Antiulcer Activity Research Articles

Synthesis, Docking Analysis, and Assessment of Chalcones for Antibacterial and Anthelmintic Activities

Background: Chalcones have been demonstrated to contain numerous therapeutic qualities in recent years, such as antibacterial, antiviral, anti-ulcerative, antioxidant, antiinflammatory, antihyperglycemic, antimalarial, antitubercular, analgesic, antiplatelet, and anticancer activities. Objective: To explorethe synthesis, docking, and characteristics of chalcones as antibacterial and anthelmintic compounds. Methods: The chalcone derivatives (3a-3k) and (6l-6v) were synthesized via two selective different reactions, based on the Claisen-Schmidt reaction. All synthesized compounds were evaluated for their antibacterial activity using an in vitro cup-plate method, and their anthelmintic activity was assessed using an in vitro earthworm paralysis and death assay. To validate these findings, conducted molecular docking experiments between the dihydrofolate reductase receptor (PDB ID: 4LAE) and the synthesised compounds (3a-3k) and (6l-6v) to determine catalytic interactions. Results: Compound 6(n) exhibited the greatest efficacy in biological in vitro activity against S. aureus compared to all other compounds examined. Compound 6(o) exhibited substantial efficacy against P. posthuma and E. coli. Emphasizing these findings, the compounds 3(a), 3(g), 3(i), 6(n), and 6(o) demonstrated hydrogen bond interactions with certain amino acid residues of the receptor, including THR 122, ASN 18, ASN19, GLN 96, SER 50, and ALA 8, during molecular docking. Conclusion: The study results showed that the synthesised derivative (E)-1-(napthalen-2-yl)-3-(4- (trifluoromethoxy)phenyl)prop-2-en-1-one 6(n) had beneficial antibacterial properties against S. aureus, while derivative (E)-1-(Napthalen-2-yl)-3-(4-trifluoromethyl)phenyl)prop-2-en-1-one 6(o) exhibited antibacterial activity against E. coli and anthlelmintic activity against P. posthuma.

Evaluation of Antiulcer Activity of Hydroalcohol Extract of Peel of <i>Musa balbisiana</i> Fruits by a New Apparatus and Model

Background: Ulcers, a prevalent gastrointestinal disorder, impose significant health burdens worldwide. There are lots of market antiulcer drugs to treat the ulcer , but due to lots of their side effects and high cost, the utility of herbal medicines is increasing day by day. Traditional experimental in vivo approaches involve animal sacrifice, raising ethical concerns, while in vitro models do not show the antiulcer effect directly on the tissue. In response, our study developed a non-invasive model, eliminating the need for animal sacrifice while ensuring reliable results. Aim: This study explored the potential antiulcer properties of Musa balbisiana fruit peel hydroalcohol extract, utilising a novel apparatus and an animal crueltyfree model. Methods: Musa balbisiana fruit peel hydroalcohol extract 400 mg as a test drug and marketed Digene tablets as a standard were assessed using the developed model, and ulcer parameters were evaluated through innovative apparatus measurements. Results: In the blue index analysis, tissue treated with Ringer-Locke’s salt solution, Ringer-Locke’s salt solution + HCl, Ringer-Locke’s salt solution with Digene 400 mg + HCl, Ringer-Locke’s salt solution with M. balbisiana fruit peel hydroalcohol extract 400 mg + HCl showed the blue index of respective values of 52.95, 83.42, 64.48, and 65.51. Conclusion: The research results demonstrated promising antiulcer effects as compared to control and standard when blue indexes are measured, suggesting the potential therapeutic value of M. balbisiana fruit peel in ulcer management. Furthermore, the utilisation of a non-invasive model underscores its applicability in ethical research practices, fostering.

Evaluation of inhibitory potential of the flavonoid-rich fraction of Myrica esculenta Buch.-Ham. ex D. Don against DSS-induced colonic inflammation in mice

ObjectiveMyrica esculenta (family Myricaceae), a valuable plant species in China and India, has been traditionally used by many tribes and local communities to manage gut disorders. Scientific validation of its anti-ulcerative colitis activity was aimed. MethodsThe ethyl acetate fraction of Myrica esculenta (MeEa) was prepared and evaluated for its potency against DSS-induced ulcerative colitis (UC) in mice at 200 and 400 mg/kg BW oral dose. The effective dose of MeEa was determined through its effect on DSS-induced UC and was further analyzed through its effects on disease activity index (DAI), colon length, colon weight/length ratio, spleen weight, serum and colon tissue cytokine level, cell count and hemoglobin content. Further, the effect was determined through histopathology and FITC-dextran-induced membrane permeability assay. ResultsBetween the two doses, MeEa at 400 mg/kg BW was found to be the most effective dose in terms of reduced DAI scores, protected colon length from shortening, decreased colon weight/length ratio, reduced spleen weight, decreased pro-inflammatory cytokine level and stabilized the anti-inflammatory cytokine level in serum and colon tissue. MeEa 400 reduced cell counts and increased hemoglobin content and platelet count. MeEa 400 also prevented the colon by protecting epithelial cells and crypts. MeEa 400 provided significant protection from intestinal leakage and reduced FITC dextran level in serum. DiscussionMeEa 400 possesses significant anti-inflammatory potential and acts via attenuation of DSS-induced UC and inhibition of DAI scores. It reduces pro-inflammatory cytokines and stabilizes anti-inflammatory cytokine levels, reduces cell count, and protects epithelial tissue and crypts in the colon, as well as intestinal membrane leakage that occurred due to FITC-dextran administration in mice.

Murraya koenigii (Curry Tree): A review of its Phytochemistry, Ethnomedicinal uses, and Pharmacology with Respect to Molecular Mechanisms

Abstract: Medicinal plants have significant therapeutic value and are a gift to humanity in pursuing healthy living. The discovery of numerous rejuvenating compounds that can stop or reduce the pathology of many diseases will be a crucial advancement in the coming years. Synthetic compounds can cause health issues and side effects, necessitating the development of molecules derived from plants and other natural resources as viable substitutes for synthetic compounds. Several plant phytochemicals and extracts have been found to have significant effects on traditional medical therapy. Murraya koenigii (M. Koenigii) is a member of the Rutaceae family, well-known in the Ayurvedic system of medicine as a therapeutically important herb of Indian origin. M. Koenigii has been used in several ancient systems of medicine, including Siddha and Unani, as a multi-potential medicinal plant. Previous research has shown that this plant's bark, roots, and leaves are abundant sources of carbazole alkaloids, which have beneficial pharmacological and biological effects. These include antioxidant, antibacterial, antidiabetic, anti-inflammatory, antihypertensive, antifungal, antiprotozoal, hepatoprotective, antihypercholesterolemic, antiulcer, cytotoxic, antidiarrheal, phagocytic, neuroprotective, and antitumor activities. The key components of the M. koenigii plant and their pharmacological activities against various diseases using preclinical models are discussed in this review. Exhaustive studies on the molecular mechanism of action of M. koenigii are needed to validate the effectiveness of curry tree and their constituents as potent therapeutic agents. However, serious efforts are required to identify, isolate and evaluate the chemical components for nutritional and medicinal potentials.

Biological activity and characterization of leaf and seed lectins from Terminalia brownii: Insights into their analgesic and antiulcer properties

Terminalia brownii Fresen, an African medicinal plant, is known for its analgesic, antiulcer, and antimicrobial properties, with its leaves, bark, and fruits deeply ingrained in indigenous healing practices. Two lectins, TerBLL (from leaves) and TerBSL (from seeds) of Terminalia brownii Fresen, were purified using salting-out and affinity chromatography on a fetuin-agarose column. The purified lectins were then assessed for protein yield, hemagglutination activity, and physicochemical properties. Both TerBLL and TerBSL have subunits with molecular weights of 57.3 and 65.7 kDa, respectively. TerBLL remains stable at 60–80 °C and is activated by Mn+2, while TerBSL is activated by Zn+2. These lectins maintain consistent activity under acidic conditions, with TerBLL demonstrating heightened activity at extreme alkaline pH. TerBLL retained 50 % of its activity in 2–8M urea, in contrast to the 13 % of TerBSL. Investigation of the properties of TerBLL revealed that it had antinociceptive effects, reducing abdominal pain and prolonging latency time in the hotplate assay, potentially through μ-opioid receptor blockade akin to that of morphine. TerBLL exhibits antiulcer activity at doses of 0.25 and 1 mg/kg, reducing ulcer formation by up to 33 %, comparable to that of pantoprazole (80 mg/kg). The physiochemical attributes of TerBLL, in addition to its pain-relieving and gastroprotective effects, underscore its therapeutic promise, which is consistent with its traditional use.

A stimuli-responsive keratin functionalized PEI coated baicalin nano-hydrogels for modulated gastric ulcer therapy

Nano-hydrogel system conjugated with polymer like polyethylieneimine offers a significant attention in the field of healthcare owing to their significant pH-specific swelling behaviour in acidic medium. The focus of this research work was to fabricate a stable and non-toxic, keratin-PEI coated nano-hydrogel formulation exhibiting synergistic effect for gastric ulcer treatment. K-PEI-BL nano-hydrogel shows particle size ~500nm with polydispersity index 0.473 ± 0.04, zeta potential of 15.4 ± 6.06mV, entrapment efficiency of 91.94 ± 0.04% and in vitro controled release of 72.78 ± 0.52% for 24h in pH 1.2. Scanning electron miscroscopy (SEM), Transmission electron microscopy (TEM) images confirmed the morphological structure of double coated nano-hydrogel particle. Ex-vivo mucoadhesive study of keratin-PEI coated-BA-NH formulation at gastric ulcer site exhibited 21h and 15min as a residence time in comparison to uncoated BA-NH formulation. In-vivo analysis displayed improvenent in ulcer treatment compared to negative control group with 86.46% and 71.86% inhibition of ulcer in standard ranitidine and K-PEI-BL nano-hydrogel treatment groups, respectively. This research study concluded that K-PEI-BL nano-hydrogel formulation with 15mg/kg dose exhibited anti-ulcer actions by reducing the severity of gastric abrasions.

Sukralfat as a Therapy for Reducing Itching and Repairing the Skin Barrier: A Systematic Review

Sucralate is an aluminum salt from sucrose octasulfate that is known for its anti-ulcer activity, mucosal protection, and anti-mucositis potential. Recently, sucralfat has been used topically for the healing of various epithelial wounds, including ulcers, inflammatory dermatitis, mucositis, and burns. This systematic review aimed to evaluate the effectiveness of sucralfat as a topical therapy in reducing itching (pruritus) and improving the skin barrier. The analysis method used is Preferred Reporting Items for Systematic Review and Meta-Analysis (PRISMA). A literature search was conducted on studies from 2004 to 2024 using keywords such as "sucralfate", "pruritus", "dermatitis", and "skin barrier" on PubMed, ProQuest, Science Direct, and Scopus databases. Inclusion criteria include topic relevance, research design, human subjects, and United Kingdom-speaking studies. Of the 141 articles found, 7 articles met the inclusion criteria. These studies involved a total of 605 subjects from different countries and used clinical trial methods and randomized controlled trials. The results showed that topical sucralfat was effective in reducing itching and improving the skin barrier in various skin conditions such as diaper dermatitis, chronic ulcers, and postoperative wounds. Sukralfat shows great potential in wound healing and skin barrier repair through the mechanism of protective layer formation, increased expression of epidermal growth factors, and anti-inflammatory properties. This effect indirectly helps reduce pruritus which often occurs due to damage to the skin barrier. Topical succulthate is effective in reducing itching and repairing the skin barrier, making it a promising therapy for a variety of inflammatory and ulcerative skin conditions.

A Review on Pharmacological Activities of Acacia ferruginea Extracts

Acacia ferruginea are also known as White bark acacia. Herbal plants are potent in curing various ailments of ancient times as they have comparatively lesser side effects. The demands for natural drugs, mostly from plant sources, are increasing over the past few decades. Because of their several medicinal properties, Acacia species are used to treat a variety of diseases. One of the species Acacia ferruginea reported its anti-inflammatory, analgesic, anti-diabetic, antibacterial, anti-fungal, anti– haemorrhoidal, antiulcer, hepatoprotective, wound healing and anti-protozoal activities. This review focus on the detailed morphology, phytochemical composition and pharmacological properties of different parts of Acacia ferruginea.

A Review of Antiulcer Activity of Some Medicinal Plants

Peptic ulcer is a gastrointestinal disorder and with increased prevalence. Peptic ulcer is breaking of endothelial lining of stomach and exposing underlying tissues. Peptic ulcer occurs due to high secretion of acid and reduced defensive factors in stomach and duodenum. It is imbalance between aggressive and defensive factors. Non-steroidal anti-inflammatory drugs and Helicobacter pylori infection also increases the risk of peptic ulcer. Indiscriminate use of synthetic drugs leads to adverse effects and concomitant use of antibiotics potentiates drug-drug interaction thus search of drugs from natural sources especially herbs is need of hour. several herbal medicines have been evaluated for its antiulcer efficacy using several ulcer inducing models in laboratory animals. Present study aims at review of gastroprotective and ulcer healing potential medicinal herbs and compilation of data. This article is only restricted to antiulcer efficacy of the medicinal plants. This review presents information about the anti-ulcer efficacy of medicinal plants and various antiulcer models used to screen them. Keywords: Peptic ulcer, Gastric ulcer, Gastroprotective activity, Phyllanthus urinaria, Adiantum lunulatum, Ulcer healing activity

The Antiulcer and Hepatoprotective Effects of Euphorbia hirta Petroleum Ether, Chloroform and Ethanolic Extracts on Paracetamol-induced Ulcerated Wistar Rats

Background: Hepatic and gastric diseases are two of the most common ailments in people. Numerous researches have been conducted to evaluate the effectiveness of herbal remedies in the treatment of hepatitis and stomach ulcers. Objective: The study aimed to determine the antiulcer and hepatoprotective activities of Euphorbia hirta petroleum ether, chloroform and ethanolic extracts on paracetamol-induced ulcerated Wistar rats. Materials and Methods: Euphorbia hirta was collected from the area of Salem, Tamil Nadu, India. The air-dried whole plant was crushed, and 500 g of the powder and petroleum ether, chloroform and ethanol were used for continuous extraction by the Soxhlet device. Phytochemical analysis of the extract was done by conventional and GC-MS analysis. Nine sets of six male Wistar rats, each weighing between 150 and 200 g, were used in this study. The standard control group, Group I, received only 1% v/v tween 80. Group II, negative control, received saline (1 ml/kg p.o.). Group III animals were given silymarin (200 mg/kg p.o.) and paracetamol (2 g/kg), which served as the standard of care. Animals in groups IV, V, VI, VII, VIII, and IX received two separate doses (200 and 400 mg/kg) of petroleum ether, chloroform, and ethanolic extracts of Euphorbia hirta L. Liver tissue was taken for histological investigation and placed in a 10% formalin solution. The liquid supernatant of liver cells was used to measure antioxidant parameters, such as catalase, superoxide dismutase, and LPO. Results: Phytochemical and GC-MS examination confirmed Euphorbia hirta extracts to have different biologically active phytoconstituents, like alkaloids, carbohydrates, glycosides, phenolic, flavonoids, tannin, sterols and alkaloids. Euphorbia hirta has been found to significantly protect against paracetamolinduced ulcer and hepatotoxicity compared to the negative control. A significant (p < 0.001) reduction in SGPT, SGOT, ALP, DB and TB levels in the EEEH 400 mg/kg extract-treated group was observed compared to the paracetamol group. The PEEH extract exhibited no significant decrease in all biochemical parameters compared to the negative control. However, the standard drug showed a significant (p < 0.001) decrease when compared to the negative control. SGPT, ALP, and DB levels demonstrated a significant (p < 0.01) reduction with EEEH 200 mg/kg. The PEEH extract induced no significant decrease in all biochemical parameters compared to the negative control, and the chloroform extract of 200 mg/kg showed a less significant (p < 0.05 & p < 0.01) difference compared to the negative control. The histopathology study confirmed EEEH 200 mg/kg to show good hepatoprotective activity. Conclusion: The findings have demonstrated Euphorbia hirta ethanolic extract to have effective antiulcer capabilities, and a decrease in LPO activity along with an increase in SOD, CAT, and LPO content have been observed, thereby leading to reduced oxidative stress. The antioxidant activity of Euphorbia hirta extract as a free radical scavenger and the hepatoprotective effect of the ethanolic extract have been indicated by the results of liver enzymes, DB and TB, and histology of liver tissue. More research is needed to recommend Euphorbia hirta as an effective supplement to treat paracetamol-induced ulcers and hepatotoxicity.

Gastroprotective Effect of oenothein B: a Romising Macrocyclic Ellagitannin

A peptic ulcer disease is a significant gastrointestinal disorder with a high prevalence of 80% in developing countries and 40% in developed countries. Oenothein B, a macrocyclic ellagitannin, has emerged as a potential therapeutic agent for this condition. The aim of this study was to investigate the anti-ulcer activity of Oenothein B and elucidate the underlying mechanisms involved in its gastroprotective effects. The anti-ulcer activity of Oenothein B was assessed using various experimental models, including ulcers induced by indomethacin, HCl/ethanol, and pyloric ligation. Several parameters were evaluated, including the quantification of volume, pH, total gastric acidity secretion, as well as catalase and superoxide dismutase activity. The role of prostaglandins in mediating the effects of Oenothein B was also examined. The results demonstrated that Oenothein B exhibited significant anti-ulcer activity when administered intraduodenally at a dose of 15 mg/kg in an acute protocol of induced ulcers. This treatment resulted in a reduction in volume and total gastric acidity secretion. Moreover, oral administration of Oenothein B was found to increase catalase and superoxide dismutase activity in the gastric mucosa. These findings suggest that Oenothein B exerts its anti-ulcer effects by reducing gastric acid secretion and enhancing the activity of antioxidant enzymes. Additionally, the modulation of endogenous prostaglandin levels appears to play a role in mediating these effects. In conclusion, Oenothein B demonstrates promising anti-ulcer activity and may serve as a potential therapeutic option for the management of peptic ulcer disease. Further investigations are warranted to elucidate the detailed mechanisms of action and evaluate its efficacy and safety in clinical settings.

Qualitative and Quantitative Determination of Secondary Metabolites and Evaluation of Antiulcer Activity of Hydroalcoholic Extract of Buchanania lanzan Leaf Extract

Qualitative and Quantitative Determination of Secondary Metabolites and Evaluation of Antiulcer Activity of Hydroalcoholic Extract of Buchanania lanzan Leaf Extract

Preparation of Jam and Jelly using star fruit and assessment of biochemical and organoleptic properties of these value-added products

Making of jam and jelly is the common method of preserving fruit, the main factor being high concentration of sugar that helps in preservation. In Bangladesh, the star fruit (Averrhoa carambola L.) BARI Kamranga-1 is available from September through October and January through February. To obtain the health benefits (anti-inflammatory, analgesic, hypoglycemic, antimicrobial, hepato-protective and anti-ulcer activity) of star fruit throughout the year, jam and jelly products were developed using star fruit. Five jams and five jellies were prepared as value-added products using different ingredients with different combinations. Biochemical properties, chemical analysis, and organoleptic observations of star fruit jam and star fruit jelly were measured to determine the quality of the products and overall public acceptance. The overall acceptability of Jam 2 was the highest, and in case of jelly , Jelly 4 showed the highest score. Additional study is needed to understand better, how star fruit can be processed because there are so many local sorts and variants of the fruit. This will enable us to decide which kinds are most suitable for developing specific goods with the potential to enhance health. Int. J. Agril. Res. Innov. Tech. 14(1): 45-52, June 2024

Evaluation of antiulcer potential of tambulin and ombuin isolated from Zanthoxylum armatum

ObjectivesZanthoxulym armatum fruit is traditionally used as carminative, anthelmintic, stomachic, and to relieve gastritis. It is commonly found in Nepal, Uttarakhand, and the Himalayan region of India. Tribal peoples used this fruit for various purposes and also as a spice ingredient. The present study aims to investigate the antiulcer potential of the fruit extract, and its isolated compounds. Materials and methodsFruits were extracted with successive extraction methods with hexane, ethyl acetate, and butanol. All the fractions were evaluated for phytochemical investigations. Further, the ethyl acetate fraction, tambulin, and ombuin were tested for antiulcer activity induced by ethanol and pylorus ligation-induced methods. The IL-1β, TNF-α, and IL-6 cytokines were also studied followed by histopathology. ResultsIt has been demonstrated that the ethyl acetate fraction possesses a major class of secondary metabolites. No acute toxicity was observed, as all the organs (heart, kidney, lung, stomach, and liver) were found in normal range and no significant weight variation was found. The antiulcer activity was performed at two different doses of all samples. Tambulin possesses the most significant activity at the dose of 50 mg/kg. Ulcer index and percent ulcer inhibition of tambulin were found to be 2.8 ± 0.6 mm2 and 69.5 ± 0.18 % in pylorus –ligated model whereas 5.2 ± 0.7 mm2 and 70.2 ± 0.15 in the ethanol-induced model. Histopathology results also support the above-mentioned data. ConclusionTambulin, a flavonoidal compound isolated from fruits of Z. armatum was found to be useful in the management of ulcers. Ethylacetate extract and ombuin also possess dose-dependent activity.

A Comparative Analysis of Vaippu Indhuppu and Commercial Indhuppu (Rock Salt)

Siddha system is one of the traditional systems of medicine in which minerals are used in the preparation of various medicines. Indhuppu is one among the mineral, which is a good laxative and it is commonly used for its anti-ulcer activity in Siddha medicine. Siddhars like Bohar, Agathiyar have mentioned vaippu process (Synthetic method) for preparing raw drugs synthetically instead of natural. This study is aimed to compare the commercial indhuppu with the Vaippu Indhuppu (synthetic). Both the samples were analyzed by FTIR, XRD, and ICP-OES. The results show that comparatively have similar crystalline structure and functional groups. This study is the preliminary analytic study for further explorative study on the vaippuindhuppu.

Comparative Antimicrobial Activity and Bioactive Constituents of Oils from Rhizomes of Zingiber Officinale Roscoe Obtained by Different Extraction Methods

Ginger, known for its rich array of bioactive compounds, holds significant therapeutic potential due to its diverse medicinal properties. This study investigated the antimicrobial activity and bioactive principles present in ginger rhizome oils obtained using three different extraction methods viz: liquid-liquid extraction, cold maceration, and soxhlet extraction. The oils’ bioactive principles were identified by Gas Chromatography Mass Spectrometry (GC-MS) while their antimicrobial activity was determined by agar well diffusion technique. The GC-MS analysis revealed the presence of thirty compounds in each of the oils from liquid-liquid extraction and cold maceration, and fifty four compounds in the soxhlet-extracted oil. The most predominant compound in both liquid-liquid (31.13%) and cold maceration (16.99%) oils was oleic acid whereas the Soxhlet-extracted oil contained predominantly linoleic acid methyl ester (9.27%). Some bioactive compounds identified in these oils include δ-elemene, isoborneol, α-Bisabolol oxide, stearic acid, undecanone, palmitic acid, α-copaene, zingiberene, aromadendrene, farnesol, 2-methylhexane and farnesene which possess antioxidant, antibacterial, antifungal, antiviral, anti-inflammatory, anti-ulcer, anti-cancer, hypolipidemic, mosquito repellant, antimicrobial, and antidiabetic activities. Additionally, the oils exhibited promising antimicrobial potential against the test organisms with Staphylococcus aureus showing the least susceptibility to all the samples. Staphylococcus aureus and Candida albicans were completely resistant to the oil obtained by Soxhlet extraction at all tested concentrations. Meanwhile, Klebsiella pneumoniae (20 mm), Proteus vulgaris (18 mm), and Pseudomonas aeruginosa (17 mm), were most susceptible to the oil obtained by liquid-liquid extraction, cold maceration and soxhlet extraction, respectively. The study highlighted the significance of extraction methods on the chemical composition and antimicrobial activity of ginger rhizome oils, underscoring the importance of choosing appropriate extraction techniques to optimize the oils' therapeutic properties for specific medicinal applications.

Cilostazol protects against gastric ulcers by regulating PPAR-γ, HO-1, PECAM-1, pErk-1, NF-κB, Bcl-2, and cleaved caspase-3 protein expression.

Millions of individuals worldwide, across all age groups, suffer from the widespread health issue of gastric ulcers. In many experiments, cilostazol (Cls), a phosphodiesterase-3 inhibitor, was recently shown to have anti-ulcer activity. Notably, Cls increases the expression and transcriptional activity of PPAR-γ in vitro and in vivo. This study aimed to evaluate the protective effect of Cls against ethanol-induced gastric ulcers and clarify the possible underlying mechanisms with an emphasis on the role of PPAR-γ. Male albino rats were treated with ethanol to induce gastric ulcers, or they were pretreated with Cls, omeprazole (Omp), GW9662, or Cls + GW9662 for 14 consecutive days before receiving ethanol. Cls protects against ethanol-induced gastric ulcers. Cls treatment significantly reduced ethanol-induced upregulation of the pro-inflammatory markers (IL-1β, IL-6, TNF-α, and NF-κB), MDA (a marker of lipid peroxidation), and caspase-3 and cleaved caspase-3 (apoptotic markers). On the other hand, Cls treatment counteracted ethanol-induced downregulation of PPAR-γ, pErk-1, HO-1 and GSH (antioxidant markers), PECAM-1 and NO (healing markers), and Bcl-2 (antiapoptotic marker). However, when combined with GW9662, a potent antagonist of PPAR-γ, Cls loses its effects. In conclusion, these results suggest that PPAR-γ and pErk-1 are essential for Cls's protective effects against ethanol-induced gastric ulcers.

Protein and sugar contents, total antioxidant capacity, analgesic and antiulcer activities of quince fruit extract

Cydonia oblonga belongs to the Rosaceae family, known in Algeria as sfarjel. It is a good source of secondary metabolites with antidiabetic, antihemolytic and antiallergic effects. The present study was undertaken to estimate total proteins and sugar contents and in vitro antioxidant, analgesic, and gastroprotective activities of quince fruit ethanolic extract (QFEE). Proteins and sugar contents of QFEE were determined to be 0.06 ± 0.002 mg BSA E/ g of dry extract and 111.95±0.02 mg GE/g of dry extract, respectively. Using total antioxidant capacity (TAC), QFEE demonstrated a critical antioxidant activity with an IC50 value of 0.39±0.008 mg/ml. Oral administration of QFEE at 200 and 600 mg/kg doses to rats gave a dose-dependent gastroprotective effect in an ethanol model-induced ulcer, with protection percentages of 77.75 and 91.81 %, respectively. The same doses of extract had analgesic activities against acetic acidinduced abdominal contraction. According to these findings, quince extract is an essential source of antioxidant compounds that may have analgesic properties and shield the stomach from developing ulcers. Keywords: Cydonia oblonga Mill, Sugar content, protein content, Antioxidant activity, Analgesic, Ulcer

Protein and sugar contents, total antioxidant capacity, analgesic and antiulcer activities of quince fruit extract

Cydonia oblonga belongs to the Rosaceae family, known in Algeria as sfarjel. It is a good source of secondary metabolites with antidiabetic, antihemolytic, and antiallergic effects. The present study was undertaken to estimate total proteins and sugar contents and in vitro antioxidant, analgesic, and gastroprotective activities of quince fruit ethanolic extract (QFEE). Proteins and sugar contents of QFEE were determined to be 0.06 ± 0.002 mg BSA E/ g of dry extract and 111.95±0.02 mg GE/g of dry extract, respectively. Using total antioxidant capacity (TAC), QFEE demonstrated a critical antioxidant activity with an IC50 value of 0.39±0.008 mg/ml. Oral administration of QFEE at 200 and 600 mg/kg doses to rats gave a dose-dependent gastroprotective effect in an ethanol model-induced ulcer, with protection percentages of 77.75 and 91.81 %, respectively. The same doses of extract had analgesic activities against acetic acidinduced abdominal contraction. According to these findings, quince extract is an essential source of antioxidant compounds that may have analgesic properties and shield the stomach from developing ulcers. Keywords: Cydonia oblonga Mill, Sugar content, protein content, Antioxidant activity, Analgesic, Ulcer.

A Comprehensive Review of the Benzimidazole Scaffold as a Potential Nucleus for Anti-Ulcer Activity

Abstract: The benzimidazole scaffold is a promising nucleus for developing novel therapeutic agents for ulcer treatment. Its unique chemical structure provides desirable pharmacological properties, such as excellent bioavailability, metabolic stability, and low toxicity, making it an attractive candidate for ulcer treatment. Several benzimidazole derivatives have shown significant anti-ulcer activity in preclinical and clinical studies, acting through multiple pathways, including inhibition of gastric acid secretion, suppression of gastric inflammation, and promotion of mucosal protection. Some benzimidazole derivatives have also demonstrated anti-Helicobacter pylori activity, suggesting their potential for eradicating bacteria associated with ulcer formation. However, challenges such as poor solubility and limited selectivity remain. Various approaches, such as prodrug design and formulation optimization, have been explored to overcome these issues and improve the therapeutic profile of benzimidazole derivatives. Overall, the benzimidazole scaffold holds great promise as a nucleus for developing novel anti-ulcer agents. Further research and optimization efforts are needed to harness its full potential and translate it into effective treatments for ulcers. With continued advancements in medicinal chemistry and drug design, benzimidazole-based compounds may offer new therapeutic options for patients suffering from ulcers and related gastrointestinal disorders. Hence, this review highlights the knowledge about benzimidazole scaffold, the mechanism of ulcer formation, and various benzimidazole derivatives with anti-ulcer activity, which can be further studied in pre-clinical and clinical trials.