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PubMed1975

[Angiographic diagnosis of paraduodenal hernia (author's transl)].

The case is reported of a 26-year-old man who had several episodes of subileus which responded to spasmolytics. Mesenteric angiography revealed a paraduodenal hernia, with displacement of several jejunal arteries towards the mesenteric root and compression of intestinal vessels at about the level of Treitz' ligament. The angiographic findings were confirmed at operation, which consisted of repositioning the jejunal loop and closing the hernial orifice. The patient has since been free of complaints.

Adult↗
PubMed2004

In vitro antispasmodic and anti-inflammatory effects of Drosera rotundifolia.

In investigations of the anti-inflammatory and spasmolytic effects of Drosera rotundifolia two extracts were tested in different in vitro assays. An aqueous and an ethanolic extract inhibited human neutrophil elastase, achieving IC50 values of 5 and 1 microg/mL, respectively. The very low naphthoquinone concentrations in the extracts seem not to be responsible for the effect, as the pure compounds were not effective in the test system used. Thus, flavonoids like hyperoside, quercetin and isoquercitrin, which were detected in the extracts in considerable concentrations, may contribute to the activity. These substances showed activity in the assay. Ellagic acid, detected especially in the ethanolic extract in higher amounts, was substantially less active than the flavonoids. In guinea-pig ileum the extracts led to an antispasmodic effect possibly by affecting an allosteric binding site of the muscarinic M3 receptors.

Animals↗
PubMed2001

General pharmacological properties of YJA20379-8, a new H+/K(+)-ATPase inhibitor with anti-ulcer activities.

The general pharmacological properties of YJA20379-8 (3-butyryl-4-[(R)-1-methylbenzylamino]-8-ethoxy-1,7-naphthyridine, CAS 187654-40-6), a new H+/K(+)-ATPase inhibitor with anti-ulcer activities, were investigated in mice, rats and guinea pigs. YJA20379-8 at oral doses of 25, 50 and 100 mg/kg did not affect the locomotor activity, hexobarbital hypnosis and motor coordination in mice. The drug did not have analgesic action and anticonvulsant action at the doses of 100 mg/kg p.o. The respiration and blood pressure were not affected at 10 mg/kg i.v. in rats. YJA20379-8 at 2 x 10(-4) g/ml did neither produce any contraction nor relaxation of isolated organs, such as guinea pig ileum, rat fundus, rat uterus and guinea pig vas deferens, and the drug antagonized the contractile responses to several spasmogens, such as acetylcholine, histamine, serotonin, L-phenylephrine, oxytocin and BaCl2. The drug up to 100 mg/kg p.o. did not affect pupil size and the intestinal propulsion of mice. And it did not show an anticarrageenan action at 100 mg/kg. In this general pharmacology study, hypothermic effect in mice, retardation in gastric emptying in rats, decreases in urine excretion in rats at oral doses of 50 and 100 mg/kg of YJA20379-8 and the spasmolytic activity could be found. However, no other effects were exhibited at a high oral dose of 100 mg/kg in animals in this study.

Animals↗
PubMed2000

[Non-opioid analgesics--irreplaceable in cancer pain therapy?

Sufficient therapy of pain is essential for the treatment of tumor patients. World Health Organisation (WHO)-guidelines recommend a combination of opioids with non-opioid-analgesics (NOA) for patients with medium to strong pain. Cancer pain is often a combination of pain caused by the tumor itself, tumor associated and pain caused by therapy. Various substances act by different mechanisms and therefore combinations may demonstrate superior effects. Opioids ("central analgesics") inhibit neuronal transduction within the spinal cord, enhance inhibiting function of midbrain nuclei on ascending pain transduction and influence pain perception via modulation of the limbic system. NOAs ("peripheral analgesics") inhibit cyclooxygenase hindering activation of the peripheral nociceptor-system. There are 2 different classes of NOAs: 1) non-acidic, antipyretic analgesics like pyrazolones (metamizol) and anilin-derivates (paracetamol) and 2) non-steroidal antirheumatics (NSAR) like salicylates (acetylsalicylic acid), derivates of propionic acid (ibuprofen, naproxen), acetate acid (indomethacin, diclofenac), enolic acid (piroxicam, meloxicam) and anthranil acid (mefenamin). Adjuvant therapy is necessary to control common NSAR-side-effects like dyspepsia, ulcer and gastrointestinal bleeding. Due to its exceptional analgesic, antipyretic and spasmolytic properties, metamizol is an essential substance in tumor therapy. As agranulocytosis-incidence of 1:1,000,000 is low, good gastrointestinal and renal tolerance makes metamizol an excellent alternative to NSAR. There is scientific evidence that adequate combinations of non-opioids, opioids and adjuvant drugs, considering adverse side effects, were effective and safe in the treatment of cancer pain.

Analgesia↗
PubMed2000

Smooth muscle relaxing activity of gentiopicroside isolated from Gentiana spathacea.

Bioassay directed fractionation of the (1:1) chloroform-methanol extract of Gentiana spathacea H.B.K (Gentianaceae) led to the isolation of gentiopicroside (gentiopricrin) (1), the major spasmolytic component of the plant. Gentiopicroside inhibited, in a concentration-dependent manner, the spontaneous contractions of isolated guinea pig ileum. Contractions induced by histamine, acetylcholine, BaCl2 and KCl on the ileum were also significantly blocked by this monoterpene glucoside, which suggests that this compound might be interfering with calcium influx into the smooth muscle cells.

Animals↗
PubMed2001

A new diterpenoid with antispasmodic activity from Salvia cinnabarina.

From the leaf surface exudate of the aerial parts of Salvia cinnabarina a new secoisopimarane diterpenoid with a non-specific spasmolytic activity on histamine-, acetylcholine-, and barium chloride-induced contractions in the isolated guinea-pig ileum was obtained. The IC50 value obtained was comparable with that obtained for papaverine. The structure of 3,4-secoisopimara-4(18),7,15-triene-3-oic acid was established by 1D and 2D NMR spectroscopic techniques.

Acetylcholine↗
PubMed2001

Hyperforin stimulates intracellular calcium mobilisation and enhances extracellular acidification in DDT1-MF2 smooth muscle cells.

Hyperforin, an acylphloroglucinol derivative, is a major constituent of St. John's wort extract (Hypericum perforatum L.), which is used in treating depressive disorders. Hyperforin has been demonstrated as a modulator of several neuronal ion channels, and inhibits smooth-muscle contraction induced by various neurotransmitters. To evaluate the spasmolytic properties of hyperforin in more detail, we performed studies on the hamster vas deferens smooth muscle cell line DDT1-MF2. In a first series of experiments, we determined the effect of hyperforin on intracellular Ca2+ concentration ([Ca2+]i) using the fluorochrome fura-2. These investigations were supplemented in a second series of assays, where the effects on cellular metabolism were analysed by measuring the rate of extracellular release of acidic metabolites with the help of a microphysiometer. Hyperforin (0.3-10 microg/ml) caused a concentration-dependent elevation of [Ca2+]i and extracellular acidification rate (ECAR). Both of these effects were independent of extracellular Ca2+. To elucidate whether the increase of [Ca2+]i by hyperforin causes or results from its ECAR-stimulating properties, we used various pharmacological tools to reveal the sequence of events and the molecular mechanisms involved. Our results suggest that hyperforin induces release of Ca2+ from as yet unidentified sources. Since the ECAR stimulation was inhibited to a different extent by the intracellular Ca2+ chelator BAPTA as well as by inhibitors of plasmalemmal and mitochondrial Na+/Ca2+ exchange, but not by inhibitors of Na+/H+ antiport, the intracellular Ca2+ increase seems to be essential for this hyperforin effect. However, further studies are needed to establish the exact mode of action, and to deduce whether this aspect of hyperforin activity contributes to its antidepressant and neuroprotective effects.

Acids↗
PubMed2002

Inhibitory effect of xanthomicrol and 3 alpha-angeloyloxy-2 alpha-hydroxy-13,14Z-dehydrocativic acid from Brickellia paniculata on the contractility of guinea-pig ileum.

Chemical fractionation of Brickellia paniculata methanolic extract by monitoring its inhibitory effect on K(+)-induced contraction in guinea-pig ileum in vitro led to the isolation of 5,4'-dihydroxy-6,7,8-trimethoxyflavone (xanthomicrol) and the labdane-diterpene 3 alpha-angeloyloxy-2 alpha-hydroxy-13,14 Z-dehydrocativic acid (AAHDD). Both compounds inhibited the tonic contraction the effect being highly potent when a mixture in a proportion of 3 : 1 (xanthomicrol/AAHDD) was assayed. The phasic component of the contractile response with K(+) was also reduced by the compounds. Xanthomicrol depressed the spasms induced with ACh, Hist, and BaCl(2) and its effect on Ca (2+) concentration-response curve showed a type of non-surmountable calcium blocking action; unlike the flavonoid, AAHDD produced a parallel rightward shift of the concentration-response curve to calcium, suggesting a competitive antagonism with an estimated pA(2) of 4.66. Obtained results support, in part, the popular use of B. paniculata as a spasmolytic remedy.

Acetylcholine↗
PubMed2003

Antispasmodic effect of the essential oil of Plectranthus barbatus and some major constituents on the guinea-pig ileum.

The effects of the Plectranthus barbatus essential oil (PBEO) at concentrations ranging form 1 to 300 microg/mL and some major constituents, i. e., alpha-pinene, myrcene and caryophyllene in the ratio and amount found in the oil, were studied on the contractility of the guinea-pig ileum. PBEO decreased the basal tonus of the ileum with a maximal response (R (max); % of K (+)-contraction) of 62.7 +/- 3.8 % compared with 36.6 +/- 4.5 % inhibition achieved with alpha-pinene and 68 +/- 2.6 % with papaverine. The other constituents had only a slight effect. PBEO also blocked the phasic contractions evoked by acetylcholine with an R (max) of 85 +/- 3.6 % compared with 54.4 +/- 3.5 % inhibition induced by alpha-pinene and 12.4 +/- 5.6 % with caryophyllene. The contractions induced by histamine or barium chloride were also decreased in amplitude by PBEO with an R (max) of 94.3 +/- 5.7 % and 100 %, respectively. In addition, PBEO relaxed tissues pre-contracted with 60 mM K (+) with an R (max) of 89.7 +/- 2.7 % compared with 55.4 +/- 4.6 % relaxation induced by alpha-pinene. The other major constituents studied had no significant effect. Furthermore, at the higher concentration used, i. e., 300 microg/mL, PBEO decreased the maximal response of calcium chloride (10 ( - 7) to 10 ( - 3) M) induced contraction in depolarized tissues by 29.1 +/- 9.53 % (p < 0.05). In addition, the component of the contraction elicited by a single dose of carbachol (CCh; 100 microM) added on nifedipine (10 microM) treated tissues or at very low extracellular calcium concentration were blocked by PBEO (300 microg/mL) in 85.7 +/- 7.8 % (p < 0.05; n = 5) and 81.2 +/- 6.4 % (p < 0.05; n = 4), respectively. These data show that PBEO has intestinal relaxant and antispasmodic activity and suggest that this effect is not related to antagonism in extracellular receptors for neurotransmitters or autacoids and it seems to occur downstream of calcium entry or release from internal stores. The main active principle for its relaxant and spasmolytic activity seems to be alpha-pinene.

Animals↗
PubMed2005

[Irritable bowel syndrome].

Patients with irritable bowel syndrome (IBS) are highly prevalent among subjects seeking medical attention at the general practitioner or specialist level. While IBS lacks any disease associated excess mortality, this disorders is relevant to the affected subjects due to the considerable burden with regard to the symptoms and an impaired quality of life. Furthermore, this disease has a substantial impact on society due to the economical consequences. In recent years substantial progress has been achieved regarding our pathophysiological understanding. However, as usual, there has been a substantial delay between the discovery of disease mechanisms and its translation into improved patient care. For diagnosing IBS standardized criteria have been established (i. e. Rome II- or the DGVS-criteria). Regarding treatment, life style advice such as avoidance of specific nutrients that precipitate or aggravate or the "little psychotherapy" (addressing patients concerns and anxiety regarding the symptoms) are considered essential. However, the overall response rate is disappointing. Evidence-based pharmacological interventions include herbal preparations, spasmolytics, low dose tricyclic antidepressants and 5-HT-3-receptor antagonists and 5-HT-4-receptor agonists. At present no cure for patients with IBS exists. Thus, all currently available treatments target palliation of symptoms. This, however, may change in the future.

Abdominal Pain↗
PubMed2005

Isolation of new rotenoids from Boerhaavia diffusa and evaluation of their effect on intestinal motility.

A bioassay-guided separation of a methanolic extract obtained from the roots of Boerhaavia diffusa L. (Nyctaginaceae) allowed us to isolate five compounds belonging to the class of rotenoids: the known boeravinone D ( 1), boeravinone E ( 2), compound 5 and two novel compounds that we have named boeravinone G ( 3) and boeravinone H ( 4). The structures of the new molecules have been determined on the basis of their HR-EI-MS, (1)H- and (13)C-NMR and 2D-NMR (HMQC, HMBC) data. All the isolated rotenoids have been evaluated for their effect on intestinal motility in vitro. Three of them (boeravinone G, boeravinone E and compound 5) exhibited spasmolytic activity. Preliminary structure-activity relationships have been established highlighting the effect of substitutions on rings B and D.

Animals↗
PubMed1997

Smooth muscle relaxing flavonoids and terpenoids from Conyza filaginoides.

Activity-guided fractionation of the smooth muscle relaxing, chloroform-methanol (1:1) extract of Conyza filaginoides (D.C.) Hieron (Asteraceae) led to the isolation of three flavonoids (quercetin 3-glucoside, rutin, and pinostrobin), one sterol (alpha-spinasterol), a sesquiterpenoid (beta-caryophyllene 4,5-alpha-oxide), and two triterpenoids (erythrodiol and 3-beta-tridecanoyloxy-28-hydroxyolean-12-ene). 3-beta-Tridecanoyloxy-28-hydroxy-olean-12-ene is a new naturally occurring terpenoid. All the isolated compounds induced a concentration-dependent inhibition of the spontaneous contractions of rat ileum. The spasmolytic activity exhibited by the extract and active principles tends to support the traditional use of C filaginoides as an antispasmodic agent.

Animals↗
PubMed1995

Apigenin, a component of Matricaria recutita flowers, is a central benzodiazepine receptors-ligand with anxiolytic effects.

The dried flower heads of Matricaria recutita L. (Asteraceae) are used in folk medicine to prepare a spasmolytic and sedative tea. Our fractionation of the aqueous extract of this plant led to the detection of several fractions with significant affinity for the central benzodiazepine receptor and to the isolation and identification of 5,7,4'-trihydroxyflavone (apigenin) in one of them. Apigenin competitively inhibited the binding of flunitrazepam with a Ki of 4 microM and had no effect on muscarinic receptors, alpha 1-adrenoceptors, and on the binding of muscimol to GABAA receptors. Apigenin had a clear anxiolytic activity in mice in the elevated plusmaze without evidencing sedation or muscle relaxant effects at doses similar to those used for classical benzodiazepines and no anticonvulsant action was detected. However, a 10-fold increase in dosage produced a mild sedative effect since a 26% reduction in ambulatory locomotor activity and a 35% decrement in hole-board parameters were evident. The results reported in this paper demonstrate that apigenin is a ligand for the central benzodiazepine receptors exerting anxiolytic and slight sedative effects but not being anticonvulsant or myorelaxant.

Animals↗
PubMed1994

Calcium-antagonist effects of quercetin on aortic smooth muscle.

Relaxation induced by quercetin was studied on aortic rings depolarized with KCl and on Ca2+ dependent aortic contraction. Quercetin's actions as a cyclooxygenase inhibitor were compared with those of indomethacin. To determine the possible effects of quercetin on internal Ca2+ mobilization, it was assayed on aortic muscle contracted with caffeine. Quercetin relaxes aortic smooth muscle contracted with KCl (RC50 = 1.8 x 10(-4) M) and induces a rightward displacement of Ca2+ curves. The relaxation induced by quercetin is higher than that produced by indomethacin, suggesting that its action is independent of cyclooxygenase inhibition. Caffeine-induced aortic contraction was not modified by quercetin, suggesting that its effect should not involve internal calcium modulation. Our results further support the thesis that the spasmolytic action of quercetin arises from its negative modulation of calcium entry to the smooth muscle.

Animals↗
PubMed1994

Identification and characterization of inhibitors of peptido-leukotriene-synthesis from Petasites hybridus.

Extracts from Petasites hybridus were found to inhibit peptido-leukotriene biosynthesis in isolated peritoneal macrophages. Chemical analysis by gas chromatography coupled with mass and infrared spectroscopy facilitated the identification of three isomeric oxopetasan esters, petasin, and isopetasin as the main compounds of these extracts. Fractionations obtained by column chromatography of the most effective extract indicated a correlation between peptido-leukotriene biosynthesis inhibition and the content of isopetasin, a sesquiterpene ester of isopetasol and angelic acid, as well as the isomeric oxopetasan esters. Petasin, a structural isomer of isopetasin, however, was found to be inactive. It may even reduce the peptido-leukotrine inhibitory effect of isopetasin. It is concluded that isopetasin and the oxopetasan esters in Petasites hybridus inhibit the biosynthesis of the vasoconstrictive peptido-leukotrienes. This effect may contribute to some of the medicinal properties of Petasites hybridus extracts such as, e.g., gastroprotection and spasmolytic activity.

Animals↗
PubMed1994

Effects of aqueous extracts of six marine microalgae on smooth muscle contraction in rat duodenum and vas deferens.

We report the effects of aqueous extracts of six marine microalgae on responses to various contractile agents in isolated rat duodenum (acetylcholine, calcium chloride, barium chloride) and vas deferens (noradrenaline). Our results suggest that only extracts of Phaeodactylum tricornutum, Skeletonema costatum, and Chlorella stigmatophora may have pharmacological potential. Extracts of these three species had spasmolytic effects on responses to the three contractile agents in duodenum. In vas deferens, P. tricornutum and C. stigmatophora inhibited the contractions induced by noradrenaline, whilst S. costatum showed a non-dose-dependent potentiation. With the aim of elucidating their mechanisms of action, we are attempting to isolate the active principles present in these extracts.

Animals↗
PubMed1992

Antispasmodic activity of beta-damascenone and E-phytol isolated from Ipomoea pes-caprae.

The crude extract (IPA) of the plant Ipomoea pes-caprae (L.) R. Br. has previously been shown to antagonize smooth muscle contractions induced by several agonists via a non-specific mechanism. Bioassay-guided fractionation of IPA resulted in isolation of the antispasmodically acting isoprenoids beta-damascenone and E-phytol. Their antispasmodic potencies were found to be in the same range as that of papaverine, a general spasmolytic agent. This effect was suggested to play a role in the previously observed anti-inflammatory activity of IPA by interfering with the contraction of endothelial cells. Severe vascular contraction has been shown to be involved in the dermatitis caused by toxic jellyfishes. It is possible that beta-damascenone and E-phytol, by interfering with the contraction of vascular smooth muscle cells, are partly responsible for the previously reported effectiveness of IPA in the treatment of such dermatitis.

Animals↗