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At least 1,279 records · Page 71Linked to original sources
PubMed1998

Mice lacking secretory phospholipase A2 show altered apoptosis and differentiation with Helicobacter felis infection.

BACKGROUND & AIMS: Infection with Helicobacter pylori uniformly leads to a chronic superficial gastritis that may progress to atrophic gastritis, a premalignant process. A mouse model of Helicobacter felis infection was used to study possible genetic determinants of the response to infection. METHODS: Three inbred mouse strains with known secretory phospholipase A2 (sPLA2) genotypes [BALB/c (+/+), C3H/HeJ (+/+), and C57BL/6 (-/-)] were orally infected with H. felis and examined longitudinally using routine histology, immunocytochemistry, electron microscopy, proliferating cell nuclear antigen, terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick-end labeling, and Northern and Western blot studies. RESULTS: Only the C57BL/6 strain showed increased gastric fundic proliferation and apoptosis in response to infection. In addition, the C57BL/6 mouse showed a marked loss of parietal and chief cells, along with a marked expansion of an aberrant gastric mucous cell lineage that stained positive for spasmolytic polypeptide. In contrast, no significant change in these cell types was observed in BALB/c and C3H/HeJ strains. Increased expression of sPLA2 was observed in BALB/c and C3H/HeJ after H. felis infection, whereas sPLA2 expression was absent in C57BL/6 mice. CONCLUSIONS: H. felis infection leads to increased apoptosis and altered cellular differentiation in the C57BL/6 mouse, a strain that lacks gastric sPLA2 expression. Because sPLA2 has been identified recently as the MOM1 (modifier of MIN) locus that influences polyp formation in the colon, these studies suggest that sPLA2 may also influence the gastric epithelial response to Helicobacter infection.

Animals↗
PubMed1976

Gas-chromatographic determination of camylofine dihydrochloride in tablets and suppositories.

A gas-chromatographic method for the quantitative determination of camylofine dihydrochloride, a spasmolytic agent, is described. The analysis is made on a porous polymer packing material, by determining the 3-methyl-1-butanol formed on alkaline hydrolysis of the drug. The method has been applied to the quantitative determination of the drug in two galenical forms, namely tablets and suppositories, in the presence of papaverine hydrochloride, codeine phosphate, novalgin and aminopyrine.

Butanols↗
PubMed1986

Atrial natriuretic factor: assessment of its structure in atria and regulation of its biosynthesis with volume depletion.

Atrial natriuretic factor (ANF) is a polypeptide that has been isolated from mammalian atrial tissue with potent natriuretic, diuretic and spasmolytic properties. Details of its biosynthesis, cleavage, storage and release are not yet fully defined. Using sequence-specific anti-peptide antisera in immunocytochemical and radioimmunoassay studies, we demonstrated the presence in atrial granules of sequences corresponding to both the large molecular weight ("prohormone") form of ANF and the carboxyterminal peptide believed to be responsible for its biological activity. However, a peptide sequence spanning the proposed site of cleavage of the "signal peptide" from preproANF was undetected. In volume-depleted rats, a 28% decrease in the relative concentrations of atrial ANF mRNA was observed as compared to that of controls (P less than 0.01). There was, however, no significant difference observed between the two groups of animals with respect to atrial levels of ANF, as measured by radioimmunoassay. We conclude from these studies that proANF, but not preproANF, is stored in atrial granules. The concentration of stored ANF remains constant in volume-depleted rats despite a 28% reduction in ambient levels of ANF mRNA. The physiologic significance of these findings is discussed.

Animals↗
PubMed1991

The effect of oxyphenonium bromide and oxybutynin hydrochloride on detrusor contractility and reflux in children with vesicoureteral reflux and detrusor instability.

In a prospective study the effects of the anticholinergic drugs oxyphenonium bromide and oxybutynin hydrochloride on detrusor contractility and reflux were studied. Although anticholinergic properties are claimed of both drugs, only oxybutynin hydrochloride proved to decrease detrusor contractility and the degree of reflux, probably due to a direct spasmolytic effect on the detrusor. Therefore, in cases of reflux and detrusor instability treatment with oxybutynin hydrochloride is recommended.

Child↗
PubMed1986

Treatment of pain owing to acute ureteral obstruction with prostaglandin-synthetase inhibitor: a prospective randomized study.

Pain owing to acute ureteral obstruction seems to be related closely to tension in the walls of the renal pelvis. Renal prostaglandins are involved intimately in the events leading to the pain. A prostaglandin-synthetase inhibitor, diclofenac sodium, was used in the treatment of acute ureteral pain, and was compared to the traditional treatment of a combination of spasmolytic and narcotic drugs. Also, the need for overhydration as part of the management was tested. The 91 patients entered into the prospective randomized trial were divided into groups. Diclofenac sodium had a 90 per cent success rate in relieving pain at 30 minutes, and the combination of pethidine and hyoscine butyl bromide had a statistically higher success rate at 97.5 per cent (p equals 0.05). However, the latter therapy had a higher rate of side effects (p equals 0.01). There was no difference in the response between the groups in relation to whether they received intravenous fluids.

Adolescent↗
PubMed1983

Action of papaverine and verapamil on norepinephrine and calcium evoked contraction of vascular and non vascular smooth muscle.

On isolated rat vas deferens both papaverine and verapamil show a non competitive antagonism against norepinephrine and a competitive antagonism against Ca2+. Verapamil is nearly 100 times more active than papaverine. On the main pulmonary artery and on the thoracic aorta of the rabbit, verapamil shows a competitive antagonism against both norepinephrine and Ca2+ but it is more effective (almost 100 times) against Ca2+ than norepinephrine. Papaverine also shows a competitive antagonism against norepinephrine but a non competitive antagonism against Ca2+. The contrasting results obtained on rat vas deferens and rabbit vessels might be due to: 1) mechanism(s) of action of the agonist; 2) properties of the biological object as far concerns receptor activation and mechanism(s) of excitation-contraction coupling; 3) mechanism(s) of action of spasmolytic drugs. All these factors act in a cooperative way in determining the quality and the quantity of the observed responses.

Animals↗
PubMed2002

Triterpenoids from the leaves of Psidium guajava.

Two triterpenoids, 20beta-acetoxy-2alpha,3beta-dihydroxyurs-12-en-28-oic acid (guavanoic acid, 3), and 2alpha,3beta-dihydroxy-24-p-z-coumaroyloxyurs-12-en-28-oic acid (guavacoumaric acid, 7), along with six known compounds 2alpha-hydroxyursolic acid (1), jacoumaric acid (2), isoneriucoumaric acid (4), asiatic acid (5), ilelatifol D (6) and beta-sitosterol-3-O-beta-D-glucopyranoside (8), have been isolated from the leaves of Psidium guajava. Their structures were determined through spectroscopic methods. Compound 5 showed dose-dependent (10-500 microg/ml) spasmolytic activity in spontaneously contracting isolated rabbit jejunum preparations.

Magnetic Resonance Spectroscopy↗
PubMed2002

Modulation of mood and cognitive performance following acute administration of Melissa officinalis (lemon balm).

Melissa officinalis (lemon balm) is a traditional herbal medicine, which enjoys contemporary usage as a mild sedative, spasmolytic and antibacterial agent. It has been suggested, in light of in vitro cholinergic binding properties, that Melissa extracts may effectively ameliorate the cognitive deficits associated with Alzheimer's disease. To date, no study has investigated the effects on cognition and mood of administration of Melissa to healthy humans. The present randomised, placebo-controlled, double-blind, balanced-crossover study investigated the acute effects on cognition and mood of a standardised extract of M. officinalis. Twenty healthy, young participants received single doses of 300, 600 and 900 mg of M. officinalis (Pharmaton) or a matching placebo at 7-day intervals. Cognitive performance was assessed using the Cognitive Drug Research (CDR) computerised test battery and two serial subtraction tasks immediately prior to dosing and at 1, 2.5, 4 and 6 h thereafter. In vitro IC(50) concentrations for the displacement of [3H]-(N)-nicotine and [3H]-(N)-scopolamine from nicotinic and muscarinic receptors in human occipital cortex tissue were also calculated. Results, utilising the cognitive factors previously derived from the CDR battery, included a sustained improvement in Accuracy of Attention following 600 mg of Melissa and time- and dose-specific reductions in both Secondary Memory and Working Memory factors. Self-rated "calmness," as assessed by Bond-Lader mood scales, was elevated at the earliest time points by the lowest dose, whilst "alertness" was significantly reduced at all time points following the highest dose. Both nicotinic and muscarinic binding were found to be low in comparison to the levels found in previous studies.

Adult↗
PubMed1999

An extended-release formulation of oxybutynin chloride for the treatment of overactive urinary bladder.

Detrusor instability, or urinary incontinence, is common in elderly patients, particularly elderly women. The clinical symptoms of overactive, or unstable, urinary bladder include urge urinary incontinence, urgency, and frequency. Mixed urinary incontinence, which comprises urge urinary incontinence and stress incontinence, is manifested by increased intraabdominal pressure on coughing or sneezing. The detrusor muscle of the bladder is under the control of the parasympathetic, or muscarinic, nervous system. The drug of choice in this condition is oxybutynin chloride, which has the ability to block acetylcholine released from parasympathetic nerves in the urinary bladder, preventing contractions of the muscle and exerting a direct spasmolytic effect on the bladder. A new extended-release oral tablet formulation, OROS oxybutynin, uses osmotic pressure to deliver the drug at a controlled rate over approximately 24 hours. It resembles a conventional tablet but has a two-part core consisting of a drug layer and below it, a "push" layer containing osmotically active components, the whole surrounded by a semipermeable membrane with a laser-drilled opening in the drug side. Water in the gastrointestinal tract enters the tablet and mixes with the drug to form a suspension. The "push" layer expands and pushes the suspended drug out of the orifice and into the gastrointestinal tract for eventual absorption. Pharmacokinetic studies have indicated a slow rise in mean plasma concentration of the isomer R-oxybutynin for 4 to 6 hours after a single dose of OROS oxybutynin, followed by maintenance of steady concentrations for up to 24 hours, minimizing the fluctuations between peak and trough associated with TID dosing of 5-mg immediate-release oxybutynin tablets. Efficacy and safety studies comparing the extended-release with the immediate-release formulation of oxybutynin demonstrated equivalent efficacy in patients with overactive urinary bladder. The adverse-event profile of oxybutynin is similar to that of a typical anticholinergic agent such as atropine--dry mouth, constipation, somnolence, blurred vision, headache, and gastrointestinal pain--although in 2 clinical studies, the incidence of dry mouth was less with the extended-release formulation. Once-daily dosing with OROS oxybutynin appears to be well tolerated and effective, as well as convenient, for the treatment of overactive bladder, particularly for elderly patients using multiple medications.

Cholinergic Antagonists↗
PubMed2000

[Efficient, immediate or emergency ESWL: an attractive strategic alternative to be considered in the treatment of renal colic!].

INTRODUCTION: Renal colic due to acute ureteral obstruction caused by lithiasic impact results in severe rise of intracavitary pressure. Traditional drug therapy (painkillers, anti-inflammatories, spasmolytics) is symptomatic and provisional, and pain can reappear when obstruction is maintained. A pathoetiological approach would be the ultimate therapy vs the symptomatic one. MATERIAL AND METHODS: From the beginning, the approach used at the Lithiasis-Lithotrity Unit at the FJD, once the ureteral stone is accurately identified during a renal colic, is that of immediate or emergency "in situ" SWEL together with the usual drug therapy. 15% of 2100 cases of ureteral lithiasis treated (1991-1999) were renal colic. RESULTS: Renal colic can be resolved in all cases (100%) even when fragmentation may be partial and/or require a second deferred SWEL on remnants of the first lithiasis. When obstruction has been resolved, pain does not reappear as it happens with the effects of analgesics. DISCUSSION: Placement of a ureteral catheter or nephrostomy for analgesia in order to perform deferred SWEL of the ureteral stone origin of the acute ureteral obstruction and the renal colic, do not improve SWEL results. There are physical reasons to support the practice of immediate or emergency "in situ" SWEL during a renal colic. Fragmentation of the obstructive stone together with the resulting ureteral oedema allow urine passage. Intracavitary pressure and pain disappear when the obstruction is withdrawn. CONCLUSIONS: Immediate, "in situ" or emergency SWEL in cases of obstructive ureteral stones during a renal colic, is an attractive strategic alternative for drug therapy that should be considered mainly in institutions with means to perform the procedure.

Colic↗
PubMed2001

New lanthanide complexes of 4-methyl-7-hydroxycoumarin and their pharmacological activity.

Complexes of cerium(III), lanthanum(III) and neodymium(III) with 4-methyl-7-hydroxycoumarin (Mendiaxon, Hymecromone) were synthesized by the mixing of equimolar amounts of the respective metal nitrates and 4-methyl-7-hydroxycoumarin sodium salt in water. The complexes were characterized and identified by elemental analysis, conductivities, IR, (1)H and (13)C NMR spectroscopies and mass spectral data. DTA and TGA have been applied to study the compositions of the compounds. The newly synthesized compounds were assayed for acute intraperitoneal and per oral toxicity, influence on blood clotting time and the most active complex was investigated for spasmolytic activity. The complexes of cerium(III) and neodymium(III) showed marginal cytotoxic activity against transformed leukemic cell lines (P3HR1 and THP-1) as compared to the inorganic salts.

Administration, Oral↗
PubMed2002

MT(1) melatonin receptor overexpression enhances the growth suppressive effect of melatonin in human breast cancer cells.

Melatonin inhibits the proliferation of estrogen receptor alpha (ERalpha)-positive (MCF-7), but not ERalpha-negative (MDA-MB-231) breast cancer cells. Here, we assessed the effect of MT(1) melatonin receptor stable overexpression in MCF-7 and MDA-MB-231 breast cancer cells on the growth-suppressive effects of melatonin. Parental and vector-transfected MCF-7 cells demonstrated a modest, but significant, growth-suppressive response to melatonin; however, melatonin treatment of MT(1)-transfected MCF-7 cells resulted in significantly enhanced growth-suppression. This response was blocked by an MT1/MT2 melatonin receptor antagonist. Interestingly, MT(1)-overexpression did not induce a melatonin-sensitive phenotype in melatonin-insensitive MDA-MB-231 cells. Finally, Northern blot analysis demonstrated an enhanced inhibition of ERalpha mRNA expression and an enhanced induction of pancreatic spasmolytic polypeptide (pS2) by melatonin in MT(1)-transfected MCF-7 cells relative to vector-transfected MCF-7 cells. These data suggest the involvement of the MT(1) melatonin receptor in mediation of melatonin effects on growth-suppression and gene-modulation in breast cancer cells.

Adenocarcinoma↗
PubMed1999

The effect of tizanidine on maximal electroshock seizures (MES) in mice.

Tizanidine, an alpha-2 adrenergic agonist, is a centrally active muscle relaxant and a spasmolytic drug. The aim of our study was to investigate the activity of tizanidine on maximal electroshock seizures (MES) in mice. In the first part of the study, convulsive current 50 (CC 50) value to produce seizures was found. Then, tizanidine was given intraperitoneally (IP) at the doses of 0.5, 1, and 2 mg/kg, and orally (PO) at the doses of 5, 10, 20, 40 mg/kg. We found that tizanidine at the doses of 1 and 2 mg/kg IP and 40 mg/kg PO caused a significant protection against MES. In the second part of the study, after pretreatment with yohimbine, an alpha-2 adrenergic receptor blocker, at the dose of 2 mg/kg, anticonvulsant effect of tizanidine is diminished. We concluded that the mode of action of the anticonvulsant effect of tizanidine may be mediated by the central alpha-2 adrenergic receptors.

Administration, Oral↗
PubMed2001

Isolation of a bronchodilator flavonoid from the Thai medicinal plant Clerodendrum petasites.

The ethanolic extract of Clerodendrum petasites was tested to evaluate the spasmolytic activity on isolated guinea-pig tracheal smooth muscle. The crude extract (2.25-9.0 mg/ml) dose-dependently caused relaxation of tracheal smooth muscle which was contracted by exposure to histamine. A bioassay-guided fractionation of the crude extract was performed by means of partitioning and centrifugal partition chromatography. Finally the active principle was isolated and identified as the flavonoid hispidulin (EC(50): (3.0+/-0.8)x10(-5) M). These results suggest that hispidulin may be beneficial in the treatment of asthma.

Animals↗
PubMed2003

Antispasmodic effect of three fractions of hydroalcoholic extract of Pycnocycla spinosa.

Hydroalcoholic extract of Pycnocycla spinosa was shown to have spasmolytic action in vitro and antidiarroheal effect in vivo. The hydroalcoholic extract of P. spinosa is composed of alkaloid-, flavonoid- and saponin-rich components. These components were separated by fractional separation technique. The pharmacological objective of this study was to look for relaxant effect of these components of hydroalcoholic extract of P. spinosa on rat isolated ileum contractions. The alkaloid-, flavonoid- and saponin-rich fractions of P. spinosa inhibited the response to 80 mM KCl in a concentration-dependent manner. The alkaloid-rich fraction was the most and saponin-rich fraction the least effective relaxant of ileum contractions. The alkaloid-rich fraction also inhibited the response to acetylcholine (ACh) and 5-hydroxytryptamine (5-HT). From this study, it can be concluded that the antispasmodic action of hydroalcoholic extract of P. spinosa could be due to components in the alkaloid-rich fraction and to a lesser extent, to its flavonoid-rich fraction.

Alkaloids↗
PubMed1997

Biological and chemical study of paico (Chenopodium chilense, Chenopodiaceae).

The methanolic extract of the aerial portion of Chenopodium chilense Schrad., used in Chilean traditional medicine as a remedy for stomach-ache, has been found to exert the major spasmolytic activity in acetylcholine contracted rat ileum. This extract, with a complex flavonoid patterns on thin layer chromatography (TLC) analysis, is practically non-toxic both for rats and brine shrimp Artemia salina in acute toxicity test.

Acetylcholine↗
PubMed1999

Calcium antagonistic activity of Bacopa monniera on vascular and intestinal smooth muscles of rabbit and guinea-pig.

The present study demonstrates the calcium antagonistic activity in ethanol extract of Bacopa monniera. The plant extract inhibited the spontaneous movements of both guinea-pig ileum (IC50 = 24+/-4 microg/ml) and rabbit jejunum (IC50 = 136+/-9 microg/ml). A marked reduction in acetylcholine- and histamine-induced responses (0.0001-10 microM) in the ileum was evident in the presence of extract (260 microg/ml). The acetylcholine (1 microM)-induced contraction in the ileum was also inhibited by the extract (100-700 microg/ml) in a concentration dependent way (IC50 = 285+/-56 microg/ml). All these results indicate a direct action of the extract on smooth muscles. Calcium chloride-induced responses in the rabbit blood vessels and jejunum were attenuated in the presence of plant extract (10-700 microg/ml) implying a direct interference of plant extract with influx of calcium ions in the cells. However, the lack of modification of either noradrenaline- or caffeine-induced contractions in the presence of extract suggests that extract has no detectable effect on mobilization of intracellular calcium. These results indicate that spasmolytic effect of the B. monniera extract in smooth muscles is predominantly due to inhibition of calcium influx via both voltage and receptor operated calcium channels of the cell membrane.

Animals↗
PubMed2002

Identification of mebeverine acid as the main circulating metabolite of mebeverine in man.

The intestinal spasmolytic drug mebeverine is known to undergo fast in vivo enzymatic hydrolysis into mebeverine alcohol and veratric acid. A reversed-phase HPLC method with coulometric detection was developed in order to assay the hitherto unidentified secondary metabolite mebeverine acid. After intake of a single oral dose of 405 mg mebeverine hydrochloride in four healthy human volunteers, peak plasma concentrations of mebeverine acid were found to be 1000-fold higher than those of mebeverine alcohol, i.e. approximately 3 microg/ml versus 3 ng/ml. The appearance of mebeverine acid in plasma (median T(max)=1.25 h) as well as its disappearance (median apparent t(1/2)=1.1 h) were rapid. The urinary excretion of mebeverine acid within the first 4 h after dosing amounted to 67% of the mebeverine dose (median range: 23-107%). Mebeverine acid appears to be a valuable marker of oral exposure to mebeverine.

Administration, Oral↗