Comparison of acid reduction in antiulcer operations

Background: Three acid-reducing operations have recently been described for the laparoscopic treatment of peptic ulcer disease. These consist of a posterior truncal vagotomy combined with either (1) an anterior seromyotomy (SERO), (2) an anterior highly selective vagotomy (AHSV), or (3) a linear stapled lesser curvature excision (STAP). The purpose of this study was to investigate the physiologic effects of these procedures in terms of basal and maximal acid outputs. Methods: Fifty New Zealand rabbits were prospectively randomized into five open laparotomy groups (n= 10): a control group without vagal manipulation (CON), a bilateral truncal vagotomy with pyloromyotomy group (VP), a SERO group, an AHSV group, and a STAP group. All animals underwent placement of a gastrostomy tube for subsequent gastric secretory analysis. On postoperative day 6, basal acid outputs (BAO) and maximal acid outputs (MAO) following IV pentagastrin stimulation (30 μg/kg/h) were measured. Results were compared statistically using the ANOVA method. Results: Pentagastrin stimulation was associated with a significant increase in MAO in the CON group (p < 0.05 vs BAO); however, this response was effectively blunted in all the experimental groups. There were no differences in BAO or MAO between any of the vagotomized groups (SERO, HSV, STAP, VP). Conclusions: We conclude that the three acid-reducing procedures modified for laparoscopy are equally efficacious in reducing gastric acid secretion and that they compare favorably with VP. To our knowledge, this is the first report comparing basal and stimulated gastric acid secretion between these new acid-reducing techniques. Received: 27 March 1996/Accepted: 17 July 1996     

银耳多糖、银耳孢子多糖及黑木耳多糖的抗溃疡作用

银耳多糖、银耳孢子多糖及黑木耳多糖以每天70mg/kg灌胃2d,均明显抑制大鼠应激型溃疡的形成;以每天165mg/kg灌胃124,能促进醋酸型胃溃疡的愈合。对胃酸分泌和胃蛋白酶活性无明显影响。本研究表明,这三种多糖均有抗溃疡作用。     

ANTIULCER ACTIVITY OF AQUEOUS STEMBARK EXTRACT OF HYMENOCARDIA ACIDA TUL (EUPHORBIACEAE)

Abstract

The antiulcer activity of an aqueous extract of Hymenocardia acida was studied in rats. Ulcers were induced by indomethacin and serotonin, or by cold restraint stress. The extract was found to exhibit significant (P <0.05) antiulcer activity in all the models studied. Phytochemical studies revealed the presence of glycosides, saponins and tannins. The LD₅₀ was found to be 483 mg/kg body weight. The extract had moderate antibacterial effects.     

2-烷基取代喹诺酮的合成及生物活性

采用两种方法合成了15个2-烷基-4(1H)-喹诺酮生物碱(IVa～g,Va～h),其中5个化合物是从吴茱萸中分离得到的(包括2个新化合物IVa,Vc),IVa,d,f;Vb,c,d,f,h等8个化合物为首次合成。并对所合成的化合物进行了初步药理试验,结果表明具有一定的扩张血管和抗溃疡的作用。IVb还有细胞毒作用。     

Antiulcer activity of ethanol leaf extract of Cassia fistula

The ethanol leaf extract (ELE) of Cassia fistula Linn. (Caesalpinaceae) was evaluated for antiulcer activity against pylorus ligation-induced gastric ulcer. Ranitidine (30?mg/kg b.w.) and ELE at doses of 250, 500, and 750?mg/kg b.w. were administered orally in different groups of rats (n = 6), 1?h prior to pyloric ligation. Four hours after pyloric ligation, the gastric juice was collected for evaluation of various parameters. The antiulcer activity of ELE was evidenced by the significant attenuation of gastric volume, pH, free acidity, and total acidity in the gastric juice of pyloric-ligated rats in a dose-dependent manner, and this protective effect could be due to strengthening of the mucosal defense mechanism. ELE pre-treatment significantly attenuated the fall in status of sialic acid and fucose accompanied by an increase in hexose, hexosamine, total non-amino polysaccharide, total carbohydrate, and C:P ratio in the gastric juice of pylorus-ligated rats, and this effect could be due to protection of the mucosal barrier system. ELE pre-treatment significantly prevented the increase in LPO and SOD accompanied by a fall in CAT, in the gastric juice of pyloric-ligated rats. This protective ability of ELE against pylorus ligation-induced gastric ulcer could be attributed to its free radical scavenging and antioxidant properties. Higher doses of ELE (750?mg/kg b.w.) produced maximum antiulcer activity comparable to ranitidine treatment. In essence, the antiulcer activity of ELE could be attributed to (i) a decrease in gastric acid secretion, (ii) protection of the mucosal barrier and restoration of mucosal secretions, (iii) inhibition of free radical generation or prevention of lipid peroxidation, and (iv) free radical scavenging or antioxidant properties.     

Gastroprotective and antidepressant effects of a new zinc(II)-curcumin complex in rodent models of gastric ulcer and depression induced by stresses

Curcumin, a yellow pigment found in the rhizome of Curcuma loga, has been used to treat a variety of digestive and neuropsychiatric disorders since ancient times in China. Curcumin can chelate various metal ions to form metallocomplexes of curcumin which show greater effects than curcumin alone. This study investigated the antiulcerogenic and antidepressant effects of a Zn(II)-curcumin complex on cold-restraint stress (CRS)-induced gastric ulcers in rats, and on the forced swimming test (FST), tail suspension test (TST) and 5-hydroxy-l-tryptophan (5-HTP)-induced head twitch test in mice. CRS disrupted the rat mucosal barrier and induced gastric ulcers by decreasing the activities of the antioxidant enzymes, and increasing H⁺-K⁺-ATPase activity and malondialdehyde (MDA) level. Pretreatment with Zn(II)-curcumin (12, 24, and 48 mg/kg) dose-dependently reversed these trends, reduced gastric lesions and H⁺-K⁺-ATPase activity, and increased antioxidant activities compared with control groups. Zn(II)-curcumin significantly increased HSP70 mRNA, and attenuated increased iNOS mRNA in the mucosa. Zn(II)-curcumin (17, 34, and 68 mg/kg) also significantly decreased immobility time in the FST and TST, and enhanced 5-HTP-induced head twitches in mice. These results demonstrate that the Zn(II)-curcumin complex showed significant gastroprotective and antidepressant effects compared with curcumin alone via a synergistic effect between curcumin and zinc.     

Pharmacokinetics and Excretion Studies on CDRI-85/92, an Antiulcer Proton Pump Inhibitor

CDRI 85/92 is an antiulcer pharmacophore and a proton pump inhibitor, which is in an advanced stage of preclinical trials. In view of its importance, pharmacokinetic and excretion were studied in Sprague Dawley rats after administering 20 mg/kg oral and intravenous doses. The compound was detectable in the serum samples as early as 5 min post-oral administration. The compound was eliminated slowly from serum with an elimination half-life of 2.1 h. Following the 20 mg/kg oral dose, maximum serum concentration (C(max)) was found to be 469.28 ± 45.52 ng/ml after 1.0 h. Based on AUC values, the absolute bioavailability of the CDRI 85/92 was 70.5% after oral administration. It was found to be excreted in urine (~15% of the dose) in intravenously treated (bile duct cannulated as well as noncannulated) rats, whereas bile and feces depicted insignificant levels of the compound.     

Evaluation of antiulcer activity of the main phenolic acids found in Brazilian Green Propolis

Aim of the study

In a previous study, our group described the gastric protective effect of the hydroalcoholic extract of Brazilian green propolis. The main compounds found in Brazilian green propolis include phenolic acids, such as: caffeic, ferulic, p-coumaric and cinnamic acids. This study was therefore carried out to evaluate the antiulcerogenic property of the main phenolic acids found in Brazilian Green Propolis.

Material and methods

The anti-ulcer assays were performed using the following protocols: nonsteroidal-antiinflammatory drug (NSAID)-induced ulcer, ethanol-induced ulcer, and stress-induced ulcer. The effects of the phenolic acids on gastric content volume, pH and total acidity, using the pylorus ligated model, were also evaluated.

Results

It was observed that treatment using doses of 50 and 250 mg/kg of caffeic, ferulic, p-coumaric and cinnamic acids and positive controls (omeprazol or cimetidine) significantly diminished the lesion index, the total area of the lesion and the percentage of lesion in comparison with the negative control groups. In addition, the percentage of ulcer inhibition was significantly higher in the groups treated with the different phenolic acids, cimetidine or omeprazol, in all the protocols used, compared with the negative control groups. In the model to determine gastric secretion, using ligated pylorus, treatment with phenolic acids and cimetidine reduced the volume of gastric juice and total acidity and significantly increased the gastric pH (p < 0.05), compared with the control group, with the exception of the group treated with 50 mg/kg of p-coumaric acid, in which no significant difference was observed, compared with the control. In relation to the acute toxicity, none sign of toxicity was observed when phenolic acids, used in this study, were administered for rats in dose of 2000 mg/kg.

Conclusions

In conclusion, the results of this study show that caffeic, ferulic, p-coumaric and cinnamic acids display antiulcer activity.     

Hancornia speciosa: indications of gastroprotective, healing and anti-Helicobacter pylori actions

Ethnopharmacological relevance

Mangaba (Hancornia speciosa Gomez) is a medicinal plant frequently cited in ethnopharmacological inventories of the central region of Brazil against gastrointestinal disorders such as diarrhoea, ulcer, gastritis and stomachache.

Aim of the study

The hydroalcoholic extract (HE) and infusion (BI) of Hancornia speciosa bark were investigated for their ability to prevent and heal rodent gastric ulcer.

Materials and methods

The preventive and healing action of both preparations of Hancornia speciosa were evaluated in experimental models in rodents that simulated this disease in human gastric mucosa.

Results

BI did not exert gastroprotective effect, in contrast to HE (500 mg/kg, p.o.) that decreased (p < 0.05) the severity of gastric damage induced by HCl/ethanol (52%), indomethacin/bethanechol (51%), stress (52%) or pylorus ligature experiments (54%). HE increased (p < 0.05) the pH and decreased acid output of gastric juice. This extract promoted increase of mucus amount (3.62 mg/wt. tissue vs. 5.81 mg/wt. tissue), healing action (67%) and displayed anti-Helicobacter pylori effect.

Conclusions

The antiulcer action of Hancornia speciosa resulted in increase of gastric mucus formation and antioxidant properties of polymeric proanthocyanidins present in the bark composition of this medicinal plant.