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PubMed2000

Bacterial spore inhibition and inactivation in foods by pressure, chemical preservatives, and mild heat.

Sucrose laurates, sucrose palmitate, sucrose stearates, and monolaurin (Lauricidin) were evaluated for inhibitory effects against spores of Bacillus sp., Clostridium sporogenes PA3679, and Alicyclobacillus sp. in a model agar system. The combined treatment of sucrose laurate, high hydrostatic pressure, and mild heat was evaluated on spores of Bacillus and Alicyclobacillus in foods. The minimum inhibitory concentrations of the sucrose esters were higher than that of Lauricidin for all spores tested in the model agar system, but Lauricidin was not the most readily suspended in the test media. The sucrose laurates and sucrose palmitate were more effective and more readily suspended than the sucrose stearates. A combined treatment of sucrose laurate (<1.0%), 392 megaPascals (MPa) at 45 degrees C for 10 to 15 min provided 3- to 5.5-log10 CFU/ml reductions from initial populations of 10(6) CFU/ml for Bacillus subtilis 168 in milk, Bacillus cereus 14579 in beef, Bacillus coagulans 7050 in tomato juice (pH 4.5), Alicyclobacillus sp. N1089 in tomato juice (pH 4.5), and Alicyclobacillus sp. N1098 in apple juice. The most notable change in the appearance of the products was temporary foaming during mixing of the sucrose laurate in the foods. The effect of sucrose laurate appeared to be inhibitory rather than lethal to the spores. The inhibitory effects observed on Bacillus and Alicyclobacillus spores by the combined treatment of pressure, mild heat, and sucrose laurate appear promising for food applications where alternatives to high heat processing are desired.

Animals↗
PubMed1975

Occupational lead exposure in Finland. IV. The polyvinyl chloride plastic industry.

One hundred and fifty-two workers from ten polyvinyl chloride (PVC) plastic factories were studied for lead exposure. Blood lead (Pb-B) concentration was measured for all the workers, urinary delta-aminolevulinic acid (ala) for 130 workers, erythrocyte alpha-aminolevulinic acid dehydratase (ala-d) activity for 59 workers, and blood hemoglobin concentration or 93 workers. The median Pb-B for all the workers was 37 mug/100 ml, and the highest median found for one factory was 63 mug/100 ml. The highest single Pb-B value found was 126 mug/100 ml. The jobs with the heaviest lead exposure were those of mixing and weighing lead stearate powder. It is assumed that replacing the powder with a granule form of lead stearate will diminish the hazard of lead exposure in the future. Urinary ALA concentrations and erythrocyte ALA-D activities corresponded well with the Pb-B concentration, but the hemoglobin values did not show any relation to lead exposure. It is concluded that in the PVC plastic industry of Finland the risk of exposure to lead is high and regular health examinations should be performed.

Aminolevulinic Acid↗
PubMed1986

Effects of a new fluorinated macrolide (P-0501A) and other erythromycins on drug metabolizing enzymes in rat liver.

The effects of a new fluorinated macrolide (P-0501A) on drug metabolizing enzymes of rat liver were compared with three erythromycins--the base, the stearate and the estolate--after 7 days of dosing (1.36 mmol/kg po daily). The three erythromycins induced the synthesis of microsomal enzymes, but the products of their metabolism inactivated cytochrome P-450 in the order base less than or equal to stearate less than estolate. N-Demethylation of erythromycin and aminopyrine increased, while O-demethylation of 4-nitroanisole was reduced and hydroxylation of aniline was not changed after in vivo treatment. Pentobarbital sleeping time was prolonged and liver glutathione levels were lower in treated rats than in controls. In contrast to the three erythromycins, P-0501A did not induce the synthesis of microsomal enzymes, did not form an inactive complex with cytochrome P-450 and did not affect mono-oxygenase activities or pentobarbital narcosis.

Administration, Oral↗
PubMed1982

Pharmaceutical Reimbursement Board; final maximum allowable cost (MAC) determinations for certain drug products--Health Care Financing Administration. Final notice.

The Pharmaceutical Reimbursement Board announces the suspension of the maximum allowable cost (MAC) limit on erythromycin stearate, oral tablets, 500 mg, effective November 17, 1982. The limit for this drug product was published in the Federal Register on December 11, 1978 (43 FR 57972) and became effective on January 25, 1979. This suspension of the MAC limit on erythromycin stearate, oral tablets, 500 mg, is based on general price increases by manufacturers that have occurred in the marketplace and the Board's concern that this drug product may no longer be widely and consistently available at the established MAC limit. The Pharmaceutical Reimbursement Board may reinstitute procedures to establish a new MAC limit on this drug product in the future.

Centers for Medicare and Medicaid Services, U.S.↗
PubMed1999

A novel Lyn-binding peptide inhibitor blocks eosinophil differentiation, survival, and airway eosinophilic inflammation.

Receptor antagonists block all receptor-coupled signaling pathways indiscriminately. We introduce a novel class of peptide inhibitors that is designed to block a specific signal from a receptor while keeping other signals intact. This concept was tested in the model of IL-5 signaling via Lyn kinase. We have previously mapped the Lyn-binding site of the IL-5/GM-CSF receptor common beta (beta c) subunit. In the present study, we designed a peptide inhibitor using the Lyn-binding sequence. The peptide was N-stearated to enable cellular internalization. The stearated peptide blocked the binding of Lyn to the beta c receptor and the activation of Lyn. The lipopeptide did not affect the activation of Janus kinase 2 or its association with beta c. The inhibitor blocked the Lyn-dependent functions of IL-5 in vitro (e.g., eosinophil differentiation from stem cells and eosinophil survival). It did not affect eosinophil degranulation. When applied in vivo, the Lyn-binding peptide significantly inhibited airway eosinophil influx in a mouse model of asthma. The lipopeptide had no effect on basophil histamine release or on the proliferation of B cells and T cells. To our knowledge, this is the first report on an inhibitor of IL-5 that blocks eosinophil differentiation, survival, and airway eosinophilic inflammation. This novel strategy to develop peptide inhibitors can be applied to other receptors.

Amino Acid Sequence↗
PubMed2001

Long-term stability characterization of a controlled release gastrointestinal therapeutic system coated with a cellulose acetate pseudolatex.

The objective of the present study was to study the long term effects of storage of osmotically controlled gastrointestinal therapeutic system (GITS) in exaggerated conditions of temperature and humidity. Bilayered osmotic tablets were obtained with atenolol, Polyox N80, Carbopol 934P and magnesium stearate in one layer, and Polyox 303, Carbopol 974, sodium chloride and magnesium stearate in the other layer. A customized cellulose acetate (CA) pseudolatex was used to provide semipermeable housing around the tablet and an orifice was drilled into the drug layer to obtain the Atenolol GITS. The GITS were stored at 4 degrees C (refrigeration), 25 degrees C, 37 degrees C, 45 degrees C, 55 degrees C, 37 degrees C/11% RH, 37 degrees C/51% RH, and 37 degrees C/91% RH. Quantitative X-ray diffraction and dissolution studies were performed at regular intervals for one year. Aqueous CA polymeric film formation continued in GITS stored at higher temperature by gradual evaporation of moisture and coalescence of polymer. At lower temperatures atenolol crystallinity increased with time, but at higher temperatures the crystallinity was decreased. At higher humidity, a decrease in crystallinity was observed. A decrease in dissolution rate and extent was observed at higher temperature and higher humidity conditions. Exaggerated temperature and humidity conditions affected the dissolution profile by modifying the CA pseudolatex membrane and crystallinity of atenolol.

Adrenergic beta-Antagonists↗
PubMedDate not supplied

[Extracellular metabolites of hydrocarbon-oxidizing bacteria as a substrate for sulfate reduction].

The relationship between bacterial oxidation of hydrocarbons and sulfate reduction was studied in the experimental system with liquid paraffin was used as a source of organic compounds inoculated with silt taken from a reservoir. Pseudomonads dominated in the hydrocarbon-oxidizing silt bacteriocenosis. However, Rhodococcus and Arthrobacteria amounted to not more than 3%. Arthrobacteria dominated the microbial association formed in the paraffin film of the model system. Sulfate-reducing bacteria were represented by genera Desulfomonas, Desulfotomaculum, and Desulfovibrio. The growth of sulfate-reducing bacteria in media containing with paraffin, successive products of its oxidation (cetyl alcohol, stearate, and acetate), and extracellular metabolites of hydrocarbon-reducing bacteria was studied. The data showed that sulfate-reducing bacteria did not use paraffin or cetyl alcohol as growth substrates. However, active growth of sulfate-reducing bacteria was observed in the presence of stearate and extracellular water-soluble or lipid metabolites of Arthrobacteria.

Gram-Negative Anaerobic Bacteria↗
PubMedDate not supplied

[Changes in the lipid physical state in human erythrocyte membranes subjected lead exposure in vitro].

The effect of lead acetate on the physical state of membrane lipids in human erythrocytes in vitro was studied using the lipophilic fluorescence probe 1,6-diphenyl-1,3,5-hexatriene and spin probes 16-doxyl-stearate and iminoxyl palmitic acid. It was shown that 2-10 microM lead acetate causes an increase in both intensity and polarization of fluorescence of 1,6-diphenyl-1,3,5-hexatriene, indicating changes in the microviscosity of the lipid bilayer of erythrocyte membranes. Judging from the parameters of EPR spectra of 16-doxyl stearate and iminoxyl palmitic acid incorporated into erythrocyte membranes, 2-10 microM lead acetate increases the heterogeneity of the lipid bilayer in surface and deep hydrophobic layers of the erythrocyte membrane.

Cyclic N-Oxides↗
PubMed2000

[The study of the microwave reaction of stearic acid and pentyl amine].

In this study, the microwave reaction of stearic acid and pentyl amine was investigated by FTIR spectroscopy. The results indicated that after mixing the two reactants together, pentyl ammonium stearate was created and it formed acid-salt structure with the stearic acid remained. The results also demonstrated that under microwave radiation, the pentyl ammonium stearate could be not only decomposed, but also dehydrated to form stearic pentyl amide. It suggested that the microwave radiation was an ideal technique to make this chemical reaction much faster and much more thorough.

Amines↗
PubMed2004

[Study of mixed dry binders in directly compressible lactoses and microcrystalline cellulose].

The paper evaluated the compressibility of dry binders prepared in the ratios of 3:1, 1:1, and 1:3 from Pharmatosa DCL 15 and DCL 21 and Avicel PH 200, and the sensitivity of the mixtures to an addition of the lubricant magnesium stearate from the standpoint of the effect on the strength of tablets. Mixtures of lactoses with Avicel PH -200 in a ratio of 3:1 proved to be most advantageous. The strengths of tablets made of these mixtures oscillated in the optimal range and they showed the least sensitivity to the added lubricant. An increase in stearate concentration did not result in a marked decrease in the strength of compacts. Pharmatosa DCL 21 in a mixture with Avicel PH 200 yielded stronger compacts at lower compression force than Pharmatosa DCL 15.

Cellulose↗
PubMed1992

Purification and characterization of fatty acid ethyl ester synthase-II from human myocardium.

Fatty acid ethyl ester synthases metabolize ethanol nonoxidatively in those extrahepatic organs most commonly damaged by alcohol abuse. This study was designed to isolate and purify human myocardial synthase-II, one of the enzymes responsible for catalyzing the formation of fatty acid ethyl esters. DEAE-cellulose chromatography of human myocardial cytosol at pH 8.0 separated synthase-I, synthase-II, and synthase-III activities, eluting at conductivities of 5, 7, and 11 mS, respectively. From this elution profile, fatty acid ethyl ester synthase-II accounts for up to 50% of total synthesis in the human heart. This enzyme species was purified over 2200-fold to homogeneity after chromatography over hydroxylapatite, CM-cellulose, and hydroxylapatite. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis of this homogeneous species showed a single band at 65 kDa which corresponded to its molecular weight determined by gel filtration. This molecular weight and its lack of glutathione transferase activity indicate that this species is not related to synthase-I and -III. Homogeneous synthase-II has a Vmax for palmitate, stearate, oleate, and linoleate of 70, 80, 140, and 120 nmol/mg/h, respectively. The Km for palmitate, stearate, oleate, and linoleate is 0.19, 0.12, 0.10, and 0.18 mM, respectively. The substrate specificity with respect to alcohol chain length was also investigated in the presence of 0.65 mM [14C]oleic acid. The Vmax for methanol, ethanol, propanol, and butanol was 180, 100, 280, and 410 nmol/mg/h, respectively. The Km for methanol, ethanol, propanol, and butanol was 1.16, 1.04, 0.58, and 0.33 M, respectively. The N-terminal 17-amino acid sequence of human synthase-II does not correspond to any known N-terminal amino acid sequence, indicating that this may be a novel protein. However, it has over 70% homology to a sequence close to the C terminus of rabbit cytochrome P-450IIC1 and over 50% homology to a sequence of human hemopexin starting at residue 16. Synthase-II does not cross-react with human hemopexin antibody and rat cytochrome P-450C antibody. Thus, this study provides evidence that synthase-II is a novel protein, distinct from synthase-I and -III, and it also provides a foundation for subsequent cloning and genetic studies of fatty acid ethyl ester synthase-II in man.

Acyltransferases↗
PubMedDate not supplied

The influence of pharmaceutical excipients on quinapril hydrochloride stability.

The objective of this study was to determine the effect of povidone. hydroxypropyl methylcellulose, hydroxypropyl cellulose, lactose and magnesium stearate on the stability of quinapril hydrochloride. The applied HPLC method was validated by the following parameters: selectivity, precision, linearity and accuracy. Binary 1:4 mixtures of quinapril hydrochloride and selected excipients were stable at 318 K/76.4%RH and at 318 K/0%RH. The kinetic parameters of the degradation reaction of quinapril hydrochloride in the presence of excipients were calculated. The degradation of quinapril hydrochloride with acidic excipients was significantly lower than that observed for the basic excipients (magnesium stearate) under the same study conditions. The degradation rate constant was approximately 100 fold greater than the decomposition in the quinapril hydrochloride alone. Thus, the pathway of degradation of quinapril hydrochloride in model drug-excipient mixtures was depended on pH of excipients and humidity.

Chromatography, High Pressure Liquid↗
PubMed1991

The autoactivation of factor XII in the presence of long-chain saturated fatty acids--a comparison with the potency of sulphatides and dextran sulphate.

The incubation of purified human factor XII (Hageman factor [HF]) in the presence of long-chain saturated fatty acids (FA) like stearate (C-18) or behenate (C-22) resulted in a time-dependent increase of amidolytic activity. The HF autoactivation progress curves were sigmoidal. The first order rate for the initial period was constant; this was followed by a period of decreasing rate and a plateau of zero rate. These progress curves were similar to those obtained on the incubation of HF in the presence of sulphatide vesicles or dextran sulphate. The initial rate of autoactivation of HF was dependent on the FA concentration of contact surface and increased with increasing concentration of HF. At constant concentration of contact surface and varying concentration of HF, autoactivation rates in the presence of behenate, sulphatide vesicles or dextran sulphate followed Michaelis-Menten kinetics. The Km values for all three contact surfaces were above the physiological plasma concentration of HF whereas the catalytic efficiency in the presence of behenate (0.034 microM-1s-1) was about 2/3 of that in the presence of sulphatide vesicles (0.053 microM-1s-1) and considerably higher than that in the presence of dextran sulphate (0.004 microM-1s-1). Long-chain saturated FA bound to human serum albumin at the high- or low-affinity sites are ineffective, whereas the crystalline non-bound stearate or behenate provided a potent contact surface.(ABSTRACT TRUNCATED AT 250 WORDS)

Dextran Sulfate↗
PubMed1990

Defective elongation of fatty acids in a recessive 25-hydroxycholesterol-resistant mutant cell line.

The Chinese hamster ovary recessive mutant, crB, has been selected for its resistance to the cytotoxic effects of 25-hydroxycholesterol in sterol-free media (Sinensky, M., Logel, J., and Torget, R. (1982) J. Cell. Physiol. 113, 314-319). Growth of crB in a chemically defined lipid-poor medium is very slow and is enhanced by a mixture of saturated and unsaturated fatty acids. Incorporation of [3H]acetate into total fatty acids is 4-fold lower in crB compared to that in parental Chinese hamster ovary K1 and in contrast to the wild-type cells, crB cells are unable to synthesize either stearate or oleate. In addition, crB cells can not elongate exogenous palmitate, while they are capable of desaturating exogenous stearate. The mutant cells are also pleiotropically defective in the regulation of mRNA levels for the enzymes of cholesterol biosynthesis. 25-Hydroxycholesterol is a poor regulator of the synthesis and degradation of the rate-limiting enzyme, 3-hydroxy-3-methylglutaryl-coenzyme A reductase in crB in comparison to the wild-type Chinese hamster ovary K1 cells. The defect in the elongation of fatty acids is reversed in revertants of crB selected for their ability to grow in lipid-poor medium. Such revertants exhibit normal regulation of 3-hydroxy-3-methylglutaryl-CoA reductase activity by 25-hydroxycholesterol. Regulation of reductase activity in crB cells can also be restored by supplementing the culture medium with a mixture of fatty acids that restores normal growth rate. The defective regulation of reductase in crB does not appear to be due to nonspecific adverse effects of fatty acid starvation nor is it due to any gross change in the fatty acid composition of cellular phospholipids. These results strongly suggest a direct relationship between the fatty acid auxotrophy of crB and defective regulation of the enzymes of cholesterol biosynthesis.

Acetates↗
PubMed1990

Efficacies of erythromycin and chloramphenicol in extinguishing fecal shedding of Campylobacter jejuni in dogs.

Oral treatment regimens of erythromycin stearate and chloramphenicol were evaluated in naturally infected laboratory colony dogs for their efficacies in extinguishing fecal shedding of Campylobacter jejuni. Of the 25 Campylobacter-infected English Foxhounds in the study, 9 were assigned to erythromycin treatment, 9 to chloramphenicol treatment, and 7 to no treatment. Antimicrobials were administered for 12 days. All of the dogs that received erythromycin stearate ceased shedding C jejuni by the fourth day of treatment and remained negative throughout the treatment period. Chloramphenicol was associated with a reduction in shedding from 100% to 57% by the ninth day of treatment. Within 9 days of the discontinuation of antimicrobial treatment, C jejuni was isolated from all chloramphenicol-treated dogs and 89% erythromycin-treated dogs.

Animals↗
PubMed1988

Size and composition of liver vitamin A reserves of human beings who died of various causes.

Postmortem livers from 77 "normal" persons, 37 patients with neoplastic disease, 10 subjects with liver insufficiency, and 7 infants were analysed for free and esterified retinol. The average concentrations of total vitamin A for the members of each group were 597, 551, 289, and 162 micrograms/g wet liver, respectively. Compared with corresponding control values, both cancer victims and patients with liver disease had significantly lower hepatic vitamin A levels. With regard to the composition of the liver vitamin A reserves, our results show that approximately 97% of this vitamin was present as retinyl ester. Additionally, minute amounts of retinol were also found in most of the liver specimens analysed. In "normal" subjects the major ester fraction recovered was palmitate/oleate followed by stearate and myristate/linoleate. By contrast, the second most abundant fatty acid in the retinyl ester fraction of cancer victims was myristic/linoleic acid together with significantly smaller quantities of stearic acid. In tissue samples obtained from patients with liver disorders, however, the myristate/linoleate fraction was increased and therefore nearly equal amounts of both retinyl stearate and myristate/linoleate were present.

Cause of Death↗
PubMed1987

Cholesteryl esters of saturated fatty acids: cosolubility and fractionation of binary mixtures.

Factors affecting the solid state miscibility of saturated chain cholesteryl esters were determined from electron diffraction and differential scanning calorimetric measurements on a homologous series which included two types of crystal packing. Electron diffraction patterns from solution- and epitaxially crystallized microcrystals gave measured unit cell constants consistent with the bilayer crystal form for myristate, pentadecanoate, palmitate, and stearate esters. Cholesteryl undecanoate crystallized as the monolayer I structure and cholesteryl laurate was polymorphic, packing in either monolayer I or bilayer forms. No evidence was found for the monolayer II form of the laurate claimed in earlier work. It is clear that solid solution formation follows general rules formulated earlier by Kitaigorodskii for molecular crystals. A symmetry criterion must be satisfied first of all, i.e., two compounds that solidify in greatly different crystal structures will not form continuous solid solutions (e.g., cholesteryl undecanoate/cholesteryl myristate). Within a given crystal structure type, solid solution is permitted when the molecular volumes are similar. (For example, cholesteryl myristate forms an ideal solid solution with cholesteryl pentadecanoate, a nonideal solution with cholesteryl palmitate, and a eutectic of solid solutions with cholesteryl stearate.) For the polymorphic cholesteryl laurate, solid solutions of either the monolayer I structure (e.g., with cholesteryl undecanoate) or bilayer structure (e.g., with cholesteryl myristate) are permitted.

Calorimetry, Differential Scanning↗
PubMed1986

Simple diagnosis of the Zellweger syndrome by gas-liquid chromatography of dimethylacetals.

The absence of peroxisomes in patients with the cerebrohepatorenal syndrome of Zellweger leads to several biochemical abnormalities, including deficient synthesis of plasmalogens as well as accumulation of very long-chain fatty acids and intermediates in bile acid biosynthesis. Accumulation of very long-chain fatty acids in serum and fibroblasts has hitherto been used most extensively for diagnosis. Due to the relatively small amounts of the very long-chain fatty acids also in the Zellweger patients, and the risk for interfering impurities, such analyses are difficult. Direct assay of plasmalogens is also relatively difficult and time-consuming. In this report, we describe a relatively simple method for diagnosis, based on gas-liquid chromatography of a lipid extract of erythrocytes after methyl transesterification. The alpha, beta-unsaturated ether in the plasmalogen is converted to the dimethylacetal of the corresponding aldehyde, and the relative amount of plasmalogen is thus reflected by the ratio between 18:0 dimethylacetal and methyl stearate as well as by the ratio between 16:0 dimethylacetal and methyl palmitate. The ratio 18:0 dimethylacetal/methyl stearate was found to be 0.28 +/- 0.03 (mean +/- SD) after analyses of erythrocytes from healthy or non-Zellweger infants, but less than 0.02 in erythrocytes from three infants with the Zellweger syndrome. Preliminary work with amniotic fluid suggests that this analysis may be suitable also for prenatal diagnosis of the Zellweger syndrome.

Acetals↗