Gastric Disturbances Research Articles

Antinociceptive and anti-inflammatory potential of extract and isolated compounds from the leaves of Salvia officinalis in mice

Ethnopharmacological relevanceSalvia officinalis L. has been used as a traditional herbal medicine for gastric disturbances and inflammatory processes. This study investigated the toxicological, antinociceptive and anti-inflammatory effects of the hydroalcoholic extract (HE) from leaves of Salvia officinalis and its isolated compounds in mice. Materials and methodsMice were treated with HE before the induction of nociceptive response by chemical agents (acetic-acid, formalin, glutamate, capsaicin and cinnamaldehyde). Total leukocytes and plasma extravasation induced by acetic acid and paw oedema induced by glutamate, capsaicin and cinnamaldehyde were also measured. The antinociceptive effect of carnosol and ursolic acid/oleanolic acid were evaluated on formalin and cinnamaldehyde models. ResultsIn the acute toxicity test the value of estimated LD50 for HE was 44.7579g/kg. Oral administration of HE (10, 30 and 100mg/kg) inhibited the number of writhings, total leukocytes and plasma extravasation induced by acetic acid. In the formalin test, HE reduced both neurogenic and inflammatory phases, effect that was affected by naloxone. The glutamate-, capsaicin- and cinnamaldehyde-induced nociception and paw oedema were reduced by HE at doses that did not affect the locomotor activity of mice in the open field test. Carnosol (10mg/kg) and ursolic acid/oleanolic acid (30mg/kg) inhibited the inflammatory phase of formalin and the nociception and mechanical allodynia induced by cinnamaldehyde. ConclusionsThese results demonstrate that HE presents significant anti-inflammatory and also antinociceptive effects on chemical behavioral models of nociception that involves an opioid mechanism. In addition, carnosol and ursolic acid/oleanolic acid contained in this plant appears to contribute for the antinociceptive property of the extract, possibly through a modulatory influence on TRPA1-receptors. However, further studies regarding the precise site and the mechanism of action of HE and carnosol and ursolic acid/oleanolic acid merited exploring further.

Inhibition of Gastric H+, K+-ATPase Activity by Compounds from Medicinal Plants

H+, K(+)-ATPase enzyme is a therapeutic target for the treatment of gastric disturbances. Several medicinal plants and isolated compounds inhibit the acid gastric secretion through interaction with the proton pump. In order to add new properties to some natural constituents, five compounds, a benzylated derivative of vincoside, a diterpene (abietic acid) and three alkaloids (cephaeline, vinblastine and vindoline), were tested for their activities on gastric H+, K(+)-ATPase isolated from rabbit stomach. All the compounds inhibited H+, K(+)-ATPase activity with varied potency. The IC50 value for benzylvincoside was 121 (50-293) microM, and for abietic acid 177 (148-211) microM. The alkaloids cephaeline, vinblastine and vindoline inhibited the H+, K(+)-ATPase activity with IC50 values of 194, 761 and 846 microM, respectively. The results suggest that benzylvincoside, abietic acid and cephaeline can be important sources for the development of anti-secretor agents.

An overview of Yellow Card reporting by NIMH practitioners

ContextThe NIMH Yellow Card Scheme was initiated in 1994 as a means for reporting adverse events directly relating to herbal medicines individually prescribed by herbal practitioners in the clinical setting. Current research in herbal medicine relies mostly on studies investigating the efficacy and adverse effects of over the counter manufactured products or isolated constituents. It does not take in to account the complex intervention of clinical herbal practice. ObjectivesTo provide an overview of adverse reactions as reported by qualified herbalists by the NIMH Yellow Card Scheme to inform clinical practice and disseminate information to the wider healthcare community. SettingClinical experience as reported by NIMH professional herbal practitioners. ResultsNo serious adverse events have been reported by the NIMH Yellow Card system meaning there have been no fatalities or lasting serious harmful effects of herbal medicines prescribed by herbal practitioners. The outcomes in all 60 reports are reported as a full recovery. Symptoms usually resolve within hours to a few days after stopping the medicine. Common reactions reported include headache; gastric disturbance; skin irritation; sleep disturbance; agitation; hypersensitivity or allergic reaction. In the event of an adverse reaction it is difficult to identify one herb involved as it is common to herbal practice to prescribe medicines on an individual basis in combination and other factors such as individual sensitivities, diet and lifestyle changes are often involved. ConclusionsThe reports provide an important information source of clinical experience and relevance to practitioners and safety issue concerns. Clinical data combined with traditional empirical documentation enhances knowledge of evidence based practice.

Effect of lactobacillus on gastric flora in rats with severe brain injury

Objective To probe into the effect of the enteral nutrition added with lactobacillus on gastric bacteria of rats with severe brain injury. Methods Severe brain injury was made in rats that were then fed with enteral nutrition (3-9 entire nutrients), lactobacillus (3-9 entire nutrients + lactobacillus) and synbiotics (3-9 entire nutrients + lactobacillus + fiber) respectively. Gastric body and gastric antrum mucosa were collected at day 1, 3 and 7 after injury to detect the change of the gastric bacteria. Results DCCE analysis showed less bacteria in sham operation group. On the first day after severe brain injury, the flora bands were increased remarkably but the number of bacteria was decreased in three groups. The similarity of denaturing gradient gel electrophoresis ( DGGE) map patterns was 65% , 64% and 53% respectively in the enteral nutrition group, lactobacillus group and synbiotics group, with no significant difference in regard of the diversity index. On the third day after severe brain injury, the flora bands showed a tendency of decrease, with the similarity of denaturing gradient gel electrophoresis (DGGE) map patterns for 72% , 58% and 62% respectively. The richness and diversity of total bacteria in the lactobacillus group was remarkably lower than that in the enteral nutrition group and synbiotics group (P＜0.01). On the seventh day after SHI, the flora bands were decreased in three groups, with the minimum number of the bacteria. The similarity of denaturing gradient gel electrophoresis ( DGGE) map patterns was 61% , 51% and 58% respectively, with higher richness and diversity of total bacteria in the synbiotics group compared with the other groups. Conclusion Lactobacillus can help improve gastric bacteria disturbance of rats with severe brain injury. In the meantime, addition of the lactobacillus is better than addition of the synbiotics. Key words: Craniocerebral trauma; Probiotics; Lactic acid; Stomach; Bacteria

Gastric motor disturbances in patients with idiopathic rapid gastric emptying

The mechanisms of 'idiopathic' rapid gastric emptying, which are associated with functional dyspepsia and functional diarrhea, are not understood. Our hypotheses were that increased gastric motility and reduced postprandial gastric accommodation contribute to rapid gastric emptying. Fasting and postprandial (300kcal nutrient meal) gastric volumes were measured by magnetic resonance imaging (MRI) in 20 healthy people and 17 with functional dyspepsia; seven had normal and 10 had rapid gastric emptying. In 17 healthy people and patients, contractility was analyzed by spectral analysis of a time-series of gastric cross-sectional areas. Logistic regression models analyzed whether contractile parameters, fasting volume, and postprandial volume change could discriminate between health and patients with normal or rapid gastric emptying. While upper gastrointestinal symptoms were comparable, patients with rapid emptying had a higher (P=0.002) body mass index than normal gastric emptying. MRI visualized propagating contractions at ∼3cpm in healthy people and patients. Compared with controls (0.32±0.04, Mean±SEM), the amplitude of gastric contractions in the entire stomach was higher (OR 4.1, 95% CI 1.2-14.0) in patients with rapid (0.48±0.06), but not normal gastric emptying (0.20±0.06). Similar differences were observed in the distal stomach. However, the propagation velocity, fasting gastric volume, and the postprandial volume change were not significantly different between patients and controls. MRI provides a non-invasive and refined assessment of gastric volumes and contractility in humans. Increased gastric contractility may contribute to rapid gastric emptying in functional dyspepsia.

Gastroprotective and ulcer healing effects of essential oil from Hyptis spicigera Lam. (Lamiaceae)

Hyptis Jacq. (Lamiaceae) is being used in traditional medicine to treat fever, inflammation and gastric disturbances. Hyptis spicigera Lam. is a native plant distributed across the central region of Brazil. The essential oil extracted from this plant is used in folk medicine as antipyretic. The effects of the essential oil obtained from the aerial parts of Hyptis spicigera (OEH) were evaluated for their gastroprotective and healing activities. OEH chemical composition was analyzed by gas chromatography-mass spectrometry (GC-MS). The gastroprotective action of the OEH was evaluated in rodent experimental models (ethanol and NSAID). To elucidate mechanisms of action, the antisecretory action and involvements of NO, SH, mucus and PGE2 were evaluated. The acetic acid-induced gastric ulcer model and Western Blot assay (COX-2 and EGF) were also used to evaluate the OEH healing capacity. GC-MS analysis of OEH indicated three monoterpenes as major compounds: alpha-pinene (50.8%), cineole (20.3%) and beta-pinene (18.3%) and, at the dose of 100 mg/Kg, p.o., OEH provided effective gastroprotection against lesions induced by absolute ethanol (97%) and NSAID (84%) in rats. OEH do not interfere with H+ secretion in gastric mucosa and its gastric protection does not depend on nitric oxide (NO) and sulfhydryl compounds (SH). The gastroprotective action of OEH occurs due to an increase in the gastric mucus production (28%) induced by PGE2 levels. Furthermore, OEH demonstrated a great healing capacity with 87% of reduction in ulcerative lesion area. It accelerated the healing of acetic acid-induced gastric lesions due to an increase in COX-2 (75%) and EGF (115%) expression in gastric mucosa. No sign of toxicity was observed in this study, considering the analyzed parameters. All these results suggest the efficacy and safety of Hyptis spicigera in combating and healing gastric ulcer. Considering the results, it is suggested that the OEH could probably be a good therapeutic agent for the development of new phytotherapeutic medicine for the treatment of gastric ulcer.

Gastroprotective Effect of Ginger Rhizome (Zingiber officinale) Extract: Role of Gallic Acid and Cinnamic Acid in H+, K+‐ATPase/H. pylori Inhibition and Anti‐Oxidative Mechanism

Zinger officinale has been used as a traditional source against gastric disturbances from time immemorial. The ulcer-preventive properties of aqueous extract of ginger rhizome (GRAE) belonging to the family Zingiberaceae is reported in the present study. GRAE at 200 mg kg−1 b.w. protected up to 86% and 77% for the swim stress-/ethanol stress-induced ulcers with an ulcer index (UI) of 50 ± 4.0/46 ± 4.0, respectively, similar to that of lansoprazole (80%) at 30 mg kg−1 b.w. Increased H+, K+-ATPase activity and thiobarbituric acid reactive substances (TBARS) were observed in ulcer-induced rats, while GRAE fed rats showed normalized levels and GRAE also normalized depleted/amplified anti-oxidant enzymes in swim stress and ethanol stress-induced animals. Gastric mucin damage was recovered up to 77% and 74% in swim stress and ethanol stress, respectively after GRAE treatment. GRAE also inhibited the growth of H. pylori with MIC of 300 ± 38 μg and also possessed reducing power, free radical scavenging ability with an IC50 of 6.8 ± 0.4 μg mL−1 gallic acid equivalent (GAE). DNA protection up to 90% at 0.4 μg was also observed. Toxicity studies indicated no lethal effects in rats fed up to 5 g kg−1 b.w. Compositional analysis favored by determination of the efficacy of individual phenolic acids towards their potential ulcer-preventive ability revealed that between cinnamic (50%) and gallic (46%) phenolic acids, cinnamic acid appear to contribute to better H+, K+-ATPase and Helicobacter pylori inhibitory activity, while gallic acid contributes significantly to anti-oxidant activity.

Controlled Transdermal Delivery of Loxoprofen from an Ethylene-Vinyl Acetate Matrix

ABSTRACT − Repeated oral administration of loxoprofen can induce many side effects such as gastric disturbances andacidosis. Therefore, we considered alternative routes of administration for loxoprofen to avoid such adverse effects. The aimof this study was to develop an ethylene-vinyl acetate (EVA) matrix system containing a permeation enhancer for enhancedtransdermal delivery of loxoprofen. The EVA matrix containing loxoprofen was fabricated and the effects of drug con-centration, temperature, enhancer and plasticizer on drug release were studied from the loxoprofen-EVA matrix. The sol-ubility of loxoprofen was highest at 40% (v/v) PEG 400. The release rate of drug from drug-EVA matrix increased withincreased loading dose and temperature. The release rate was proportional to the square root of loading dose. The activationenergy (Ea), which was measured from the slope of log P versus 1000/T, was 5.67 kcal/mol for a 2.0% loaded drug dosefrom the EVA matrix. Among the plasticizer used, diethyl phthalate showed the highest release rate of loxoprofen. Amongthe enhancers used, polyoxyethylene 2-oleyl ether showed the greatest enhancing effect. In conclusion, for the enhancedcontrolled transdermal delivery of loxoprofen, the application of the EVA matrix containing plasticizer and penetrationenhancer could be useful in the development of a controlled drug delivery system.Key words

Relationship between non-ulcerative functional dyspepsia, occlusal pairs and masticatory performance in partially edentulous elderly persons

To relate occlusal state, masticatory performance and non-ulcerative functional dyspepsia. In spite of the relationship between gastric disturbances and number of present teeth being recognised, the influence of the number of occlusal pairs and masticatory performance, expressed as median particle size, has not been considered. Thirty-eight subjects (mean age = 71.8 ± 7.7 years) diagnosed with non-ulcerative functional dyspepsia were selected. A further 38 healthy subjects (mean age = 71.9 ± 7.0 years) acted as controls. Subjects were subdivided according to their number of occlusal pairs: (1) 0-4, (2) 5-9 and (3) 10-14. Masticatory performance was evaluated by using the sieving method. Data were analysed using 2-way anova and Bonferroni post-hoc, Chi-square and Odd ratio tests. Subjects presenting with non-ulcerative functional dyspepsia and 0-4 occlusal pairs showed the lowest masticatory performance (p < 0.01). No association between the dyspepsia and the number of occlusal pairs (χ(2) = 0.48, p = 0.785) was observed, however results showed association between functional dyspepsia and masticatory performance (χ(2) = 4.07, p = 0.0437) presenting an odds ratio = 3.46 (Confidence Interval = 0.99-12.10). Changes in masticatory performance were associated with the presence of non-ulcerative functional dyspepsia.

Enhanced Controlled Transdermal Delivery of Hydrochlorothiazide from an Ethylene-vinyl Acetate Matrix

ABSTRACT Š Repeated oral adm inistration of hy drochlorothiazide, a loop diuretic, due to transient high blood levels, m aycause adverse effects such as gastric disturbance, nausea, high blood sugar, and hy per lipidem ia. Transderm al adm inistrationcould avoid som e of these sy stemic side eff ects and gastric disorders. We have developed a m atrix using ethylene-viny l ace-tate (EVA ), a heat-processible and flexible m aterial, for transdermal delivery of hydrochlorothiazide. Drug solubility washighest at 40% PEG -400 volume fraction. Drug release increased as concentration increased w ith a linear relationshipbetween the release rate and the square root of loading dose. Increasing tem perature increased drug release f rom the EVAmatrix. The activation energy, measured from the slope of log P versus 1000/T, was 11.9 kcal/m ol for a 2.5% loading dosefrom EVA matrix. Diethy l phthalate had the highest plasticizing effects on the release of hydrochlorothiazide. To increasethe skin permeation of hy drochlorothiazide from theA EV m atrix, enhancers such as the saturated fatty acids, the unsaturatedfatty acids, and the non-nicoi surfactants w ere aded to thed A m EVatrix, an sdk nepi rmeatnoi w as evaluated using a modifiedKeshary -Chien diffusion cell fitted with intact excised rat skin. Polyoxy ethy lene 23-laury l ether showed the highest enhanc-ing eff ects. In conclusion, transderm al delivery of hy drochlorothiazide could be improved from an EVA m atrix containingplasticizer and perm eation enhancer.Key words

M2012 Gastric Motor Disturbances in Functional Dyspepsia With Rapid Gastric Emptying

M2012 Gastric Motor Disturbances in Functional Dyspepsia With Rapid Gastric Emptying

Inhibition of H+/K+ ATPase in the gastroprotective effect of Baccharis illinita DC

Baccharis illinita DC (Compositae) is used in folk medicine to treat gastric disturbances. Preliminary studies with other extracts of B. Illinita showed gastric protection against ethanol-, indometacin- and stress-induced ulcers and the inhibition of gastric secretion. Based on these data, the aim of this study was to verify the pathways involved in the inhibition of gastric secretion. The chloroform extract (CE) of flowers from B. illinita (3, 10, 30 and 100 mg kg(-1) i.p.) tested on rats with pylorus ligature reduced the volume and the total acidity of gastric content by approximately 50% (ED50 = 69 mg kg(-1)). Treatment with CE (100 mg kg(-1) i.p.) reduced the gastric total acidity stimulated by histamine, bethanechol and pentagastrin to 42%, 27% and 57% of that in the stimulated control group, respectively. The CE (10, 30 and 100 microM) inhibited H+/K+ ATPase activity in-vitro, with an IC50 of 37 microM. The isolated flavonoid luteolin (1, 3, 10 and 30 microM) also inhibited H+/K+ ATPase activity by 50%, at a dose of 30 microM. Our results suggest that the reduction in gastric secretion occurs through inhibition of H+/K+ ATPase, which is the final step in acid secretion and therefore one of the most important steps.

Short-term Outcomes of Roux-en-Y Stapled Anastomosis after Distal Gastrectomy for Gastric Adenocarcinoma

BackgroundSince 2003, we have begun to perform gastrojejunostomy by mechanical stapling for Roux-en-Y reconstruction in distal gastrectomy. We performed a retrospective study to compare the short-term outcomes of anastomosis by mechanical stapling and hand suturing. MethodsWe evaluated the data of 701 consecutive patients of gastric adenocarcinoma who underwent conventional open distal gastrectomy with Roux-en-Y reconstruction. The data collected included details on the method used for the Roux-en-Y reconstruction, the disease stage, extent of lymph node dissection, performance rate of truncal vagotomy, operation time, operative blood loss, length of hospital stay, and postoperative complications. ResultsThe operation time was significantly shorter in the group in which mechanical stapling was used for the anastomosis (MS group) than in the group in which anastomosis was performed by hand suturing (HS group; 241.1±56.8 vs. 166.4±48.3 min; p < 0.05). Postoperatively, delayed gastric emptying occurred in 14 (1.9%) patients, including seven (4.2%) from the MS group and seven (1.3%) from the HS group (p = 0.038). ConclusionThere were no significant disadvantages of employing mechanical stapling for anastomosis, except for the high rate of delayed gastric emptying. More consideration therefore needs to be given to decreasing the frequency of gastric emptying disturbance post surgery using mechanical staples.

Mechanisms of gastric emptying disturbances in chronic and acute inflammation of the distal gastrointestinal tract

It is unclear why patients with inflammation of the distal bowel complain of symptoms referable to the upper gastrointestinal tract, specifically to gastric emptying (GE) disturbances. Thus we aimed to determine occurrence and putative pathomechanisms of gastric motor disorders in such patients. Thirteen healthy subjects (CON), 13 patients with Crohn's disease (CD), 10 with ulcerative colitis (UC), and 7 with diverticulitis (DIV) underwent a standardized (13)C-octanoic acid gastric emptying breath test. Plasma glucose, CCK, peptide YY, and glucagon-like peptide-1 (GLP-1) were measured periodically and correlated with GE parameters. Results were given in means +/- SD. Compared with CON, GE half time (T) was prolonged by 50% in CD (115 +/- 55 vs. 182 +/- 95 min, P = 0.037). Six CD, 2 DIV, and 2 UC patients had pathological T (>200 min). Postprandial plasma glucose was increased in all patients but was highest in DIV and correlated with T (r = 0.90, P = 0.006). In CD, mean postprandial CCK levels were increased threefold compared with CON (6.5 +/- 6.7 vs. 2.1 +/- 0.6 pmol/l, P = 0.027) and were correlated with T (r = 0.60, P = 0.041). Compared with CON, GLP-1 levels were increased in UC (25.1 +/- 5.2 vs. 33.5 +/- 13.0 pmol/l, P = 0.046) but markedly decreased in DIV (9.6 +/- 5.2 pmol/l, P < 0.0001). We concluded that a subset of patients with CD, UC, or DIV has delayed GE. GE disturbances are most pronounced in CD and might partly be caused by excessive CCK release. In DIV there might be a pathophysiological link between decreased GLP-1 release, postprandial hyperglycemia, and delayed GE. These explorative data encourage further studies in larger patient groups.

Utilisation des médicaments prokinétiques en réanimation : indications et limites ?

Enteral feeding is often limited by gastric and intestinal motility disturbances in critically ill patients, particularly in patients with shock. So, promotility agents are frequently used to improve tolerance to enteral nutrition. This review summaries the pathophysiology, presents the available pharmacological strategies, the clinical data, the counter-indications and the principal limits. The clinical data are poor. No study demonstrates a positive effect on clinical outcomes. Metoclopramide and erythromycin seems to be the more effective. Considering the risk of antibiotic resistance, the first line use of erythromycin should be avoided in favor of metoclopramide.

Survival of Cronobacter Species in Reconstituted Herbal Infant Teas and their Sensitivity to Bovine Lactoferrin

Cronobacter is a new genus containing 5 species previously known as Enterobacter sakazakii. The popularity of "natural" substances and alternative medicine has extended the use of natural antimicrobials and herbs to foods, and some herbs are claimed to relieve gastric disturbances in infants. The present study investigated the antimicrobial activity of bovine lactoferrin (LF) and Cronobacter survival in commercial herbal infant teas (HITs) reconstituted with water at different temperatures. Cronobacter cells were able to grow in all reconstituted HITs at 37 or 21 degrees C after 6 h. A 4-log reduction in Cronobacter was achieved by reconstituting herbal infant tea at > or = 60 degrees C. LF was able to reduce Cronobacter species viability in herbal infant tea. No viable cells were recovered after 4 h at 37 degrees C in the presence of > or = 5 mg LF/mL. The bactericidal activity of LF was reduced at lower concentrations and lower temperatures. This study demonstrates that if present in reconstituted herbal infant tea, Cronobacter can grow and this may compromise the safety of these products. Therefore, addition of LF to reconstituted HIT may be a promising approach for the effective control of this organism. Practical Application: Cronobacter species can be isolated from herbal teas, and these products are claimed to relieve gastric disturbances in infants. This study demonstrates that Cronobacter cells present in reconstituted herbal infant teas (HITs) can grow if not held at acceptable temperatures. It was shown that reconstitution of these tea formulas with > or = 60 degrees C water reduced the potential risk from Cronobacter. Furthermore, use of lactoferrin (LF) may be a promising approach for effective control of these organisms in HIT held at nonrefrigeration temperatures (10 to 37 degrees C) for short periods.

Gastric myoelectrical differences between Parkinson's disease and multiple system atrophy

The electrogastrogram (EGG) was recorded for 24 hours in 17 Parkinson's disease (PD) patients, 17 multiple system atrophy (MSA) patients, and 8 healthy control subjects to elucidate the differences in the EGG findings between the two diseases. Eight EGG segments (3 preprandial, 3 postprandial, and 2 sleep segments) were selected from the total recording for spectral analysis, from which we obtained the dominant frequency (DF), instability coefficient of DF (ICDF), and low (LFR%), normal (NFR%), and high (HFR%) range power percentages of the total power. PD patients showed irregular slow waves, high HFR%, and high ICDF, whereas MSA patients showed regular slow waves and low ICDF. Although DF and NFR% increased after meal in controls, postprandial increases in DF and NFR% were less significant in both patient groups compared to the controls. The PD patients presented gastric dysrhythmias indicating gastric pacemaker disturbances. The MSA patients showed regular slow waves with low variability of the slow wave rhythm (low ICDF), which might have resulted from the involvement of gastric autonomic nerve function.

Muscarinic-dependent inhibition of gastric emptying and intestinal motility by fractions of Maytenus ilicifolia Mart ex. Reissek

Ethnopharmacological relevance Maytenus ilicifolia Mart. ex. Reissek (Celastraceae) is widely used in Brazilian folk medicine to treat gastric disturbances. Aim of the study This work intended to characterize the effects of Maytenus ilicifolia on gastrointestinal motility. Materials and methods Gastric emptying and intestinal transit were measured in the same animal. Mice received a semisolid marked with phenol red, half an hour after treatment with extracts. The amount of marker in the stomach and the distance reached in the intestine after 15 min were measured as index of gastrointestinal emptying and intestinal transit, respectively. Results Intraperitoneal administration of a flavonoid-rich extract potently reduced the gastric emptying (ED 50 = 89 mg/kg) and the intestinal transit (ED 50 = 31 mg/kg) of mice. Bio-guided purification of the flavonoid-rich extract by chemical partition with solvents of decreasing polarity yielded fraction insF with about 12–14 times higher activity than the initial flavonoid extract in both the gastric emptying and the intestinal transit. The inhibitory effects of the insF (9.7 mg/kg, i.p.) on gastric emptying and intestinal transit were reversed by co-administration of bethanechol (10 mg/kg, s.c.) but not by co-administration of metoclopramide (30 mg/kg, p.o.) indicating muscarinic but not dopaminergic interaction of the compounds of Maytenus. Chemical investigation of the insF fraction by HPLC–MS allowed the identification of 4 free flavonoids (catechin, epicatechin, quercetin and kaempferol), 29 flavonol glycosides and 8 tannins. The flavonol glycosides ranged from 1 to 4 monosaccharide units, having mainly quercetin and kaempferol as aglycone moieties, and the tannins were composed by catechin/epicatechin and/or afzelechin/epiafzelechin. Conclusions Overall, the results indicate that the components of Maytenus ilicifolia have a potential use in the treatment of gastrointestinal motility disturbances such as diarrhea.

Relationship between clinical features and gastric emptying disturbances in diabetes mellitus

Gastric emptying (GE) may be delayed or rapid in diabetes mellitus. We sought to ascertain differences in risk factors or associated features (i.e. diabetic 'phenotype') among patients with diabetes who have rapid, slow or normal GE. From a database of patients in whom gastrointestinal transit was assessed by scintigraphy, we compared the diabetic phenotype in diabetic patients with rapid, slow and normal GE. Of 129 patients, 55 (42%) had normal, 46 (36%) had delayed and 28 (22%) patients had rapid GE. In each GE category, there was an approximately equal number of type 1 and type 2 diabetes. In multivariable analyses, significant weight loss (OR, 2.81; 95% CI, 1.09-7.23) and neuropathy (OR, 3.60; 95% CI, 1.007-12.89) were the risk factors for delayed and rapid GE, respectively. Insulin therapy (OR, 0.08; 95% CI, 0.01-0.53) was associated with a lower risk of rapid compared to normal GE. However, other manifestations or characteristics of the diabetes 'phenotype' (i.e. type and duration of diabetes, glycosylated haemoglobin levels, and extraintestinal complications) were not useful for discriminating normal from delayed or rapid GE. At a specificity of 60%, clinical features were 73% sensitive for discriminating between normal and delayed GE and 80% sensitive for discriminating normal from rapid GE. Diabetes is associated with slow and rapid GE. Because the diabetic phenotype is of limited utility for identifying disordered GE, GE should be assessed in patients with diabetes and gastrointestinal symptoms.

Prulifloxacin: Clinical Studies of A Broad-Spectrum Quinolone Agent

Prulifloxacin, the lipophilic prodrug of ulifloxacin, is a new oral fluoroquinolone with a broad spectrum of in vitro activity against various Gram-positive and Gram-negative microorganisms. Currently, it is the most potent in vitro fluoroquinolone against Escherichia coli and Pseudomonas aeruginosa, and also has the lowest potential of inducing the emergence of resistant strains for these bacteria. It exhibits good penetration in target tissues and fluids, and possesses a long half-life, thus allowing for once-daily administration. Prulifloxacin has been successfully tested in Phase III randomized, controlled trials including patients with acute exacerbations of chronic bronchitis, uncomplicated and complicated urinary tract infections, and chronic bacterial prostatitis. Results are awaited from recently completed and ongoing Phase III randomized, placebo-controlled studies testing prulifloxacin for the treatment of traveler's diarrhea. Prulifloxacin has an acceptable toxicity profile, comparable to that of other fluoroquinolones, with gastric disturbances, diarrhea, nausea and skin rash of mild-to-moderate severity being the most frequent adverse events. Additional research is needed to further elucidate the promising role of prulifloxacin in the treatment of infections sustained by multidrug-resistant pathogens and to consolidate the wide spectrum of activity from a clinical standpoint.