Journal of Pharmacy And Bioallied Sciences

: 2011  |  Volume : 3  |  Issue : 3  |  Page : 361--367

Role of phenolic compounds in peptic ulcer: An overview

Sabiha Sumbul1, Mohd. Aftab Ahmad1, Mohd. Asif1, Mohd. Akhtar2,  
1 Department of Ilmul Advia (Pharmacology), Faculty of Unani Medicine, Hamdard University, New Delhi, India
2 Department of Pharmacology, Faculty of Pharmacy, Hamdard University, New Delhi, India

Correspondence Address:
Mohd. Akhtar
Department of Pharmacology, Faculty of Pharmacy, Hamdard University, New Delhi


Peptic ulcer is the most common gastrointestinal tract (GIT) disorder in clinical practice, which affects approximately 5-10% of the people during their life. The use of herbal drugs for the prevention and treatment of various diseases is constantly developing throughout the world. This is particularly true with regard to phenolic compounds that probably constitute the largest group of plants secondary metabolites. Phenolic compounds have attracted special attention due to their health-promoting characteristics. In the past ten years a large number of the studies have been carried out on the effects of phenolic compounds on human health. Many studies have been carried out that strongly support the contribution of polyphenols to the prevention of cardiovascular diseases, cancer, osteoporosis, neurodegenerative diseases, and diabetes mellitus, and suggest a role in the prevention of peptic ulcer. Polyphenols display a number of pharmacological properties in the GIT area, acting as antisecretory, cytoprotective, and antioxidant agents. The antioxidant properties of phenolic compounds have been widely studied, but it has become clear that their mechanisms of action go beyond the modulation of oxidative stress. Various polyphenolic compounds have been reported for their anti-ulcerogenic activity with a good level of gastric protection. Besides their action as gastroprotective, these phenolic compounds can be an alternative for the treatment of gastric ulcers. Therefore, considering the important role of polyphenolic compounds in the prevention or reduction of gastric lesions induced by different ulcerogenic agents, in this review, we have summarized the literature on some potent antiulcer plants, such as, Oroxylum indicum, Zingiber officinale, Olea europaea L., Foeniculum vulgare, Alchornea glandulosa, Tephrosia purpurea, and so on, containing phenolic compounds, namely, baicalein, cinnamic acid, oleuropein, rutin, quercetin, and tephrosin, respectively, as active constituents.

How to cite this article:
Sumbul S, Ahmad M, Mohd. Asif, Mohd. Akhtar. Role of phenolic compounds in peptic ulcer: An overview.J Pharm Bioall Sci 2011;3:361-367

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Sumbul S, Ahmad M, Mohd. Asif, Mohd. Akhtar. Role of phenolic compounds in peptic ulcer: An overview. J Pharm Bioall Sci [serial online] 2011 [cited 2020 Jun 3 ];3:361-367
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Peptic ulcer disease (PUD), encompassing gastric and duodenal ulcers, is the most prevalent gastrointestinal disorder. [1] For over a century, peptic ulcer disease has been one of the leading causes of gastrointestinal surgery, with high morbidity and mortality rates. It affects a lot of people in the world, and hence, some researchers consider this disease a new plague of the twenty-first century. [2] The pathophysiology of the PUD involves an imbalance between offensive (acid, pepsin, and Helicobacter pylori) and defensive factors (mucin, prostaglandin, bicarbonate, nitric oxide, and growth factors). [3] There have been two main approaches for treating peptic ulcer. The first deals with reducing the production of gastric acid and the second with re-enforcing gastric mucosal protection. [1],[3] Modern medicines have their own limitations, especially against ulcers with a complex pathology, indicating a need of substitute medication from an alternative system of medicine. A number of drugs including proton pump inhibitors, prostaglandins analogs, histamine receptor antagonists, and cytoprotective agents are available for the treatment of peptic ulcers. However, most of these drugs produce several adverse reactions including toxicities and may even alter biochemical mechanisms of the body upon chronic usage. [4] The clinical evaluation of these drugs showed the development of tolerance and incidence of relapses and side effects that make their efficacy arguable. Many of these drugs do not fulfill all the requirements and have side effects. [5] Emerging evidence indicates that proton pump I therapy, particularly with long-term and/or high-dose administration, is associated with several potential gastrointestinal adverse effects, including, risks of Clostridium difficile colitis, other enteric infections, small bowel bacterial overgrowth, and possibly spontaneous bacterial peritonitis, and other non-gastrointestinal tract (GIT) side effects, such as, community-acquired pneumonia, hip fracture, vitamin B 12 deficiency, and food allergies, all of which have received much attention recently. [6]

Hence, herbal medicines are generally used in such cases when drugs are to be used for chronic periods. [7] In recent years, abundant work has been carried out on herbal medicine to clarify their potential efficacy in peptic ulcer prevention or management. Drugs of herbal origin reduce the offensive factors and have proved to be safe, clinically effective, relatively less expensive, globally competitive, and with better patient tolerance. [8] These drugs may be slow in action, but mostly augment the defensive factors and are reliable and safe. Therefore, there has been the rationale for the development of new antiulcer drugs that offer better protection and decreased relapse. Clinical research has confirmed the efficacy of several plants for the treatment of gastroduodenal diseases. [9] Use of medicinal plants is in continuous expansion all over the world, for the prevention and treatment of different pathologies, and natural products are recovering space and importance in the pharmaceutical industry as inspiring sources of potentially new bioactive molecules. [10] The medicinal properties of many plants are attributed mainly to the presence of flavonoids, coumarins, alkaloids, terpenoids, tannins, phenolic acids, and antioxidant micronutrients, for example, Copper (Cu), Manganese (Mn), and Zinc (Zn). [11] The therapeutic effects of many traditional medicines may be related in many cases to the presence of phenolic compounds. [12]

Phenolic compounds occur as secondary metabolites and are widely distributed in plants from the roots to the seeds. [13] These are widespread in nature and range from simple structures with one aromatic ring to highly complex polymeric substances such as tannins and lignins. [14] Polyphenols are classified as flavonoids and non-flavonoids, according to their chemical composition. The flavonoid type polyphenols include anthocyanins, catechins, flavanones, flavones, flavonols, and isoflavones. Non-flavonoid type polyphenols are phenolic acids and hydroxycinnamic acids. In terms of chemical classification, polyphenols are generally divided into hydrolyzable tannins and phenylpropanoids, such as lignins, flavonoids, and condensed tannins. The phenolic compounds of pharmaceutical interest are simple phenolic compounds (catechol, eugenol, vanillin, caffeic acid, ferulic acid, and salicin), flavones (apigenin, tangeritin, tangerine, and luteolin), isoflavones (genistein, daidzein, and glycitein), isoflavonoids (rotenone and genistin), flavonols (quercetin, gingerol, kaempferol, myricetin, and rutin), flavanones (hesperetin, naringenin, and eriodictyol), anthocyanidins (cyanidin, delphinidin, malvidin, and petundin), anthocyanins (haematien), coumarins (umbelliferone, aesculetin, and scopoletin), tannins (gallic acids, ellagitannins, catechins, gallitannins, and catechins), lignans (silymarin, matairesinol, pinoresinol, lariciresinol, and secoisolariciresinol), and lignins. [13],[14]

Research on flavonoids and other polyphenols, their antioxidant properties, and their effects in disease prevention, truly began after 1995. [15] At present, reports on the potential health benefits of polyphenols have increased enormously. [16] Polyphenolic compounds play a vital role in the prevention of cardiovascular illnesses, certain kinds of cancer, diabetes, brain dysfunction or other conditions associated with the aging process. [15],[17] They display a broad spectrum of physiological activities. For example, a wide variety of pharmacological activities have been reported for these substances, including antiviral, [18] anti-allergic, [19] antiplatelet, [20] anti-estrogenic, anticancerogenic, anti-inflammatory, antiproliferative, antiangiogenic, and antioxidant properties, and their ingestion typically produces very little or no toxicity. [21] Polyphenolic compounds have also been reported to have a beneficial role in gastric ulcers, as it has been suggested that phenols stimulate PGE 2 formation. [22] Polyphenols clearly improves the status of different oxidative stress biomarkers. [23] The biological mechanisms of these possible effects have been attributed to their antioxidant properties through several possible mechanisms, such as their ability to scavenge free radicals, break radical chain reactions, directly reducing peroxides, and stimulating the antioxidative defense enzyme activities. [24]

Flavonoids have been reported to act in the gastrointestinal tract, having antispasmodic, [25] anti-secretory, antidiarrheal, [26] antiulcer, and antioxidant properties. [27],[28],[29] Flavonoids are among the cytoprotective materials for which anti-ulcerogenic efficacy has been extensively confirmed. [30],[31],[32] They protect the gastric mucosa against a variety of ulcerogenic agents via several mechanisms of action, mainly free-radical scavenging and antioxidant properties, increased mucus production, antisecretory action, and inhibition of the Helicobacter pylori growth. [31] Tannins prevent ulcer development due to their protein precipitating and vasoconstricting effects. [33] Their astringent action can help to precipitate microproteins on the ulcer site, thereby, forming an impervious layer over the lining, which hinders induced gastric ulcer in rats, as evidenced by the gut secretions, and protects the underlying mucosa from reduction in the ulcer scores. [34],[35],[36]

 Experimentally studied plants possessing phenolic compounds

Considering the important role of polyphenolic compounds in the prevention or treatment of gastric or duodenal lesions, in this review, we have presented the literature on plants containing polyphenolic compounds with significant anti-ulcerogenic activity. Hence, an attempt has been made to confirm that polyphenolic compounds have a therapeutic potential for the effective treatment of peptic ulcers with a view to aid further research, to prepare ideal antiulcer drugs. The antiulcer activities of such plants validated by pharmacological studies are summarized below:

Oroxylum indicum (Broken bones plant, Indian calosanthes, Indian trumpet)

Fifty percent alcohol extract of the root bark of Oroxylum indicum (Bignoniaceae) and its different fractions, namely, petroleum ether, chloroform, ethyl acetate, and n-butanol, were studied against ethanol and pyloric ligation-induced gastric mucosal damage in animals. Out of all these fractions, petroleum ether (96%) and n-butanol (99%) fractions showed maximum inhibition of gastric lesions against ethanol-induced gastric mucosal damage. Treatment with both active fractions showed significant antioxidant activity as was evident from the reduction in the extent of lipid peroxidation that was measured in terms of malondialdehyde, along with a significant rise in the superoxide dismutase, catalase, and reduced glutathione levels, when compared with the control group. In pylorus-ligated animals, active fractions of the drug showed significant reduction in the ulcer index, in total acidity, total acid output, pepsin activity and pepsin output, along with a significant rise in the total carbohydrate-to-protein ratio (reflecting mucin activity) when compared to the control group. The mechanism of its antiulcer activity could be attributed to a decrease in gastric acid secretion and antioxidant activities, leading to gastric cytoprotection. Baicalein was found to be a major flavonoid present both in petroleum ether and n-butanol hydrosylate. Hence, this activity could also be linked to the presence of baicalein in the root bark of the plant. [37]

The gastroprotective activities of hexane and acetone extracts of O. indicum were investigated for crude extracts and the isolates against aspirin, ethanol, cold restrain and pylorus ligation induced lesions in Wistar rats. Acetone extract displayed better gastroprotective activity than hexane extract. Chemical investigation of hexane and acetone extracts from the stem bark of O. indicum resulted in the isolation and characterization of two flavonoid glycosides along with seven known compounds as constituents of O. indicum. In conclusion the antiulcer properties of the extract may be attributed to the flavonoids content that are present in it. [38]

Erythrina indica Lam. (Indian coral tree)

A study was carried out to investigate the antiulcer activity of the methanol extract of Erythrina indica (Fabaceae) leaves in pylorus ligated and indomethacin-induced ulceration in albino rats. The methanolic extract of E. indica leaves showed significant antiulcer properties in both the ulcer models. The extract showed a significant decrease in the gastric volume, total acidity and free acidity. The preliminary phytochemical analysis of the E. indica extract showed the presence of alkaloids, flavonoids, triterpenoids, carbohydrates, and glycosides. Flavonoids like flavone glycoside and isoflavonoid (Indicanine B and Indicanine C) have been isolated from its root bark. Flavonoids are among the cytoprotective materials and these active compounds stimulate mucus, bicarbonate, and prostaglandin secretion, and counteract with the deteriorating effects of reactive oxidants in the gastrointestinal lumen. Therefore, the antiulcer activity of E. indica may be attributed to its flavonoids content. [39]

Zingiber officinale (Ginger)

The ulcer-preventive property of the aqueous extract of Zingiber officinale (Zingiberceae) rhizome was evaluated by swim/ethanol stress-induced ulcers in rats. Increased H + , K + -ATPase activity, and thiobarbituric acid reactive substances (TBARS) were observed in ulcer-induced rats, while drug-fed rats showed normalized levels, and the drug also normalized the depleted/amplified anti-oxidant enzymes in the 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 drug treatment. The study demonstrated that the aqueous extract of ginger was able to protect the gastric mucosa from stress-induced mucosal lesions and inhibited gastric acid secretion, probably by blocking H+, K+-ATPase action, inhibiting growth of Helicobacter pylori, and offering antioxidant protection against oxidative stress-induced gastric damage. Compositional analysis of the extract revealed the presence of cinnamic (50%) and gallic (46%) phenolic acids. Cinnamic acid appeared to contribute toward better H + , K + -ATPase, and Helicobacter pylori inhibitory activity, while gallic acid contributed significantly to anti-oxidant activity. [40]

The gastroprotective effect of 50% ethanolic extract of Z. officinale rhizome was assessed in rats in the ethanol and acetic acid-induced ulcer models, at different doses. The extract showed a dose-dependent inhibition of the ulcer index in ethanol and acetic acid-induced ulcers. It prevented the oxidative damage of the gastric mucosa by blocking lipid peroxidation and by a significant decrease in superoxide dismutase and increase in catalase activity. The significant gastroprotective activity of Z. officinale might be due to the gastric defense factors, and gingerols might be the main constituents responsible for this activity. [41]

Avicennia officinalis (Indian mangrove)

The gastroprotective effect of cold and hot water extracts on Avicennia officinalis (Avicenniaceae) leaves was analyzed in a model of NSAID (non-steroidal anti inflammatory drug)-induced ulcer in rats. Pretreatment with the extract significantly decreased the ulcerated area, volume, and acidity of the gastric juice in rats. The ulcer healing capacity of A. officinalis was due to several mechanisms, such as coating the wound, forming complexes with the proteins in the cell wall, chelating free radicals and reactive oxygen species, stimulating the contraction of the wound, and increasing the formation of new capillaries and fibroblasts. The gastroprotective effects of A. officinalis may be related to the presence of polyphenolic compounds in a fair quantity, detected by phytochemical analysis. The major active principles of the plant are flavonoids, which are characterized by their polyphenolic nature, with cytoprotective properties. [42]

Ficus arnottiana Miq. (Crow fig)

The antiulcer activity of the Ficus arnottiana (Moraceae) leaf methanolic extract was studied in Wistar rats in an ethanol-induced model, for ten days. The results of the study showed that the F. arnottiana leaf methanolic extract possessed a gastroprotective activity, as evidenced by its significant inhibition in the formation of ulcers induced by ethanol. The protective effect was confirmed by histological examination showing prevention of mucosal lesions and submucosal edema. As flavonoids were identified in the methanolic extract, the antiulcer activity of this extract was probably due to the antioxidant activity of the flavonoids present in the extract. Moreover, flavonoids have already been reported for their anti-ulcerogenic activity and gastric protection. [43]

Foeniculum vulgare(Fennel, sweet fennel)

The anti-ulcerogenic and antioxidant effects of the aqueous extract of Foeniculum vulgare (Umbelliferae) were examined on ethanol-induced gastric lesions in rats. The pretreatment with F. vulgare significantly reduced ethanol-induced gastric damage. F. vulgare decreased the lipid peroxidation and increased the non-enzymatic antioxidant. Antioxidant properties may be one of the possible mechanisms by which F. vulgare decreased the ethanol-induced gastric lesions. The preliminary phytochemical screening of F. vulgare showed the presence of volatile oil, flavonoids (rutin, quercetin, and kaempferol glycosides), coumarins, sterols, and sugars. Flavonoids, sterols, tannins, and coumarins of some plants are also known to possess antiulcer activity. Therefore, the presence of flavonoid content and other bioactive compounds in F. vulgare may be associated with the ulcer preventing action. [44]

Olea europaea Linn. (Olive)

The anti-ulcer activity of the Olea europaea (Oleaceae) was investigated in rats by inducing gastric mucosal injuries by a corrosive concentration of ethanol. The olive leaf extract caused a significant attenuation of the gastric damage induced by ethanol, suggesting a respectable gastroprotective activity. This activity could be related to the ability of its constituents to scavenge reactive oxygen species, which initiate lipid peroxidation. The actual anti-ulcer potential is probably related to its ability to maintain the integrity of the cell membrane, by its anti-lipid peroxidative activity, and to protect the gastric mucosa in this manner against oxidative damage, and by its ability to strengthen the mucosal barrier, the first line of defense against exogenous and endogenous ulcerogenic agents. Seven phenolic compounds were identified and quantified in this extract. The major constituent of the olive leaf extract was oleuropein (19.8%), a well-known antioxidant. The other identified components were caffeic acid, luteolin-7-O-glucoside, apigenine-7-O-glucoside, and quercetin. These constituents of the olive leaf possess antioxidative properties, which were experimentally confirmed in several studies. [45]

Alchornea glandulosa (Canela-raposa)

The methanolic extract obtained from the leaves of Alchornea glandulosa (Euphorbiaceae) was investigated for anti-ulcer activity in HCl/ethanol and NSAID-induced ulcer models in rats. A. glandulosa significantly decreased the severity of the gastric lesions and also induced antisecretory action via local and systemic routes, with and a significant decrease in the total gastric acid content. The phytochemical investigation of A. glandulosa led to the isolation of phenolic compounds like myricetin-3-O-alpha-L-rhamnopyranoside, quercetin-3-O-alpha-L-arabinopyranoside, quercetin-3-O-beta-D-galactopyranoside, quercetin, amentoflavone, methyl gallate, gallic acid, and pterogynidine. Plants containing substances like quercetin and gallic acid were effective in preventing ulcers, mainly because of their antioxidant properties. Kahraman et al. revealed that quercetin inhibited the development of mucosal gastric ulcers induced by the administration of ethanol. [46] These compounds probably contribute to the anti-ulcerogenic effects of the polar extract of A. glandulosa leaves. [47]

Tephrosia purpurea (Fish poison, wild indigo)

The antiulcer activity of the aqueous extract of the roots of Tephrosia purpurea (Fabaceae) was studied in rats, in which gastric ulcers were induced by oral administration of ethanol or 0.6 M HCl, indomethacin and by pyloric ligation, and duodenal ulcers were induced by the oral administration of cysteamine HCl. The antiulcer activity was assessed by determining and comparing the ulcer index in the test drug group with that of the vehicle control group. The results suggested that T. purpurea possessed a significant antiulcer property, which could be due to the cytoprotective action of the drug. The protective effect of T. purpurea against cysteamine-induced duodenal ulcers could be due to the strengthening of the duodenal mucosa or by other mechanisms like increased gastric and duodenal alkaline secretion or by increased luminal prostaglandin levels. It was likely that flavonoidal compounds, tephrosin, pongaglabol, and semiglabrin present in the T. purpurea could be involved in this action, as flavonoids have been reported to possess significant antiulcer activity [48] in various experimental models of gastric and duodenal ulceration. [49]

Byrsonima crassa Niedenzu (Murici)

The anti-ulcerogenic effect of hydromethanolic, methanolic, and chloroformic extracts obtained from the leaves of Byrsonima crassa (Malpighiaceae) was evaluated in mice. The oral administration of all the extracts significantly reduced the formation of lesions associated with HCl/ethanol administration. Phytochemical evaluation showed that B. crassa contained quercetin-3-O-beta-d-galactopyranoside, quercetin-3-O-alpha-l-arabinopyranoside, biflavonoid amentoflavone, (+)-catechin, and (−)-epicatechin. As, catechins and flavonoids are secondary metabolites found in the active extracts of B. crassa, they may be involved in the scavenging of the reactive oxygen species on the surface of gastric mucosa, thus protecting cells from gastric injury. [50]

Bidens pilosa var.( Hairy beggarticks, shepherd's needles, butterfly needles, cobbler's pegs)

The ethanolic extract of Bidens. pilosa (Compositae) was studied for antiulcer activity in indomethacin- and pylorus-ligated rats. B. pilosa extract decreased the gastric juice volume, acid secretion, as well as pepsin secretion in pylorus-ligated rats. The extract showed antiulcer activity against indomethacin induced gastric lesions. The results indicated that the ethanolic extract of B. pilosa exerted a cytoprotective effect, in addition to its gastric antisecretory activity that could be due to the presence of flavonoids, of which quercetin was identified by high performance liquid chromatography (HPLC). [51]

The effects of B. pilosa were investigated on different experimental gastric mucosal lesions induced by HCl/EtOH, NSAIDs, and cold-restraint stress, by comparing these results with those of rutin and anti-ulcerogenic drugs (cimetidine or sucralfate). The results indicated that the drug protected against acute gastric mucosal lesions. B. pilosa protected the tissue against peroxidative stress and reduced thiobarbituric acid reactive substances (TBARS), the index of lipid peroxidation in gastric mucosa. The key components in B. pilosa are seven flavonoids, including rutin and six caffeic acid derivatives, as identified by the HPLC chromatogram and these components have antioxidant activities. B. pilosa exerts gastroprotective activity, possibly by suppressing the oxidative stress in the gastric mucosa. [52]

Cissus quadrangularis (Veld grape, winged treebine, bone setter)

The methanolic extract from the Cissus quadrangularis (Vitaceae) stem was studied for anti-ulcer activity on aspirin-induced ulcerogenesis in pyloric-ligated model in rats. The results suggested that C. quadrangularis promoted ulcer protection by the decrease in ulcer index, gastric secretions, and increase in the glycoprotein level, gastric mucin content, and non-protein sulfhydryl (NPSH) concentration. C. quadrangularis extract showed a significant increase in NPSH concentration, which might attribute to its direct cytoprotection and antioxidant activities. The antiulcer activity might be attributed to the presence of biological compounds such as tannins, triterpenoids, glycosides, saponins, sitosterol, and amino acids in the extract. These constitutents present in the C. quadrangularis extract might have the ability to protect against ulceration. [53]

The anti-ulcerogenic property of aqueous ethanolic extracts of the aerial parts of C. quadrangularis was evaluated in various ulcer models in animals. The drug was found to increase the defensive factors by virtue of its ulcer score, carbohydrate protein ratio, and decrease the aggressive factors like free acidity and pepsin, apart from other biochemical parameters. The extract significantly reduced the formation of gastric and duodenal lesions by virtue of its cyto-protective and mucin-productive activities. [54]

Bauhinia racemosa (Mountain ebony, bidi leaf tree)

The antiulcer effect of the dried fruit powder of Bauhinia racemosa (Casaelpinaceae) was studied in paracetamol-induced gastric ulcers in Wistar albino rats. The results indicated that there was a decrease in the percent of incidence of ulcers and ulcer index in a dose-dependent manner when compared with the control group. Francesca and Angelo (2000) reported the use of plant flavonoids from B. racemosa as antiulcer remedies. [55] Therefore, the gastroprotective effect could be due to the presence of flavonoids present in the plant, which reduced the gastric secretion and peptic activity and prevented the formation of gastric ulcers. [56]

The anti-ulcerogenic activity of the methanolic extract of B. racemosa (flower buds) was investigated in aspirin-induced gastric ulcers in rats. The extract showed significant gastroprotection by inhibiting the ulcer index. [57]

Trachyspermum ammi (Bishop's weed)

The ethanolic extract of the Trachyspermum ammi (Umbelliferae) fruit was investigated for antiulcer activity by using pylorus ligation, indomethacin, ethanol, and cold restraint stress-induced ulcer model in rats. The results suggested that the extract showed significant protection (P < 0.001) by reducing the ulcerative lesions when compared with the control group in all models. The study demonstrated that the extract exhibited antiulcer activity, probably as a result of antisecretory and cytoprotective action. T. ammi significantly increased mucus secretion as observed from the increase in mucopolysaccharides like hexose, hexosamine, and fucose. Hence, increase in the synthesis of mucus may be one of the important contributing factors for the ulcer protective role of T. ammi fruit. The preliminary phytochemical screening of T. ammi revealed the presence of carbohydrate, glycoside, proteins, volatile oils, and tannins. Thus, the presence of tannins in T. ammi could be responsible for its antiulcer activity. [58]

Nigella sativa Linn. (Black cumin, black seed)

The effect of the alcoholic extract of Nigella sativa (Ranunculaceae) was investigated in rats, to evaluate the antiulcer activity, by using two models, that is, pyloric ligation and aspirin-induced gastric ulcer. The parameters taken to assess the antiulcer activity were volume of gastric secretion, free acidity, total acidity, and ulcer index. The results indicated that the alcoholic extract significantly (P < 0.001) decreased the volume of gastric acid secretion, free acidity, total acidity, and ulcer index with respect to control. The preliminary phytochemical studies revealed the presence of flavonoids in alcoholic extract of N. sativa, so the possible mechanism of anti ulcer action of N. sativa may be due to its flavonoids content. [59]

Cucumis sativum L. (Cucumber)

The antioxidant and anti-ulcer effect of the methanolic extract of Cucumis sativum L. (Cucurbutaceae) seeds was studied by using pyloric ligation and water immersion stress-induced ulcer models in rats. The anti-oxidant activity was measured by the DPPH method, and the drug showed significant free radical scavenging activity. The results suggested that the methanolic extract of C. sativum seeds possessed significant antiulcer potential, which could be due to its antioxidant activity. Preliminary phytochemical screening of the methanolic extract showed the presence of tannins, proteins, amino acids, triterpenoids, phytosterols, and carbohydrates. Therefore, the antiulcer activity of C. sativum could be attributed to its tannin content. [60]

Wilbrandia ebracteata (Taiuia)

Leaf fractions obtained of the methanolic extract from Wilbrandia ebracteata (Cucurbitaceae) were investigated for anti-ulcerogenic effects in ethanol and indomethacin-induced gastric ulcer assays in mice. The W. ebracteata leaves provided a significant antiulcer effect against gastric ulcers in mice. The data suggested that flavonoids were active anti-ulcerogenic compounds found in the leaves of W. ebracteata. Seven flavonoids, 3',4', 5, 6, 7, 8-hexahydroxyflavonol, orientin, isoorientin, vitexin, isovitexin, luteolin, and 6-methoxi-luteolin were isolated from the leaves of W. ebracteata by chromatographic methods and identified by their spectral data. The ability of scavenging free radicals was evaluated by the DPPH reduction assay. The anti-ulcerogenic effect may be related to the flavonoids that may be involved in the scavenging of the reactive oxygen species on the surface of the gastric mucosa. [61]

The hydromethanol extract from the leaves of W. ebracteata was investigated for anti-ulcerogenic effects in ethanol and indomethacin-induced gastric ulcer damage in mice. Oral administration of the leaf extract significantly reduced 73.3% of the total area of the lesion in ethanol-induced gastric damage, but was inactive in the indomethacin-induced gastric damage test. Leaves of W. ebracteata reacted positively for steroids, flavonols, flavanones, saponins, tannins, and xanthones. The results indicated that this extract could increase the gastric defensive factors, probably due to the presence of flavonoids. [62]

Apium graveolens (Wild celery, garden celery)

The ethanolic extract of Apium graveolens L. (Apiaceae/Umbelliferae) was evaluated for antigastric ulcer activity using various experimental gastric ulcer models in rats. Ulcers were induced by indomethacin, cytodestructive agents (80% ethanol, 0.2 M NaOH, and 25% NaCl), cold restraint stress, and pylorus ligation. In addition to gastric wall mucus, non-protein sulfhydryl and malondialdehyde were also estimated in gastric tissues after 80% ethanol treatment. Celery extract showed the ability to significantly replenish the ethanol-induced depleted levels of gastric wall mucus and gastric mucosal non-protein sulfhydryl. The gastric mucosal malondialdehyde level was also significantly lowered in extract pretreated rats. The results suggested that A. graveolens extract significantly protected gastric mucosa in all experimentally induced gastric lesions. Phytochemical screening showed the presence of various chemical constituents such as flavonoids, tannins, volatile oils, alkaloids, sterols, and/or triterpenes. Hence, the antiulcer activity of this plant is probably due to the antioxidant potential of flavonoids and tannins. [63]


Polyphenolic compounds represent a highly diverse class of secondary metabolites distributed widely in the plant kingdom. Recently, they are a subject of considerable scientific and therapeutic interest mainly due to their antioxidant properties and related health promoting benefits. The evidences strongly support the contribution of polyphenols in the prevention of cardiovascular diseases, cancers, osteoporosis, neurodegenerative diseases, and diabetes mellitus. They exhibit several biological activities in the gastroprotective area, including anti-secretory, cytoprotective, and antioxidant actions. The studied plants possessing polyphenolic compounds have shown gastroprotective and antiulcer properties. These compounds protect the gastrointestinal mucosa from lesions produced by various experimental ulcer models, against different necrotic agents. Moreover, these can be utilized as an alternative or an additive agent to the current therapy. Therefore, these compounds can have a more effective and less toxic therapeutic potential for the treatment of peptic ulcers.


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