins. Each fraction (Cohn Fractions II, III, IV, and V) was assigned a protein concentration value that was determined by the biuret method, which we calibrated with purified monomer of human serum albumin. All three turbidimetric methods (those involving sulfosalicylic acid/sodium sulfate, trichloroacetic acid, and alkaline benzethonium chloride) gave acceptable results for Fraction V with crystallized human serum albumin as the reference material, but there was bias by each of the three methods for the three globulin fractions. The method involving alkaline benzethonium chloride with measurement at 450 nm had the best sensitivity within the range of linearity and the most consistent bias among the three globulin fractions. These results define the dilemma for valid calibration of these methods for total serum protein in cerebrospinal fluid and urine.

Biuret↗
PubMed1982

Studies on viral respiratory disease in laboratory cats. I. Isolation of feline herpesvirus and choice of proper disinfectant.

In the laboratory cat colony consisted of 14 Korats and 8 Japanese native cats, the disease characterized by upper respiratory signs occurred. Seven cytopathogenic agents were isolated from the oropharyngeal swabs and necropsy materials of affected cats by means of inoculation to primary feline kidney cell cultures. One of the isolates (KS-1 strain) was identical with feline herpesvirus (FHV), and appeared to be a causal agent of the trouble. Properties of the KS-1 strain were in general agreement with the known strains of FHV. Serologic examination and clinical analysis suggested that Japanese native cats became carriers, re-excreted the virus and spread it to susceptible cats. Virucidal activities of several disinfectants against FHV, comparing with a feline calicivirus (FCV), were studied and the following conclusions reached: 1) Sodium hypochlorite, iodine complex, benzethonium chloride and chlorhexidine were effective against FHV at commonly used concentrations. 2) Among chemicals tested sodium hypochlorite was most effective against FCV and followed by iodine complex. 3) Benzethonium chloride and chlorhexidine had little efficacy against FCV at commonly used doses.

Animals↗
PubMed1979

Direct spectorphotometric assay of quaternary ammonium compounds using bromthymol blue.

Benzalkonium chloride, benzethonium chloride, and chlorhexidine gluconate were assayed quantitatively by a direct spectrophotometric method with bromthymol blue buffered at pH 7.5. The method shows good results at concentrations of 0--300 microgram/ml and in the presence of epinephrine bitartrate, phenylephrine hydrochloride, pilocarpine hydrochloride, and polyvinyl alcohol.

Benzalkonium Compounds↗
PubMed1996

A nonpeptidal peptidomimetic agonist of the insect FLRFamide myosuppressin family.

Benzethonium chloride (Bztc) is the first totally nonpeptide ligand for an insect, indeed an invertebrate, peptide receptor. Bztc mimics the inhibitory physiological activity of the myosuppressins, a subfamily of the FLRFamides, in three different insect bioassay systems. The inhibitory action of leucomyosuppressin and the nonpeptide Bztc in both the cockroach hindgut and the mealworm neuromuscular junction can be blocked by the lipoxygenase inhibitor, nordihydroguaiaretic acid, providing evidence for similar modes of action. Lipoxygenase metabolites of arachidonic acid may mediate inhibition of neuromuscular transmission by these two factors. In addition, Bztc competitively displaces a radiolabeled myosuppressin analogue from high- and low-affinity receptors of the locust oviduct. Thus, the nonpeptide interacts with both binding and activating regions of myosuppressin receptors. Molecular dynamics experiments in which selected functional groups of Bztc were fit onto corresponding functional groups of low-energy myosuppressin pentapeptide structures indicate how Bztc may mimic the myosuppressins at a molecular level. The discovery of Bztc as a nonpeptidal peptidomimetic analogue provides an opportunity to develop new pest management strategies by targeting an insect's own peptide receptor.

Amino Acid Sequence↗
PubMed1999

The modulation of skeletal muscle contraction by FMRFamide-related peptides of the locust.

The external ventral protractor muscle of the VIIth abdominal segment, M234, is a skeletal muscle that possesses receptors that recognize a range of FMRFamide-related peptides and application of these peptides results in an increase in the amplitude of neurally evoked contractions with little or no effect on basal tonus. FLRFamide itself has the same biologic activity as the extended peptides, whereas truncation to LRFamide or RFamide results in a peptide with no biologic activity. The receptors recognizing these extended FLRFamides, which include SchistoFLRFamide, seem to be different from the SchistoFLRFamide receptors found on locust oviduct visceral muscle. SchistoFLRFamide and the non-peptide mimetic, benzethonium chloride (Bztc), increase the frequency and amplitude of miniature endplate potentials, increase the amplitude of neurally evoked excitatory junction potentials, and result in a hyperpolarisation of resting membrane potential. Bztc, however, also abolishes the active membrane response that may explain its ability to decrease neurally evoked contractions.

Amino Acid Sequence↗
PubMed1990

Acanthamoeba keratitis--resistance to medical therapy.

Successful medical therapy of Acanthamoeba keratitis has been reported with combination therapy; topical Brolene and neomycin. Resistance has not so far been identified as a problem, but was the basis for recurrent disease observed in a patient with bilateral infection. Eradication of amoebae was finally achieved following prolonged topical therapy and two corneal grafts in each eye. Topical anti-amoebic therapy with paromomycin, benzethonium chloride, clotrimazole and R11/29 (a phenanthridinium compound), was continued for three months post-operatively. No further recurrences occurred during 14 months' follow-up. Drug sensitivities were performed for three isolates of Acanthamoeba sp (group II) which demonstrated the development of resistance to Brolene and arsenic. In addition, the resistant isolates were temperature-sensitive mutants which would not grow at temperatures above 30 degrees C. This could explain 'culture-negative' results in some cases of clinical recurrence when incubation of laboratory samples had only been performed at 37 degrees C.

Acanthamoeba Keratitis↗
PubMed1995

A nonpeptide agonist of the invertebrate receptor for SchistoFLRFamide (PDVDHVFLRFamide), a member of a subfamily of insect FMRFamide-related peptides.

We describe a nonpeptide mimetic analog of an invertebrate peptide receptor. Benzethonium chloride (Bztc) is an agonist of the SchistoFLRFamide (PDVDHVFLRFamide) receptors found on locust oviducts. Bztc competitively displaces [125I-labeled Y1]SchistoFLRFamide binding to both high- and low-affinity receptors of membrane preparations. Bztc mimics the physiological effects of SchistoFLRFamide on locust oviduct, by inhibiting myogenic and induced contractions in a dose-dependent manner. Bztc is therefore recognized by the binding and activation regions of the SchistoFLRFamide receptors. This discovery provides a unique opportunity within insects to finally target a peptide receptor for the development of future pest management strategies.

Amino Acid Sequence↗
PubMed2001

Effectiveness of manual cleaning and disinfection of gastroendoscopes with 3% glutaraldehyde for decreasing risk of transmission of hepatitis C virus.

OBJECTIVES: The effectiveness of manual cleaning and disinfection of gastroendoscopes with 3% glutaraldehyde in decreasing the risk of transmission of hepatitis C virus (HCV) was examined. METHODS: Gastroendoscopes used for treatment of endoscopic esophageal variceal ligation in patients with HCV infection were manually cleaned and disinfected with 3% glutaraldehyde (n = 25), 2% glutaraldehyde (n = 17), or 0.1% benzethonium chloride (n = 25). Samples were obtained by pouring 20 ml of 0.9% NaCl solution into the biopsy-suction channel of the scope before and after cleaning and disinfection. HCV was detected with the polymerase chain reaction. RESULTS: Of the 25 scopes in 3% glutaraldehyde group, nine (36%) were positive for HCV before cleaning and disinfection, but all became negative after cleaning and disinfection; the difference was statistically significant (p < 0.01). In contrast, in 2% glutaraldehyde group and in the routine cleaning group, there were no significant differences in the number of positive samples between before and after cleaning and disinfection. CONCLUSION: Manual cleaning and disinfection of gastroscopes with 3% glutaraldehyde is useful for decreasing the risk of transmission of HCV among patients.

Benzethonium↗
PubMed2002

In vitro evaluation of skin sensitivity of povidone-iodine and other antiseptics using a three-dimensional human skin model.

Povidone-iodine (PVP-I) is an antiseptic which has been widely used in various fields. It was reported to have a weaker skin irritancy than other antiseptics in the Draize skin irritation test using rabbits. Recent increased concern for animal welfare requires us to use skin models in the tests as an alternative to animal testing. Actually, there are some skin models already commercialized, which are available to evaluate skin irritancy caused by e.g. chemical reagents, cosmetics or medicines. In this study, we evaluated the potential of a PVP-I solution and other antiseptics to cause irritation using a cultured human skin model (three-dimensional skin model) under conditions similar to clinical use. This skin model has two layers like a real skin, such as the dermis and epidermis which includes the cornified layer. For the evaluation of skin irritancy in this model, cell viability was evaluated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay as an endpoint. Antiseptic formulations such as benzalkonium chloride (BAC), benzethonium chloride (BEC), chlorhexidine gluconate (CHG) and alkyldiaminoethylglycine hydrochloride (AEG) were used in this study. As a result, PVP-I showed a significantly weaker skin irritancy compared to the other antiseptics. The present in vitro study results revealed a correlation with the results of previously conducted in vivo skin irritancy tests using rabbits.

Anti-Infective Agents, Local↗
PubMed2006

In vitro short-time killing activity of povidone-iodine (Isodine Gargle) in the presence of oral organic matter.

In order to estimate the clinical efficacy of a povidone-iodine oral antiseptic (PVP-I) on oral bacterial infectious diseases, we studied the effect of oral organic matter on the in vitro killing activity of PVP-I. In addition, we compared the in vitro short-time killing activity of PVP-I with those of other oral antiseptics using mouth-washing and gargling samples collected from healthy volunteers. When any of the mouth-washing and gargling samples was used, the standard (0.23-0.47%) or lower concentrations of PVP-I killed methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa, including multidrug-resistant strains, within 15-60 s in the presence of oral organic matter. 0.02% benzethonium chloride (BEC) and 0.002% chlorhexidine gluconate (CHG) did not show effects against MRSA and P. aeruginosa (including multidrug-resistant strains) in mouth-washing and gargling samples even after 60 s. The above-mentioned results show that the in vitro killing activity of the standard concentration of PVP-I was hardly affected by the oral organic matter and that a mouth-washing or gargling solution containing PVP-I has a stronger bactericidal activity than BEC and CHG. Although mouth-washing and gargling samples were obtained from healthy individuals in this study, PVP-I may be used for protection against infections in patients with various diseases, if proper concentrations and usage are encouraged.

Anti-Infective Agents↗
PubMed1997

Inactivation of human viruses by povidone-iodine in comparison with other antiseptics.

Inactivation of a range of viruses, such as adeno-, mumps, rota-, polio- (types 1 and 3), coxsackie-, rhino-, herpes simplex, rubella, measles, influenza and human immunodeficiency viruses, by povidone-iodine (PVP-I) and other commercially available antiseptics in Japan was studied in accordance with the standardized protocol in vitro. In these experiments, antiseptics such as PVP-I solution, PVP-I gargle, PVP-I cream, chlorhexidine gluconate, alkyldiaminoethyl-glycine hydrochloride, benzalkonium chloride (BAC) and benzethonium chloride (BEC) were used. PVP-I was effective against all the virus species tested. PVP-I drug products, which were examined in these experiments, inactivated all the viruses within a short period of time. Rubella, measles, mumps viruses and HIV were sensitive to all of the antiseptics, and rotavirus was inactivated by BAC and BEC, while adeno-, polio- and rhinoviruses did not respond to the other antiseptics. PVP-I had a wider virucidal spectrum, covering both enveloped and nonenveloped viruses, than the other commercially available antiseptics.

Adenoviridae↗
PubMed2006

Ormosil nanocomposite materials as modifiers for acrylic coating systems.

Organically modified silica (ormosil) particles were prepared using hydrolytic sol-gel methods and the miniemulsion polymerisation approach. Methyl-, ethyl-, and phenylsilsesquioxane nanoparticles with diameters in the range 50-180 nm were obtained using the modified Stöber method with an aqueous sodium silicate solution used as a seed for further growth of the particles. Methyl- and phenylsilsesquioxane particles were prepared by a sol-gel method in the presence of benzethonium chloride used as a surfactant. The miniemulsion polymerisation approach has been extended to the production of methacrylate-modified silica nanoparticles with vinylpyridine or lauryl methacrylate used as comonomers both in the presence and in the absence of a surfactant. Styryl-modified silica particles with diameters in the range 300-800 nm were obtained by the Stöber method using pre-formed SiO2 nanoparticles as the seeds for silsesquioxane nanoparticle formation. The effect of incorporation of the particles produced using different synthetic methods on hardness and water resistance of acrylic coating systems was studied here.

Acrylates↗
PubMed1981

Long-term antiplaque, anticalculus, and antigingivitis effects of benzethonium/polymer complex in beagle dogs.

An electrostatic complex of 0.1% benzethonium chloride (BTC) plus 0.05% copolymer of methoxyethylene and maleic acid was evaluated in vitro for antibacterial effect. The complex by itself showed as much antibacterial activity as 0.1% BTC. The adsorption of 14C-BTC on saliva-coated hydroxyapatite disks and teeth in vitro was lower from the complex than the BTC solution, although in vivo activity was the same. The complex, BTC, and polymer solutions were evaluated in a 28-week study in 16 beagle dogs against plaque, gingivitis, and calculus formation. BTC and the complex significantly (alpha = 0.05) reduce plaque and gingivitis. There was no significant difference between the two active groups. BTC (0.1%) significantly increased calcified deposits at 22-28 wk compared to the water control group, while the complex and the polymer groups showed significantly (alpha = 0.05) less calculus. Thus, the complex was not only effective in vivo, but also significantly (alpha = 0.05) reduced tendencies of cationic antibacterials to induce calcified deposits on teeth.

Adsorption↗
PubMed1999

[Quantitative analysis of factors to influence the environment of the clean room and clean bench during preparation of intravenous hyperalimentation (IVH) admixtures].

We quantitatively studied factors influencing the environment cleanliness for intravenous hyperalimentation (IVH) admixing. The environment cleanliness was evaluated by measuring the counts of particles (> 0.5 micron) and bacteria floating in 1 ft3 of the air inside the clean room (23.6 m3) and in the clean bench built in the department of pharmacy, The University of Tokyo Hospital in 1998. The number of particles at the center of the clean room during IVH admixing by 4 pharmacists was higher than that at the medicine passing area (150 +/- 50/ft3 vs. 260 +/- 60/ft3; mean +/- S.D., n = 12). The cleanliness inside the clean room was improved as the measurement point became higher from the floor (600 +/- 180/ft3, 150 +/- 50/ft3, and 35 +/- 15/ft3 at 50, 100, and 150 cm height, respectively) and the number of persons working inside the room decreased. The changes in the counts of floating bacteria were similar to that of floating particles under the same conditions. In addition the effect of disinfection on the counts of bacteria was clearly observed. When the cleanliness of the room became lower by turning off the air conditioning, the particle counts inside the clean bench became lower along with the distance from the front glass becoming deeper (i.e., 1400 +/- 550/ft3, 140 +/- 70/ft3, and 40 +/- 30/ft3 at 0, 5, and 15 cm, respectively). From these lines of evidence, the following items were suggested in order to maintain the environment cleanliness for IVH admixing. First, the number of persons residing in the clean room should be kept to be minimum. Second, the clean bench should be set up in the center of the clean room. Finally IVH admixing operation should be performed at more than 15 cm depth inside the front glass surface of the clean bench. Moreover, the effect of mopping-up of the clean room with 0.1% benzethonium chloride clearly demonstrated the importance of disinfection on a routine basis.

Air Conditioning↗