Antiulcer Activity Research Articles

Diverse Pharmacological Potential of Pyridazine Analogs against Various Diseases.

Pyridazinone analogs possess diverse types of pharmacological activities, such as anticancer, antimicrobial, anticonvulsant, analgesic, anti-inflammatory, antioxidant, antihypertensive, antisecretory, antiulcer, and other useful pharmacological activities. They also possess cyclooxygenase (COX) inhibitors, dipeptidyl peptidase inhibitors, phosphodiesterase inhibitors, glutamate transporter activators, adenosine receptor antagonists, serotonin receptors antagonists, lipooxygenase, cholinesterase, vasodilator, and anesthetics. Pyridazine rings are the essential structure for some marketed drugs, such as pimobendan, levosimendan as a cardiotonic drug, and emorfozan as an analgesic and anti-inflammatory (Non-steroidal anti-inflammatory drug) agent. So, researchers all over the world have paid attention to synthesizing various pyridazinone compounds mainly due to the ease of design and synthesis of different analogs and variables in the pharmacological responses. This review article focuses on the pharmacological activities of different pyridazine analogs.

Aloe vera gel confers therapeutic effect by reducing pyroptosis in ethanol-induced gastric ulcer rat model: Role of NLRP3/GSDMD signaling pathway

BackgroundGastric ulcer (GU) is a common gastrointestinal tract illness. Aloe vera has anti-inflammatory, antioxidant, and healing characteristics. This research sought to explore the therapeutic impact of Aloe vera gel on ethanol-provoked GU in rats and to elucidate the underlying mechanisms involved.MethodsAn ethanol-induced GU rat model was constructed using forty male Wistar rats distributed at random into four groups: control, ulcer, pantoprazole, and Aloe vera. Gross evaluation of the stomach, ulcer index (UI), inhibition index, and gastric pH estimation were analyzed. Gastric malondialdehyde (MDA) and reduced glutathione (GSH) were determined using the spectrophotometric method, and serum gastrin level was measured by an enzyme-linked immunosorbent assay. Gastric nucleotide-binding domain, leucine-rich repeat, and pyrin domain PYD containing protein 3 (NLRP3) and gasdermin D (GSDMD) mRNA expression levels were estimated by quantitative real-time PCR. Finally, the histopathological examination of the glandular part of stomach tissue was done.ResultsThe ulcer group revealed a significant increase in MDA, gastrin, NLRP3, and GSDMD and a decrease in gastric pH and GSH compared to the control group. Gross investigations of the ulcer group revealed a hemorrhagic lesion in the stomach and an increase in UI. Also, histopathological results for this group showed severe epithelial loss, haemorrhage, inflammatory cell infiltration, and blood vessel congestion. However, Aloe vera treatment improved the gross, biochemical, molecular, and histopathological alterations induced by ethanol when compared to the ulcer group.ConclusionsAloe vera exerted antiulcer activities through modulation of oxidant/antioxidant status, anti-secretory properties, and mitigation of pyroptosis.

An Unexplored Drug Mamajjaka (Enicostemma Littorale Blume)-A Drug Review

Traditional medicinal system of India consist variety of natural herbs which are playing significant role in human health. Among them Enicostemma littorale Blume is one the herbaceous plant of the Gentianaceae family. The biter nature plant help in curing fever, act as a laxative, useful in skin disorders, rheumatism, snake bite, abdominal disorders, diabetes, obesity and in many more diseases. The plant used in folklore since long time in many diseases. The plant constituents having antimicrobial, antioxidant, antiulcer, anti-inflammatory, hypolipidemic, hypoglycaemic, hepatoprotective and antitumor activity. This review consists of detail description along with its literature review, ethnobotanical uses, phytochemical, pharmacological properties, and toxicological study of Enicostemma littorale Blume. The methodology adopted in this review is using Ayurvedic literature and modern scientific research-based publications including journal and periodicals. This review provide base for future research work in different aspect in the field of drug research.

Evaluation of the Anti-ulcer Activity of Curcumin and Linseed Oil in an NSAID-induced Gastric Ulcer Model in Rats

Evaluation of the Anti-ulcer Activity of Curcumin and Linseed Oil in an NSAID-induced Gastric Ulcer Model in Rats

Synthesis, modification and biological activity of 2,3-indoles of Glycyrrhetinic acid

The synthesis of 2,3-indoles of Glycyrrhetinic acid (GLA) and its methyl ester was carried out by the Fischer reaction. Reductive transformations of GLA methyl ester 2,3-indole 3a were carried out to obtain 11-deoxo- and 9,12-diene analogs. N-methylation of 2,3-indole 3a gave N-methyl-indole-11-oxo-18β-olean-12-en-30-oic acid. The antiulcer and anti-inflammatory activity of 2,3-indole 3a was studied in rats and mice. It was found, compound 3a exhibied a pronounced antiulcer activity in the indomethacin model of ulcers in rats and anti-inflammatory activity in the carrageenan model of acute edoema in mice, at a dose of 50 mg/kg. This is the first report of anti-ulcer and anti-inflammatory activities of 2,3-indolo-GLA derivatives.

Molecular docking, characterization, ADME/toxicity prediction, and anti-ulcer activity of new quercetin derivatives on indomethacin-induced gastric ulcer in mice

Gastric ulcer (GU) is a serious upper gastrointestinal tract disorder that affects people worldwide. The drugs now available for GU treatment have a high rate of relapses and drug interactions, as well as mild to severe side effects. As a result, new natural therapeutic medications for treating GU with fewer negative side effects are desperately needed. Because of quercetin's (QCT) diverse pharmacological effects and unique structural features, we decided to semi-synthesize new QCT derivatives and test them for antiulcer activity. Docking assays were performed on the synthesized compounds to determine their affinity for TLR-4/MD-2, MyD88/TIR, and NF-κB domains, an important inflammatory pathway involved in GU development and progression. Mice were given oral famotidine (40 mg/kg/day), QCT, QCT pentamethyl (QPM), or QCT pentaacetyl (QPA) (50 mg/kg/day) for 5 days before GU induction by a single intraperitoneal injection of indomethacin (INDO; 18 mg/kg). QPM and QPA have a stronger binding affinity for TLR-4/MD-2, MyD88/TIR and NF-κB domains than QCT. In comparison, they demonstrated the greatest reduction in ulcer score and index, gastric MDA and nitric oxide (NO) contents, MyD88 and NF-κB expressions, and gastric TLR-4 immunostaining. They also enhanced the levels of GSH, CAT, COX-1, and COX-2 in the gastric mucosa, as well as HO-1 and Nrf2 expression, with histological regression in gastric mucosal lesions, with QPA-treated mice demonstrating the best GU healing. QPA is safe against all of the target organs and adverse pathways studied, with good ADME properties. However, further in vitro experiments are necessary to demonstrate the inhibitory effects of QPM and QPA on the protein targets of interest. In addition, preclinical research on its bioavailability and safety is essential before clinical management can be undertaken. Overall, the new QPA derivative could one day serve as the basis for a new class of potential antiulcer drugs.

Antinociceptive and anti-ulcerogenic effect of hydroethanolic stem bark extract of Ricinodendron heudelotii (Baill.) Pierre ex. Heckel (Euphorbiaceae): Involvement of the opioidergic pathway and attenuation of oxidative stress

Background and aimApproximately 80% of the population in developing countries is affected by gastric ulcers Gastric ulcers are associated with pain,and there is an urgent need for drugs that can manage both conditions. Ricinodendron heudelotii (Baill.) Pierre ex. Heckel has long been regarded used in managing gastric ulcers and pain in African Traditional Medicine. In the present study, the antinociceptive and anti-ulcer activity of Ricinodendron heudelotii (Baill.) Pierre ex. Heckel hydroethanolic stem bark extract (RHE) was evaluated. Experimental procedureThe antinociceptive effect of RHE was tested in ICR mice using the hot plate test, the glutamate-induced nociceptive test, and the formalin test. Gastric ulcers were induced in healthy male adult albino rats in acidified alcohol-induced ulcer (AAIU) and indomethacin-induced ulcer (IIU) models. After ulcer induction, the rats were treated with either RHE (30, 100, or 300 mg/kg, p.o.) or 10 mg/kg omeprazole. The stomachs of the sacrificed animals were removed for further analysis. Results and conclusionRHE (30, 100, and 300 mg/kg) exhibited an anti-nociceptive effect in the hot plate, formalin and glutamate tests. The opioid receptor antagonist, naloxone, reversed the analgesic effect, indicating that the extract may be acting via the opioidergic pathway. But compared to the model group in both AAIU and IIU, oral administration of RHE decreased ulcer index, raised pH levels, increased tissue levels of total antioxidant capacity, catalase, total thiols, and glutathione, and kept gastric histoarchitecture intact. RHE exhibited anti-nociceptive effects, possibly via the opioidergic pathway and anti-ulcer activity via reduction of oxidative stress.

Evaluation of antioxidant and antacid activities of crude methanol and peptide extracts of Momordica charantia, Luffa cylindrica, and Jatropha curcas

Background: There are many uses for therapeutic-based compounds in the food and pharmaceutical industries, and natural products are one of the best sources of these compounds. Momordica charantia (Family Cucurbitaceae), Luffa cylindrica (Family Cucurbitaceae), and Jatropha curcas (Family Euphorbiacece) have been documented for various medicinal applications. Objective: This study aimed to assess the anti-ulcer and antioxidant properties of M. charantia, L. cylindrica and J. curcas extracts and their crude peptide. Methods: The plant samples were collected, identified, and authenticated at Forest Herbarium, Ibadan, Nigeria. The samples were allowed to air dry, were pulverized, and then were extracted using methanol. The peptidic principles were extracted using Dichloromethane: Chloroform: Water mixtures in the ratio 1:1:0.5 and concentrated in vacuo. The peptidic extracts were screened for peptide and peptide-related compounds by TLC bioautography using Ninhydrin, Pyridine, and modified G-250 reagents. The extracts were assessed for antioxidant (2,2-diphenyl-1-picrylhydrazyl, DPPH), free radical scavenging activity, total phenolic content (TPC), total flavonoid content (TFC), and antiulcer activity. The antiulcer activity was evaluated using the artificial gastric acid neutralizing activity. Results: It was observed that all M. charantia, L. cylindrica, and J. curcas and their crude peptide extracts contain phenols and flavonoids. The TPC values of the crude methanol extracts were greater than those of the corresponding peptide extracts for all three species. The TFC of M. charantia and L. cylindrica crude methanol extracts were lower than their crude peptide extracts, while the TFC of J. curcas crude methanol extract was higher than the TFC value for its crude peptide extract. The DPPH radical scavenging activity of the crude extracts and crude peptide extract of M. charantia, L. cylindrica, and J. curcas was low when compared to the standard (Gallic acid). The M. charantia crude peptide extract had the lowest IC50 value of 282.4 μg/mL, indicating that it had better scavenging efficacy compared to the other extracts that were examined, while the lowest IC50 value was obtained from J. curcas methanol extracts (411.7 μg/mL). The result from this study shows that M. charantia, L. cylindrica, and J. curcas and their crude peptide possess artificial gastric acid neutralizing activity, which implies that they can be used as antacids to reduce the acidity of the stomach. Hence, the plants were evaluated for their efficacy in managing peptic ulcers by their ability to reduce the acidity of the stomach by raising the pH of the stomach. This is the first report on the antacid potential of Momordica charantia, Luffa cylindrica, and Jatropha curcas in literature. Conclusions: The results from this study support the ethnomedicinal claims that M. charantia, L. cylindrica, and J. curcas can be used in the management of peptic ulcers, and these plants could serve as sources of lead compounds to produce natural antiulcer drugs. There were traces of the presence of linear peptides and cyclic peptides (cysteine-rich cyclotides). Keywords: Antiulcer, Antioxidant, Peptides, Momordica charantia, Luffa cylindrica, Jatropha curcas

Evaluation of Anti Ulcer Activity of Methanolic Leaf Extract of Jacquemontia Caerulea Against Experimentally Induced Ulcers in Wistar Rats

Objective: To evaluate the anti-ulcerogenic effect of Jacquemontia caerulea Leaf Methanolic Extract (JCLME) against aspirin, ethanol, cold stress induced and pylorus ligation induced gastric ulcers in Wistar rats. Methods: The methanolic extract of fresh leaves of the plant, Jacquemontia caerulea (Family Convolvulaceae) was prepared and assessed for anti-ulcer effect with different doses and the standard drugs (Risperidone and Amitriptyline respectively) by using aspirin, ethanol, cold stress induced and pylorus ligation methods. Results: JCLME was assessed and compared statistically with the anti-ulcer effects in the control rats which was treated with saline (NaCl, 0.9%). It was found that JCLME at doses of 200 and 400 mg/kg reduced the ulcer index significantly when compared to control group (p< 0.05). It was found that JCLME significantly reduced the free acidity, total acidity and ulcer index (p<0.05) and increased the gastric content when compared with the control group. Hence, the current study shows that the JCLME has potent anti-ulcer, cytoprotective and antisecretory property thereby making it a great ulcero-protective agent.

A Comprehensive Review on the Traditional Uses, Phytochemical Compositions and Pharmacological Properties of an Ethnomedicinal Herb, Paederia foetida

Background:: Paederia foetida L. (Family – Rubiaceae) is a common herb found available in the temperate and tropical Asia. The ethnomedicinal applications of this plant are widely elaborated In Chinese Traditional Medicine, Ayurveda, and other ancient scriptures throughout the world. Different ethnic groups use this plant in the treatment of alimentary and digestive disorders, bone related diseases like rheumatoid arthritis, bone fractures as well as in the ailments of diabetes, coughs, asthma, itches, wounds, body ache, toothache, cancer etc. Objectives:: This comprehensive review aims to provide an insightful understanding of traditional uses, chemical composition, and pharmacological properties of P. foetida (from 1976 up to 2023), which may provide a foundation for further study and for the proper utilization of P. foetida resources. Methods:: Literature survey was conducted using known databases and the relevant keywords. Results:: P. foetida has been widely used in Chinese traditional medicine (CTM) for the treatment of dyspepsia, jaundice, pains, diarrhea and others. Several ethnic groups throughout the world used this plant to cure common health complaints namely, abdominal pain, gastritis, dysentery, diarrhoea, constipation, joint pain, etc. A total of 24 bioactive phytocompounds, such as asperuloside, paederosidic acid, sitosterols, stigmasterol, campesterol, ellagic acid, iridoids, ursolic acid, epifriedelinol, and others are reported to possess antiulcer, antidiarrheal, antihyperglycemic, antioxidant, antitussive, anthelmintic, and hepatoprotective activities. Conclusion:: The present review not only summarizes the alternative approaches using this herb by ethnic people for treating various disorders, but also focuses on the latest scientific investigations to elucidate different bioactivities of this plant, thereby facilitating the understanding of its correlation with contemporary pharmacology. However, till date, very few studies elucidated the biological properties of these phytochemicals that were isolated exclusively from this particular plant. Moreover, the correlation between phytocompounds from P. foetida and its pharmacological activities aiming towards clinical drug development is still lacking. Finally, further research should be oriented towards determining the optimal dosage and toxicological limits, and thereby providing guidance for clinical applications.

Design of floating formulations and antiulcer activity of Desmostachya bipinnata

The study aims to design and optimize the floating formulations of the aqueous extract of Desmostachya bipinnata (ADB) to treat peptic ulcers. The trial concentrations of HPMC E50, HPMC K4M, and Carbopol 940 were used as factors, and floating lag time, total floating time, and % drug release at 12 h were used as responses. The formulation underwent evaluation for different parameters: aspirin-induced ulcers in rats assessed the antiulcer activity, and X-ray studies in rabbits evaluated the gastroretentive nature. The optimized formulation has shown a floating lag time of 32 s and floated in the gastric medium for more than 9 h with a maximum drug release of 93% at the end of 12 h by following the Korsmeyer-Peppas drug release mechanism. The optimized formulation has good flow properties. The FT-IR, DSC, and XRD studies show ADB and excipients didn't show any incompatibility. The formulation has shown significant antiulcer activity against aspirin-induced ulcers in rats, with an ulcer index of 3.38 ± 0.24 and inhibition of 76.67 ± 0.56%. The in vivo X-ray imaging proved the gastric retention of the formulations for more than 8 h. The results of the formulations demonstrate the floating ability and sustained drug release of the tablet responsible for treating peptic ulcers to show a localized effect in the gastric region and to maintain the ROS levels.Graphical

Apium extract alleviates indomethacin-induced gastric ulcers in rats via modulating the VEGF and IK-κB/NF-κB p65 signaling pathway: insights from in silico and in vivo investigations

BackgroundGastric ulcers represent a worldwide health problem, characterized by erosions that affect the mucous membrane of the stomach and may even reach the muscular layer, leading to serious complications. Numerous natural products have been assessed as anti-ulcerogenic agents, and have been considered as new approaches for treatment or prevention of gastric ulcers. The present research investigated the preventive benefits of Apium graveolens L. (Apiaceae), known as celery, seed extract towards indomethacin-induced ulceration of the stomach in rats.MethodsMetabolomic profiling, employing liquid chromatography coupled to high-resolution electrospray ionization mass spectrometry (LC-HR-ESI–MS), was implemented with the aim of investigating the chemical profile of the seeds. Histopathological analysis of gastric tissues, as well as assessment of numerous inflammatory cytokines and oxidative stress indicators, confirmed the in vivo evaluation.ResultsThe prior treatment with A. graveolens seed extract resulted in a substantial reduction in the ulcer index when compared to the indomethacin group, indicating an improvement in stomach mucosal injury. Moreover, the gastroprotective effect was demonstrated through examination of the oxidative stress biomarkers which was significantly attenuated upon pre-treatment with A. graveolens seed extract. Vascular endothelial growth factor (VEGF), a fundamental angiogenic factor that stimulates angiogenesis, was markedly inhibited by indomethacin. A. graveolens seed extract restored this diminished level of VEGF. The dramatic reductions in NF-κB protein levels indicate a considerable attenuation of the indomethacin-induced IKκB/NF-κB p65 signaling cascade. These activities were also correlated to the tentatively featured secondary metabolites including, phenolic acids, coumarins and flavonoids, previously evidenced to exert potent anti-inflammatory and antioxidant activities. According to our network pharmacology study, the identified metabolites annotated 379 unique genes, among which only 17 genes were related to gastric ulcer. The PTGS2, MMP2 and PTGS1 were the top annotated genes related to gastric ulcer. The top biological pathway was the VEGF signaling pathway.ConclusionA. graveolens seed extract possesses significant anti-ulcer activity, similar to famotidine, against gastric lesions induced by indomethacin in rats. It is worth highlighting that the extract overcomes the negative effects of conventional chemical anti-secretory drugs because it does not lower stomach acidity.

Green Synthesis of Silver Nanoparticles from Bark Extract to Detect Anti Ulcer Activity in Swiss Albino Rats

The anti-ulcer activity of Butea monosperma silver nanoparticles (SNBM) was estimated in Swiss albino rats using ulcers caused by histamine, drugs, and ethanol. The effects of the SNBM at the doses of 300 and 550 mg/kg per os (p.o.) were compared with those of the reference pharmaceuticals, famotidine (35 mg/kg b.w.), and revealed substantial safeguards against ulcers generated by indomethacin and histamine. Additionally, the extract demonstrated excellent resistance against stomach ulcers brought on by ethanol. In addition, in ethanol-induced stomach ulceration, SNBM drastically lowered the spike in lipid peroxide level [(Thiobarbituric acid reactive substances (TBARS)] and restored the altered glutathione level. According to the study, SNBM demonstrates anti-ulcer efficacy by enhancing the gastric mucosa's antioxidant capacity and minimizing mucosal damage.

Plants with Anti-Ulcer Activity and Mechanism: A Review of Preclinical and Clinical Studies.

Ulcer disorders including the oral mucosa, large intestine, and stomach mucosa, cause significant global health burdens. Conventional treatments such as non-steroid anti-inflammatory drugs (NSAIDs), proton pump inhibitors (PPIs), histamine H2 receptor antagonists (H2RAs), and cytoprotective agents have drawbacks like mucosal injury, diminish gastric acid secretion, and interact with concurrent medications. Therefore, alternative therapeutic approaches are needed to tackle this health concern. Plants are rich in active metabolites in the bark, roots, leaves, fruits, and seeds, and have been utilized for medicinal purposes since ancient times. The use of herbal therapy is crucial, and regulations are necessary to ensure the quality of products, particularly in randomized studies, to assess their efficacy and safety in treating ulcer disorders. This study aims to explore the anti-ulcer activity of medicinal plants in treating peptic ulcer disease, ulcerative colitis, and aphthous ulcers. Articles were searched in Scopus and PubMed, and filtered for publication from 2013 to 2023, resulting in a total of 460 from Scopus and 239 from PubMed. The articles were further screened by title and abstract and resulted in 55 articles. Natural products, rich in active metabolites, were described to manage ulcer disease by protecting the mucosa, reducing ulcer effects, inhibiting pro-inflammatory factors, and reducing bacterial load, thus improving patients' quality of life. Natural extracts have proven effective in managing other health problems, including ulcers by reducing pain and decreasing lesions. This review provides an overview of preclinical and clinical studies on medicinal plants, focusing on their effectiveness in treating conditions like peptic ulcers, ulcerative colitis, and aphthous ulcers.

Synthesis and Antiulcer Activity of Aromatic and Heterocyclic Amides of 3-O-Acetylglycyrrhetic Acid

Synthesis and Antiulcer Activity of Aromatic and Heterocyclic Amides of 3-O-Acetylglycyrrhetic Acid

In-vivo Pharmacological Evaluation of Anti-Ulcerative Colitis Activity of Ethanolic Bark Extract of Ficus religiosa in Swiss Albino Mice

Ulcerative colitis is an idiopathic chronic disease of the intestine with unknown etiology involving multiple immune, genetic and environmental factors. The present study was carried out based on traditional claims to assess anti-ulcerative colitis activity. The extraction of the bark powdered of Ficus religiosa was carried out using ethanol as a solvent in the soxhlet apparatus. The % yield of the ethanol extract of Ficus religiosa was calculated and it was found to be 21%. The quantitative preliminary phytochemical screening revealed the presence of alkaloids, flavonoids, glycosides, saponins, amino acids, and protein in ethanolic extract of Ficus religiosa. Ulcerative colitis was induced in mice by induction of 2ml of 3% acetic acid through intrarectally. The low dose and high dose (200mg/kg and 400mg/kg) of extract was administered orally in mice. Prednisolone (1.14mg/kg) was used as the standard drug for comparison. All acetic acid- induced mice showed typical clinical manifestations of ulcerative colitis. Colon length increased significantly and colon weight decreased significantly of the treatment groups when compared to the standard groups. The MPO activity is significantly higher in Ficus religiosa treated group (200mg/kg and 400mg/kg) in comparison to standard drug Prednisolone (1.14mg/kg) treated group. It was observed that the inflammation in the colonic tissue of Ficus religiosa treatment group was significantly higher than standard group. The two treatment group shows nearly equal effect as that of the standard drug. All parameters suggest that the 400 mg/kg dose is more effective than the lower dose.

Studies on neurobehavioural properties of Caralluma dalzielii N.E Br. aqueous aerial parts extract in mice

Ethnopharmacological relevanceCaralluma dalzielii (Asclepiadiaceae) is a shrub used in folkloric medicine to treat epilepsy, pain and infertility in sub-Saharan Africa. Previous studies demonstrated its analgesic, antiulcer, anticonvulsant, and anti-inflammatory activities. AimThis study aimed to determine the neurobehavioural properties of Caralluma dalzielii aqueous aerial parts extract (CDAE) in mice using standard experimental models. Materials and methodsNeurobehavioural activities of CDAE were evaluated (100, 200, and 400 mg/kg) in Swiss Albino mice using the beam walk, staircase, hole board, object recognition, open field assay, Y-maze and forced swimming tests. Phytochemical constituents were analysed using GC-MS. ResultsCDAE significantly increased the mean number of head dips, recognition index and spontaneous alternation in hole board (14.03 at 400 mg/kg and 6.01 in distilled water group; p < 0.05), object recognition (68.16% at 400 mg/kg compared with 51.66% of distilled water group) and Y maze (9.16 at 400 mg/kg as against 4.66 of distilled water group; p < 0.05) tests respectively. It decreased the rearing counts as well as the peripheral and central square crossing in the staircase (4.2 at 400 mg/kg as against 7.87 of the distilled water group; p < 0.05) and open field tests (central, 0.81; peripheral, 1.66 at 400 mg/kg as against central, 5.23; peripheral 11.83 of the distilled water control group; p < 0.05), respectively. There were no significant effects on beam walk assays and forced swim tests. The GC-MS analysis identified a hundred compounds in CDAE. Some compounds which have been reported to possess neurobehavioural activity that were identified include 3,5-Dimethylpyrazole, 2-Amino-5-methylbenzoic acid, Acetophenone, and Tetrahydropyran. ConclusionCDAE demonstrated anxiolytic, anti-hyperactivity, and memory-improving effects in mice. The extract may possess GABAergic and glutamatergic properties. More studies are needed to confirm this. Isolation of the bioactive compounds is currently ongoing to unravel the bioactive constituents present in C. dalzielii extract.

Prevención de úlceras estomacales inducidas por etanol en ratas utilizando extracto de hoja de Senecio perralderianus

Senecio perralderianus belongs to the family of Asteraceae and is only found in Algeria. Some species of this family are used to heal gastrointestinal issues in conventional medicine for their antioxidant and anti-inflammatory properties. This research was performed in order to determine if methanolic extract from the leaves of S. perralderianus had any protective effects on gastroenteritis brought on by alcohol consumption. Wistar rats were fed with 100% ethanol orally to induce gastric ulcer, and pre-treated with 50, 100, and 200 mg·kg-1 of the extract in addition to 5 mg·kg-1 of Ranitidine as a positive reference drug. The extract had shown a positive effect to protect ethanol-induced gastric ulcers with a protection percentage of 71 to 88%. In addition, pretreatment of rats significantly increased levels of GSH, CAT, and SOD in vivo as non-enzymatic and enzymatic antioxidants, and also reduced the level of lipid peroxidation. Histopathological sections, which showed the action of the therapeutic extract, substantially confirmed these findings on the reduction of the inflammation zone and the reduction of immune cell filtration caused by ethanol toxicity with increased extract dosages compared to Ranitidine. The antiulcer activity is due to inhibition of oxidative stress and gastritis. It is associated with a total polyphenol, flavonoids, chlorophyll (a, b), and carotenoids substantial amounts.

Chemical Composition and Antibacterial and Antiulcerative Colitis Activities of Essential Oil from Pruni Semen.

This study was sought to investigate the chemical composition and antibacterial and antiulcerative colitis (UC) effects of essential oil from Pruni Semen (PSEO). A GC-MS assay showed that the major compounds in PSEO were products of amygdalin hydrolysis, which possessed great antibacterial and anti-inflammatory potential. In vitro antibacterial experiments demonstrated that PSEO treatment inhibited activity of four kinds of intestinal pathogens probably by disrupting the cell wall. Further in vivo studies showed that PSEO administration significantly improved physiological indexes, attenuated histopathological characteristics, and inhibited proinflammatory cytokine production in dextran sulfate sodium (DSS)-induced UC mice. Network pharmacology and molecular docking results predicted that PSEO might prevent UC via regulating the PI3K/AKT pathway. Western blotting and immunofluorescence assays were further conducted for verification, and the results evidenced that PSEO intervention significantly regulated the PI3K/AKT pathway and the expression of its downstream proteins in DSS-induced mice. PSEO might provide a new dietary strategy for UC treatment.

Anti-ulcerative colitis effects of chemically characterized extracts from Calliandra haematocephala in acetic acid-induced ulcerative colitis.

Background: Ulcerative colitis is a chronic immune-mediated inflammatory bowel disease that involves inflammation and ulcers of the colon and rectum. To date, no definite cure for this disease is available. Objective: The objective of the current study was to assess the effect of Calliandra haematocephala on inflammatory mediators and oxidative stress markers for the exploration of its anti-ulcerative colitis activity in rat models of acetic acid-induced ulcerative colitis. Methods: Methanolic and n-hexane extracts of areal parts of the plant were prepared by cold extraction method. Phytochemical analysis of both extracts was performed by qualitative analysis, quantitative methods, and high-performance liquid chromatography (HPLC). Prednisone at 2mg/kg dose and plant extracts at 250, 500, and 750mg/kg doses were given to Wistar rats for 11days, which were given acetic acid on 8th day through the trans-rectal route for the induction of ulcerative colitis. A comparison of treatment groups was done with a normal control group and a colitis control group. To evaluate the anti-ulcerative colitis activity of Calliandra haematocephala, different parameters such as colon macroscopic damage, ulcer index, oxidative stress markers, histopathological examination, and mRNA expression of pro and anti-inflammatory mediators were evaluated. mRNA expression analysis was carried out by reverse transcription quantitative real-time polymerase chain reaction (RT-qPCR). Results: The phytochemical evaluation revealed polyphenols, flavonoids, tannins, alkaloids, and sterols in both extracts of the plant. Results of the present study exhibited that both extracts attenuated the large bowel inflammation and prevented colon ulceration at all tested doses. Macroscopic damage and ulcer scoreswere significantly decreased by both extracts. Malondialdehyde (MDA) levels and nitrite/nitrate concentrations in colon tissues were returned to normal levels while superoxide dismutase (SOD) activity was significantly improved by all doses. Histopathological examination exhibited that both extracts prevented the inflammatory changes, cellular infiltration, and colon thickening. Gene expression analysis by RT-qPCR revealed the downregulation of pro-inflammatory markers such as tumor necrosis factor-alpha (TNF-α) and cyclooxygenase-2 (COX-2) whereas the anti-inflammatory cytokines including Interleukin-4 (IL-4) and Interleukin-10 (IL-10) were found to be upregulated in treated rats. Conclusion: It was concluded based on study outcomes that methanolic and n-hexane extracts of Calliandra haematocephala exhibited anti-ulcerative colitis activity through modulation of antioxidant defense mechanisms and the immune system. In this context, C. haematocephala can be considered as a potential therapeutic approach for cure of ulcerative colitis after bioassay-directed isolation of bioactive phytochemicals and clinical evaluation.