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At least 127 records · Page 7Linked to original sources
PubMed1989

Revised amino acid sequence of pancreatic spasmolytic polypeptide exhibits greater similarity with an inducible pS2 peptide found in a human breast cancer cell line.

The published amino acid sequence of pancreatic spasmolytic polypeptide (Thim, L., Thomsen, J., Christensen, M. and Jørgensen, K.H. et al. (1985) Biochim. Biophys. Acta 827, 410-418) has been checked by a combination of mass spectroscopy and Edman degradation. The pyroglutamyl blocking group was positively identified, and residue assignments at four positions were corrected: Lys48 (not Ser), Ser63 (not Lys), Cys68 (not Ser) and Ser74 (not Cys). The revised sequence exhibits greater similarity with pS2 peptide, a 60 residue polypeptide which is induced by oestrogen in the human breast cancer cell line MCF-7 and found in malignant but not in non-malignant breast tissue.

Amino Acid Sequence↗
PubMed1995

The trefoil peptides spasmolytic polypeptide and intestinal trefoil factor are major secretory products of the rat gut.

Spasmolytic polypeptide (SP) and intestinal trefoil factor (ITF) are trefoil peptides expressed by gut mucus cells. Using specific antisera we have quantified and characterized the molecular forms and distribution of these peptides in the rat gut. SP predominates in the gastric antrum as a 12 kDa form. ITF (7 kDa) is highly expressed throughout the small intestine. Both peptides are distributed in the apical secretory compartment of antral mucus cells (SP) and goblet cells (ITF), and on the lumenal surface. This study quantifies SP and ITF for the first time, and confirms them as major secretory products of the rat gut.

Amino Acid Sequence↗
PubMed1991

Expression of the breast cancer associated gene pS2 and the pancreatic spasmolytic polypeptide gene (hSP) in diffuse type of stomach carcinoma.

Expression of the pancreatic spasmolytic peptide (hSP) gene and pS2 (a gene isolated from oestrogen-induced breast carcinoma cells) were analysed in 36 samples of human stomach carcinoma. 17 tumours were investigated at the RNA level (by northern blots) as well as at the gene product level (by immunochemistry). Since pS2 had been shown to be expressed in normal stomach mucosa its activity in carcinoma samples was expected. Surprisingly, strong pS2 immunoreactivity was noted in the diffuse carcinoma type, whereas the intestinal type displayed weak reactivity. The tumour samples showing strong immunostaining expressed the regular 0.6 kb pS2 RNA band and weak staining was paralleled by aberrant transcripts. Additionally, only in tumour samples with regular pS2 transcription was the typical 0.7 kb hSP RNA band seen; samples with aberrant pS2 bands did not express hSP at all. This is the first demonstration of hSP gene activity in a human tumour.

Blotting, Northern↗
PubMed1993

Pancreatic spasmolytic polypeptide: first three-dimensional structure of a member of the mammalian trefoil family of peptides.

BACKGROUND: The trefoil peptides are a rapidly growing family of peptides, mainly found in the gastrointestinal tract. There is circumstantial evidence that they stabilize the mucus layer, and may affect the rate of healing of the mucosal epithelium. RESULTS: We have determined the structure of porcine pancreatic spasmolytic polypeptide (PSP) to 2.5 A resolution. The polypeptide contains two trefoil domains. The domain structure is compact, and is composed of a central short antiparallel beta-sheet with one short helix above and one below it. This is a novel motif. The two domains are related by two-fold symmetry, and each domain contains a cleft. CONCLUSIONS: The cleft within each domain could accommodate a polysaccharide chain, and may therefore be responsible for binding mucin glycoproteins. We suggest that PSP may cross-link glycoproteins, explaining its ability to stabilize the mucus layer.

Amino Acid Sequence↗
PubMed2006

Design, microwave-assisted synthesis, and spasmolytic activity of 2-(alkyloxyaryl)-1H-benzimidazole derivatives as constrained stilbene bioisosteres.

A simple, fast, and efficient method for the preparation of several 2-(alkyloxyaryl)-1H-benzimidazole derivatives is reported. Compounds were synthesized through a rapid one-pot three component reaction via microwave irradiation, starting from commercially available aldehydes and o-phenylenediamine, in the presence of Na(2)S(2)O(5) and solvent-free conditions. The design of these compounds explore the hypothesis that the stilbene framework could be mimicked with an appropriate 2-(Alkyloxyphenyl)benzimidazole scaffold. This framework has a similar structural motif as the 6-phenylnaphthalene and behaves like stilbene bioisosteres. The spasmolytic activity of these compounds was recorded using isolated rat ileum test. Compound 12 was the most active of the series, showing an IC(50) of 1.19 microM.

Aldehydes↗
PubMed2006

Comparative study of nicorandil and a spasmolytic cocktail in preventing radial artery spasm during transradial coronary angiography.

BACKGROUND: Radial artery spasm is one of the most common complications during coronary angiography via the transradial approach, causing patient discomfort or sometimes interrupting the procedure. This study was designed to compare the spasmolytic effect between nicorandil and a cocktail during transradial coronary angiography. METHODS: A randomized study to compare 4 mg of nicorandil and a cocktail (mixture of normal saline, 200 microg of verapamil) was performed in 150 patients. We examined vasospasms of the radial artery that were expressed as stenosis of the radial artery vessel diameter after the procedure. RESULT: The reductions of systolic and diastolic blood pressures showed no significant differences between the two groups (15.4+/-11.5/7.7+/-7.8 mmHg for nicorandil and 16.3+/-13.4/6.2 mmHg for cocktail). Both agents induced a significant radial artery vasodilation after transradial administration at proximal and mid segments (P < 0.001 for all). Nicorandil showed a significant increase of the mean change of the radial artery diameter compared to the cocktail at mid-segment (0.32+/-0.23 mm for nicorandil and 0.24+/-0.15 mm for a cocktail, P < 0.05). There was no statistically significant difference between the two groups in radial artery spasm (50.7% vs. 52.0% in nicorandil and a cocktail, respectively) after catheterization. CONCLUSION: Nicorandil with vasodilator effects by a dual mechanism was effective as the cocktail in preventing radial artery spasm during transradial coronary angiography.

Coronary Angiography↗
PubMed2004

Cholinesterase inhibitory and spasmolytic potential of steroidal alkaloids.

A new steroidal alkaloid, isosarcodine (1) along with four known bases, sarcorine (2), sarcodine (3), sarcocine (4) and alkaloid-C (5) were isolated from the MeOH extract of Sarcococca saligna. The structures of these alkaloids were identified by spectral data interpretation. These compounds were subjected to acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition studies, and were found to be noncompetitive inhibitors of AChE (Ki = 21.8, 90.3, 32.2, 16.0 and 50.0 microM, respectively) and uncompetitive or noncompetitive inhibitors of BChE (Ki = 8.3, 7.5, 15.6, 5.0 and 12.0 microM, respectively). The compounds (2-5) also showed dose-dependent spasmolytic activity in the rabbit jejunum intestinal preparations and also relaxed the high K+ (80 mM)-induced contraction, indicative of a calcium channel-blocking mechanism. Structure-activity relationship suggested that the nitrogen substituents at C-3 and/or C-20 of steroidal skeleton and the hydrophobic properties of the pregnane skeleton are the key structural features contributed to the inhibitory potency of these steroidal alkaloids against AChE and BChE.

Acetamides↗
PubMed1997

Inhibitory effects of various spasmolytics on the vagal afferent gastric excitatory response in cats.

The inhibitory effects of atropine, cimetropium, pirenzepine and N-butylscopolamine on the vagal afferent gastric excitatory response in cats under anesthesia with pentobarbital sodium and infusion of gallamine were examined. Electrical stimulation of vagal trunk in left side (10 Hz in frequency, 3 msec in duration, 15 V in intensity and for 10 sec) caused an initial gastric excitatory response during the period of stimulation followed by a late excitatory gastric response after stimulation in normal cats. The initial response was inhibited by atropine (100 microg/kg, i.v.) and hexamethonium (10 mg/kg, i.v.), while the late response was inhibited by atropine but not by hexamethonium (10 mg/kg, i.v.). In chronic supranodose vagotomized cats 11-15 days after the operation, stimulation of the vagal trunk caused a late gastric excitatory response after the stimulation period, which was inhibited by atropine (100 microg/kg, i.v.) but not by hexamethonium (10 mg/kg, i.v.). The two types of gastric responses in normal cats have been defined as follows: the initial gastric excitatory response (atropine- and hexamethonium- sensitive) is due to activation of vagal efferent fibers and the late gastric excitatory response (atropine-sensitive and hexamethonium-resistant) is due to activation of vagal afferent fibers. ED50 values of atropine, cimetropium, pirenzepine and N-butylscopolamine in inhibiting the vagal afferent gastric response were 7.2 microg/kg (n=4), 2.4 microg/kg (n=6), 82.6 microg/kg (n=3) and 93.0 microg/kg (n=4), respectively. The inhibitory effects of atropine and cimetropium on the vagal afferent gastric excitatory response (hexamethonium-resistant) were more potent than those of pirenzepine and N-butylscopolamine. These results suggested that the potent inhibitory effects of cimetropium and atropine on the vagal afferent gastric response may involve a potent spasmolytic effect.

Animals↗
PubMed1998

Spasmolytic effect of acidic fibroblast growth factor in early cerebral vasospasm in the rat.

BACKGROUND: In animal models of subarachnoid hemorrhage (SAH), basilar artery spasm has been described. Since fibroblast growth factors (FGFs) dilate rat basilar artery in vivo, we tested whether systemic administration of acidic fibroblast growth factor (aFGF) can reverse the basilar artery spasm following rat SAH. METHODS: SAH was mimicked by injecting autologous blood into the cisterna magna. We used a digital substraction angiography system in order to evaluate the spasmolytic effect of aFGF administered via the axillary artery 7 minutes after the injection of the autologous blood. Control animals received vehicle solution in the same manner. RESULTS: Intraarterial bolus injection of 2.6 micrograms aFGF, but not the solvent, reverses the acute basilar artery narrowing caused by SAH (23.05% of the baseline value at 5 minutes post-SAH). CONCLUSIONS: Our results suggest an important role for FGFs in the cerebral tone regulation and support a clinical interest of FGFs in preventing cerebral ischemia following SAH, particularly if these vasoactive effects are added to the known neuroprotective effects of FGFs.

Angiography, Digital Subtraction↗
PubMed1997

Role of spasmolytic polypeptide in healing of stress-induced gastric lesions in rats.

Stress is known to induce gastric ulcerations but the mechanism of their healing has been little studied. This paper describes the studies on mucosal expression and the effect on ulcer healing of spasmolytic peptide (SP), one of the members of the trefoil peptide family. Gastric ulcerations were induced in rats by the exposition to 3.5 h of water immersion and restraint stress. It was found that the number of these lesions gradually declined at 4, 8 and 12 h after stress and this spontaneous healing was significantly accelerated by s.c. infusion of human recombinant SP in a constant dose of 50 micrograms kg-1 h-1. The healing of the stress-induced ulcerations was accompanied by a gradual restoration of gastric mucosal blood flow and the decrease in gastric acid and pepsin secretion towards the normal values. The expression of SP in rats (rSP) was detected by RT-PCR in the intact mucosa and during all tested time periods reaching a peak at 4 h after the stress. Immunostaining for rSP in the intact mucosa was confined to the mucous neck cells, but following the exposure to stress it was significantly enhanced and occurred also in the cells of the basal region of gastric glands, reaching a peak at 4 h after the stress. We conclude that SP plays an important role in healing of stress-induced gastric lesions possibly by the acceleration of the mucosal repair, the enhancement of mucosal blood flow and the inhibition of gastric secretion.

Animals↗
PubMed2000

Antiamoebic and spasmolytic activities of extracts from some antidiarrhoeal traditional preparations used in Kinshasa, Congo.

Three major extracts from some traditional preparations, based on medicinal plants, used as antidiarrhoeal agents were investigated for their putative antiamoebic and spasmolytic activities in vitro. Results indicated that both biological activities are concentrated in the polyphenolic fraction, and not in the saponin or alkaloid containing fractions. The most active polyphenolic extracts were those from Euphorbia hirta whole plant, leaves of Alchornea cordifolia, Crossopteryx febrifuga, Nauclea latifolia, Psidium guajava, Tithonia diversifolia, stem bark of Harungana madagascariensis, Mangifera indica, Maprounea africana and Psidium guajava, inhibiting Entamoeba histolytica growth with MAC < 10 micrograms/ml. The same extracts, at a concentration of 80 micrograms/ml in an organ bath, also exhibited more than 70% inhibition of acetylcholine and/or KCl solution-induced contractions on isolated guinea-pig ileum.

Amebicides↗
PubMed2000

Constipating and spasmolytic effects of Khat (Catha edulis Forsk) in experimental animals.

The constipating and spasmolytic effects of Catha edulis Forsk (Khat) were investigated in whole mice and on isolated guinea pig ileum. D-amphetamine was employed in both experiments for comparison. The total distance travelled (expressed in percentage) by charcoal suspension in the gastrointestinal tract of mice was determined before and after khat administration. The procedure was repeated with amphetamine and normal saline. The results were compared. Amplitudes of contraction were recorded with standard spasmogens, histamine and carbachol, in the presence and absence of khat extract of different concentrations. The same was done with amphetamine. Khat extract was observed to reduce the total distance travelled by charcoal suspension, comparable to D-amphetamine. The spasmogenic effects of both histamine and carbachol were observed to be antagonized by the khat extract in a concentration-dependent manner. The antispasmodic effect of khat extract was observed to be similar to that of D-amphetamine.

Animals↗
PubMed1999

The monoterpene alkaloid cantleyine from Strychnos trinervis root and its spasmolytic properties.

Cantleyine, a monoterpene alkaloid isolated from the root bark of Strychnos trinervis, was submitted to a broad spectrum pharmacological screening, in which the principal effect observed was a nonspecific relaxation of isolated smooth muscles. Cantleyine relaxed (IC50 2.1 x 10(-4) M) the guinea-pig trachea, pre-contracted by carbachol and antagonized in a nonspecific manner; carbachol (IC50 2.1 x 10(-4) M) and histamine (IC50 1.4 x 10(-4) M) induced contractions in the guinea-pig ileum; and phenylephrine (IC50 3.8 x 10(-4) M) responses in the rat aorta. Cantleyine antagonized (pD'2, 3.82) cumulative concentration response curves to histamine in the ileum in a noncompetitive, reversible (slope, 4.84) and concentration dependent manner. The tonic contractions induced by histamine and KCl were also inhibited in a concentration-dependent and reversible manner (IC50 7.2 x 10(-5) and 1.8 x 10(-4) M, respectively), suggesting that cantleyine should be acting on voltage-dependent Ca2+ channels. This hypothesis was confirmed by the observation that cantleyine inhibited (pD'2, 3.35), in a concentration dependent manner, the CaCl2 induced contraction in depolarizing medium. These results suggest that cantleyine produces nonspecific spasmolytic effects in smooth muscle and that in guinea-pig ileum this effect is, in part, due to the inhibition of Ca+2 influx through voltage-dependent Ca2+ channels.

Alkaloids↗
PubMed1992

1H NMR-based determination of the secondary structure of porcine pancreatic spasmolytic polypeptide: one of a new family of "trefoil" motif containing cell growth factors.

Two-dimensional 1H NMR spectroscopy has been used to obtain comprehensive sequence-specific resonance assignments for the putative cell growth factor porcine pancreatic spasmolytic polypeptide, which is a 106-residue protein containing two "trefoil" domains. The patterns of sequential (i,i+l), medium-range (i,i less than 5), and long-range NH to NH, alpha CH to NH, and alpha CH to alpha CH nuclear Overhauser effects clearly show that the protein's two trefoil domains adopt essentially the same secondary structure in solution. The main feature of each domain is a seven-residue helix followed by a short antiparallel beta-sheet formed from two strands of four amino acids each. This is a novel supersecondary structure, which clearly identifies the trefoil motif as a new class of growth factor associated module, distinct from other types of highly disulfide cross-linked domains, such as those found in epidermal growth factor and insulin-like growth factor I.

Amino Acid Sequence↗
PubMed1982

Synthesis and spasmolytic activities of 2-(1,2-benzisoxazol-3-yl)-3-[[omega-(dialkylamino)alkoxy]phenyl]acrylonitriles.

Several 2-(1,2-benzisoxazol-3-yl)-3-[[omega-(dialkylamino)alkoxy]phenyl]acrylonitrile derivatives were synthesized and screened for potential spasmolytic activity. The effect of structural variation of these molecules on biological activities was systematically examined. Among these compounds, (Z)-2-(1,2-benzisoxazol-3-yl)-3-[2-(2-piperidinoethoxy)-phenyl]acrylonitrile (1d), (Z)-2-(1,2-benzisoxazol-3-yl)-3-[2-(2-morpholinoethoxy)phenyl]acrylonitrile (1f), and their analogues (3c,d) having a methoxy substituent at C5 of the benzoisoxazole ring showed potent antispasmodic activities in the in vitro and in vivo studies.

Acrylonitrile↗
PubMed2000

Spasmolytic constituents from Eucalyptus camaldulensis var. obtusa leaves.

Phytochemical studies on the leaves of Eucalyptus camaldulensis var. obtusa have resulted in the isolation of a new triterpenoid camaldulin (3beta-formyloxyurs-11-en-28,13beta-olide) (1) along with ursolic acid lactone acetate (2), ursolic acid lactone (3), betulinic acid (4), and beta-sitosterol 3-O-beta-D-glucopyranoside (5). The structures were assigned on the basis of 1D and 2D NMR studies. Compounds 1-3 were tested for spasmolytic activity and were found to possess calcium antagonist activity.

Calcium Channel Blockers↗