Anti-ulcerative Colitis Activity Research Articles

Design, synthesis, and biological evaluation of novel sesquiterpene lactone derivatives as PKM2 activators with potent anti-ulcerative colitis activities

Pyruvate kinase isoform 2 (PKM2) is closely related to the regulation of Th17/Treg balance, which is considered to be an effective strategy for UC therapy. Parthenolide (PTL), a natural product, only possesses moderate PKM2-activating activity. Thus, five series of PTL derivatives are designed and synthesized to improve PKM2-activated activities and anti-UC abilities. Through detailed structure optimization, B4 demonstrates potent T-cell anti-proliferation activity (IC50 = 0.43 μM) and excellent PKM2-activated ability (AC50 = 0.144 μM). Subsequently, through mass spectrometry analysis, B4 is identified to interact with Cys423 of PKM2 via covalent-bond. Molecular docking and molecular dynamic simulation results reveal that the trifluoromethoxy of B4 forms a stronger hydrophobic interaction with Ala401, Pro402, and Ile403. In addition, B4 has a significant effect only on Th17 cell differentiation, thereby regulating the Th17/Treg balance. The effect of B4 on Th17/Treg imbalance can be attributed to inhibition of PKM2 dimer translocation and suppression of glucose metabolism. Finally, B4 can notably ameliorate the symptoms of dextran sulfate sodium (DSS)-induced colitis in mouse model in vivo. Thus, B4 is confirmed as a potent PKM2 activator, and has the potential to develop as a novel anti-UC agent.

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.

Effect of vinegar steaming on the composition and structure of Schisandra chinensis polysaccharide and its anti-colitis activity.

In this study, infrared spectroscopy, high-performance liquid chromatography, and matrix-assisted laser desorption ionization-time-of-flight-mass spectrometry (MALDI-TOF-MS) technology were applied to systematically explain the Schisandra chinensis's polysaccharide transformation in configuration, molecular weight, monosaccharide composition, and anti-ulcerative colitis (UC) activity after vinegar processing. Scanning electron microscopic results showed that the appearance of S. chinensis polysaccharide changed significantly after steaming with vinegar. The MALDI-TOF-MS results showed that the mass spectra of raw S. chinensis polysaccharides (RSCP) were slightly lower than those of vinegar-processed S. chinensis polysaccharides (VSCP). The RSCP showed higher peaks at m/z 1350.790, 2016.796, and 2665.985, all with left-skewed distribution, and the molecular weights were concentrated in the range of 1300-3100, with no higher peak above m/z 5000. The VSCPs showed a whole band below m/z 3000, with m/z 1021.096 being the highest peak, and the intensity decreased with the increase of m/z. In addition, compared to RSCPs, VSCPs can significantly increase the content of intestinal short-chain fatty acids (SCFAs). This study showed that the apparent morphology and molecular weight of S. chinensis's polysaccharides significantly changed after steaming with vinegar. These changes directly affect its anti-UC effect significantly, and its mechanism is closely related to improving the structure and diversity of gut microbiota and SCFA metabolism.

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.

Purification, characterization, anti-ulcerative colitis activity of Sanghuangporus vaninii acidic polysaccharide A-3 (SVP-A-3)

Currently, Sanghuangporus vaninii, a large edible fungus of significant interest, is primarily utilized in its entirety for functional food. To unlock its potential as a health food, this study investigates its polysaccharide composition. We first analyzed the structural characteristics of the Sanghuangporus vaninii polysaccharide, then examined its therapeutic effect on ulcerative colitis (UC) in mice, identified the bioactivity of its acidic polysaccharide fraction (SVP-A-3), and investigated its anti-inflammatory mechanism. We purified SVP-A-3, which has a molecular weight of 3.3 kDa and primarily consists of Gal, Glc, Man and GlcA. The specific rotation degree of SVP-A-3 is +18°, and its structure is right-handed. In vivo, results indicated that SVP-A-3 reduced glandular loss and intestinal mucosal tissue damage in mouse colons and decreased the number of inflammatory factors in colon tissue. The expression of p-AKT, p-ERK1/2, p-JNK1/2, p-p38, and p-p65 was down-regulated in the colon of C57BL/6 mice treated with SVP-A-3. Its specific mechanism may be associated with the regulation of NF-κB, MAPK, and AKT signaling pathways. Furthermore, in this paper, we found that SVP-A-3 could modulate the intestinal microenvironment and could significantly increase the abundance of probiotic Anaerostipes, Lactobacillus and Muribaculaceae. We concluded that SVP-A-3 demonstrated superior anti-inflammatory effects in in vivo animal experiments and has high exploitation potential. Our results provide important structural information about SVP and provide the basis for their further development and application.

Evidence for the Involvement of Cytokines Modulation and Prokinetic Properties in Gastric Ulcer Healing Effects of Helicteres sacarolha A. St.-Hil. A. Juss.

Preparations of Helicteres sacarolha (Malvaceae) leaves and roots are used in the form of decoction, infusion or maceration, to treat gastrointestinal disturbances, among others. Studies supporting some of its ethnomedicinal uses are still incipient. The present study aimed to investigate it potential effect on chronic ulcer, ulcerative colitis and possible prokinetic activities as part of its mechanism of action. The powdered leaves of Helicteres sacarolha (HEHs) was prepared by maceration in 70 % hydroethanolic solution. Its qualitative phytochemical constituents were investigated by direct flow injection analysis coupled to atmospheric pressure chemical ionization ion trap tandem mass spectrometry (FIA-APCI-IT-MSn ). The gastric ulcer healing effect was evaluated in acetic acid induced chronic ulcer in mice and the lesions were evaluated, including analysis of blood plasma cytokine levels. The prokinetic properties (gastric emptying and intestinal transit) were carried out in mice. Potential anti-ulcerative colitis activity was evaluated in rats using 2,4,6-trinitrobenzenesulfonic acid (5 % TNBS) -induced colitis. All animal experiments were carried out at the doses of 20, 50 and 250 mg/kg (p.o.). Eight compounds were putatively identified, specifically lariciresinol, and its derivatives, kaempferol derivatives and Tricin-O-Glc. The extract promoted increased gastric ulcer healing at all doses tested. Modulation of the cytokines involved inhibition of some key pro-inflammatory cytokines with maximum effect on IL-1β (70 %, 50 mg/kg, p<0.05), TNF-α (79 %, 20 mg/kg, p<0.01), and in the anti-inflammatory cytokines, namely IL-10 (57 %, 50 mg/kg, p<0.05) and IL-17 (79 %, only at 50 mg/kg, p<0.05). Histological findings demonstrated a mitigated inflammatory activity, and tissues undergoing regeneration. HEHs treatment caused delayed gastric emptying, and increased intestinal transit, but had no effect in the experimentally induced ulcerative colitis. We report for the first time putatively the presence of Lariciresinol and tricin derivatives from the hydroethanolic leaves extract of H. sacarolha. Its possible mechanism of actions of gastric ulcer healing involves cytokines modulation, mitigation of inflammatory response and tissue regeneration and provoked opposing effect in the gastrointestinal system. The present study demonstrates the therapeutic potential of H. sacarolha leaves used in Brazilian ethnomedicine in the treatment of chronic gastric ulcer.

Enhancement of antioxidant and anti-inflammatory activities of flavonoid primuletin in DSS induced colitis in C57BL/6 mice

Background: Inflammatory Bowel Disease is a syndrome comprising of Ulcerative colitis and Crohn’s disease characterized by rectal bleeding, abdominal pain, diarrhoea, progressive weight loss and rarely infections. There are lot of drugs like corticosteroids, immunosuppressants, antibiotics to treat the disease, yet no effective treatment for the disease is available apart from treating symptomatically. Flavonoids especially Primuletin was selected as test drug to prove its anti-ulcerative colitis activity and to establish it as an effective drug for treating IBD. Materials and methods: The in-vitro activity of Primuletin was investigated against RAW 246.7 cell lines in DMEM medium. The in-vitro cytotoxicity of the drug was estimated using MTT assay and the in-vitro estimation of inflammatory markers (TNFα, IL-6) was performed using indirect Elisa. Acute oral toxicity studies were performed to determine the toxicity of Primuletin in swiss albino mice. In-vivo anti-ulcerative colitis activity of Primuletin was investigated in DSS induced IBD in C57BL/6 and the results were compared with the standard drug. Results: Primuletin treatment significantly lowered the inflammatory markers in-vitro. In DSS Primuletin treatment significantly prevented drastic variations in the body weight of mice.

Pharmacological and metabolomic profiles of Musa acuminata wastes as a new potential source of anti-ulcerative colitis agents

Musa acuminata (MA) is a popular fruit peels in the world. Non-food parts of the plant have been investigated for their antioxidant and anti-ulcerative colitis activity. Metabolomic approaches were found to be informative as a screening tool. It discovered different metabolites depending on statistical analysis. The antioxidant activity content was measured by colorimetric method. Seventy six investigated metabolites were observed. The identities of some of these markers were confirmed based on their MS2 fragmentation and NMR spectroscopy. These include: cinnamic acid and its dimer 2-hydroxy-4-(4-methoxyphenyl)-1H-phenalen-1-one beside; gallic acid and flavonoids; quercetin, quercetin-3-O-β-d-glucoside, luteolin-7-O-β-d-glucopyranoside. GC/MS analysis of MA peels essential oil led to identification of 37 compounds. The leaves, pseudostem and fruit peels extracts were tested for their safety and their anti-ulcerative colitis efficacy in rats. Rats were classified into: normal, positive, prednisolone reference group, MA extracts pretreated groups (250–500 mg/kg) for 2 weeks followed by induction of ulcerative colitis by per-rectal infusion of 8% acetic acid. Macroscopic and microscopic examinations were done. Inflammatory markers (ANCA, CRP and Ilβ6) were measured in sera. The butanol extracts showed good antioxidant and anti-inflammatory activities as they ameliorated macroscopic and microscopic signs of ulcerative colitis and lowered the inflammatory markers compared to untreated group. MA wastes can be a potential source of bioactive metabolites for industrial use and future employment as promising anti-ulcerative colitis food supplements.

Protective Effect of Nelumbo nucifera Plant on Dextran Sodium Sulfate-Induced Ulcerative Colitis in Rats

Objectives Ulcerative colitis is a global disease with increasing incidence and worldwide prevalence. So this study was undertaken to observe antiulcerative colitis activity of ethanolic extract of seeds of Nelumbo nucifera plant on dextran sodium sulfate (DSS)-induced ulcerative colitis in rats. Materials and Methods The effect of ethanolic extract of N. nucifera seed (EENNS) was studied on DSS-induced ulcerative colitis in albino Wistar rats for 11 days. Disease pathogenesis was assessed by evaluation of disease activity index (DAI) including the following parameters: change in body weight, stool constituency, rectal bleeding in animals. Estimation of myeloperoxide (MPO), nitric oxide (NO), and antioxidant parameters like malondialdehyde (MDA), superoxide dismutase (SOD), and catalase level was performed in colon homogenate of animals. TNF-α (tumor necrosis factor- α) level was measured in colon homogenate using rat TNF-α ELISA kit. Statistical Analysis Significant differences (mean ± standard error of the mean) were detected using one-way analysis of variance followed by post-test using Graphpad prism 7.0 for multiple comparisons. Results EENNS (400 mg/kg) significantly improved the disease progression, body weight, and colon length of the animals as compared with the disease control group. Animal treated with EENNS (400 mg/kg) showed significantly improved colon mucosal damage index (1.66 ± 0.21) and DAI (11.66 ± 4.01) as compared with the disease control group. A higher level of SOD and catalase and a lower level of MDA were observed in animals treated with EENNS (400 mg/kg) as compared with the disease control group. Animals treated with EENNS (400 mg/kg) significantly decreased in NO and MPO levels as compared with the disease control group. A lower level of TNF-α (561.94 ± 14.84) was observed in EENNS (400 mg/kg)-treated animals as compared with the disease control group (736.92 ± 15.3). These observations were comparable to those of the standard control group. Histopathological data showed that EENNS (400 mg/kg) has shown reversal of tissue inflammation as compared with the disease group and evidence of less cell infiltration of lymphocytes and monocytes with normal structures of goblet cell and crypts as compared with the disease group. Conclusion EENS (400 mg/kg) can decrease the severity of the UC produced by DSS. EENNS showed a protective effect against DSS-induced ulcerative colitis which may be due to its antioxidant and anti-inflammatory activity.

Anti-Ulcerative Colitis Activity of the Aqueous Leaves Extract of Khaya Senegalensis in Acetic Acid-Induced Colitis Rat Model

intestinal tract mainly colon. The disease is characterized by diarrhoea, blood in the stool, abdominal pain, and weight loss. Khaya senegalensis a plant commonly called dry zone Mahogany has been used as a remedy for several human gastrointestinal ailments. Objectives: To investigate the effect of aqueous leaves extract of Khaya senegalensis in the acetic acid-induced ulcerative colitis rat model. Study design: Preclinical randomised controlled trial. Methods: extraction was done using water, initial phytochemical screening and oral LD50 were determined. Colitis was induced in rats using 4% acetic acid administered intra rectally. The rats were divided into five groups, group 1 received water, groups 2, 3, and 4 received graded doses of leaves extract while group 5 received prednisolone as the positive control. Symptomatic parameters like the daily stool consistency and appearance and histological parameters such as ulcer area, lesson severity score, ulcer index, weight/length ratio and percentage cure were measured. Results; The leaves extract showed presence of alkaloids, tannins, flavonoids, saponins, steroids, volatile oil etc. The oral LD50 was greater than 5000mg/kg and the efficacy of the 400mg/kg extract administered group was not statistically significantly different from the positive control group that received the standard drug prednisolone. Conclusion: It can be concluded that the aqueous leaves extract of Khaya senegalensis possess significant anti-ulcerative colitis activity on acetic acid-induced ulcerative colitis rat models and appears to be safe.

Genus Sophora: a comprehensive review on secondary chemical metabolites and their biological aspects from past achievementsto future perspectives.

Sophora is deemed as one of the most remarkable genera of Fabaceae, and the third largest family of flowering plants. The genus Sophora comprises approximately 52 species, 19 varieties, and 7 forms that are widely distributed in Asia and mildly in Africa. Sophora species are recognized to be substantial sources of broad spectrum biopertinent secondary metabolites namely flavonoids, isoflavonoids, chalcones, chromones, pterocarpans, coumarins, benzofuran derivatives, sterols, saponins (mainly triterpene glycosides), oligostilbenes, and mainly alkaloids. Meanwhile, extracts and isolated compounds from Sophora have been identified to possess several health-promising effects including anti-inflammatory, anti-arthritic, antiplatelets, antipyretic, anticancer, antiviral, antimicrobial, antioxidant, anti-osteoporosis, anti-ulcerative colitis, antidiabetic, anti-obesity, antidiarrheal, and insecticidal activities. Herein, the present review aims to provide comprehensive details about the phytochemicals and biological effects of Sophora species. The review spotlighted on the promising phytonutrients extracted from Sophora and their plethora of bioactivities. The review also clarifies the remaining gaps and thus qualifies and supplies a platform for further investigations of these compounds.

Desmethylbellidifolin Attenuates Dextran Sulfate Sodium-Induced Colitis: Impact on Intestinal Barrier, Intestinal Inflammation and Gut Microbiota.

Ulcerative colitis has been recognized as a chronic inflammatory disease predominantly disturbing the colon and rectum. Clinically, the aminosalicylates, steroids, immunosuppressants, and biological drugs are generally used for the treatment of ulcerative colitis at different stages of disease progression. However, the therapeutic efficacy of these drugs does not satisfy the patients due to the frequent drug resistance. Herein, we reported the anti-ulcerative colitis activity of desmethylbellidifolin, a xanthone isolated from Gentianella acuta, in dextran sulfate sodium-induced colitis in mice. C57BL/6 mice were treated with 2% dextran sulfate sodium in drinking water to induce acute colitis. Desmethylbellidifolin or balsalazide sodium was orally administrated once a day. Biological samples were collected for immunohistological analysis, intestinal barrier function evaluation, cytokine measurement, and gut microbiota analysis. The results revealed that desmethylbellidifolin alleviated colon shortening and body weight loss in dextran sulfate sodium-induced mice. The disease activity index was also lowered by desmethylbellidifolin after 9 days of treatment. Furthermore, desmethylbellidifolin remarkably ameliorated colonic inflammation through suppressing the expression of interleukin-6 and tumor necrosis factor-α. The intestinal epithelial barrier was strengthened by desmethylbellidifolin through increasing levels of occludin, ZO-1, and claudins. In addition, desmethylbellidifolin modulated the gut dysbiosis induced by dextran sulfate sodium. These findings suggested that desmethylbellidifolin effectively improved experimental ulcerative colitis, at least partly, through maintaining intestinal barrier integrity, inhibiting proinflammatory cytokines, and modulating dysregulated gut microbiota.

Sanhuang Shu'ai decoction alleviates DSS-induced ulcerative colitis via regulation of gut microbiota, inflammatory mediators and cytokines

BackgroundSanhuangshu’ai decoction (SH), a traditional Chinese medicine (TCM) prescription, has been safely used to treat diarrhea, dysentery and other inflammatory diseases with little side effect and low cost for thousands of years. However, its mechanism remains elusive. This study was designed to investigate the anti-ulcerative colitis (UC) activity of SH and mechanism by detecting its anti-inflammatory, anti-oxidative, and intervention effects of intestinal flora with the dextran sodium sulfate (DSS)-induced colitis mice. MethodsThe DSS-induced colitis mice was orally administered SH for 1 week with 0.8 or 1.6 g kg−1 d-1 dosage. A clinical disease activity score was evaluated daily. The colonic tissues of the mice were collected and prepared to detect its anti-inflammatory, anti-oxidative, intervention effects of intestinal flora and hydrogen peroxide(H2O2) in vivo, cytotoxicity and ROS influencing effects in vitro. Histological colitis severity and expression of cytokines were also determined. ResultsOral administration of SH significantly prevented the development of colitis. It reduced the expression of interleukin (IL)-1, IL-6, and tumor necrosis factor (TNF)-α in the colon. Moreover, SH administration alleviated the oxidative stress in the colon of DSS-induced colitis mice, evidenced by the decrease of myeloperoxidase (MPO) activity and malondialdehyde (MDA) level, and increase of ROS level. Furthermore, SH can prevent the decrease ofLactobacillus sp. and population abundance of intestinal flora caused by DSS. ConclusionSH significantly ameliorates the symptoms of DSS-induced colitis mice and the potential mechanism of SH may involve in multiple kinds of metabolic pathway including the regulation of gut microbiota, inflammatory mediators and cytokines.

Anti-Inflammatory Activity of a Peptide from Skipjack (Katsuwonus pelamis).

In this paper, the effect of skipjack (Katsuwonus pelamis) enzymatic peptide (SEP), which was prepared and purified from a byproduct of skipjack, on inflammation, ulcerative colitis and the regulation of intestinal flora was studied in a mouse ulcerative colitis model and a transgenic zebrafish inflammation model. The aggregation of transgenic granulocyte neutrophils in zebrafish from a normal environment and from a sterile environment was calculated, and the anti-inflammatory activity of SEP was evaluated. To evaluate the anti-ulcerative colitis activity of SEP, DSS-induced colitis mice were given SEP, salicylazosulfapyridine (SASP), or SASP + SEP. Then, the concentrations of IL-6, IL-10 and TNF-α in the serum were detected, the HE-stained colon tissue was examined by microscopy the species composition and abundance distribution of the intestinal flora was analyzed. The results showed that 500 μg/mL SEP treatment significantly alleviated neutrophil granulocyte aggregation in the zebrafish inflammation model; Diarrhea, hematochezia and body weight loss were alleviated to a certain extent in mice gavaged with SEP and SASP, and the combination of SASP with SEP was the most effective in mice. The damage to villi in the intestine was completely repaired, and the levels of IL-6, IL-10 and TNF-α, which are associated with inflammation, were all reduced. In addition, the proportion of intestinal probiotics or harmless bacteria increased, while that of pathogenic bacteria decreased, and the effect of the combined treatment was the most pronounced. These results show that SEP could relieve inflammation, cure ulcerative colitis, regulate intestinal flora and enhance the therapeutic effect of the clinical drug SASP. This study provides a theoretical basis for the development of SEP as an anti-inflammatory adjuvant therapy and intestinal flora regulator.

A unique polysaccharide from Hericium erinaceus mycelium ameliorates acetic acid-induced ulcerative colitis rats by modulating the composition of the gut microbiota, short chain fatty acids levels and GPR41/43 respectors

Ulcerative colitis (UC) is an idiopathic, chronic inflammatory disorder of the colonic mucosa. Risk of colorectal cancer in ulcerative colitis is increased in patients with long-standing disease compared with the general population. Hericium erinaceus (HE) has been used in traditional folk medicine and medicinal cuisine in China, Korea and Japan with anti-gastritis and anti-ulcerative colitis activities. EP-1, a purified unique polysaccharide isolated from HE mycelium, has recently been identified as the active component responsible for anti- ulcerative colitis activity by using a cell model for identification. In this study, our data shows that EP-1 was effective in relieving the symptoms of acetic acid induced UC rats. Based on the Illumina MiSeq platform, 16S rRNA sequencing of the rat colonic contents indicated that the intestinal flora structure remarkably changed in the model rats and the tendency was alleviated to a certain degree by EP-1. The further results showed that in the acetic acid induced UC rats EP-1 modulated the gut microbiota community and increased short chain fatty acids (SCFAs). And immunoblot analyses showed that after treated by EP-1, GPR41 and GPR43 were significantly suppressed expression in colonic tissues of the UC rats. In the meanwhile, EP-1 also showed its antioxidant, anti-inflammatory and enhancing immune activities. Thus, the polysaccharide purified from HE showed potential for anti-UC activity and the complementary and alternative medicine (CAM) herb therapy.

A polysaccharide from cultured mycelium of Hericium erinaceus relieves ulcerative colitis by counteracting oxidative stress and improving mitochondrial function

EP-1 is a polysaccharide with a molecular weight of approximately 3100 Da, which is extracted from the cultured mycelium of Hericium erinaceus. Its anti-ulcerative colitis activity was evaluated in experimental systems using rats with ulcerative colitis and Caco-2 cells as models for experimentation. Our results showed that the treatment of EP-1 could increase SOD enzyme activity as well as decrease ROS content and oxidative damage both in vivo and in vitro. As a consequence, mitochondria function improved significantly, indicated by the increase of oxygen consumption and ATP production. In addition, increased respiration activity accelerated the elimination of excessive ROS substrate and enhanced bioenergy generation. Finally, upon treatment with EP-1, apoptosis of intestinal epithelial cells was reduced and UC was relieved accordingly. Thus, EP-1 shows potential for the development of new functional foods and drugs, especially in regard to treating ulcerative colitis.

Evaluation of anti-ulcer and ulcerative colitis of Sonchus oleraceus L

Sonchus oleraceus L. was evaluated for its gastro antiulcerogenic and anti-ulcerative colitis activities Different extracts and fractions from Sonchus oleraceus aerial parts and roots were evaluated at different dose; total alcohol extracts of aerial parts SA and roots SR were evaluated doses 250 & 500 mg/kg, While Successive extracts (SAL, SRL, CSA, CSR, BSA & BSR) were evaluated at dose of 150 mg/kg. Absolute ethanol-induced ulcer model was used for evaluation of the anti-ulcerogenic activity. The root extract showed promising antiulcerogenic activity as the total alcohol extract of the root SR (500 mg/kg) produced 88.5% protection from control ulcer which is significantly more effective than the standard drug omeprazole (20 mg/kg), in addition, the butanol fraction of the root extract BSR also produced 76.66% protection from control ulcer. On the other hand, the aerial parts total extract SA showed low antiulcerogenic activity in both tested doses (250 & 500 mg/kg) as it produced 25% & 28.33% protection from control ulcer respectively. Only the butanol fraction of the aerial parts extract BSA showed promising activity 54.16%. In the acetic acid-induced ulcerative colitis model, among the investigated extracts of Sonchus oleraceus; only the total extract of the aerial parts (SA) at dose 500 mg/kg showed strong anti-ulcerative colitis activity and this activity is followed by the activity of the butanol and chloroform fractions of the aerial parts, they produced 77.28%, 57.4% & 47.68% protection from control colitis respectively. The standard drug dexamethasone produced 63.36% protection from control colitis. The total alcohol extracts SR & SA showed no alteration on liver and kidney functions and these extracts are safe up to 5000 mg/kg. Phytochemical screening of the investigated extracts revealed the presence of carbohydrates, flavonoids, tannins, unsaturated sterols, proteins and lactones which could be responsible for the activities.

Propagation Measurements during Daytime for RazakSAT S-band Space to Earth Satellite Signal Transmission

Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-ptolyl-3H-quinazolin-4-one (5) and 2-p-Tolyl-3-[3,4,5-trimethoxy-benzylidene-amino]-3H-quinazolin-4- one (6) in addition to one acetamide derivative named as 2-(2-Hydroxycarbonylphenylamino)-N-(4- aminosulphonylphenyl) 11 were synthesized, and evaluated for their anti-ulcerogenic & AntiUlcerative colitis activities. All of the three compounds showed curative activity against acetic acid induced ulcer model at a dose of 50 mg/kg, they produced 65%, 85% & 57.74% curative ratio for compounds 5, 6 & 11 respectively. The effect of the tested compounds 5, 6 & 11 at dose 50 mg/kg were significantly (P < 0.01) more effective than dexamesathone (0.1 mg/kg) in reducing all parameters. Compounds showed curative activity of for peptic ulcer (induced by absolute alcohol (at a dose of 50 mg/kg, it produced Curative of control ulcer 56.00%, 61.70% & 87.1% for compounds 5, 6 & 11 respectively at dose 50 mg/kg, while the standard drug (Omeprazole 20 mg/kg) produced 33.3%. In both tests, the activity of our target compounds were higher than the standard drugs used for treatment of peptic ulcer and ulcerative colitis. No side effects were reported on liver and kidney functions upon prolonged oral administration of this compounds. (C) 2017 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University.

Antiulcer and Anti-ulcerative Colitis Activities of Haplophyllum tuberculatum (Forsskal)

Antiulcer and Anti-ulcerative Colitis Activities of Haplophyllum tuberculatum (Forsskal)