Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “PROPIONATES”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 1,567 records · Page 87Linked to original sources
PubMed2002

Controlled trial of inhaled fluticasone propionate in moderate to severe COPD.

Inhaled corticosteroids are often used in the treatment of stable chronic obstructive pulmonary disease (COPD), however, studies of these agents have had mixed results. Previous trials have often excluded subjects with bronchodilator response, have failed to evaluate effect on gas exchange, and have usually looked at only post- rather than prebronchodilator forced expiratory volume (FEV). Our objective was to better assess the efficacy of topical corticosteroids in the treatment of COPD. We used a prospective, randomized, double-blinded, placebo-controlled, crossover study at the Outpatient Department, Department of Veterans Affairs Medical Center. Thirty-six COPD patients with a mean (+/- SD) FEV1 of 1.10 +/- 0.43 L, with or without significant bronchodilator response participated in the study. Subjects received a 3-month course of inhaled fluticasone propionate (220 micro g/puff) or identical-appearing placebo by metered-dose inhaler at 2 puffs twice daily, followed by crossover to the alternative inhaler for an additional 3 months. Fluticasone treatment resulted in a higher prebronchodilator FEV1 (1.17 +/- 0.08 L [mean +/- SEM] versus 1.07 +/- 0.08 L, p = 0.001), a higher PaO2 (66.6 +/- 1.4 mmHg versus 63.6 +/- 1.6 mmHg, p = 0.002), and a better dyspnea score on the chronic respiratory questionnaire (3.70 +/- 0.18 versus 3.47 +/- 0.19, p = 0.03). A trend towards fewer exacerbations with fluticasone did not quite meet statistical significance (p = 0.11). Inhaled fluticasone over 3 months improved prebronchodilator airflow obstruction and oxygenation while decreasing dyspnea in moderate to severe COPD. Postbronchodilator FEV1 was not significantly changed.

Acute Disease↗
PubMed2006

New splicing mutations in propionic acidemia.

Propionic acidemia results from mutations in either of the two genes, PCCA or PCCB, that encode the two subunits of the propionyl-CoA carboxylase (PCC) enzyme. In this study, we report the identification and analysis of seven novel splicing mutations involving consensus donor and acceptor splice sites. Most of them were identified in patients with a Central Asian origin, and some present in several alleles, probably reflecting founder effects. The functional consequences of the splicing mutations were analyzed in patients' fibroblasts, as well as transcript quantification using real-time PCR methods. In the PCCA gene, two mutations were demonstrated to affect 5' splice sites (c.231+1G>C and c.1209+3A>G) and two 3' acceptor splice sites (c.1210delG and c.1430G>T), all causing skipping of the exons involved, with no detectable levels of normally spliced transcript. In the PCCB gene, all three mutations involved 5' donor splice sites-two affected exon 1 splicing (c.154_183+17del46 and c.183+2T>C), the latter activating a cryptic splice site in intron 1, and the remaining mutation (c.1498+2T>C) resulted in exon 14 skipping. The results highlight the necessity to perform transcript analysis in addition to genomic DNA sequencing to characterize the effect of splicing mutations and add relevant information on the genetic epidemiology of the disease.

Alternative Splicing↗
PubMed2006

The effect of aerosolized and intravenously administered clenbuterol and aerosolized fluticasone propionate on horses challenged with Aspergillus fumigatus antigen.

Beta-agonists have been shown to display anti-inflammatory properties in several experimental models. The aim of this study was to investigate the anti-inflammatory properties of clenbuterol (CB), administered either intravenously or by aerosol, in comparison with fluticasone propionate (FP) in recurrent airway obstruction (RAO)-susceptible horses. Eight horses, of which five were known to be susceptible to RAO, underwent an inhalation challenge with Aspergillus fumigatus (AF) antigen and were treated with CB intravenously, CB by aerosol, or FP by aerosol. Twenty-four hours after the challenge, bronchoalveolar lavage was performed, the total and differential cell counts were assessed, and cytokines were measured in isolated alveolar macrophages. After challenge with AF, RAO-susceptible horses showed an increase in total cell count, based on an increase in macrophages and lymphocytes, which was inhibited by treatment with intravenous CB, aerosolized CB and aerosolized FP. Neutrophil ratios were decreased when treated with aerosolized CB and FP. Expression of interleukin (IL)-1beta and IL -8 was significantly increased after AF challenge . Interleukin -1beta was significantly decreased following treatment with intravenous CB, aerosolized CB and aerosolized FP, whereas only FP decreased the expression of IL-8. These data suggest that the anti-inflammatory property of CB provide new opportunities in the therapeutic intervention of early inflammation in RAO.

Administration, Inhalation↗
PubMedDate not supplied

Development of indole-3-propionic acid (OXIGON) for Alzheimer's disease.

The accumulation of amyloid-beta and concomitant oxidative stress are major pathogenic events in Alzheimer's disease. Indole-3-propionic acid (IPA, OXIGON) is a potent anti-oxidant devoid of pro-oxidant activity. IPA has been demonstrated to be an inhibitor of beta-amyloid fibril formation and to be a potent neuroprotectant against a variety of oxidotoxins. This review will summarize the known properties of IPA and outline the rationale behind its selection as a potential disease-modifying therapy for Alzheimer's disease.

Alzheimer Disease↗
PubMed1984

3-(p-hydroxyphenyl)propionic acid as a new fluorogenic reagent for amine oxidase assays.

A detailed procedure of a new and extremely sensitive fluorometric assay for amine oxidases is presented. Hydrogen peroxide, produced by the oxidase reaction, reacted with 3-(p-hydroxyphenyl)propionic acid in the presence of peroxidase to yield a fluorescent compound by which enzyme activity could be determined. The enzyme reaction was terminated by NaOH solution, which increased the fluorescence intensity three- to fivefold. The detection limit thus obtained was as little as 0.02 nmol. The alkalinization also contributed to stopping the enzyme reaction and to the clarification of assay mixtures containing turbid enzyme preparations.

Amine Oxidase (Copper-Containing)↗
PubMed1984

Cross-linking of wheat germ RNA polymerase II with dithiobis(succinimidyl propionate).

The subunit arrangement of wheat germ RNA polymerase II was examined using the cleavable cross-linking reagent dithiobis(succinimidyl propionate). Conditions were chosen such that the enzyme was active prior to treatment, and that most of the subunits were reactive towards the reagent. Our results indicate that the enzyme is made up from a central core involving the two large subunits, around which the small subunits are independently arranged. Possible relations between the overall structure and the role of individual subunits in transcription are discussed.

Chemical Phenomena↗
PubMed1983

Studies on the mechanism of action of the hypoglycemic agent, 2-(3-methylcinnamylhydrazono)-propionate (BM 42.304).

A new hypoglycemic agent, 2-(3-methylcinnamylhydrazono)-propionate MCHP (BM 42.304) was shown to be an inhibitor of the transfer of long-chain fatty acids across the mitochondrial inner membrane. The following data support this conclusion: the drug, at already 5 microM, inhibited ketogenesis from oleate but not from octanoate in the perfused guinea-pig liver; likewise, ketogenesis from L-(-)-palmitoylcarnitine and palmitoyl-CoA + L-(-)-carnitine, but not from octanoate, was depressed in isolated guinea-pig liver mitochondria. Oxigraphic measurements of the oxygen uptake by isolated mitochondria showed that the drug impaired oxygen uptake with the long-chain fatty acid derivatives but not with octanoate. Finally, in vivo effects of the drug such as hypoketonemia and an increased concentration of free fatty acids in blood are in agreement with the above formulated mechanism of action. A comment is given on the relationships between fatty acid oxidation and gluconeogenesis in the guinea-pig liver.

Animals↗
PubMed1984

In vivo and in vitro effects of a new hypoglycemic agent, 2-(3-methylcinnamylhydrazono)-propionate (BM 42.304) on glucose metabolism in guinea pigs.

A new compound, 2-(3- methylcinnamylhydrazono )-propionate (BM 42.304), showed a dose dependent hypoglycemic effect in starved guinea pigs after both oral and intraperitoneal administration. In contrast to biguanides (phenformin and metformin) the new compound produced only a moderate increase in blood lactate concentration and did not alter the content of adenine nucleotides in the freeze-clamped liver in vivo. Gluconeogenesis from a variety of precursors in the perfused guinea-pig liver was also inhibited by BM 42.304. These properties suggest that the compound deserves further investigation in connection with its potential usefulness for the treatment of diabetes.

Animals↗
PubMed1984

Inhibition of prostaglandin synthesis by sodium 2-[4-(2-oxocyclopentylmethyl)phenyl] propionate dihydrate (CS-600), a new anti-inflammatory drug, and its active metabolite in vitro and in vivo.

A new anti-inflammatory agent, sodium 2-[4-(2-oxocyclopentylmethyl)phenyl]propionate dihydrate (CS-600), was investigated for its inhibition of prostaglandin (PG) synthesis in vivo and in vitro. CS-600 caused a marked decrease in the level of urinary PGE2 and PGF2 alpha in rats. The dose of CS-600 which resulted in a 50% decrease of urinary PGE2 excretion was 1.9 mg/kg, p.o., and this value agreed well with the ID50 of the drug for carrageenin edema (1.2 mg/kg, p.o.). This suggests that CS-600 inhibits prostaglandin synthesis in vivo. However, CS-600 had only weak inhibitory activity against in vitro prostaglandin synthesis by bovine seminal vesicle microsomes (IC50:760 microM). A main plasma metabolite of CS-600, which was produced by stereospecific reduction of the cyclopentanone moiety to transhydroxy cyclopentane, exhibited potent inhibitory activity toward the prostaglandin synthetase of bovine seminal vesicle microsomes (IC50:11 microM). In cell cultures of 3T6 fibroblasts from mice, CS-600 inhibited production of PGE2 and PGF2 alpha by the cells at low concentrations (IC50 for PGE2:1.6 microM). The active metabolite exhibited more potent inhibition (IC50:0.29 microM), and conversion of CS-600 into the active metabolite occurred in the cell system. Inhibition of prostaglandin synthetase in the membrane fraction of the fibroblast cells was also investigated. Available evidence indicates that CS-600 is a pro-drug and exerts its pharmacological activities after conversion to the active metabolite.

Animals↗
PubMed1988

3-(2,2,2-Trimethylhydrazinium)propionate (THP)--a novel gamma-butyrobetaine hydroxylase inhibitor with cardioprotective properties.

A protein fraction containing gamma-butyrobetaine hydroxylase (sp.act. 1.54 mU/mg) was isolated from the rat liver by differential precipitation with ammonium sulphate. 3-(2,2,2-Trimethylhydrazinium)propionate (THP), a noncompetitive enzyme inhibitor, when administered orally to rats for 10 days (150 mg/kg) elicited a reduction in myocardial free carnitine and long-chain acyl carnitine content by 63.7 and 74.3%, respectively. This reduction in free carnitine concentration causes a suppression of the free fatty acid oxidation, as measured by the production of 14CO2 and ketone bodies. The inhibition of fatty acid oxidation is particularly manifest when their metabolism is stimulated by feeding a fat-rich diet to the animals or in fasting rats. The inhibition of fatty acid metabolism at the stage of activation (acyl carnitine formation) can account for the cardioprotective effect of THP, which is assessed by its ability to prevent a decrease in ATP level and myocardial energy charge as well as to prevent a rise in creatine phosphokinase and lactic dehydrogenase (myocardium-specific isozyme) activity in rat blood serum in response to isoproterenol and epinephrine. Regulation of the carnitine-dependent fatty acid metabolism in ischaemia is a pathogenetically justified approach to pharmacological treatment of ischaemic myocardium. In its biochemical mechanism, THP significally distinguishes itself from other known inhibitors of fatty acid oxidation.

Animals↗
PubMed1982

Masculinization of the female rat spinal cord following a single neonatal injection of testosterone propionate but not estradiol benzoate.

We previously reported that a motor nucleus of the rat spinal cord, the spinal nucleus of the bulbocavernosus (SNB), has more and larger neurons in males than females. The SNB is significantly masculinized in adult female rats receiving 1 mg of testosterone propionate (TP) on the second day of life, compared to that of their oil treated sisters. This masculinization consists of more neurons in the region of the SNB. These results are consistent with the hypothesis that the action of androgens during the early perinatal period is responsible for the sexually dimorphic development of the SNB. Neonatal TP caused no detected masculinization, i.e. enlargement of the size of individual neurons in this region in females. Male rats given TP on day 2 had significantly smaller testes and smaller SNB somas in adulthood than oil treated males. In female rats given 100 micrograms of estradiol benzoate (EB) on day 2, the SNB was not masculinized in either number of size when observed in adulthood. The lack of a masculinizing effect of EB suggests that the aromatization of testosterone to estradiol is not sufficient for this dimorphic development.

Animals↗
PubMed1984

Pre- and postnatal influence of testosterone propionate and diethylstilbestrol on differentiation of the sexually dimorphic nucleus of the preoptic area in male and female rats.

The volume of the sexually dimorphic nucleus in the preoptic area (SDN-POA) of the rat brain is several fold larger in males than in females. When female rats were treated pre- and postnatally with testosterone propionate (TP) or with diethylstilbestrol (DES) they became anovulatory and their SDN-POA developed equivalent in size to that of normal males. Identical treatment of male rats resulted in deficient testicular development, but had no influence on SDN-POA volume. The results indicate that the gross morphological sex difference in SDN-POA volume can exclusively be controlled by the hormonal environment during the critical period of sexual brain differentiation, and that non-steroidal estrogens are just as effective as convertible androgens in stimulating SDN-POA differentiation.

Animals↗
PubMed1990

Chronic testosterone propionate treatment decreases the concentration of [3H]quipazine binding at 5-HT3 receptors in the amygdala of the castrated male rat.

Chronic administration of testosterone propionate (TP) was found to decrease the concentration of [3H]quipazine binding at 5-HT3 receptors in the lateral and basal amygdaloid nuclei of the brains of castrated male rats. TP had no effect on the binding of [3H]quipazine at 5-HT3 receptors in the posterolateral or posteromedial cortical amygdaloid nuclei, or in the amygdalohippocampal areas. It is suggested that the effects of testosterone on sexual and other social behaviors in male rats may be mediated, at least in part, by decreases in the activation of 5-HT3 receptors in the amygdala.

Amygdala↗
PubMed1993

Lateral hypothalamic injections of glutamate, kainic acid, D,L-alpha-amino-3-hydroxy-5-methyl-isoxazole propionic acid or N-methyl-D-aspartic acid rapidly elicit intense transient eating in rats.

A convergence of evidence suggests that stimulation of lateral hypothalamic (LH) neurons can elicit eating, but the neurotransmitters that mediate this effect are unknown. To determine whether glutamate might be involved, it was injected through chronic guide cannulas directly into the LH of satiated adult male rats and consequent food intake was measured. Glutamate produced a dose-dependent eating response (mean intakes of 3.7 g at 300 nmol and 5.2 g at 900 nmol) only within the first hour after injection. As a first step in determining the receptor types mediating this response, agonists for specific excitatory amino acid (EAA) receptors were similarly tested. Kainic acid (KA), D,L-alpha-amino-3-hydroxy-5-methyl-isoxazole propionic acid (AMPA) or N-methyl-D-aspartic acid (NMDA) injected into the LH each elicited eating in a dose-dependent fashion beginning at 0.33 to 1.0 nmol. At maximally effective doses (1.0-33 nmol), each agonist elicited food intakes of approximately nine grams within 1 h. Finally, analysis of meal and behavioral patterns produced by LH injection of glutamate (600 nmol) and KA (1.0 nmol) revealed that the elicited eating usually began 2-3 min postinjection and consisted of a single normal to large size meal. There were no other behavioral effects during this initial postinjection period and no effects on other oral behaviors, like drinking or gnawing, at any time. Collectively, these findings suggest that glutamate may act through several subtypes of its receptors on some LH neurons to elicit eating.

Animals↗
PubMed1994

Expression and characterization of the alpha 2 subunit of the alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA)-selective glutamate receptor channel in a baculovirus system.

Using a baculovirus expression vector system, the alpha 2 subunit of the mouse alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA)-selective glutamate receptor (GluR) channel was expressed in Spodoptera frugiperda insect cells. Immunoblotting using the antibody made to the synthetic peptide corresponding to the C-terminus of GluR alpha 2 and [35S]methionine/[35S]cysteine metabolic radiolabeling revealed the major 102-kDa and the minor 98-kDa protein bands. Metabolic radiolabeling with tunicamycin suggested that the two bands correspond to glycosylated and unglycosylated forms, respectively. The recombinant GluR alpha 2 proteins expressed in insect cells were also identified by immunofluorescence staining. The results of [3H]AMPA binding assay using whole cells suggested that, in infected Sf21 cells, binding sites of the GluR alpha 2 proteins were possibly located on the extracellular side. Scatchard analysis of AMPA binding showed the following parameters: Kd = 16 nM, Bmax = 1.9 x 10(5) binding sites per cell or 1 pmol/mg protein in the total particulate fraction. The ligand binding characteristics of the receptors expressed in insect cells were examined. From the effect of various agonists on [3H]AMPA binding of the receptors expressed in insect cells, the rank order potency of agonists was quisqualate > AMPA > L-glutamate > kainate. Thus, the baculovirus-insect cell expression system provides high-efficiency expression of the receptor sufficient to permit structural and functional analyses.

Animals↗
PubMed1992

Identification of urinary metabolites of (+/-)-2-(p-isobutylphenyl)propionic acid (Ibuprofen) by routine organic acid screening.

Ibuprofen [(+/-)-2-(p-isobutylphenyl)propionic acid] has recently been introduced as a pediatric anti-inflammatory agent. To determine how this agent interferes with urine organic acid analysis, an important pediatric investigation, we have analyzed urine from two subjects pre- and post-Ibuprofen dosage and two subjects on chronic Ibuprofen therapy. A distinctive pattern of drug interference on the organic acid profile was detected. There were three major components, corresponding to unmetabolized Ibuprofen and to the oxidation products hydroxy Ibuprofen and carboxy Ibuprofen. Therefore, the major mechanism of Ibuprofen metabolism appears to be microsomal, although mitochondrial and peroxisomal routes cannot be excluded. Laboratories carrying out routine organic acid analysis should be aware of the nature and magnitude of the organic aciduria caused by Ibuprofen.

Adult↗
PubMed1992

Modulation of N-methyl-D-aspartate and (R,S)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) responses of spinal nociceptive neurons by a N-terminal fragment of substance P.

The effects of an N-terminal fragment of substance P, substance P-(1-7) [SP-(1-7)], on the responses of dorsal horn nociceptive neurons to N-methyl-D-aspartate (NMDA) and (R,S)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) were tested by combined single-unit extracellular recordings/microiontophoresis. While SP-(1-7) had no effects when applied by itself, it was a potent and long-lasting modulator of both NMDA- and AMPA-mediated excitation of spinal dorsal horn nociceptive neurons. NMDA responses were transiently decreased (by an average of 36% of control at minimum) by SP-(1-7) followed by a more sustained increase (by 76% at maximum). In contrast, AMP responses were only increased by SP-(1-7) (by 81% at maximum). It is hypothesized that the actions of SP-(1-7) on excitatory amino acid (EAA) responses of dorsal horn nociceptive neurons reflect a novel mechanism by which SP and EAAs interact to modulate pain transmission.

Animals↗
PubMed1986

Uterine position and the activation of male sexual activity in testosterone propionate-treated female guinea pigs.

Fetal female guinea pigs were delivered surgically and their position within a uterine horn relative to male fetuses was noted. When adult they were ovariectomized, injected daily with testosterone propionate, and examined for male copulatory behaviors in response to the presence of a receptive female. Females that developed contiguous to a caudal male were functionally similar to those that had been situated between two males; both exhibited enhanced levels of mounting relative to females that were located contiguous to no males (with and without the presence of a caudal male) and to females contiguous to a cephalic male. Therefore, both contiguity and positioning of the male fetus are necessary conditions for prenatal masculinization of the female guinea pig. Lastly, four animals that had resided singly in the uterus displayed the lowest levels of copulatory behaviors.

Animals↗