Antiulcer activities

The bilberry (Vaccinium myrtillus) has traditionally been used to treat ulcers, because bilberry might stimulate the production of the stomach mucus and 

In addition, silybin might interact with the free radical intermediates produced during the metabolic activation of CCI4 and methylhydrazine. These effects suggest that silybin is potentially protective against harmful free radical-mediated toxic damage [62]. 

The comparative pharmacokinetics of silipide (IdB 1016, a silybin-phosphatidylcholine complex) and silybin flavanolignan of flavonoids were 

---

The discovery of the antiulcer activity of H2 antihistamine antagonists has revolutionized the treatment of that disease. A benzimidazole. Omeprazole (55), inhibits gastric secretion and subsequent ulcer formation by a quite different mechanism. Studies at the molecular level suggest that this compound inhibits K /H dependent ATPase and consequently shuts down the proton pumping action of this enzyme system. 

Yanagisawa, T., Wakabayashi, S., Tomiyama, T., Yasunami, M., and Takase, K. (1998). Synthesis and antiulcer activities of sodium alkylazulene sulfonates. Chem. Pharm. Bull. 36 641. 

The antimicrobial activity of Bi(III) against the bacterium Helicobacter pylori appears to be important for its antiulcer activity (458). This organism may be involved in other conditions such as cancer. The mechanism of antimicrobial activity may involve interference in Fe(III) or Zn(II) biochemical pathways. Bismuth(III) is not known to bind to DNA. Attempts to synthesize new Bi(III) complexes with activity against H. pylori include those of Keppler et al. (459), who have found that Bi(III)-tropolonato complexes such as 98 are highly active... 

Antisecretory activity, 2 Antitussive, 11 Antiulcer activity, 2 Apazone, 475... 

Ethyl l-oxo-6-piperidino-l//-pyrimido[l,2-a]quinoline-2-carboxylate showed potent in vitro anticoccidial activity (92AAC2338). anhydro-1,3-Diethyl-2-hydroxy-4-oxo-4//-pyrimido[2,l-a]isoquinolinium hydroxyde (318) exhibits nonselective Ar and A2-adenosine receptor activities (84JMC1364) and proved to be an inhibitor of cyclic-AMP phosphodiesterase (81JMC1284). 8,9,10,ll-Tetrahydro-3-(l//-5-tetrazolyl)-4//-pyrimido[2,l-a]iso-quinolin-4-one exhibits antiulcer activity (84USP4457932). 

ACTIVE HERBAL PRODUCTS WITH ANTIULCER ACTIVITY... 

Flavonoids are a group of about 4000 naturally occurring compounds with a wide range of biological effects, including antiulcer activity. They are important constituents of the human diet (a daily diet contains approximately 1 g of flavonoids per day) and are also found in several medicinal plants used in folk medicine around the world. Several mechanisms have been proposed to explain the gastroprotective effect of flavonoids ... 

Plant materials often contain triterpenoid saponin in considerable amounts. With regard to plants with antiulcer activity, licorice root contains about 2 to 12% of glycyrrhizic acid and the seeds of the horse chestnut up to 13% of aescin. Several plants containing high amounts have been shown to possess antiulcer activity in several experimental ulcer models (Table 64.2). 

Plants Containing Saponins with Antiulcer Activity... 

Tannins are used in medicine primarily because of their astringent properties, which are due to the fact that they react with the proteins of the layers of tissue with which they come into contact. Tannins are known to tan the outermost layer of the mucosa and to render it less permeable and more resistant to chemical and mechanical injury or irritation however, the correlation between the molecular structures of tannins and the astringent/antiulcer activity is not known. 

Several plants with antiulcer active which contain tannins have been reported (Table 64.3). 

A crude extract of Linderae umbellatae exhibited antipeptic and antiulcerogenic activity, and these effects were considered ascribable to the presence of tannins or related compounds. Nine condensed tannins (monomers, dimers, trimers, and tetramers) have been isolated and their antipeptic and antiulcer activity confirmed experimentally (pylorus ligated in rats and stress-induced gastric lesions in mice). 

Licorice, the root and rhizome of different varieties of Glycyrrhiza glabra (Leguminosae), has been extensively used in medicine for its antiulcer activity. The principal constituent of licorice is glycyr-rhizinic acid, a triterpenoid saponin. This chemical class is known to offer protection against ulcers. 

---